| 摘要 |
1511187 Chromanes BEECHAM GROUP Ltd 23 March 1977 [2 April 1976 10 Aug 1976] 13536/76 and 33178/76 Heading C2C Compounds of the general Formula (I) (R 1 = H, C 1-4 alkyl optionally substituted by Cl, Br, OH or C 1-4 alkoxy or acyloxy; R 2 =H, C 1-4 alkyl or NR 1 R 2 =5-8 membered ring optionally substituted by one or more methyl groups; Y=COR 3 , CO 2 R 3 , SOR 3 , SO 2 R 3 , SO . OR 3 , SO 2 . OR 3 , CH(OH)R 3 , C(R 3 )NOH, C(R 3 )NNH 2 , CONH 2 , CONR 4 R 5 , SONR 4 R 5 , SO 2 NR 4 R 5 ; R 3,4 =C 1-8 hydrocarbyl optionally substituted by Cl, Br, OH, C 1-4 alkoxy or acyloxy, or by three fluorine atoms on the same carbon atom; R 5 = H, C 1-4 alkyl) and their esters and salts are prepared by reacting a corresponding 2,2 - dimethyl - 3,4 - epoxychromane (IV) with R 1 R 2 NH, optionally followed by (a) conversion of a ketone to its oxime, hydrazone or the corresponding secondary alcohol, (b) acylation and/or (c) salt formation. The starting material may be substituted by a precursor for Y, e.g. a cyano group which may be hydrolysed to a carbamoyl group. The starting materials are prepared by the following route (Y<SP>1</SP>= inert group Y, or precursor). The above compounds are antihypertensive agents, and may be administered in the form of pharmaceutical preparations containing them in association with a carrier. |
