Methods for synthesis of substituted tetrahydrofuran compound
The invention includes inter alia new methods for preparation of the pharmaceutically active compound 2-(4-fluorophenoxymethyl)-5-(4-N-hydroxyureidyl-1-butynyl)-tetrahydrofuran and precursors thereof.
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(2008/06/13)
Synthesis of CMI-977, a potent 5-lipoxygenase inhibitor
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-γ-butyrolactone.
Cai, Xiong,Chorghade, Mukund S.,Fura, Aberra,Grewal, Gurmit S.,Jauregui, Karen A.,Lounsbury, Heather A.,Scannell, Ralph T.,Yeh, C. Grace,Young, Michelle A.,Yu, Shaoxia,Guo, Liang,Moriarty, Robert M.,Penmasta, Raju,Rao, Munagala S.,Singhal, Rajesh K.,Song, Zhengzhe,Staszewski, James P.,Tuladhar, Sudersan M.,Yang, Sanmin
p. 73 - 76
(2013/09/08)
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