期刊
ORGANIC PROCESS RESEARCH & DEVELOPMENT
卷 25, 期 3, 页码 529-540出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.oprd.0c00486
关键词
catalysis; C-H functionalization; iridium; borylation
This paper presents an improved and scalable method for manufacturing nemiralisib, a phosphatidylinositol-3-kinase delta inhibitor. By incorporating three consecutive catalytic reactions, including a palladium-catalyzed C-H functionalization and an iridium-catalyzed borylation, the synthetic sequence was significantly simplified and shortened. The revised route was successfully implemented in a pilot plant on a multikilogram scale to deliver over 100 kg of product.
This paper describes the development of an improved and scalable method for the manufacture of nemiralisib, a phosphatidylinositol-3-kinase delta inhibitor. Incorporation of three consecutive catalytic reactions, including a palladium-catalyzed C-H functionalization and an iridium-catalyzed borylation, significantly simplified and shortened the synthetic sequence. The revised route was successfully implemented in a pilot plant on a multikilogram scale to deliver >100 kg of product.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据