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对映体拆分消旋体苯恶洛芬的改进、高效、简易方法:一种非甾体类抗炎药(NSAID)。

Improved, Efficient, and Simple Methodology for the Resolution of Racemic Benoxaprofen: A Nonsteroidal Anti-Inflammatory Drug (NSAID).

机构信息

Chemical Research Department, APL Research Centre-II, Aurobindo Pharma Limited, Hyderabad, Telangana, India.

Department of Engineering Chemistry, A. U. College of Engineering (A), Andhra University, Visakhapatnam, Andhra Pradesh, India.

出版信息

Chirality. 2024 Sep;36(9):e23713. doi: 10.1002/chir.23713.

Abstract

The present article discloses an improved, efficient, and simple resolution methodology for the preparation of (S)-benoxaprofen which is a nonsteroidal anti-inflammatory drug (NSAID). The resolution of racemic benoxaprofen uses an easily available, efficient, recoverable, and cost-effective chiral reagent, namely, (1R,2S)-(+)-cis-1-amino-2-indanol. This novel resolution process is having a very high purity of (S)-benoxaprofen, greater than 99%, substantially free from (R)-benoxaprofen (less than 1%).

摘要

本文公开了一种改进的、高效的、简单的(S)-苯恶洛芬的拆分方法,(S)-苯恶洛芬是一种非甾体抗炎药(NSAID)。外消旋苯恶洛芬的拆分使用了一种易得、高效、可回收且经济高效的手性试剂,即(1R,2S)-(+)-顺-1-氨基-2-茚醇。这种新型拆分工艺得到的(S)-苯恶洛芬纯度非常高,大于 99%,基本上不含(R)-苯恶洛芬(小于 1%)。

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