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US 4,067,868 AGranted
Production of quinazolinone compounds
AssigneeSumitomo Chemical Company, Limited
InventorsKikuo Ishizumi, Kazuo Mori, Michihiro Yamamoto, Masao Koshiba, Shigeho Inaba, Hisao Yamamoto
Life of this patent
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Abstract
2(1H)-Quinazolinone derivatives, which are useful as anti-inflammatory agents, are prepared by heating or hydrolyzing an acylurea derivative. The acylurea derivative can be prepared by either reacting an indole derivative with an oxidizing agent or reacting an imidazolidine derivative with water, an alkanol or ammonia.
Claims4
A process for preparing a quinazolinone of the formula, ##STR8## wherein R.sub.1, R.sub.2 and R.sub.3 are independently a hydrogen atom, a halogen atom, trifluoromethyl, nitro, lower alkyl, or lower alkoxy;
- and R.sub.4 is a hydrogen atom, lower alkyl, polyhalo C.sub.1 -C.sub.3 alkyl or (C.sub.3 -C.sub.6 cycloalkyl) C.sub.1 -C.sub.4 alkyl, which comprises the steps of
- a. reacting an indole derivative of the formula, ##STR9## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as defined above;
- and R.sub.5 is a lower alkoxy or benzyloxy, with chromic acid or chromic anhydride to form an acylurea of the formula ##STR10## R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above;
- and b. hydrolyzing or heating said acylurea of the formula (IV) to prepare said quinazolinone of the formula (I).
1 more element
Dependencies are inferred from the claim text.