Sughrue Mion, PLLC
Method for production of cis-4-fluoro-L-proline derivatives
The present invention provides a safer method for production of a cis-4-fluoro-L-proline derivative under milder conditions and in good yield to give a product of high purity on an industrial scale at low cost. Namely, the present invention provides a method for producing a cis-4-fluoro-L-proline derivative, which comprises reacting a trans-4-hydroxy-L-proline derivative of the following Formula [I]:(wherein R1 represents a protecting group for an α-amino group, and R2 represents a protecting group for a carboxyl group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride-scavenger.
Taisho Pharmaceutical Co., Ltd.
C Y
C07D Y02P
inventional additional
Kazuyuki Chihiro Tomomichi Dai
Tomisawa Yokoo Yoshida Tatsuta