Synthesis of CMI-977, a Potent 5-Lipoxygenase Inhibitor

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• 作者：Xiong Cai ; Mukund S. Chorghade ; Aberra Fura ; Gurmit S. Grewal ; Karen A. Jauregui ; Heather A. Lounsbury ; Ralph T. Scannell ; C. Grace Yeh ; Michelle A. Young ; Shaoxia Yu ; Liang Guo ; Robert M. Moriarty ; R
• 刊名：Organic Process Research & Development
• 出版年：1999
• 出版时间：January 1999
• 年：1999
• 卷：3
• 期：1
• 页码：73 - 76
• 全文大小：103K
• 年卷期：v.3,no.1(January 1999)
• ISSN：1520-586X

文摘

CMI-977 is a potent 5-lipoxygenase inhibitor that intervenesin the production of leukotrienes and is presently beingdeveloped for the treatment of chronic asthma. It is a singleenantiomer with an all-trans (2S,5S) configuration. Of the fourisomers of CMI-977, the S,S isomer was found to have the bestbiological activity and was selected for further development.The enantiomerically pure product was synthesized on a 2-kgscale from (S)-(+)-hydroxymethyl--butyrolactone.