923563-75-1

Upstream product

• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 261380-31-8 (R)-N-(1,1-dimethylethoxycarbonyl)-2,5-difluorophenylalanine 
• 837430-11-2 (R)-N-(1,1-dimethylethoxycarbonyl)-2,5-difluorophenylalanine methyl ester 

Downstream Products

• 923564-19-6 [(1R,2S)-3-(3-tert-butylcarbamoyl-6-trifluoromethyl-pyridin-2-yl)-1-(2,5-difluoro-benzyl)-2-hydroxy-propyl]-carbamic acid tert-butyl ester 
• 923564-18-5 [(R)-3-(3-tert-butylcarbamoyl-6-trifluoromethyl-pyridin-2-yl)-1-(2,5-difluoro-benzyl)-2-oxo-propyl]-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

Development of a pratical synthisis of DPP IV inhibitor LY2497282

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 iV-dibenzyl-protected α-amino aldehyde 12, which was derived from iV-acetyl-protected amino ester 14 without epimerization. The desired Felkin-Anh nonchelation controlled anti-amino alcohol 11 was isolated with >99% HPLC area and > 99% ee by crystallization. After removing the dibenzyl protecting group under transfer hydrogenation conditions, LY2497282 (1) was finally obtained in 39% overall yield with a six-step longest linear sequence starting from N-acetyl-protected amino ester 14.

PHENYL COMPOUNDS

The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (xx) ; X is selected from CH, CF and N, R5 is selected from H, C1-C6 alkyl, C1-C6 fluoroa

PYRIDINE DERIVATIVES AS DIPEPTEDYL PEPTIDASE INHIBITORS

The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (1); X is selected from CH, CF and N; R5 is selected from H, C1-C6 alkyl, C1-C6 fluoroalk