论文部分内容阅读
本文报道合成的关键步骤是由4-(N-甲基氨基)-1,2-环氧环己烷(1)在干燥的N-甲基毗咯烷酮中加热反应使分子内反式双直立键过氧化物开环形成内-氮杂双环结构2,2再与α-环戊基扁桃酸甲酯在正庚烷存在下加入氢化钠回流得3,后者加入溴甲烷的2-丁酮溶液在室温静置后,经重结晶可得标题化合物4。化合物1可由4-(三氟乙酰胺基)环已烯经甲基化、环氧化、脱酰基而得。药理试
The key step of the synthesis reported here is the reaction of 4- (N-methylamino) -1,2-epoxycyclohexane (1) in dry N-methylpyrolidinone to make intramolecular trans bis The ortho-bond peroxide ring-opens to form the endo-azabicyclo structure 2,2 and then with methyl α-cyclopentyl mandelate sodium hydride in the presence of n-heptane refluxed 3, the latter methyl bromide 2-butanone After the solution is allowed to stand at room temperature, the title compound 4 is obtained by recrystallization. Compound 1 can be 4- (trifluoroacetamido) cyclohexene by methylation, epoxidation, deacyl derived. Pharmacological test