Process for production of cis-4-fluoro-l-proline derivatives

Details Process for production of cis-4-fluoro-l-proline derivatives Process for production of cis-4-fluoro-l-proline derivatives

C - Chemistry, Metallurgy

07

D

C07D 207/16 (2006.01)

Patent

CA 2534884

A process for producing high-purity cis-4-fluoro -L-proline derivatives highly safely under milder conditions in high yield, characterized by reacting a trans-4-hydroxy -L-proline derivative represented by the general formula [I]: (wherein R1 is an .alpha.-amino-protecting group; and R2 a carboxyl-protecting group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride scavenger.

La présente invention concerne un processus de production de dérivés de cis-4-fluoro-L-proline de haute pureté de manière très sûre dans des conditions légères à haut rendement, qui consiste à faire réagir un dérivés de trans-4-hydroxy-L-proline représenté par la formule générale (I) suivante : (I), (dans cette formule R?1¿ est un groupe de protection amino .alpha. et, R?2¿ est un groupe de protection carboxyle) avec N, N-diéthyl-N-(1, 1, 2, 3, 3, 3, -hexafluoropropyle) amine en présence d'un capteur de fluorure d'hydrogène.

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