Novel process for preparing rac-bicalutamide and its...

C - Chemistry – Metallurgy – 07 – C

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Details

C07C 69/675 (2006.01) C07C 255/49 (2006.01) C07C 255/50 (2006.01) C07C 255/58 (2006.01) C07C 315/04 (2006.01) C07C 317/14 (2006.01) C07C 319/14 (2006.01) C07C 317/46 (2006.01) C07C 323/52 (2006.01)

Patent

CA 2448571

The present invention relates to a new process for the synthesis of racemic and optically active bicalutamide starting from ethyl pyruvate and methyl methacrylate. The present invention discloses processes of preparing bicalutamide intermediates including ethyl-[2-{4-fluorophenyl sulfone}]-2- hydroxy propionate, 1,2-epoxy-2-methyl propionate and 2-hydrox-2-methyl-3-(4- fluorophenylthio) propionic acid. The present invention further discloses micronized rac-bicalutamide and the preparation thereof.

L'invention concerne un nouveau procédé pour la synthèse de bicalutamide racémique et actif au niveau otpique, à partir de pyruvate d'éthyle et de méthacrylate de méthyle. Cette invention concerne plus spécifiquement des procédés pour préparer des produits intermédiaires de bicalutamide comprenant du propionate éthyl-[2-{4-fluorophényle sulfone}]-2-hydroxy, du propionate 1,2-époxy-2-méthyle et de l'acide 2-hydrox-2-méthyl-3-(4-fluorophénylthio) propionique. Cette invention concerne également du rac-bicalutamide micronisé ainsi que la préparation de celui-ci.

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