2-substd-1 3-diazacyclopentene 2-derivs hypotensives

摘要

Process: R1 = H, lower alkyl or halogen X = halogen or cyano. The nitro group in (II) is catalytically reduced to the primary amino group which is diazotised and the diazonium salt formed heated with Cu-(1)-halide or -cyanide. (I) are known hypotensives. Compounds (I) with mixed substitution can be prepared in a simple way and in good yields. An added halogen atom or cyano group can be positioned exactly without formation of isomers which are difficult to separate. (I) is prepared from (II) as described above. When introducing a fluorine atom, the diazonium salt obtained may be isolated and converted to the corresponding diazoniumboronfluoride. 2-(4-amino-2-chlorophenylamino)-1, 3-diazacyclopentene-(2) in a yield of 2.3 g.