| 摘要 |
3,3-Diarylpropylamine derivs. of formula (I) [R1=divalent aliphatic hydrocarbon or single bond; R2, R3=H, alkyl or 4- to 6-membered N- contg. heterocyclic ring; R4=H, halo, OH, CN, alkoxy or halo (un) substd. alkyl; X= -N= or -CH= ; A=B=H are prepd. Thus, (E)-3-(6-(3- pyrrolidino-1-(4-toryl)prop-1E-enyl)-2-pyridyl) acrylic acid is prepd. from 2,6-dibromopyridine, 4-MeC6H4CN, EtO2CH2P(0) (0Et)2, and (2-pyrrolidinoethyl)triphenylphosphonium bromide in 5 steps. (I) exhibit antihistamine activity for treating nasal congestion, rhinitis, urticaria, angioneurotic oedema, allergic conjunctivitis. |
