A practical and improved synthesis of (3S,5S)-3-[(tert-butyloxycarbonyl)methyl]- 5-[(methanesulfonyloxy)methyl]-2- pyrrolidinone |
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| Authors: | Yee Nathan K Dong Yong Kapadia Suresh R Song Jinhua J |
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| Institution: | Department of Chemical Development, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, Connecticut 06877-0368,USA. nyee@rdg.boehringer-ingelheim.com |
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| Abstract: | A practical and improved synthesis of (3S,5S)-3-(tert-butyloxycarbonyl)methyl]-5-(methanesulfonyloxy)methyl]-2-pyrrolidinone (1) is described. The key transformations involve a highly efficient reaction sequence consisting of ethoxycarbonylation, alkylation, hydrolysis, and decarboxylation to produce compound 10. The process described herein is practical, robust, and cost-effective, and it has been successfully implemented in a pilot plant to produce a multikilogram quantity of mesylate 1. |
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