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将N-(2-吡咯甲酰基)-β-丙氨酸甲酯(Ⅲ)与卤代烃经烷基化反应得到的产物水解,得到N-(1-烷基-2-吡咯甲酰基)-β-丙氨酸(Ⅱa～Ⅱc),收率84.7%～91.2%;以化合物Ⅱ为原料,在多聚磷酸-P2O5作用下,经分子内环化反应合成了标题化合物1-烷基-6,7-二氢-1H,5H-吡咯并[2,3-c]氮杂-4,8-二酮(Ⅰa～Ⅰc),收率69.1%～77.2%。3步反应总收率为61.8%～69.1%。测定了3个标题化合物对α-葡萄糖苷酶的抑制作用。
Hydrolysis of the product obtained by the alkylation of the N- (2-pyrrolidinoyl) -β-alanine methyl ester (III) with the halogenated hydrocarbon gives the N- (1-alkyl-2-pyrroyl) -β-alanine (Ⅱa ~ Ⅱc) in the yield of 84.7% ~ 91.2%. The compounds Ⅱ were synthesized by the intramolecular cyclization reaction of polyphosphoric acid-P2O5 with compound Ⅱ as the starting material. 6,7-dihydro-1H, 5H-pyrrolo [2,3-c] azepine-4,8-dione (Ia ~ Ic). The yield was 69.1% ~ 77.2%. The total yield of 3-step reaction was 61.8% -69.1%. Three title compounds were tested for their inhibitory effect on alpha-glucosidase.