吡咯并[2,3-c]氮杂卓-4,8-二酮衍生物的合成

Synthesis of Pyrrolo[2,3-c]azepine-4,8-dione Derivatives

摘要:

N-（2-吡咯甲酰基）-β-丙氨酸甲酯（3）与卤代烃经烷基化反应，并将所得烷基化产物水解，得到N-（1-烷基-2-吡咯甲酰基）-β-丙氨酸（2a ~ 2c），收率84.7% ~ 91.2%；化合物2为原料，多聚磷酸P2O5作用下，经分子内环化合成了标题化合物1-ethylaldisin、1-butylaldisin 和 1-benzylaldisin（1a ~ 1c），收率69.1% ~ 77.2%。三步反应的总收率为61.8% ~ 69.1%。测定了三个标题化合物对α-葡萄糖苷酶的抑制作用。

Abstract:

3-(1H-pyrrole-2-carbonyl)propionic acids (2a ~ 2c) were synthesized, in yields of 84.7 % ~ 91.2 %, by alkylations of methyl 3-(1H-pyrrole-2-carbonyl)aminopropionate (3) with alkyl halides and followed by hydrolyzation; the title compounds, 1a ~ 1c, were obtained via cyclizations of the acids (2a ~ 2c) in the presence of polyphosphoric acid and diphosphorus pentoxide, in yields of 69.1 % ~ 77.2 %. The overall yields of the three step reactions were 61.8 % ~ 69.1 %. And the α-glucosidase inhibitions of the three title compounds have also been studied.