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). TCI Chemicals offers the compound at >98.0% purity with a melting point of 52.0–56.0°C and a specific rotation of +20.0 to +23.0° (c=5, MeOH), demonstrating the availability of ultra-high-purity grades for demanding pharmaceutical applications.

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. The specific (S)-stereochemistry of the hydroxyl group at the C3 position is crucial for the biological activity of the final drug molecule. 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. Piperidine derivatives exhibit many pharmacological activities and are characteristic substructures of many bioactive natural products, drugs, and drug candidates. The compound is also used in the preparation of antagonists of the human P2X7 receptor, an ATP-gated ion channel heavily involved in inflammatory and immune responses, as well as selective irreversible inhibitors for Bruton’s tyrosine kinase. With the expansion of Ibrutinib’s indications, including chronic lymphocytic leukemia and lymphoplasmacytic lymphoma, (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 scaffold is commonly used in kinase inhibitor design, GPCR modulator development, and lead optimization programs. The compound also finds applications in the development of new materials, particularly in creating polymers with specific properties.

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 ≥99% chiral purity; AKSci, offering 95% purity; and BOC Sciences. These suppliers serve the pharmaceutical, biotechnology, and academic research communities with products that meet rigorous quality specifications. MuseChem offers the compound at ≥95% purity, while Apollo Scientific supplies 98% purity material.

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 include AstaTech (Chengdu) Pharmaceutical Co., Ltd., Cangzhou Enke Pharma-tech Co., Ltd., Suzhou Lipin Chemical Co., Ltd., Shenzhen Feisi Biotechnology Co., Ltd., and Shaanxi BLOOM Tech Co., Ltd.. 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 broader 1-Boc-3-hydroxypiperidine market was valued at USD 0.12 billion in 2024 and is projected to reach USD 0.25 billion by 2034, registering a compound annual growth rate of 7.5%. 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. Chinese market research reports indicate extensive analysis of the (S)-1-Boc-3-hydroxypiperidine industry through 2030.

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. Suppliers such as AKSci stock and ship products from the SF Bay Area, California.

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. TCI Chemicals and other distributors serve the European market with in-stock availability.

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. The compound is not classified as hazardous material for DOT/IATA transport.

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) and H319 (Causes serious eye irritation). Precautionary statements include P264 (Wash skin thoroughly after handling), P280 (Wear protective gloves/eye protection/face protection), P305+P351+P338 (IF IN EYES: Rinse cautiously with water for several minutes; remove contact lenses if present and easy to do; continue rinsing), and P302+P352 (IF ON SKIN: Wash with plenty of soap and water). The compound should be stored in a cool, dark place at room temperature (recommended <15°C), or long-term at –20°C. Personal protective equipment including lab gloves and safety glasses 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. The HS number for the compound is 2933.39.9200.

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. Asymmetric reduction methods can theoretically convert 100% of the substrate to the desired (S)-enantiomer with >99% enantiomeric excess.
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 P2X7 receptor research: The P2X7 receptor’s involvement in inflammatory and immune responses makes antagonists of significant therapeutic interest, supporting demand for the compound as a key intermediate.

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: MFCD04115306
• 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 room temperature (<15°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
• Scaffold for kinase inhibitor design and GPCR modulator development

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

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

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