Method of preparing substituted quinazolin-4-ones

Details Method of preparing substituted quinazolin-4-ones Method of preparing substituted quinazolin-4-ones

C - Chemistry, Metallurgy

07

D

C07D 401/06 (2006.01) A61K 31/505 (2006.01) C07D 239/91 (2006.01) C07D 401/04 (2006.01) C07D 401/14 (2006.01) C07D 403/00 (2006.01) C07D 405/00 (2006.01) C07D 409/00 (2006.01) C07D 413/00 (2006.01) C07D 417/00 (2006.01)

Patent

CA 2260701

Disclosed is a process for the preparation of quinazolin-4-one derivatives of the structural formula (see fig. I) and the pharmaceutically acceptable salts and atropisomers thereof, wherein Ar is optionally substituted phenyl, R1 is halo, cyano, etc., R2 is hydrogen or hydroxyl, X is hydrogen, halo, etc., and Y is N or CH. The quinazolin-4-one derivatives prepared according to the method of this invention are .alpha.-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) inhibitors and are useful for the treatment of various neurologic disorders and conditions including Parkinson's Disease, epilepsy, emesis, eschemia, stroke, traumatic brain and spinal. cord injury, and so forth. The process comprises dehydration of the ethyl analog at position 2 of the quinazolin-4-one portion of formula I when R2 is OH, or oxidation of the ethyl analog when R2 is H.

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