2-substd-1 3-diazacyclopentene 2 derivs hypotensives

摘要

Process: (I) R1 = H, lower alkyl, nitrile, trifluoromethyl or pref. halogen X = halogen. (I) are known hypotensives. The process is simple and gives good yields. Compounds which are difficult to prepare using the known isothiuronium salt method are obtained in good yield. Introduction of substituents in ways known for halogenating phenols. The method is esp. quick by reacting compounds or mixtures which develop active halogen in situ such as mixtures of conc. HCl and an oxidising agent such as 30% aqueous H2O2. The new substituents are usually attached at the same posn. as in a corresponding substd. phenol. 2-(2-chloro-4-cyanophenyl)amino-1, 3-diazacyclopentene-(2)-hydrochloride.