An Efficient, Economical Synthesis of the Novel Anti-tumor Agent CPI-613

被引：9

作者：

Gibson, Frank S. ^{[1
]}

Gupta, Deepak ^{[1
]}

Shorr, Robert ^{[1
]}

Rodriguez, Robert ^{[1
]}

机构：

[1] Cornerstone Pharmaceut, Cranbury, NJ 08512 USA

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2011年 / 15卷 / 04期

关键词：

ALPHA-LIPOIC ACID; PREVENTION;

D O I：

10.1021/op200091t

中图分类号：

O69 [应用化学];

学科分类号：

070301 [无机化学];

摘要：

An efficient and practical synthesis of the novel anti-tumor compound 6,8-dithiobenzyl octanoic acid, CPI-613 (2), was developed and executed on a practical scale. CPI-613 can be made in a single vessel from (+/-)-lipoic acid (1) via reductive opening of the disulfide ring followed by benzylation of the sulfhydryls with benzyl bromide. CPI-613 was isolated by simple crystallization in high yield and purity. The process is scaleable and has been demonstrated at up to 100 kg.

引用

页码：855 / 857

页数：3

共 9 条

[1]

Carlson David A., 2008, V24, P235

[2]

Antioxidant Properties of an Endogenous Thiol: Alpha-lipoic Acid, Useful in the Prevention of Cardiovascular Diseases [J].