(Bi)cyclic thiourea deriv. drug intermediate prepn. - from di:amine, di:chloromethane and sulphur in organic solvent in presence of base

摘要

Prepn. of cyclic thiourea derivs. of formula (I), i.e. 2-mercaptoimidazoline (Ia), 2-mercapto-1,4,5,6-tetrahydropyrimidine (Ib) or 2-mercapto-3,4,5,6,7,8-hexahydrobenzimidazoline (Ic), comprises reacting the corresp. diamine of formula (II), i.e. ethylene diamine (IIa), 1,3-diaminopropane (IIb) or 1,2-diaminocyclohexane (IIc), with dichloromethane and sulphur in an organic solvent in presence of an acid binder, pref. with heating. m = 0 and n = 0 in (Ia) and (IIa); m = 0 and n = 1 in (Ib) and (IIb); or m = 4 and n = 0 in (Ic) and (IIc). USE/ADVANTAGE - (I) are intermediates for medicaments. (I) are prepd. simply from readily available and easily handled starting materials. Use of thiophosgene and carbon disulphide is avoided.