Development of a Practical Synthesis of DPP IV Inhibitor LY2497282†

…, RN Richey, JR Stout, MA LaPack, R Gu…

Index: Yu, Hannah; Richey, Rachel N.; Stout, James R.; LaPack, Mark A.; Gu, Ruilin; Khau, Vien V.; Frank, Scott A.; Ott, Joel P.; Miller, Richard D.; Carr, Michael A.; Zhang, Tony Y. Organic Process Research and Development, 2008 , vol. 12, # 2 p. 218 - 225

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Citation Number: 8

Abstract

A new synthetic route to LY2497282 (1), a potent and selective DPP IV inhibitor for the potential treatment of diabetes, suitable for the preparation of multikilogram quantities is described. The key step involved a stereoselective addition of the dianion of nicotinamide 8 to N-dibenzyl-protected α-amino aldehyde 12, which was derived from N-acetyl-protected amino ester 14 without epimerization. The desired Felkin-Anh nonchelation controlled anti ...