柯蒂斯重排
试剂
过程开发
人类免疫缺陷病毒(HIV)
化学
组合化学
格氏试剂
过程(计算)
有机化学
计算机科学
医学
工艺工程
病毒学
工程类
程序设计语言
作者
Michael A. Ischay,Brittanie Hoang,Dietrich Steinhuebel,Matthew R. Chin,Darryl D. Dixon,Danielle Elfgren,Lars V. Heumann,Willard Lew,Devon A. Mundal,Sean Neville,Nisha P. Shah,Bing Shi,Jonathan C. Tripp,Queenie Wang
标识
DOI:10.1021/acs.oprd.2c00153
摘要
Compound 1 is a densely functionalized iminohydantoin that possesses a quaternary stereocenter and is under development as an HIV protease inhibitor. Key challenges that are discussed include the preparation of a neopentyl Grignard reagent via magnesium insertion, development of a one-pot Curtius reaction that generated a volatile isocyanate and was trapped with an alcohol, and removal of a CBz protecting group to isolate a succinate salt. This study describes process development efforts that enabled the first scale-up of 1.
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