【摘要】 合成了 N,N -二苄基 -2 -甲氧羰基 -六氢 -1 H-1 ,4 -二氮 艹卓 (3 )。 3经还原、氯取代、胺取代、胺脱苄、单酰化及酰化反应后得到了 1 0个带有 (1 -芳乙酰胺基 -2 -叔氨基 )乙烷结构的六氢 -1 H-1 ,4 -二氮 艹卓 类目标化合物 (9a～9i和 1 0 )更多还原

【Abstract】 In order to get some selective κ opioid receptor agonists, which can elicit analgesia while lack serious side effects , the basic modified structures of 1,4 dibenzyl 2 methoxycarbonyl hexahydro 1[WT5BX]H 1,4 diazepine([ST5HZ]3), was prepared starting from [WT5BX]N,N dibenzyl 1,3 propylene diamine and methyl 2,3 dibromo propionate. Then, nine target compounds of hexahydro [WT5BX]1H 1,4 diazepine analogues carrying the segment of (1 arylacetamide 2 tertiaryamide)ethane([ST5HZ]9a~9i) were synthesized through reduction, chlorination, amine substitution, amine debenzylation, single amidation and amidation of compound [ST5HZ]3. The target compound [ST5HZ]10 containing hydrophilic group of hydroxy was also achieved through oxydebenzylation of [ST5HZ]9b. The structures of these products were characterized by elementary analysis, IR, EIMS and 1H NMR.更多还原