A convenient synthesis of the enantiomerically pure β-blocker (S)-betaxolol using hydrolytic kinetic resolution

RA Joshi, DR Garud, M Muthukrishnan, RR Joshi…

Index: Joshi, Ramesh A.; Garud, Dinesh R.; Muthukrishnan; Joshi, Rohini R.; Gurjar Tetrahedron Asymmetry, 2005 , vol. 16, # 23 p. 3802 - 3806

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Citation Number: 22

Abstract

To the best of our knowledge, there are only two reports on the asymmetric synthesis of (S)-betaxolol 1, one is a lipase catalysed chemoenzymatic route 7 and the other involves asymmetric synthesis starting from oxazolidinone derivative. 8a In the chemoenzymatic method, the enantiomeric excess of (S)-betaxolol was 82%, which was further improved to 91% ee after crystallising its hydrochloride salt. On the other hand, asymmetric synthesis using an oxazolidinone derivative has ...

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