Sodium 2-[(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-y1]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-4H-quinazolin-4-yl]acetate monohydrate, its preparation and use

A method of preparation of crystalline sodium 2-[(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-4H-quinazolin-4-yl]acetate monohydrate of formula (I)

• comprising the steps:
• A-1) providing a suspension of sodium 2-[(4S)-8-fluoro-2-[4-(3-methoxyphenyl)-piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-4H-quinazolin-4-yl]acetate in diisopropylether,
• B-1) stirring the suspension obtained in step A-1 at a temperature in the range of from 40 °C to 60 °C for at least 10 hours, and
• C-1) removing the diisopropylether to obtain sodium 2-[(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-4H-quinazolin-4-yl]acetate monohydrate as a crystalline solid,
• or, alternatively to steps A-1, B-1 and C-1:
• A-2) providing a solution of sodium 2-[(4S)-8-fluoro-2-[4-(3-methoxyphenyl)-piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-4H-quinazolin-4-yl]acetate in methylene chloride,
• B-2) stirring the solution obtained in step A-2 at a temperature in the range of from 40 °C to 60 °C for at least 30 minutes;
• and
• C-2) removing the methylene chloride to obtain sodium 2-[(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-4H-quinazolin-4-yl]acetate monohydrate as a crystalline solid.