9-氨基-1,2,3,4-四氢吖啶衍生物的合成

为了降低第一个用于治疗老年痴呆症药物他克林的毒副作用,提高其药理活性,对其侧链氨基进行了改性研究.分别对他克林进行了乙酰化、丁酰化及氯乙酰化反应,制备了相应的衍生物.鉴于哌嗪基团的亲水性,将其引入吖啶分子中,合成出化合物9-(2-哌嗪乙酰氨基)-1,2,3,4-四氢吖啶.所有化合物的结构均经元素分析、红外光谱、核磁共振氢谱和质谱表证.

Synthesis of Derivatives of 9-Amino-1,2,3,4-Tetrahydroacridine

In order to improve tacrine's pharmacological activity and reduce its adverse effects, three of tacrine derivatives have been synthesized through acetylation, chloroacetylation and butylation of the amino group of tacrine. In view of the excellent hydrophilicity of piperazinyl group, it was incorporated into the acridine molecule and 9-(2-piperazinyl)acetylamino-1,2,3,4-tetrahydroacridine was synthesized. The structures of these compounds were characterized by elemental analysis, IR, ()~1H NMR and MS.