Crystal of bicalutamide and production method thereof

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 315/02 (2006.01) A61K 31/277 (2006.01) A61P 5/28 (2006.01) A61P 43/00 (2006.01) C07C 315/06 (2006.01) C07C 317/46 (2006.01)

Patent

CA 2469594

The invention relates to crystals of bicalutamide having a specific crystal form, and industrially practicable processes for the production of bicalutamide and crystals thereof which are excellent in environmental friendliness, economical efficiency, and safeness. The invention provides a process for the production of bicalutamide represented by formula (1): (1) characterized by comprising at least the step of reacting a compound represented by formula (3) with an oxidizing agent: (3) a process for the production of crystals of bicalutamide; and a crystal form of bicalutamide as determined by X-ray diffraction (XRD) or solid-state 13C NMR spectroscopy.

L'invention se rapporte à des cristaux de bicalutamide ayant une forme cristalline spécifique et à des procédés industriels de production de bicalutamide et de ses cristaux s'avérant excellents en terme de respect de l'environnement, d'efficacité économique et de sécurité. Le procédé de production bicalutamide de cette invention est représenté par la formule (1) : et consiste à faire au moins réagir un composé représenté par la formule (3) avec un agent oxydant : (3). L'invention concerne un procédé de cristaux de bicalutamide et une forme cristalline de bicalutamide que l'on obtient par diffraction des rayons X (XRD) ou par spectroscopie de la résonance magnétique nucléaire (NMR) à l'état solide C?13¿.

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