Rapid Development of a Commercial Process for Linrodostat, an Indoleamine 2,3-Dioxygenase (IDO) Inhibitor

Kenneth J. Fraunhoffer,Albert J. DelMonte,Gregory L. Beutner,Michael S. Bultman, Kathryn Camacho,Benjamin Cohen,Darryl D. Dixon,Yu Fan,Dayne Fanfair,Adam J. Freitag,Andrew W. Glace,Francisco Gonzalez-Bobes,Manjunath Gujjar,Matthew W. Haley,Matthew R. Hickey, Jeanne Ho,Vidya Iyer,Prantik Maity, Sunil Patel,Victor W. Rosso,Michael A. Schmidt,Jason M. Stevens,Yichen Tan, Christopher Wilbert,Ian S. Young, Miao Yu

Organic Process Research & Development（2019）

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摘要

The process development and the kilogram-scale synthesis of linrodostat (BMS-986205, 1) are described. The synthesis features several highly efficient telescoped processes and the use of Evans auxiliary to install a methyl-bearing stereocenter. The target was prepared in 12 steps with 7 isolations in an overall yield of 31%.

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关键词

SNAr,chiral auxiliary,TCFH,methylation,sulfolane

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