Preparation of Novel Acylguanidines with Potential H2 -Blocking Activity

Abstract

3- chlorocyclohex-2-enone(2) was obtained directly by reaction of cyclohex-1,3-dione with triphyenylphosphine in CCl . Guanidine hydrochloride was treated with sodium methoxide to give the free base. The free base was treated with 3- chloro-cyclohex-2-enone (2) in methanol and yielded the acylguanidine (3). Also reaction of 5,5-dimethyl-3-methoxycyclohex-2~enone (8) with 2- amino-1,4,5,6- tetrahydro-pyrimidine (9) in isopropanol gave 2- (5,5-dimethyl-3-oxocyclohex-2-enylamine)~ 1,4,5,6-tetrahydropyrimidine (10). They both can be considered as new lead compounds with potential H -blocking activity. Further investigation will be needed to prepare modified strctures and effective H -blockers and evaluate their properties.