Efficient and Scalable Enantioselective Synthesis of a CGRP Antagonist
- David K. Leahy (2042089)
- Yu Fan (111503)
- Lopa V. Desai (2042092)
- Collin Chan (2042083)
- Jason Zhu (2042095)
- Guanglin Luo (1399393)
- Ling Chen (25698)
- Ronald L. Hanson (1508707)
- Masano Sugiyama (1804990)
- Thorsten Rosner (1504984)
- Nicolas Cuniere (2042086)
- Zhiwei Guo (335819)
- Yi Hsiao (771103)
- Qi Gao (133189)
DOIAbstract
An enantioselective synthesis of the CGRP antagonist BMS-846372, amenable to large scale preparation, is presented. This new synthesis showcases a chemo- and enantioselective reduction of a cyclohepta[b]pyridine-5,9-dione as well as a Pd-catalyzed alpha-arylation reaction to form the key carbon–carbon bond and set the absolute and relative stereochemistry
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