Oxidative removal of p-methoxybenzyl-amino protecting group in the presence of a proximal hydroxy function:: A solution to a process problem in SUSTIVA® (efavirenz) synthesis

被引：4

作者：

Choudhury, A ^{[1
]}

Pierce, ME ^{[1
]}

Confalone, PN ^{[1
]}

机构：

[1] Dupont Pharmaceut Co, Proc Res Facil, Chem Proc R&D Dept, Deepwater, NJ 08023 USA

来源：

SYNTHETIC COMMUNICATIONS | 2001年 / 31卷 / 23期

关键词：

D O I：

10.1081/SCC-100107021

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A practical and scaleable synthetic procedure for the deprotection of a p-methoxy benzyl group from the tertiary carbinol 2 in the commercial synthesis of SUSTIVA (R) (efavirenz) I is described. The methodology involves a two step, one pot operation with an isolated yield of 82.5% with a product purity of > 99.5%.

引用

页码：3707 / 3714

页数：8

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