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The Enantiopure Chiral Piperidine Building Block for BTK Inhibitors, Analgesics, and Neuroscience Research: (S)-1-Boc-3-hydroxypiperidine (CAS# 143900-44-1)

(S)-1-Boc-3-hydroxypiperidine (CAS# 143900-44-1), also known as (S)-N-Boc-3-hydroxypiperidine, (S)-tert-butyl 3-hydroxypiperidine-1-carboxylate, or (S)-1-Boc-3-piperidinol, is a chiral piperidine derivative with the molecular formula C₁₀H₁₉NO₃ and a molecular weight of 201.26 g/mol. Its molecular structure features a piperidine ring bearing a tert-butoxycarbonyl (Boc) protecting group at the nitrogen atom and a stereodefined hydroxyl group at the C3 position in the (S) configuration. As a white to tan powder or crystalline solid with a melting point of 34–40°C and a boiling point of 292.3±33.0°C, the compound exhibits solubility in methanol and common organic solvents, with an optical rotation of [α]²²/D +10.0° (c=1 in chloroform).

This enantiopure chiral building block is the validated (S)-enantiomer intermediate for Bruton’s tyrosine kinase (BTK) inhibitor manufacturing, most notably Ibrutinib (Imbruvica®). The compound’s defined stereochemistry is non-negotiable for downstream pharmaceutical activity, as racemic or (R)-enantiomer mixtures compromise API efficacy. Based on its chemical characteristics and industrial significance, this article systematically analyzes the key properties, core application areas, global market structure, regulatory landscape, and future outlook of this strategically important chiral piperidine building block.

Core Application Fields and Demand

Market demand for (S)-1-Boc-3-hydroxypiperidine (CAS# 143900-44-1) is concentrated in three primary sectors: pharmaceutical development and API manufacturing (approximately 65–70% of global consumption), organic synthesis and research (approximately 20–25%), and neuroscience and materials science research (approximately 5–10%). Its enantiopure (S)-configuration and versatile Boc-protected piperidine scaffold serve as the core drivers of sustained demand growth.

In pharmaceutical development and API manufacturing, (S)-1-Boc-3-hydroxypiperidine is the key chiral intermediate in the synthesis of Ibrutinib (Imbruvica®) , a first-in-class, potent, and irreversible inhibitor of Bruton’s tyrosine kinase (BTK). Ibrutinib was approved by the US Food and Drug Administration in 2013 for the treatment of mantle cell lymphoma, in 2014 for chronic lymphocytic leukemia, and in January 2015 for lymphoplasmacytic lymphoma. Dysregulation of the BTK signaling pathway is implicated in the survival and proliferation of malignant B-cells, making this target critically important in oncology. Beyond Ibrutinib, the compound serves as an important intermediate in the synthesis of various pharmaceuticals, particularly in the development of analgesics and anti-inflammatory drugs. It is also used in the preparation of biologically active compounds such as antagonists of the human P2X7 receptor. Piperidine derivatives exhibit many pharmacological activities and are characteristic substructures of many bioactive natural products, drugs, and drug candidates. With the expansion of Ibrutinib’s indications, (S)-1-Boc-3-hydroxypiperidine is considered a highly useful synthetic synthon in the pharmaceutical industry.

In organic synthesis and research, (S)-1-Boc-3-hydroxypiperidine serves as a versatile building block for creating more complex molecules, allowing chemists to explore new chemical pathways and develop innovative compounds. Its structural features—particularly the stereodefined hydroxyl group and the Boc-protected amine—make it an invaluable intermediate for the synthesis of complex, biologically active molecules. The compound is valuable in chiral synthesis due to its stereochemical properties, enabling the production of enantiomerically pure substances that are crucial in drug formulation.

In neuroscience and materials science research, researchers utilize (S)-1-Boc-3-hydroxypiperidine to investigate the role of piperidine derivatives in neurological processes, contributing to the understanding of neuropharmacology. The compound also finds applications in the development of new materials, particularly in creating polymers with specific properties. It is also used as a biochemical reagent for life science related research.

Major Market Participants

The global supply system for (S)-1-Boc-3-hydroxypiperidine (CAS# 143900-44-1) features a pattern of “specialized chiral building block suppliers, multinational chemical distributors, and Chinese manufacturers serving distinct market segments.” As a specialized chiral piperidine building block rather than a bulk commodity, the market is characterized by a moderate number of suppliers catering to pharmaceutical R&D, API manufacturing, and academic research.

In the global research and high-purity segment, key international suppliers include Thermo Fisher Scientific (Alfa Aesar), offering the compound at 97% purity; TCI Chemicals, providing >98.0% (GC) purity; Toronto Research Chemicals (TRC); Chem-Impex International, offering the compound under product number 28962; AKSci, offering 95% purity; and BOC Sciences. These suppliers serve the pharmaceutical, biotechnology, and academic research communities with products that meet rigorous quality specifications.

In the industrial and large-scale production segment, Chinese manufacturers have emerged as dominant players in the global supply chain. XinChem is a reliable manufacturer and supplier of high-purity (S)-1-Boc-3-hydroxypiperidine from China, offering the compound at 98–99% purity in packaging sizes ranging from grams to kilograms. Other Chinese suppliers are concentrated in major chemical manufacturing regions including Hubei, Shanghai, Shandong, Jiangsu, and Hebei. Chinese suppliers offer the compound at various purity grades (typically 97% to 99%) and packaging options, serving both domestic and export markets with competitive pricing. Bulk quantities are available with Certificates of Analysis confirming enantiomeric excess.

Regional Market Dynamics

The global (S)-1-Boc-3-hydroxypiperidine market exhibits distinct regional characteristics, with production concentrated in Asia-Pacific (particularly China) and consumption distributed across North America, Europe, and the Asia-Pacific region, aligned with the pharmaceutical, biotechnology, and academic research industries in these regions. The market is driven by the continued growth of targeted cancer therapies, particularly BTK inhibitors.

The Asia-Pacific region has emerged as a significant production hub for (S)-1-Boc-3-hydroxypiperidine, with China hosting numerous manufacturers and suppliers including XinChem. The region’s competitive advantages include lower production costs, established chemical infrastructure, and proximity to rapidly growing pharmaceutical industries. Chinese suppliers offer the compound at various purity grades and packaging options, serving both domestic and export markets. The growing pharmaceutical R&D and API manufacturing sectors in China, India, Japan, and South Korea continue to drive regional consumption growth.

North America remains a key market for high-purity and research-grade (S)-1-Boc-3-hydroxypiperidine, driven by demand from the pharmaceutical industry, biotechnology companies, and academic research institutions. The United States hosts numerous research organizations, pharmaceutical companies, and contract research organizations that require high-quality chiral building blocks for drug discovery, API manufacturing, and Ibrutinib-related research. The region’s well-established regulatory framework and emphasis on product quality support demand for high-grade research chemicals and pharmaceutical intermediates.

Europe is characterized by stringent regulatory requirements and a strong focus on quality and sustainability in pharmaceutical and chemical research. European pharmaceutical companies, research institutions, and API manufacturers demand high-purity chiral building blocks with comprehensive documentation. The region’s strong pharmaceutical and biotechnology sectors support steady demand for enantiopure piperidine derivatives.

Japan represents a specialized market where (S)-1-Boc-3-hydroxypiperidine is supplied by TCI Chemicals and other distributors for pharmaceutical research and API manufacturing applications.

Regulatory and Safety Considerations

As a pharmaceutical intermediate and research chemical, (S)-1-Boc-3-hydroxypiperidine (CAS# 143900-44-1) is subject to regulatory oversight in major global economies. Compliance with relevant regulations is essential for market access and trade.

In the United States, (S)-1-Boc-3-hydroxypiperidine is used as a pharmaceutical intermediate in API manufacturing. For Ibrutinib-related applications, the compound must meet ICH Q6A-compliant stereochemical purity standards to support ANDA/drug master file requirements. Achievable >99% enantiomeric excess via biocatalytic routes is available, with validated chiral HPLC methods for (R)-isomer quantification.

In the European Union, the compound must comply with REACH registration requirements for import and use. Manufacturers and suppliers must provide comprehensive Safety Data Sheets (SDS) and maintain appropriate documentation.

GHS classification and handling: (S)-1-Boc-3-hydroxypiperidine is classified with the signal word “Warning”. Hazard statements include H315 (Causes skin irritation), H319 (Causes serious eye irritation), and H335 (May cause respiratory irritation). Precautionary statements include P261, P264, P271, P280, P302+P352, P304+P340, P305+P351+P338, P403+P233, P405, and P501. The compound should be stored in a dry, dark place at room temperature for short-term storage (days to weeks) or at –20°C for long-term storage (months to years). Personal protective equipment including lab gloves, safety glasses, or face shields should be worn during handling, and good ventilation conditions should be maintained.

For international transport, (S)-1-Boc-3-hydroxypiperidine is not classified as hazardous material for DOT/IATA transport purposes. Proper packaging, labeling, and documentation are nevertheless required for international shipping in compliance with the International Maritime Dangerous Goods Code (IMDG Code) and other transport regulations.

Future Outlook

The market outlook for (S)-1-Boc-3-hydroxypiperidine is positive, supported by several key growth drivers across its major application segments. While the compound remains a relatively specialized chiral building block, its role as a key intermediate for Ibrutinib and other BTK inhibitors positions it for steady growth in the coming years.

Key growth drivers include:

  1. Expansion of BTK inhibitor therapeutics: The continued success of Ibrutinib and the development of next-generation BTK inhibitors for B-cell malignancies, autoimmune diseases, and inflammatory conditions drive demand for the key chiral intermediate.
  2. Growth in pharmaceutical R&D: Increasing investment in drug discovery and development, particularly in oncology, analgesics, and anti-inflammatory therapeutics, supports demand for versatile chiral piperidine building blocks.
  3. Expansion of biocatalytic production: The development of efficient, green enzyme-catalyzed synthesis methods for (S)-1-Boc-3-hydroxypiperidine using ketoreductases is improving production efficiency and sustainability.
  4. Increasing focus on chiral synthesis: The growing emphasis on stereochemically pure pharmaceutical compounds drives demand for enantiopure chiral building blocks like (S)-1-Boc-3-hydroxypiperidine.
  5. Expansion of neuroscience research: Growing interest in piperidine derivatives for neurological applications supports demand from academic and industrial research laboratories.

Challenges and considerations:

  • Regulatory compliance: Increasingly stringent pharmaceutical and chemical regulations may require ongoing investment in quality systems and documentation.
  • Stereochemical purity requirements: The specific requirement for the (S)-enantiomer (not the racemic mixture or (R)-enantiomer) necessitates rigorous quality control and enantiomeric purity assurance.
  • Competition from alternative synthetic routes: The market faces competition from alternative synthetic methods and chiral building blocks for BTK inhibitor synthesis.
  • Limited scale: As a relatively specialized compound, the market for (S)-1-Boc-3-hydroxypiperidine is smaller than that of commodity chemicals.

To succeed in this evolving market landscape, suppliers must focus on product quality (particularly enantiomeric purity, chemical purity, and batch-to-batch consistency), supply chain reliability, regulatory compliance, and responsive customer service. Companies that can offer high-purity products with comprehensive Certificates of Analysis (COA) confirming enantiomeric excess, flexible packaging options, and technical support for pharmaceutical applications will be well-positioned to capture growing demand.


Shanghai XinChem Co., Ltd. (XinChem)

As a world-leading supplier of organic chemicals and chiral building blocks, Shanghai XinChem Co., Ltd. (XinChem) is dedicated to meeting the innovative needs of the pharmaceutical, biotechnology, and fine chemical industries. Leveraging extensive experience and advanced manufacturing capabilities, XinChem provides high-quality (S)-1-Boc-3-hydroxypiperidine (CAS# 143900-44-1) to customers worldwide. As a trusted manufacturer and supplier based in China, XinChem combines competitive pricing, reliable supply, and exceptional service to establish itself as a preferred partner for research institutions, pharmaceutical companies, and API manufacturers seeking this versatile enantiopure chiral piperidine building block.

1. Technical Advantages

Advanced Synthesis and Purification Processes
XinChem utilizes state-of-the-art manufacturing facilities and rigorous quality control measures to ensure the purity, consistency, and safety of its (S)-1-Boc-3-hydroxypiperidine products. The production process incorporates advanced synthetic routes—including chemical resolution methods and biocatalytic ketoreductase-based synthesis—enabling the delivery of products with purity ≥98% to ≥99% (GC/HPLC) to meet diverse application requirements. Strict process control ensures consistent enantiomeric purity ((S)-configuration, >99% ee), minimal impurities, and batch-to-batch reproducibility, providing customers with reliable performance in pharmaceutical synthesis, API manufacturing, and research applications.

Full-Chain Quality Control
The production process strictly adheres to international quality standards, with comprehensive quality control covering raw material sourcing, in-process monitoring, and finished product testing. Each batch is accompanied by a detailed Certificate of Analysis (COA) documenting physical and chemical properties, purity data (GC/HPLC), enantiomeric excess, melting point, optical rotation, and impurity profiles. This commitment to quality ensures that XinChem’s (S)-1-Boc-3-hydroxypiperidine meets the stringent requirements of pharmaceutical R&D, API manufacturing, and research applications.

2. Product Advantages

High Purity and Consistent Quality
XinChem offers (S)-1-Boc-3-hydroxypiperidine with purity ≥98% to ≥99% (GC/HPLC) and enantiomeric excess >99% ee, ensuring optimal performance in pharmaceutical synthesis, API manufacturing, and research applications. The product’s high purity minimizes the risk of unwanted side reactions and impurities, making it suitable for demanding applications in drug discovery and pharmaceutical development.

Comprehensive Specifications
Key specifications include:

  • Molecular Formula: C₁₀H₁₉NO₃
  • Molecular Weight: 201.26 g/mol
  • CAS Number: 143900-44-1
  • Synonyms: (S)-N-Boc-3-hydroxypiperidine, (S)-tert-butyl 3-hydroxypiperidine-1-carboxylate, (S)-1-Boc-3-piperidinol
  • MDL Number: MFCD06659041
  • Appearance: White to tan powder or crystalline powder
  • Purity: ≥98% to ≥99% (GC/HPLC)
  • Enantiomeric Excess: >99% ee
  • Melting Point: 34–40°C
  • Optical Rotation: [α]²²/D +10.0° (c=1 in chloroform)
  • Storage: Dry, dark place; short-term at 0–4°C, long-term at –20°C

Flexible Packaging Solutions
XinChem provides a range of packaging options to accommodate diverse customer needs, from laboratory-scale quantities (grams) to industrial-scale packaging (kilograms) and bulk shipments. Customized packaging solutions are available upon request, ensuring safe handling, storage, and transportation.

3. Application Fields

As a versatile enantiopure chiral piperidine building block, (S)-1-Boc-3-hydroxypiperidine (CAS# 143900-44-1) exhibits wide application value across multiple industries:

Pharmaceutical Development and API Manufacturing:

  • Key chiral intermediate for Ibrutinib (Imbruvica®), a first-in-class BTK inhibitor for B-cell malignancies
  • Intermediate for analgesics and anti-inflammatory drugs
  • Building block for P2X7 receptor antagonists
  • Precursor for antiviral and antibacterial agents

Organic Synthesis and Research:

  • Versatile building block for creating complex molecules
  • Chiral synthesis for enantiomerically pure substances
  • Reagent for peptide and small molecule synthesis

Neuroscience Research:

  • Investigation of piperidine derivatives in neurological processes
  • Tool for neuropharmacology research

Materials Science:

  • Development of polymers with specific properties

Biochemical Research:

  • Biochemical reagent for life science research

4. Service Support

Technical Expertise and Customized Solutions
XinChem’s team of experienced chemists and pharmaceutical scientists provides full technical support throughout the customer journey—from product selection and specification development to application guidance and troubleshooting. Whether customers require optimization of synthetic routes, guidance on deprotection strategies, or assistance with regulatory documentation, XinChem’s technical experts are ready to help. Custom synthesis and contract manufacturing with flexible scaling from R&D to commercial quantities are available upon request.

Global Logistics and Reliable Supply
With established supply chains serving markets across Europe, North America, Asia-Pacific, and beyond, XinChem ensures timely delivery and consistent product availability. The company’s logistics team manages all aspects of international shipping, including customs clearance and documentation, with appropriate temperature control for product stability.

Regulatory Support
XinChem provides comprehensive documentation to support regulatory compliance, including Safety Data Sheets (SDS), Certificates of Analysis (COA), and other required certificates. The company stays current with evolving regulatory requirements in major markets, including REACH, TSCA, and other regional regulations, helping customers navigate the complexities of global trade.

5. Reasons to Choose XinChem

  • Professionalism: Extensive experience and deep expertise in chiral building block synthesis and supply.
  • Quality: Rigorous quality control, high purity (≥98% to ≥99%), >99% ee, and adherence to international standards.
  • Reliability: Stable supply, competitive pricing, and timely delivery.
  • Flexibility: Customized solutions to meet diverse customer needs, including custom synthesis and packaging.
  • Service: Responsive technical support and comprehensive documentation including COA confirming enantiomeric excess.

Contact us today to start your partnership with XinChem!

Website: www.xinchem.com

Email: sales1@xinchem.com

WhatsApp: +86 18049800532


Post time: Sep-01-2026