Synthesis of CMI-977, a potent 5-lipoxygenase inhibitor

被引：31

作者：

Cai, X

Chorghade, MS

Fura, A

Grewal, GS

Jauregui, KA

Lounsbury, HA

Scannell, RT

Yeh, CG

Young, MA

Yu, SX

Guo, L

Moriarty, RM

Penmasta, R

Rao, MS

Singhal, RK

Song, ZZ

Staszewski, JP

Tuladhar, SM

Yang, SM

机构：

[1] CytoMed Inc, Cambridge, MA 02139 USA

[2] Steroids Ltd, Chicago, IL 60612 USA

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 1999年 / 3卷 / 01期

关键词：

D O I：

10.1021/op980209l

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

CMI-977 is a potent 5-lipoxygenase inhibitor that intervenes in the production of leukotrienes and is presently being developed for the treatment of chronic asthma, It is a single enantiomer with an all-trans (2S,5S) configuration, Of the four isomers of CMI-977, the S,S isomer was found to have the best biological activity and was selected for further development. The enantiomerically pure product was synthesized on a 2-kg scale from (S)-(+)-hydroxymethyl-gamma-butyrolactone.

引用

页码：73 / 76

页数：4

共 11 条

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[2]

CAI X, 1997, 214 NAT M AM CHEM SO

[3]

CARTER GW, 1991, J PHARMACOL EXP THER, V256, P929

[4] TOTAL SYNTHESIS OF (+/-)-FUMAGILLIN [J].