| 摘要 |
<p>1,256,593. 3,4 - Dihydroquinazolin - 2 - ones. SANDOZ Ltd. 13 June, 1969 [1 July, 1968; 26 Dec., 1968; 25 April, 1969], No. 30194/69. Heading C2C. The invention comprises compounds of formula wherein n is 1 or 2, R when n = 1 is H, F, Cl, Br, C 1-5 alkyl, C 1-4 alkoxy, alkythio or alkylamino, di(C 1-4 alkyl)amino, NO 2, CN, NH 2, OH, SH, AcNH or CF 3, R when n = 2 is H, F, Cl, Br, C 1-5 alkyl or C 1-4 alkoxy, R 1 is C 1-5 alkyl, R 2 is H, C 1-5 alkyl or omega-di(C 1-4 alkyl)- amino-C 1-4 -alkyl, and R 3 is Ph possibly containing up to 2 substituents which are F, Cl, Br, C 1-4 alkyl or C 1-4 alkoxy and/or a CF 3 group. These compounds may be prepared by (1) hydrogenating the 3,4 - dehydro analogues; (2) alkylating the 3-position; (3) reacting the 3,4- dehydro analogues with an alkyl-lithium or Grignard compound; (4) cyclizing a corresponding 1 - alkyl - 1 - (2 - benzoyl)phenylurea or a 1 -alkyl- 1 -phenylurea/benzaldehyde mixture; (5) alkylating in the compound where R is amino or alkylamino, to give an alkylamino or dialkylamino group; (6) reductively alkylating the compound where R is nitro. Starting materials.-Details are given for the preparation of 2-isopropylamino-4-methylbenzophenone, N-isopropyl-m-toluidene and its N- carbamyl derivative, p-chloro-N-methylaniline and its N-formyl derivative, 2-amino-5-chloro- 4-methylbenzhydrol and its N-isopropyl derivative, and 2-(N-ethyl or -isopropyl)amino-5- nitrobenzophenone. Therapeutic compositions having antiinflammatory, and in some cases antipyretic or analgesic activity, comprise compounds of the above formula in association with a physiologically acceptable diluent or carrier for oral or parenteral administration.</p> |
