A scalable chemoenzymatic process for 7-amino-3-[Z-2-(4-methylthiazol-5-yl)vinyl]-3-cephem-4-carboxylic acid (ATCA)

被引：0
|
作者：
Chun Hui Gao
Cheng Guo Jia
Wei Li
Yue Zhang
Yi Feng Yu
机构：
[1] Hebei University of Science and Technology,School of Chemical Engineering
[2] Brant Pharmaceuticals Co.,Department of R&D
[3] Ltd.,undefined
来源：
Research on Chemical Intermediates | 2013年 / 39卷
关键词：
Cefditoren pivoxil; ATCA; Deprotection; Trichloroacetic acid; Immobilized penicillin acylase; Process;
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摘要：
An efficient chemoenzymatic process has been developed for preparation of 7-amino-3-[Z-2-(4-methylthiazol-5-yl)vinyl]-3-cephem-4-carboxylic acid, featuring removal of para-methoxybenzyl by trichloroacetic acid and cleavage of phenylacetyl E-isomer by immobilized penicillin acylase enzyme. The E-isomer of 7-amino-3-[Z-2-(4-methylthiazol-5-yl)vinyl]-3-cephem-4-carboxylic acid could be easily decreased to less than 0.2 % by salt formation. Importantly, trichloroacetic acid and immobilized penicillin acylase enzyme could be recovered and reused. The enzyme reaction could be run in a flow reactor. Only two crystallizations are involved as the purification procedure in the six-step sequence.
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页码：3911 / 3917
页数：6
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