Asymmetric Hydrogenation Platform

Asymmetric Hydrogenation Platform

Chiral compounds are active ingredients in many small-molecule drugs, so the controlled synthesis of chiral molecules has become a key step in drug development. BOC Sciences has the world's leading asymmetric hydrogenation technology platform, which can provide efficient synthesis services for chiral intermediates and APIs. We also have hydrogenation reactors of different capacities from laboratory small scale to pilot scale to commercial production to meet production needs of various scales.

Asymmetric Hydrogenation Platform

Chiral compounds exhibit different properties in terms of steric selectivity, reactivity with chiral substances, and optical activity. Its synthesis methods mainly include natural extraction, resolution, enzymatic method and asymmetric hydrogenation synthesis. Among many synthetic methods, asymmetric hydrogenation has the advantages of high efficiency, economy and environmental protection, and also meets the current concept of green chemistry. It is for this reason that we focus on the research of asymmetric hydrogenation and build asymmetric hydrogenation platform for the synthesis of chiral molecules.

Efficient Catalyst Production

BOC Sciences has developed various types of efficient and highly selective catalysts for asymmetric hydrogenation, and further utilizes these catalysts to complete the synthesis of chiral compounds. Our chemical engineering and process research departments have dedicated organometallic chemists with extensive screening expertise. In addition, we are equipped with specialized equipment capable of efficiently producing large quantities of chiral ligands and catalysts.

Asymmetric hydrogenation of 2-amidoacrylates catalyzed bydifferent transition-metals. Fig.1 Asymmetric hydrogenation of 2-amidoacrylates catalyzed bydifferent transition-metals.[1]

Using asymmetric hydrogenation technology, we have innovatively optimized the synthetic route of a series of pharmaceutical intermediates, such as: asymmetric synthesis of levodopa, aliskiren, pregabalin, duloxetine, ramipril, sitagliptin, taranabant and other intermediates.

BOC Sciences' proprietary catalyst production line reduces project costs and greatly increases operational freedom when developing synthetic routes for pharmaceutical intermediates. In addition, chiral catalysts have air sensitivity and require high temperature and humidity, so it is difficult to control the reaction stability when expanding the scale. Combining the catalyst characteristics and production process, BOC Sciences is equipped with equipment related to anhydrous and oxygen-free operation, to ensure the stable supply of catalysts while promoting the project in an orderly manner.

Examples of types of catalytic reactions

  • Ketones
  • Imines
  • Olefins
  • α-Dehydroamino acids and their derivatives
  • β-Carbonyl esters
  • Heteroaromatics
  • Unsaturated carboxylic acids
  • (+) - Biotin

Focus on Efficient Chemical Syntheses

Constrained by economics and processing cost-effectiveness, our project team opted for a direct method of synthesizing the desired chemical intermediates. For chiral drugs, our mission is to incorporate asymmetric hydrogenation into every development stage of drug candidate synthesis, from preclinical research all the way to those stages of commercialization. Focusing on overall synthetic efficiency, BOC Sciences developed the concept of "fitting catalytic steps to the process" to rapidly screen a large number of available chiral catalysts with a minimum of valuable intermediates.

If you are interested in our asymmetric hydrogenation platform, please contact us immediately.

Reference

  1. Yawen Hu, et al. Nickel-Catalyzed Asymmetric Hydrogenation of 2-Amidoacrylates[J]. Angewandte Chemie, 2019.

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