由丙二酸二乙酯作原料制得色胺（Ⅰ），再和芳香醛经Ｐｉｃｔｅｔ－Ｓｐｅｎｇｌｅｒ环合、脱氢反应而合成六个Ⅰ－芳（杂）基取代的β－咔啉化合物（Ⅲ），总收率３８％～６０％，其中五个为未见文献报道的新化合物。经体外受体放射配基竞争性结合试验，均显示与大鼠脑内ＢＺ受休有较好的特异性亲和力，其中１－位具吸电子基苯基取代衍生物Ⅲ－２、Ⅲ－４和Ⅲ－５的ＩＣ５０（１０－６ｍｏ１／Ｌ）与经典ＢＺ类化合物利眠宁（ｃｈｌｏｒｄｉａｚｅｐｏｘｉｄｅ）相近，因而为进一步的体内生物试验提供了基础。 The tryptamine (I) was prepared from diethyl malonate as a starting material and then cyclized and dehydrogenated with an aromatic aldehyde via Pictet-Spengler to synthesize six I-aryl (hetero) substituted β-carboline compounds Ⅲ), the total yield of 38% to 60%, of which five new compounds have not been reported in the literature. The competitive binding assay of radioligand in extracorporeal receptor showed a good specific affinity to BZ in rat brain, and the 1-position with electron-withdrawing phenyl substituted derivatives Ⅲ-2, Ⅲ-4 And IC50 (10-6mo1 / L) of III-5 are similar to the classical BZ compound chlordiazepoxide, thus providing a basis for further in vivo biological assays.