摘要 |
1292768 Benzylimidazolidinones F HOFFMANN-LA ROCHE & CO AG 19 April 1971 [24 Feb 1970] 22437/71 Heading C2C Novel compounds I in which R 1 is -OCH 3 and R 2 is -OC 2 H 5 or R 1 is ethoxy, isopropoxy or butoxy and R 2 is methoxy, are prepared by (a) treating a compound II with alkaline soln.; (b) reacting a compound III with phosgene; (c) treating a compound IV with alcoholic alkali at elevated temperature or (d) reacting a compound V wherein one of R 1 <SP>1</SP> and R 2 <SP>1</SP> is OH and the other is as R 1 or R 2 in Formula I with an appropriate alkylating agent. Compounds II are prepared by hydrogenating compounds VI to give compounds VII, reacting compounds VII with hydrazine to give compounds VIII, reacting the hydrazides VIII with nitrous acid by a modified Curtius reaction to give compound IX and hydrogenating these to give the compounds II Compounds III are prepared by acid hydrolysis of compounds II. Compounds IV are prepared by reacting compounds III with chloroethyl carbonate. Compounds V are prepared similarly to compounds II with an additional cyclization step. 3 - Butoxy - 4 - methoxy - benzaldehyde is prepared by reaction of an isovanillin sodium salt with butyl iodide. Pharmaceutical compositions for oral or parenteral administration as cardiovascular agents comprise a compound I together with suitable carriers. |