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

被引：1
|
作者：
Gao, Chun Hui [1 ]
Jia, Cheng Guo [2 ]
Li, Wei [2 ]
Zhang, Yue [1 ]
Yu, Yi Feng [1 ]
机构：
[1] Hebei Univ Sci & Technol, Sch Chem Engn, Shijiazhuang 050018, Hebei, Peoples R China
[2] Brant Pharmaceut Co Ltd, Dept R&D, Shijiazhuang 050000, Hebei, Peoples R China
来源：
RESEARCH ON CHEMICAL INTERMEDIATES | 2013年 / 39卷 / 08期
关键词：
Cefditoren pivoxil; ATCA; Deprotection; Trichloroacetic acid; Immobilized penicillin acylase; Process; ORAL ACTIVITY; ME1207;
D O I：
10.1007/s11164-012-0907-0
中图分类号：
O6 [化学];
学科分类号：
0703 ;
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：7
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