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Identification and Elimination of an Unexpected Catalyst Poison in Suzuki Coupling
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2017-12-13 00:00:00 , DOI: 10.1021/acs.oprd.7b00342
Jing Liu 1 , Kyle Kimmel , Kimkim Dao 1 , Yang Liu 2 , Ming Qi
Affiliation  

A Suzuki coupling reaction gave an uncharacteristically low conversion in a GMP campaign. Initial investigation revealed a palladium catalyst poison in the starting material. A temporary solution was developed along with contingency plans to enable successful material delivery. Further systematic studies led to the identification of elemental sulfur as the culprit. A “sulfur-free” synthesis of the starting material was developed for the next round of manufacturing.

中文翻译:

铃木联轴器中意外催化剂毒物的鉴定和消除

铃木偶联反应在GMP运动中转化率异常低。初步调查显示,原料中存在钯催化剂毒物。开发了一个临时解决方案以及应急计划,以确保成功交付物料。进一步的系统研究导致将元素硫鉴定为罪魁祸首。为下一轮生产开发了原材料的“无硫”合成方法。
更新日期:2017-12-13
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