Method for the production of 6,7-dimethoxy-4-amino-2-...

Details Method for the production of 6,7-dimethoxy-4-amino-2-... Method for the production of 6,7-dimethoxy-4-amino-2-...

C - Chemistry, Metallurgy

07

D

260/253

C07D 405/14 (2006.01) C07C 331/28 (2006.01) C07D 307/68 (2006.01)

Patent

CA 1092117

ABSTRACT OF THE DISCLOSURE A novel process is provided for the preparation of 6,7-dimethoxy-4- amino-2[4-(2-furoyl)-1-piperazinyl]quinazoline. It includes as a final step, cyclizing methyl-N-(3,4-dimethoxy-6-cyanophenyl)-[4-(2-furoyl)-1-piperazinyl] thioformamidate by heating, together with ammonia, in a polar solvent, in the presence of an alkali metal amide. The methyl-N-(3,4-dimethoxy-6-cyanophenyl)- [4-(2-furoyl)-1-piperazinyl]thioformamidate is preferably formed by reacting 3,4-dimethoxy-6-[4-(2-furoyl)-1-piperazinyl-thiocarbamido]benzonitrile with methyl chloride. By this process the quinazoline ring in prazosine is produced within the molecule, rather than in a reaction between two different molecules.

293065

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