Purinyl hydroxy alkanoic acid derivs - useful as hypocholesterolaemic agents

摘要

9 Purinyl hydroxy alkanoic acid derivs useful as hypocholesterolaemic agents. M3A. And their salts are new cmpds. of formula (I) (where A = N or N right arrow O; R1 = H, Hal, OH, SH, OAlkyl, SAlkyl, OAralkyl, NH2, NHAlkyl, N(Alkyl)2, NHAralkyl, NHAcyl, or NHOH; R2 and R3 = H, Hal, OH, SH, NH2, Alkyl, Aryl, OAlkyl, OAralkyl or SAlkyl; R4 = alkylene (pref. 2-6C) substd. by one or more OH groups (but no OH on the C atom attached to the N atom) opt. protected by acyl, alkyl, aralkyl or, where OH groups exist on adjacent C atoms, alkylidene or aralkylidene groups, R5 = OH, OAlkyl, NH2, NHAlkyl, N(Alkyl)2). Preferred cmpds. (I) are 4-purine-9-yl-4-desoxy-D-erythronic acids, amides and esters esp. where A=N, R2=R3=H,R1=NH2 and R5 = OH1 OMe, OEt or NH2 or R1 = EtNH, PhCONH, or OH and R5 = OH or R1=OH, R2=NH2, R3=H, and R5=OH, or R1=NH2, R2=H, R3=Me and R5=OH and the cmpd. (I1 R1 = NH2R2=R3=H, A=N O, R4 = CH-CHOH-CHOH- and R5 =OH).