|
Org. Process Res. Dev. 2020, 24, 2478. DOI: 10.1021/acs.oprd.0c00252 ◆The requirement for a greater excess of EF and KOt-Bu in the batch−batch process was attributed to the unproductive consumption of EF by KOt-Bu ◆The team developed a flow process leading to a significantly greener process. As an added benefit, the newly developed flow−batch process is more robust and can tolerate a wide range of conditions ◆Using less EF and KOt-Bu ensured less alkoxide was left in the solution at the end of formylation and that guanidine was less likely to be converted to biguanide and, ultimately, triazine byproduct (5). The number of equivalents of KOt-Bu required to drive the reaction to completion was decreased from 2.25 to 1.4 (a 38% reduction), the number of equivalents of EF from 2.0 to 1.3 (a 35% reduction), and the number of equivalents of G·HCl from 8.0 to 4.0 (a 50% reduction). 招聘上海合成工艺研究员 设计、优化I类新药的工艺合成路线，各反应条件、参数，包括后处理，撰写报告、跟踪并解决GMP生产技术问题 待遇从优，有意向请直接联系我！18521511651（微信同号）
|
|
|
