吡咯并[2,3-c]氮杂-4,8-二酮衍生物的合成  

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

作　　者：曾向潮[1] 黎冬冬[1] 胡斌斌[1] 

机构地区：[1]暨南大学化学系,广东广州510632

出　　处：《精细化工》2012年第7期683-687,共5页Fine Chemicals

基　　金：广东省自然科学基金项目(06300581)~~

摘　　要：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。3- （1H-pyrrole-2-carbonyl） propionic acids （ Ⅱ a - Ⅱ c ） were synthesized, in the yields of 84. 7 % - 91.2 %, by alkylation of methyl 3- （ 1H-pyrrole-2-carbonyl ） aminopropionate （ Ⅲ ） with alkyl halides and followed by hydrolyzation. The title compounds Ⅰ a - Ⅰ c, were obtained via cyclization of the acids Ⅱ a - Ⅱ c in the presence of polyphosphoric acid and diphosphorus pentoxide, in the yields of 69. 1% -77.2%. The overall yields of the three-step reactions were 61.8% - 69. 1%. And the α-glucosidase inhibition of the three title compounds have also been studied.

关 键 词：1-烷基-6 7-二氢-1H 5H-吡咯并[2 3-c]氮杂-4 8-二酮 N-(1-烷基-2-吡咯甲酰基)-β-丙氨酸 α-葡萄糖苷酶抑制 医药原料 

分 类 号：TQ465.91[化学工程—制药化工]