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Sabinsa – “Chiral Pool” Approach for enantiomeric intermediates: a powerful, simple, and economic solution

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Abstract

In the last few years, increased demand for enantiopure products in pharmaceutical, agrochemical, flavor and fragrance industry has led to renaissance of several asymmetric synthesis methods in both industry and academic research. When it comes to effective conversion of naturally occurring chiral materials (amino acids and sugars, often referred as “Chiral Pool”) into enantiomerically pure intermediate compounds, it is considered as the most economic, robust and scalable option to date. Several chiral intermediate products have been successfully developed from the chiral pool amino acids and sugars, which are of high-quality pharmaceutical and fine chemical grade, and many of these intermediates form a part of several drugs and investigational drug molecules


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INTRODUCTION

Most active drugs are in the chiral form due to the presence of one or more asymmetrically tetrahedral carbon atoms. Single enantiomers may have lesser adverse drug reactions, improved therapeutic profile and fewer chances of drug interactions than racemic mixtures, and hence they are pharmacologically different (1). Thus, with recent developments in science and technology, chiral intermediates are used as building blocks for many pharmaceuticals, agrochemicals, flavor and fragrance, and other fine chemical industries2. A brief note on the conversion chemistry of amino acids or sugars to enantiopure intermediates is provided below.


CHIRAL INTERMEDIATES

(S)-2-Amino γ-Butyrolactone Hydrochloride (1) is obtained with very high ...




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