3,4-亚甲二氧苯基甲酰哌啶的新合成方法及其晶体结构

摘要

An allosteric α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid( AMPA) receptor positive modulator, l-( 1,3-benzodioxol-5-ylcarbonyl)piperidine(l), was synthesized using a new method by the esterification of piperic acid with N-succinimidyl-trifluoroacetate, then reacted with piperidine in total yield of 73%. The structure was confirmed by 1H NMR, IR, MS, XRD and elemental analysis. 1 belongs to orthorhombic, space group Pnma with a = 1.463 6(6) run, 6=0.781 0(3) nm, c =2.014 7(8) nm, V = 2.303 1(16) nm3 and final R1=0.098 5, ωR2 = 0.300 4.%采用胡椒酸与三氟乙酸N-琥珀酰亚胺酯反应,再与六氢吡啶反应的新方法合成了α-氨基羟甲基噁唑丙酸(AMPA)受体调节剂——3,4-亚甲二氧苯基甲酰哌啶(1),总产率73％,其结构经1H NMR,IR,MS,XRD和元素分析确证.1属正交晶系,Pnma空间群,晶胞参数a=1.463 6(6) nm,b=0.781 0(3) nm,c=2.014 7(8)nm,V=2.303 1(16) nm3,Z =2(296 K).最终偏离因子R1=0.098 5,ωR2=0.300 4.