Chirality is a fundamental feature of biological systems and a critical consideration in modern drug discovery. Asymmetric synthesis, the selective construction of specific stereoisomers, is essential for optimizing the pharmacological potency and metabolic stability of drug candidates while minimizing off-target effects caused by unwanted enantiomers. BOC Sciences offers comprehensive asymmetric synthesis services, leveraging advanced chemocatalysis, biocatalysis, and chiral pool strategies. We assist medicinal chemists in accessing complex Chiral Building Blocks, scaffolds, and APIs with high enantiomeric excess (ee) and diastereomeric ratios (dr). From route scouting to gram-scale delivery, our solutions accelerate the development of stereochemically complex molecules.
We design and evaluate concise synthetic routes to establish chiral centers efficiently. Our team prioritizes convergent strategies that maximize atom economy and yield, utilizing retrospective analysis to identify the most viable precursors and stereoselective steps for your target molecules.
Access our extensive library of chiral ligands and transition metal catalysts. We perform high-throughput screening to identify optimal reaction conditions that achieve superior stereocontrol, ensuring high ee values for challenging substrates.
Beyond de novo synthesis, we offer classical resolution via diastereomeric salt formation and enzymatic kinetic resolution. We also provide preparative chiral chromatography services to isolate pure enantiomers from racemic mixtures for biological evaluation.
BOC Sciences delivers expert stereoselective synthesis services with guaranteed optical purity to support your lead optimization and SAR studies.
Utilizing Rh, Ru, and Ir complexes with chiral phosphine ligands, we perform enantioselective reduction of prochiral olefins, ketones, and imines. This method is highly scalable and efficient for generating chiral amines and alcohols.
We employ small organic molecules (e.g., proline derivatives, chiral phosphoric acids) to catalyze reactions without transition metals. This approach is ideal for avoiding metal contamination and enabling unique activation modes for C-C and C-heteroatom bond formation.
Leveraging engineered enzymes (ketoreductases, transaminases, lipases), we achieve exquisite selectivity under mild conditions. Biocatalysis is particularly effective for highly functionalized molecules where chemocatalysis may lack selectivity.
We utilize stoichiometric chiral auxiliaries (e.g., Evans oxazolidinones, Myers pseudoephedrine) to induce stereochemistry. This reliable method is excellent for early-stage discovery when catalyst screening time is limited.
Our team explores cutting-edge enantioselective C-H functionalization strategies to introduce chirality directly onto unfunctionalized hydrocarbons, shortening synthetic sequences and enabling access to novel chemical space.
BOC Sciences supports the synthesis of diverse chiral architectures essential for modern pharmaceutical research.
Submit your target structure and specifications. Our chemistry team will propose the most efficient stereoselective route tailored to your research timeline.
We analyze the target structure to identify potential chiral disconnection points. A proposal is generated outlining the synthetic strategy, timeline, and cost.
For challenging transformations, we screen a matrix of catalysts, ligands, solvents, and temperatures to optimize yield and enantioselectivity (ee).
Our chemists execute the synthesis, applying crystallization or chiral chromatography if necessary to upgrade optical purity to project specifications.
Compounds are delivered with a full Certificate of Analysis (CoA), including NMR, MS, and chiral HPLC traces proving identity and stereochemical purity.
We rapidly synthesize focused libraries of stereoisomers to help you determine the eutomer (active enantiomer) and explore Structure-Activity Relationships (SAR) related to stereochemistry. Our speed enables quick iteration cycles in early discovery.
As structures become more complex, we develop robust asymmetric routes to access advanced leads. We focus on establishing scalable chemistry early, avoiding "dead-end" routes that rely on unsustainable resolutions or scarce starting materials.
For candidates advancing to toxicity studies, we redesign synthetic pathways to replace expensive reagents or hazardous steps with cost-effective, catalytic asymmetric methods suitable for kilogram-scale production.
When asymmetric synthesis is not immediately feasible, we provide efficient classical or kinetic resolution services. We screen resolving agents to separate enantiomers quickly, providing material for initial biological testing.
Partner with BOC Sciences to solve your most complex stereochemical challenges. From quaternary centers to multiple chiral axes, our asymmetric synthesis expertise ensures you get the right isomer, on time, with high purity.
We strive for perfection in stereocontrol. Our optimization protocols are designed to achieve >98% ee, reducing the need for difficult downstream purification and maximizing overall yield.
Our team is proficient in the "toolbox" of modern asymmetric synthesis: transition metal catalysis, organocatalysis, and biocatalysis, allowing us to choose the best tool for your specific molecule.
We possess a comprehensive suite of chiral analytical instruments. We develop robust methods to separate enantiomers, ensuring that the data you receive is accurate and reproducible.
We understand the value of your proprietary structures. All synthesis is conducted under strict confidentiality agreements, and we support the generation of data for your patent filings.
Client Challenge: A biotech client needed a key intermediate containing a sterically hindered quaternary carbon center. Previous attempts using chiral auxiliaries resulted in poor yields and low diastereoselectivity (dr < 3:1), stalling the project.
Technical Obstacles: The steric bulk of the substrate prevented effective approach of standard reagents. The separation of diastereomers was difficult via standard flash chromatography.
Our Solution:BOC Sciences engineered a robust asymmetric phase-transfer catalysis (PTC) strategy to tackle the sterically congested center. By systematically screening our proprietary library of Cinchona alkaloid-derived quaternary ammonium salts, we identified a specific catalyst that provided precise facial discrimination. We further optimized reaction kinetics through solvent-base modulation, successfully establishing the difficult quaternary stereocenter with high efficiency.
Outcome: We successfully synthesized the intermediate with 95% yield and >20:1 dr. The optimized route eliminated two synthetic steps compared to the original auxiliary route, rapidly advancing the client's lead optimization program.
Client Challenge: A pharmaceutical company required a highly pure chiral alcohol intermediate. The chemical reduction route utilized hazardous reagents and produced heavy metal waste, which was not ideal for their long-term sustainability goals.
Technical Obstacles: The ketone substrate was sensitive to harsh acidic/basic conditions, leading to degradation during traditional workups. Chemoselectivity was also an issue due to other reducible groups on the molecule.
Our Solution: Leveraging our advanced biocatalysis platform, we screened an extensive panel of Ketoreductases (KREDs) to replace the hazardous metal-hydride route. We pinpointed a specific enzyme variant that exhibited 100% chemoselectivity towards the target ketone while leaving other reducible functionalities intact, and established an efficient cofactor recycling system to ensure economic viability and process sustainability.
Outcome: Delivered the chiral alcohol with >99% ee and established a "green" process. The biocatalytic route simplified the workup significantly, ensuring high recovery of the sensitive product.
Client Challenge: A client needed to scale up the synthesis of a chiral amine from milligrams to 500 grams for animal studies. The original route relied on chiral HPLC separation, which was cost-prohibitive and slow at that scale.
Technical Obstacles: Developing a scalable asymmetric synthesis in a short timeframe. The substrate had low solubility in preferred hydrogenation solvents.
Our Solution: To address scalability and cost challenges, our process chemists redesigned the synthetic route using Asymmetric Transfer Hydrogenation (ATH) with a tethered Ruthenium (Ru) complex. We performed rigorous Design of Experiments (DoE) to optimize solvent effects and hydrogen donor ratios, successfully transitioning the process from a chromatography-dependent workflow to a streamlined, crystallization-driven isolation suitable for multi-hundred gram production.
Outcome: We delivered 500g of the target amine with 98.5% ee within 6 weeks. This transition from chromatographic resolution to asymmetric catalysis reduced the cost per gram by 60%.
Asymmetric synthesis typically employs catalyst-controlled, chiral auxiliary, or substrate-controlled strategies to achieve high stereoselectivity. BOC Sciences has extensive experience in asymmetric synthesis and can provide customized strategy design based on target molecule structure, optimizing chiral center construction to efficiently obtain the desired stereochemistry.
Enhancing chiral selectivity relies on catalyst design, solvent choice, and reaction condition optimization. BOC Sciences offers a variety of metal and organocatalyst systems and can perform high-throughput screening and reaction optimization to significantly improve product stereoselectivity and yield for diverse synthetic needs.
Asymmetric synthesis is typically suitable for substrates with reactive functional groups or those capable of forming chiral centers, such as aldehydes, ketones, and alkenes. BOC Sciences can assess complex substrates and provide customized reaction route design to achieve efficient stereocontrol of challenging molecules.
The type, configuration, and concentration of catalysts decisively affect stereoselectivity and reaction efficiency in asymmetric synthesis. BOC Sciences provides a rich library of chiral metal and organocatalysts and can perform customized catalyst screening and optimization to ensure high selectivity and scalable synthetic solutions.
Synthesizing complex chiral molecules involves constructing multiple stereocenters with precise stereocontrol. BOC Sciences integrates multi-step asymmetric strategies and finely tunes reaction conditions, offering feasibility analysis and technical support to enable efficient, high-quality stereosynthesis of complex targets.
We were stuck on a chiral separation for months. BOC Sciences proposed an asymmetric synthesis route that not only solved the purity issue but also improved our overall yield. Their chemistry team is truly top-notch.
— Dr. James, Medicinal Chemistry Lead, Biotech Startup
The chiral building blocks we ordered were delivered on time and exceeded our purity specifications. The accompanying analytical data was comprehensive and gave us full confidence in the materials.
— Dr. Emily, Senior Scientist, Research Institute
Throughout the catalyst screening project, the BOC Sciences team kept us informed with weekly updates. Their transparency and technical insights helped us make quick decisions on route selection.
— Dr. Thomas, Director of Chemistry, Pharma Company
Transitioning our bench-scale synthesis to a scalable asymmetric process was seamless with BOC Sciences. They handled the optimization expertly, delivering the gram-scale quantities we needed for our in vivo studies.
— Dr. Olivia, VP of R&D, Biopharma Developer
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