苯甲酰胺类抗精神病药物的研究:若干3α-去甲托品烷衍生物的合成

Reductive amination of8- benzyl-nortropinone(3 )with ammonium acetate andsodium cyanoborohydride yielded the 3 α-amino nortropane derivative 4 which was condensed withsubstituted benzoic acids using 2-bromo-N-methyl-pyridinium iodide as condensing reagent to give thetarget compounds 2a～ein an overall yield of 50～60%.Compound 2e showed marked and selectiveaffinity for D-2 receptor.Compound 2d showed definite affinity for D- 1 receptor besides markedaffinity for D-2 receptor.