Semicontinuous Process for GMP Manufacture of a Carbapenem Intermediate via Carbene Insertion Using an Immobilized Rhodium Catalyst,Organic Process Research & Development

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Semicontinuous Process for GMP Manufacture of a Carbapenem Intermediate via Carbene Insertion Using an Immobilized Rhodium Catalyst
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-06-15 , DOI: 10.1021/acs.oprd.0c00133
James R. Gage _{1,

2} , Furong Chen _{1,

2} , Changming Dong _{1,

2} , Miguel A. Gonzalez _{1,

2} , Yong Jiang _{1,

2} , Yong Luo _{1,

2} , Mark D. McLaws _{1,

2} , Jian Tao _{1,

2}

Affiliation

A two-stage flow process for cGMP manufacture of a commercially important carbapenem intermediate was developed. Stage 1 featured an intramolecular N–H insertion reaction catalyzed by an immobilized rhodium catalyst. In stage 2, phosphorylation of the resulting keto ester intermediate afforded the target, which was isolated in batch mode. The equipment design and process control strategy leading to validation of the process at the 100 kg scale are discussed.

中文翻译：

使用固定化铑催化剂通过碳插入通过GMP生产中间体碳青霉烯的半连续工艺

开发了用于cGMP生产商业上重要的碳青霉烯中间体的两阶段流程。第一阶段的特点是固定化铑催化剂催化分子内NH插入。在阶段2中，所得酮酸酯中间体的磷酸化得到目标，将其以分批方式分离。讨论了设备设计和过程控制策略，以验证100千克规模的过程。

更新日期：2020-06-15

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