CRYSTALS OF BICALUTAMIDE AND PROCESS FOR THEIR PRODUCTION

WIPO Patent Application WO/2003/053920

A1

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&semi and a crystal form of bicalutamide as determined by X−ray diffraction (XRD) or solid−state ¹³C NMR spectroscopy.

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SHINTAKU TETSUYA (JP)
KATSURA TADASHI (JP)
ITAYA NOBUSHIGE (JP)

PCT/JP2002/013058

July 03, 2003

December 13, 2002

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SUMIKA FINE CHEMICALS CO LTD (JP)
SHINTAKU TETSUYA (JP)
KATSURA TADASHI (JP)
ITAYA NOBUSHIGE (JP)

A61P5/28; A61P43/00; C07C315/02; C07C315/06; C07C317/26; C07C317/46; A61K; A61P; C07C; (IPC1-7): C07C315/02; C07C315/06; C07C317/46; A61K31/277; A61P5/28; A61P43/00

WO2002024638A1	2002-03-28
WO2001000608A1	2001-01-04

TUCKER HOWARD ET AL.: "Nonsteroidal antiandrogens. Synthesis and structure-activity relationships of 3-substituted derivatives of 2-hydroxypropioanilides", JURNAL OF MEDICINAL CHEMISTRY, vol. 31, no. 5, 1988, pages 954 - 959, XP000605264

Takashima, Hajime (2-14 Fushimimachi 4-chome, Chuo-k, Osaka-shi Osaka, JP)

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