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1-Benzyl-3-Azetidinecarboxylic Acid

    • Product Name 1-Benzyl-3-Azetidinecarboxylic Acid
    • Alias 1-Benzyl-azetidine-3-carboxylic acid
    • Einecs 68481-37-6
    • 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

    394581

    Product Name 1-Benzyl-3-Azetidinecarboxylic Acid
    Cas Number 142463-84-1
    Molecular Formula C11H13NO2
    Molecular Weight 191.23 g/mol
    Appearance White to off-white solid
    Melting Point 97-101°C
    Purity Typically ≥98%
    Solubility Slightly soluble in water; soluble in organic solvents like DMSO, methanol
    Storage Condition Store at 2-8°C, protected from light and moisture
    Smiles C1CN(C1)CC2=CC=CC=C2C(=O)O
    Inchi InChI=1S/C11H13NO2/c13-11(14)10-7-12(8-10)9-5-3-1-2-4-6-9/h1-6,10H,7-8H2,(H,13,14)
    Synonyms 1-Benzylazetidine-3-carboxylic acid

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

    Packing & Storage
    Packing Packaged in a 25g amber glass bottle with a secure screw cap, labeled with compound name, quantity, and hazard warnings.
    Shipping **Shipping Description:** 1-Benzyl-3-Azetidinecarboxylic Acid is shipped in tightly sealed, chemically compatible containers to prevent leakage and contamination. The package is clearly labeled with hazard and handling information and shipped according to local, national, and international regulations for laboratory chemicals. Temperature and moisture controls may be applied to ensure product stability during transit.
    Storage **1-Benzyl-3-Azetidinecarboxylic Acid** should be stored in a tightly sealed container away from moisture and direct sunlight. Keep it at room temperature in a cool, dry, and well-ventilated area, away from incompatible substances such as strong oxidizing agents. Properly label the container and use appropriate personal protective equipment when handling to ensure safety.
    Application of 1-Benzyl-3-Azetidinecarboxylic Acid

    Applications of 1-Benzyl-3-Azetidinecarboxylic Acid in Industrial Manufacturing

    1-Benzyl-3-azetidinecarboxylic acid acts as a critical intermediate in pharmaceutical, agrochemical, and fine chemical manufacturing, contributing unique azetidine scaffolding to enhance molecular properties in a range of commercial products. Our facility produces this compound under strict quality control to meet exacting industry requirements. Below are established application tracks where customers routinely integrate this raw material into downstream synthesis pipelines.

    1. Active Pharmaceutical Ingredient (API) Synthesis

    Innovators in pharmaceutical manufacturing use this raw material during the multi-step synthesis of advanced drug molecules containing azetidine fragments, typically to optimize the pharmacokinetic profiles or metabolic stability of novel therapeutics. This compound enters as either a core fragment or intermediate for next-stage coupling and cyclization chemistry in both large-scale and clinical lot production settings.

    Industry compliance standards

    • ICH Q7 Good Manufacturing Practice for Active Pharmaceutical Ingredients
    • US FDA 21 CFR Part 211 (Current Good Manufacturing Practice for Finished Pharmaceuticals)
    • European Pharmacopoeia (Ph. Eur.) monograph requirements for APIs
    • WHO GMP for pharmaceutical substances

    Typical usage ratio

    • 1–8 mol% as an intermediate, based on synthetic route and final drug molecular weight; ratios optimized according to route yield and impurity profile of each API

    Downstream process integration

    • Introduced at early or mid-stage of multi-step organic synthesis, typically by Grignard addition, amidation, or peptide coupling reactions in reactor trains

    Final product types

    • Small-molecule APIs with central azetidine motifs (antivirals, CNS drugs, oncology candidates, antivirals with cyclic amine cores)
    • Clinical candidate libraries for combinatorial screening

    2. Chiral Auxiliary in Asymmetric Synthesis

    Chemical and pharmaceutical manufacturers value this compound as a versatile chiral auxiliary for stereoselective transformations, such as asymmetric hydrogenation and aldol reactions. Its rigid azetidine backbone provides defined stereochemistry, which downstream chemists exploit to construct enantiomerically pure synthetic intermediates at scale.

    Industry compliance standards

    • Pharmaceutical GMP (ICH Q7, ICH Q11 Guidelines)
    • ISO 9001:2015 for industrial chemical production quality management
    • European Medicines Agency (EMA) guidelines on chiral purity for drug intermediates

    Typical usage ratio

    • 0.1–0.5 molar equivalents relative to substrate, depending on transformation, adjusted for target enantiomeric excess in final product

    Downstream process integration

    • Used as an auxiliary or ligand in batch and continuous stereoselective reaction setups, followed by removal and recovery (when possible) after asymmetric induction

    Final product types

    • Chiral pharmaceutical building blocks
    • Enantiomerically enriched specialty chemicals
    • Candidate drug substance intermediates

    3. Agrochemical Intermediate Manufacturing

    This material finds utility as a building block in the synthesis of advanced crop protection agents, particularly in producing azetidine-substituted herbicides and fungicides, where molecular rigidity improves bioavailability and environmental stability compared to open-chain analogues. Agrochemical manufacturers rely on this input during development of proprietary actives for global agricultural markets.

    Industry compliance standards

    • FAO/WHO Specifications and Evaluations for Agricultural Pesticides
    • ISO 9001:2015 for agrochemical manufacturing
    • EU Regulation (EC) No 1107/2009 concerning the placing of plant protection products on the market

    Typical usage ratio

    • 5–15% by mass in final active ingredient synthesis batch, adjusted based on desired functionalization pattern of final pesticide or fungicide molecule

    Downstream process integration

    • Fed into core cyclization and functional group derivatization processes within reactor networks for active ingredient formation

    Final product types

    • Azetidine-derivative herbicides and fungicides
    • Precursor molecules for insecticide R&D compounds

    4. Fine Chemical and Specialty Polymer Synthesis

    Producers of specialty fine chemicals and performance polymers incorporate this compound to introduce rigid cyclic amine groups, enhancing mechanical strength or introducing specific reactivity for coatings, adhesives, or elastomeric networks. The acid functionality allows straightforward integration via amidation or esterification during controlled batch or continuous production.

    Industry compliance standards

    • ISO 9001:2015 for fine chemicals and specialty polymer production
    • REACH Regulation (EC) No 1907/2006 for chemicals manufactured or imported into the EU
    • Local occupational safety and environmental regulations for polymerization plants

    Typical usage ratio

    • 2–10 wt% in copolymerization mixtures, based on targeted modification properties and cross-link density for end material

    Downstream process integration

    • Typically introduced during pre- or mid-polymerization stages for formation of functionalized side chains or cross-links in batch or continuous reactors

    Final product types

    • Azetidine-modified thermoset and thermoplastic polymers
    • Performance coatings for electronics or auto parts
    • Specialty chemical intermediates for adhesive and sealant applications

    5. Contract Research and Medicinal Chemistry Services

    CROs and CDMOs use this compound in customer-driven, structure-activity relationship exploration, employing it as a unique cyclic amine handle in focused libraries and fragment-based design. In these settings, the compound’s acid group enables direct coupling to heterocycles or aryl systems, reducing synthesis steps in prototype design or scale-up batches.

    Industry compliance standards

    • GLP (Good Laboratory Practice) for medicinal chemistry screening
    • ISO 17025 for analytical and research chemistry laboratories
    • Pharmaceutical R&D SOPs for handling and storage of regulated intermediates

    Typical usage ratio

    • Variable, typically 0.25–2 equivalents per target scaffold; usage tailored to project-specific reaction scope and library design needs

    Downstream process integration

    • Used in parallel synthesis, fragment coupling, or automated synthesizer platforms for high-throughput compound library assembly

    Final product types

    • Fragment libraries for early discovery
    • Medicinal chemistry lead analogs
    • Custom reference standards
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    Certification & Compliance
    More Introduction

    Introducing 1-Benzyl-3-Azetidinecarboxylic Acid: Innovation from the Source

    Direct Insights from Years of Manufacturing Practice

    As a manufacturer who has worked with a range of azetidine derivatives for over a decade, I have witnessed how subtle changes in chemical structure can influence both process and performance in the lab and on the factory floor. Among the compounds that have drawn real attention for their versatility is 1-Benzyl-3-Azetidinecarboxylic Acid. Our daily involvement in producing this molecule from raw materials to quality control has given us a perspective not often shared outside the manufacturing walls.

    Core Features of Our 1-Benzyl-3-Azetidinecarboxylic Acid

    This compound stands out for chemists interested in building novel scaffolds or complex intermediates. The essential part of its value comes directly from its azetidine core—a four-membered ring paired with a carboxylic acid group at the third carbon and a benzyl substituent at the nitrogen atom. The presence of the benzyl group raises its lipophilicity compared to unsubstituted azetidinecarboxylic acids, making it favored for synthetic routes that aim for increased organic solubility or particular pharmacological profiles.

    Our typical output meets a high standard of purity, aiming for research and pharmaceutical development. In practice, we've achieved and maintained HPLC purity levels above 98 percent, which gives our customers reliable, reproducible results. The compound appears as an off-white to white crystalline powder, easily handled in bench-scale and production settings. Melting points remain consistent within narrow ranges, reflecting stable quality from batch to batch.

    What Sets Our Production Apart

    As a direct producer, we control every variable—raw input quality, reaction temperature and duration, purification, and rigorous analytical checks—including NMR, MS, LC, GC, and chiral chromatography when needed. This commitment avoids the pitfalls common among traders or resellers who source externally and may lack process transparency. Customers who formulate or design new molecules quickly realize the difference in how our product behaves in both scale-up and sensitive syntheses.

    Handling and storage also matter, especially for compounds used in medicinal chemistry and advanced materials. We double-seal and nitrogen-flush the packaging to maintain chemical integrity, reducing the risk of degradation. Many companies skip these details, but over years of feedback and returns, we've come to appreciate how even small changes in storage can affect material quality and, downstream, experimental success.

    Experience with Use Cases in Real-World Settings

    Our technical team frequently works with groups targeting central nervous system active molecules, anti-infectives, and agrochemical leads. The azetidine ring, being less common than piperidine or pyrrolidine, offers new binding geometry and strain energy, which medicinal chemists often leverage for bioactivity. The benzyl group can either serve as a functional handle for further transformation or improve membrane permeability, depending on design needs.

    Custom synthesis partners frequently request 1-Benzyl-3-Azetidinecarboxylic Acid for ring-opening reactions, side-chain installation, or as a precursor to protected amino acids. In cross-coupling, the benzyl moiety stands firm under a range of palladium-catalyzed conditions, letting you explore Suzuki, Buchwald-Hartwig, and more without the product breaking down or giving inconsistent yields. For solid-phase synthesis, the compound loads onto resins cleanly, and its carboxylic acid introduces versatility into peptide or polymer conjugates.

    In working with formulation chemists, we’ve seen advantages over other azetidinecarboxylic acids when it comes to solubility in less polar organic solvents. This can save time at the late stages where re-solubilization or purification cost hours or days per batch. Crucially, because we supply directly from our plant, our clients have the opportunity to request tailored salt forms or custom particle sizes, mitigating some downstream formulation headaches.

    Proven Benefits Grounded in Direct Experience

    Comparisons with more common analogs, especially unsubstituted 3-azetidinecarboxylic acid, highlight tangible benefits. The benzyl group’s influence goes beyond simple steric and electronic effects. In one drug discovery project early in our production history, a partner switched from a methyl- to benzyl-protected azetidine intermediate and saw a 25 percent improvement in overall synthetic yield, without significant adjustment to their protocol. That outcome steered us to refine our purification process, further reducing minor side products that can undermine scale-up efficiency or throw off screening campaigns.

    For manufacturers working with downstream hydrogenation or deprotection, experience has shown that our benzylated acid can be smoothly converted to the parent amine with standard catalytic conditions. Batch records from both our site and our customers’ pilot plants indicate that standard 5% Pd/C at atmospheric pressure in ethanol cleaves the benzyl cleanly, yielding product ready for next steps. Such operational consistency saves days on troubleshooting and optimizations.

    Addressing Challenges with Confidence

    Chemical supply chains require careful stewardship. Over the course of making and shipping 1-Benzyl-3-Azetidinecarboxylic Acid around the world, we’ve learned firsthand the pitfalls of variable storage temperature, packaging failures, or inadequate regulatory paperwork. These aren’t just compliance issues—they affect scene-to-scene lab results and reputational risk for both supplier and user.

    We have invested steadily in analytical capability and compliance. From international transport to in-country regulations and customs clearance, our logistics team works closely with local authorities on documentation and safety. Protecting the chain of custody directly supports the integrity of both proprietary and common syntheses built on our product.

    Unique Aspects of Our Process Technology

    A substantial part of our development effort centers on the sourcing and pre-treatment of key starting materials. By negotiating direct offtake and properly vetting suppliers, we sidestep the typical supply and quality fluctuations that plague many chemical markets. Our reactors allow for controlled addition and real-time monitoring, while process analytical technology flags any off-specification event in-process rather than waiting for post-synthesis analysis.

    Over the years, we have improved both throughput and quality yield with incremental changes—better agitation to minimize temperature gradients, upgraded filtration systems to reduce carryover of fine particles, automation of solvent recovery to cut waste, and iterative improvement in product rinsing. These might seem like minor adjustments, yet together they create measurable improvements in reliability and usability.

    Practical Differences Over Similar Building Blocks

    Among all the azetidine derivatives available, it’s the substitution pattern at the nitrogen and the ring positions that set functional behavior apart. Unlike N-unsubstituted or N-methyl analogs, the N-benzyl group readily tolerates a wider range of chemical manipulation, allowing for selective transformations with predictable results. It also provides protection under acidic and some basic conditions, freeing up the user to introduce additional modifications elsewhere on the molecule.

    For customers evaluating between N-benzyl and N-Boc azetidinecarboxylic acids, empirical trials show that the benzyl variant survives a broader range of reductive and coupling conditions. In applications requiring deprotection, the benzyl can be removed via catalytic hydrogenation often much more selectively than the acid-sensitive carbamate group on N-Boc analogs.

    From an operational standpoint, our logistics teams frequently get feedback from formulation and API development labs that N-benzyl products ship and store with greater resilience. Boc-protected and N-unsubstituted acids can slowly hydrolyze or lose structure in humid environments, especially over months. Consistently, return rates and product complaints on our benzylated version remain well below industry average.

    Building Trust through Consistent Quality

    Our internal test panel includes not just the usual purity and identity checks, but also comparative assessment on solubility, crystallization, and moisture uptake. Users in pharmaceutical research report fewer issues with clumping or polymorphic changes, helping their teams focus on innovation rather than troubleshooting. Early-stage synthesis groups, CROs, and advanced material teams have commented that the lot-to-lot consistency of melting point and spectrum match reduces the need for re-purification, a tangible value-add for high-throughput workflows or urgent development campaigns.

    Because we're manufacturing at scale, we field a range of questions from groups in academia, publicly traded pharma, and private start-ups. Every conversation pushes us to improve, clarify, and document each step of our process, sharpening both our attention to detail and our ability to pass on savings or innovations directly.

    Supporting the Broader Research Community

    Our team frequently collaborates on method development and troubleshooting. Over the years, we've helped partners overcome solubility bottlenecks, improve assay reproducibility, and validate stability in blended formulations. Direct feedback led us to offer variant salt forms and to optimize particle size distributions for specialized applications.

    We maintain an open line with both chemical and business development teams, sharing insight from our own runs and learning from users' experiences. This partnership approach has sparked adjustments in drying times, led to new batch sizes, and influenced advances in quality controls.

    Advancing Both Science and Operations

    By remaining close to both production and user communities, we bring together long-term reliability and practical use. For us, it’s not just about making a product, but about providing consistency that scientists and process engineers can depend on. From nucleophilic substitution, protection-deprotection sequences, peptide conjugation, to custom derivatization, our 1-Benzyl-3-Azetidinecarboxylic Acid meets the test both in routine and frontier applications.

    Our group keeps investing in talent development, safety improvements, and green chemistry alternatives wherever possible. We have worked to replace some traditional chlorinated solvents with more sustainable options and keep reducing overall waste. Trials now underway are exploring new routes using renewable starting materials, aiming to lower carbon footprint even as we tighten qualitative controls.

    Looking to the Future

    The field of azetidine chemistry is evolving, with an increasing number of new drugs, agrochemicals, and advanced materials emerging from this class of heterocycles. As adoption grows, the pressure rises to deliver not just at the scale of milligrams or grams, but kilos and beyond. Our role, as we see it, is to anticipate shifts in demand, continually refine our processes, and work with users to enable both speed and predictability.

    As manufacturers, our reputation stands on the verifiable, real-world performance of every batch released. We commit to carrying out frequent review, internal sharing, and outside consultation to keep our methods and outcomes aligned with current expectations. The real measure lies in seeing chemists, engineers, and developers reach their next innovation with fewer roadblocks and more confidence.

    1-Benzyl-3-Azetidinecarboxylic Acid may be a single building block in a complex landscape, but it’s one built up through years of technical progress, transparent collaboration, and a focus on practical value. For those aiming to break new ground, having dependable, process-informed supply makes all the difference.