| 摘要 |
(A) Cpds. (I) where R R1 = H, OH, O-alkyl R2 R5 R6 = H, alkyl, aryl R3 = H, aryl, aralkyl R4 = H, -CO-alkyl, -CH2C triple bond CH, -CH2CH2NH -NH2, - -NH2, and -CH2CH2 = NOH Pref. alkyl, aryl, and aralkyl are lower groups. (B) Salts of (I) with non-toxic acids. N.B. includes cis- and trans- isomers of (I). (I) are useful as antihypertensive agents. (a) Prepn. of (III; R=R1=R2=R5=R6, R3=Ph Mixture of (II; R=R1=R2=R5=R6=H) (5.6 g.), PhNH2 (2.5g.) and a trace of p-TsOH in toluene (50 ml.) was refluxed through a Dean-Stark trap for 12 hrs., and evapd. in vacuo. Residue was extra. with n-hexane, and org. layer was evapd. to give the imine (2.14 g.), m.p. 129-131 deg. (from Et2O). Hydrogen. of the imine (2.14g.) in EtOH over PtO2 provided the title-cpd. (2.2g.). (b) Prepn. of cis- and trans- (A). Foregoing (III) (20.6 g.) was refluxed with (EtCO)2O (100 ml.) for 1 hr. Evapn., and isoln. of basic material afforded (A) (10.05 g.), m.p. 125-126 deg. (from Et2O). |
