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1-Boc-3-Iodoazetidine

    • Product Name 1-Boc-3-Iodoazetidine
    • Alias 1-Boc-3-iodo-azetidine
    • Mininmum Order 1 g
    • Factory Site Tengfei Creation Center,55 Jiangjun Avenue, Jiangning District,Nanjing
    • Price Inquiry admin@sinochem-nanjing.com
    • Manufacturer Sinochem Nanjing Corporation
    • CONTACT NOW
    VTB
    Specifications

    HS Code

    746831

    Chemical Name 1-Boc-3-Iodoazetidine
    Cas Number 1445997-34-7
    Molecular Formula C8H14INO2
    Molecular Weight 283.11
    Appearance White to off-white solid
    Purity Typically > 95%
    Melting Point 56-58°C
    Storage Conditions Store at 2-8°C, protected from light and moisture
    Synonyms tert-Butyl 3-iodoazetidine-1-carboxylate
    Smiles CC(C)(C)OC(=O)N1CC(C1)I
    Solubility Soluble in organic solvents (e.g., DMSO, dichloromethane)
    Inchi InChI=1S/C8H14INO2/c1-8(2,3)12-7(11)10-4-6(9)5-10/h6H,4-5H2,1-3H3

    As an accredited 1-Boc-3-Iodoazetidine factory, we enforce strict quality protocols—every batch undergoes rigorous testing to ensure consistent efficacy and safety standards.

    Packing & Storage
    Packing 1-Boc-3-Iodoazetidine, 5g, is supplied in a sealed amber glass bottle with a tamper-evident cap and chemical safety labeling.
    Shipping **Shipping Description:** 1-Boc-3-Iodoazetidine is shipped in tightly sealed containers, protected from light and moisture, under ambient or refrigerated conditions as required. The chemical is packed in compliance with safety and regulatory standards for hazardous materials, ensuring safe transit. Appropriate labeling and documentation are included to meet international shipping and handling regulations.
    Storage 1-Boc-3-Iodoazetidine should be stored in a cool, dry, and well-ventilated area, away from light and incompatible substances such as strong acids, bases, and oxidizers. Keep the container tightly closed under an inert atmosphere, such as nitrogen or argon, to prevent degradation. Ideally, storage should be at 2–8°C (refrigerator conditions) to maintain chemical stability.
    Application of 1-Boc-3-Iodoazetidine

    Applications of 1-Boc-3-Iodoazetidine in Industrial Manufacturing

    As a manufacturer specializing in high-purity 1-Boc-3-Iodoazetidine, we supply this advanced heterocyclic intermediate to leading pharmaceutical and fine chemical producers worldwide. The compound’s unique structure and reliable Boc protection deliver precise reactivity and selectivity in multiple downstream applications, especially within regulated environments. Below, we outline key industrial segments utilizing this material, focusing on operational parameters, compliance standards, and final product profiles.

    1. API Intermediate Synthesis for CNS Medications

    Global pharmaceutical companies rely on 1-Boc-3-Iodoazetidine as a specialized building block in the production of active pharmaceutical ingredients (APIs) for central nervous system (CNS) drug candidates. Its protected azetidine ring supports nucleophilic substitution and coupling reactions, enabling the manufacture of next-generation therapeutic moieties targeting neurological indications.

    Industry compliance standards

    • ICH Q7 Good Manufacturing Practice for Active Pharmaceutical Ingredients
    • 21 CFR Part 211 (U.S. FDA drug GMP)
    • European Pharmacopoeia (Ph. Eur.) API monograph requirements
    • Japan Pharmacopoeia (JP) raw material controls

    Typical usage ratio

    • Employed at 1–5 mol% relative to target API core structure; actual ratio is process-optimized per route and desired yield

    Downstream process integration

    • Introduced during early-stage heterocycle assembly via palladium-catalyzed coupling or nucleophilic substitution under strictly inert, anhydrous conditions before Boc deprotection

    Final product types

    • Pyrrolidine-based CNS APIs (e.g., modafinil derivatives, novel antidepressants, cognitive enhancers)
    • Advanced intermediates for neuroreceptor modulators
    • Preclinical batch APIs for clinical trial supply

    2. Chiral Azetidine Derivative Manufacturing

    Specialty chemical companies use 1-Boc-3-Iodoazetidine as a reactive intermediate to build optically active azetidines for asymmetric catalysis or advanced chiral ligands. This application leverages the compound’s halogen atom for selective introduction of functional groups, resulting in new chiral scaffolds for fine chemical synthesis.

    Industry compliance standards

    • ISO 9001 Quality Management System
    • REACH Regulation (EU) 1907/2006 (for chemical substances)
    • California Prop 65 Substances Control (if exported to US-West Coast customers)
    • Hazardous Substances Control (international transportation via UN 3077 guidelines)

    Typical usage ratio

    • 0.2–1.2 equivalents per synthesis batch, adjusted for catalyst loading, enantiomeric yield, and ligand formation efficiency

    Downstream process integration

    • Added after base preactivation phase as the iodo coupling agent in transition metal-catalyzed asymmetric synthesis

    Final product types

    • Chiral azetidine ligands for metal-catalyzed reactions
    • Catalytic intermediates used by fine chemical and agrochemical companies
    • Azetidine-based organocatalysts

    3. Peptidomimetic Development for Peptide Drug Research

    Research laboratories and peptide technology companies incorporate 1-Boc-3-Iodoazetidine into synthetic peptide sequences to confer enhanced stability and bioactive conformations. By introducing substituted azetidine rings at specific positions, they generate non-natural peptides with improved resistance to enzymatic degradation and modified pharmacokinetics.

    Industry compliance standards

    • ICH Q11 Development and Manufacture of Drug Substances
    • USP <797> Compounding Sterile Preparations (for clinical peptides)
    • CFR Title 21 Part 210–211 (GMP for bulk peptide production)
    • ISO/IEC 17025 Calibration and Testing for Analytical Validation

    Typical usage ratio

    • Used at 1.0 equivalent per insertion site; batch formulation may require 2–3 mol% excess to compensate for incomplete coupling or side product formation

    Downstream process integration

    • Applied during solution-phase or solid-phase synthesis after amino acid activation, preceding Boc deprotection and downstream cyclization or elongation

    Final product types

    • Investigational peptidomimetic compounds
    • Protected peptide fragments for pharmaceutical R&D
    • Azetidine-modified peptide reference standards for preclinical testing

    4. Building Block for Specialty Agrochemical Active Ingredients

    Producers of modern agrochemical actives utilize 1-Boc-3-Iodoazetidine as a critical intermediate to introduce azetidine-based moieties for crop protection products. Its controlled reactivity and stable protection group facilitate synthesis of insecticidal, herbicidal, or fungicidal molecules exhibiting improved field stability and target selectivity.

    Industry compliance standards

    • OECD Principles of Good Laboratory Practice (GLP)
    • EPA 40 CFR Part 158 Data Requirements for Pesticide Registration (United States)
    • FAO/WHO Specifications for Plant Protection Products
    • ISO 17034 Reference Material Producer Requirements

    Typical usage ratio

    • 1–3 molar equivalents per functionalization sequence, calculated by stoichiometry based on final active target structure; excess may be required to drive full conversion in multi-step routes

    Downstream process integration

    • Charged at the N-protection or intermediate displacement stage, after initial backbone synthesis and before final ring closure or acylation

    Final product types

    • Azetidine-based insecticide and herbicide actives
    • Key protected intermediates for diversified crop protection agents
    • Reference standards and analytical markers for regulatory submission

    5. Scaffold in Discovery-Stage Medicinal Chemistry

    Drug discovery groups and custom synthesis organizations value 1-Boc-3-Iodoazetidine as a core azetidine scaffold for rapid analog screening and hit-to-lead optimization. With high Boc stability under storage and controlled reactivity for cross-coupling, the compound streamlines scaffold diversification, SAR studies, and early CMC development pipelines.

    Industry compliance standards

    • ALCOA+ Data Integrity for Research Data (FDA and EMA guidance)
    • OECD Series on Testing and Assessment for Chemicals
    • EU Directive 2001/83/EC for pharmaceutical starting materials (if scaled)
    • GLP Accreditation for discovery laboratory environments

    Typical usage ratio

    • 0.5–2.0 equivalents per combinatorial library synthesis, modulated per analog diversity requirements and functional group compatibility

    Downstream process integration

    • Inserted at the core construction phase, preceding late-stage functionalization and deprotection steps; typically coupled via Suzuki-Miyaura or Buchwald-Hartwig methodologies

    Final product types

    • Medicinal chemistry screening libraries
    • Structure-activity relationship (SAR) compound sets
    • Lead-optimized candidates for advancement to preclinical studies
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    Certification & Compliance
    More Introduction

    Introducing 1-Boc-3-Iodoazetidine: A Perspective from Production

    Turning Ideas into Practice: The Pathway to Reliable 1-Boc-3-Iodoazetidine

    Years on the production floor and in the lab have shown just how critical each precursor and intermediate is for building complex molecules with practical functions. 1-Boc-3-Iodoazetidine carries its weight in research and custom synthesis, opening doors for medicinal chemists and process developers. This compound’s design reflects an ongoing need in the marketplace: clean, well-characterized building blocks that allow for straightforward modifications and reliable downstream chemistry.

    Our team has been making 1-Boc-3-Iodoazetidine for projects that span from pilot studies on small-batch APIs to gram-scale batches supporting hit-to-lead programs. The molecule’s four-membered azetidine ring, combined with the bulky Boc (tert-butoxycarbonyl) protecting group and the reactive iodine at the 3-position, makes it versatile for researchers pushing boundaries in heterocyclic chemistry. Every molecule has a story, and this one traces back to carefully controlled halogenation and protection steps—processes refined by years of attention, not just bench-scale improvisation.

    What Sets This Intermediate Apart?

    In real-world chemistry, selectivity and reliability push projects forward. 1-Boc-3-Iodoazetidine stands out by aligning molecular reactivity with physical stability. The Boc group does more than just protect the nitrogen—it holds up under a variety of conditions, letting synthetic chemists run reactions that more delicate molecules wouldn’t survive. The iodine substituent stands ready for cross-coupling, nucleophilic substitution, and other classic applications, driving value in practical chemistry. There’s no guesswork or drift in what comes off our line. Each batch undergoes NMR and LCMS checks, giving end users results that hold up to scrutiny.

    A lot of azetidines on the market cut corners around purity or skip quality documentation. Some handle the Boc protection with little attention to stability, leaving end users to deal with degraded stock or unreliable reactivity down the chain. From our vats to your workbench, this compound keeps its promise: protected, pure, and actively ready to couple. The difference isn’t only in measured specifications—it shows up in how quickly reactions run, the quality of downstream products, and the consistency from one batch to the next.

    Direct Insights Into Specification and Quality Values

    Our technical team pays attention to the details that matter most—moisture levels, color, residual solvents, and impurity profiles. In practice, 1-Boc-3-Iodoazetidine comes as a white to off-white solid, with a melting range matching published literature and tight limits on iodide impurities. Strict controls on solvents like dichloromethane and THF mean no hidden process residues creep into your final products. Characterization isn’t an afterthought; we publish spectra, check for water by Karl Fischer titration, and calibrate our instruments with known standards.

    Lab-scale purity often means little when production moves to kilogram lots. Packing, storage, and transit put real stress on molecular stability. From clean purging after synthesis to inert atmosphere packaging, every step locks in quality. There’s no judgment call here—either the batch passes purity criteria with room to spare, or it never leaves production. Each record is kept for traceability, making it easier for researchers to meet regulatory and documentation demands, not just technical ones.

    Usage Patterns: Why Synthetic Chemists Specify This Molecule

    The real value of 1-Boc-3-Iodoazetidine shows up at the bench. Medicinal chemistry teams constantly explore structure-activity relationships, testing the effects of novel azetidine scaffolds in small-molecule libraries. The iodo group offers easy access to Suzuki, Sonogashira, or Buchwald–Hartwig couplings. We’ve seen projects using this compound to create beta-lactam analogs, CNS-targeted molecules, and novel kinase inhibitors with newly installed azetidine features.

    This molecule shortens syntheses that otherwise require laborious, multi-step manipulations. Catalytic cross-coupling handles the iodo group with much higher efficiency than upgrading from bromides or chlorides. The Boc-protected nitrogen enables selective deprotection under acid, freeing up the azetidine for localized activation—big advantages in convergent and late-stage functionalization strategies. Our customers echo this: robust yield, high conversion, and little tailing on chromatograms. The time savings, and the avoidance of tricky purification, come directly from the care taken during synthesis and purification.

    Supporting Complex Projects: Scale, Documentation, and Supply Chain Strengths

    1-Boc-3-Iodoazetidine isn’t just about what happens in a flask. Supply chain delays or inconsistent documentation sideline expensive development programs. Our production runs work to tight windows, lined up with planning from purchasing and project management on the receiving end. Each lot comes with detailed Certificates of Analysis, all backed by in-house testing and signed off by experienced chemists. CoAs record everything from moisture content to batch origin, providing transparency to support regulated R&D programs and quality audits.

    Most requests hit the lab-scale sweet spot—grams to tens of grams—but our facility can pivot to supply kilo-scale quantities on short timelines if a project needs it. This means fewer delays, fewer retests, and no nasty surprises with feedstock purity just when a project ramps up. By managing production flow directly, we control every aspect of scale-up, putting careful eyes on crystallization, drying, and packaging. This cuts off the chance of stockouts caused by third-party bottlenecks.

    From speaking directly with partners who have tried to source this intermediate elsewhere, it’s clear that many challenges stem from small variations that wreak havoc at scale. Differences in particle size, poorly understood polymorphism, and low repetitive purity can turn a promising campaign into a trail of troubleshooting and lost time. Our consistent output, tracked batch to batch and year to year, provides the reliability needed for demanding synthesis and ever-tightening review requirements.

    Building Safety and Sustainability into Each Step

    Chemical manufacturing faces real pressures from sustainability and safety. Iodination and Boc-protection require vigilant management of waste streams, hazardous gases, and temperature extremes. In many early methods, solvent losses and uncontrolled side reactions created risk for the environment and for staff. We invested early in closed systems, continuous monitoring for emissions, and tailored scrubbing units—each step aligns production with environmental stewardship and regulatory compliance.

    Process improvements don’t just tick boxes for compliance. They make a real difference in uptime, product quality, and operating costs. Automated solvent recovery and energy-balancing reduce waste. Careful quenching and neutralization strategies limit halogenated byproducts and reduce overall footprint. Each improvement supports the wider industry trend to less hazardous chemistries, and makes our facility safer and cleaner for the long term.

    Team members actively monitor and update process safety documentation, adapting quickly to new findings or incidents elsewhere in the industry. Lessons learned during scaling, handling of high-iodine materials, and crisis avoidance get built into training for all operators and technicians. Each shift carries a real responsibility for quality, sustainability, and safety—values taught by experience, not just by compliance manuals.

    Comparisons with Other Azetidine Intermediates

    Many chemists debate what sets one azetidine intermediate apart from the rest. 1-Boc-3-Iodoazetidine brings advantages over unprotected or less-activated azetidine derivatives. With simple azetidine or 3-iodoazetidine hydrochloride, the nitrogen sits exposed to nucleophiles and bases, often forcing harsh protection or incompatible downstream chemistry. Boc-protection offers a straightforward route to differentiated chemistry; it resists many bases and non-aqueous acids, and it deprotects cleanly under mild acid.

    Compared to 1-Boc-3-Bromoazetidine or 1-Boc-3-Chloroazetidine, the iodo derivative enables faster coupling, improved yields, and broader substrate scope in popular C–C and C–N bond-forming reactions. Iodoarenes and alkyl iodides accelerate key transformations in the hands of a skilled chemist, saving material and reducing purification hassles. Downstream steps such as amide formation, ring opening, or selective functionalization run cleaner, with less side reaction from competing nucleophiles. Documentation from industry partners confirms that iodo-azetidines deliver more robust conversions under both transition-metal and organocatalytic regimes.

    On the shelf, 1-Boc-3-Iodoazetidine holds up better than less-protected analogs. The Boc group stands against hydrolysis and air exposure, useful for operations where handling delays or transport over long distances test the limits of stability. We’ve tested storage for extended periods, even under suboptimal shipping scenarios, and results demonstrate lasting chemical integrity—a feature not shared by all specialty intermediates on the market.

    Answering Demands for Innovation and Rapid Delivery

    Our ongoing work with contract research and pharmaceutical partners shapes how we produce and supply specialized azetidines. Discovery teams don’t just ask for a batch; they need trusted delivery, responsive technical service, and honest feedback on synthesis challenges. By anchoring production directly at the source, we close loops faster, offering authentic technical answers to questions about reactivity, compatibility, and downstream handling.

    Modern process development pivots quickly between targets. With 1-Boc-3-Iodoazetidine’s established track record, teams know what to expect from each delivery: repeatable performance in key transformations, full documentation, and real-time support for troubleshooting or tailoring product specs. We’ve seen our intermediates plug into dozens of candidate synthesis routes with little drama—validating years of refining, testing, and listening to feedback from the world’s innovators in small-molecule pharmaceuticals and advanced materials.

    Direct supply over indirect distribution cuts wait times and shortens communication chains. Projects cycle faster from order to delivery, translating to measurable gains in lead optimization and scale-up. Every improvement in transit, documentation, or technical transparency tightens integration between bench chemistry and pilot plant manufacturing.

    From the Factory Floor: People, Process, and Progress

    Product quality always traces back to people and practice. Long experience in handling air- and moisture-sensitive reagents means more than having the right equipment—it requires gut-level awareness, careful observation, and decisive problem-solving. Every operator, analytical technician, and supervisor who touches a batch of 1-Boc-3-Iodoazetidine brings hard-won skill and takes pride in clear labeling, careful sampling, and honest reporting.

    Running batch reactors or prep-scale columns doesn’t fit easy routines. Each cycle brings variables: the tightness of purification, daily temperature swings, variations in material from suppliers. We use small-scale test runs, gather feedback from analysts, and keep process logs that feed continuous improvement. As chemists ourselves, we look forward to advancing both technique and outcome—not because compliance demands it, but because we want partners in research and development to succeed.

    Why Reliability and Quality Matter

    Missed specs or unexpected impurities don’t just eat into project returns—they can invalidate months of hard work. Our close relationship between synthesis, quality control, and logistics means every lot shipped reflects our own benchmarks. We speak candidly with partners about challenges faced in handling high-iodine chemistries, sharing what we learn and adapting with every production run.

    1-Boc-3-Iodoazetidine delivers flexibility, reliability, and efficiency for those pushing boundaries in synthetic chemistry. Investing in quality from early lab work through to commercial scale pays off: fewer failures, trusted supply, and real progress for innovative research. While documentation and compliance are necessary, experience earns trust—one batch, one collaboration, one molecule at a time. Our journey with this compound is still ongoing, shaped by the shared ambition of every researcher, process chemist, and project manager we serve.