Process for the preparation of amidino phenyl pyrrolidine...

C - Chemistry – Metallurgy – 07 – D

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C07D 207/273 (2006.01) C07C 323/43 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2207102

The invention herein is directed to a process for producing a lactam of formula (2) from a methionine analog of the formula (1) by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent. The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.

L'invention porte sur un procédé d'obtention d'un lactame de formule (2) à partir d'un analogue de méthionine de formule (1) consistant à traiter ledit analogue de méthionine par un halogénure de triméthylsulfonium ou de triméthylsulfoxonium en présence d'une base, dans un solvant aprotique approprié. L'invention porte également sur la préparation d'analogues d'amidinophénylpyrrolidinyl .beta.-alanine urée en utilisant comme intermédiaires lesdits composés de méthionine et de lactame. Ces analogues de la .beta.-alanine urée s'avèrent utiles comme antithrombotiques.

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