血管活性肽P6A类似物的合成  

Synthesis of analogue of P6A

作　　者：甄宇红[1] 黄珊珊[1] 

机构地区：[1]大连医科大学药物化学教研室,辽宁大连116027

出　　处：《大连医科大学学报》2003年第4期250-252,共3页Journal of Dalian Medical University

摘　　要：[目的 ]合成抗血栓活性多肽P6A的结构类似物 ,以获得稳定性好生物利用度高的抗血栓药物。 [方法 ]以哌嗪为原料与氯化氢形成哌嗪二盐酸盐 ;二盐酸盐和间硝基氯苄反应生成 3-硝基苄基哌嗪盐酸盐 ;硝基物经铁粉还原成 3-氨基苄基哌嗪 ;γ -氨基丁酸经甲酰化生成N -甲酰基γ-氨基丁酸 ,后者与 3-氨基苄基哌嗪缩合得目标产物 1 - (4 -甲酰氨基 )丁酰基 - 4- [3- (4 -甲酰氨基 )丁酰基 ]苄基哌嗪。 [结果 ]终产物经H -NMR及MS证明结构正确 ,为目标化合物。 [结论 ]通过上述合成方法能够获得目标化合物。To obtain a stable and effective analogoue of P6A as an anti-thrombus drug. Piperazine was reacted with hydrochloric acid to give piperazine dihydrochloride,which was further treated with 3-nitro-benzylchloride to produce 3-nitro-benzyl-piperazine hydrochloride.The nitro-compound was reduced by Fe powder to 3-amino-benzyl-piperazine.N-formyl-γ-amino-butyric acid prepared by formylation of GABA was reacted with 3-amino-benzyl-piperazine to give the target compound 1-(4-formamido)butyryl-4-[3-(4-formamido)butyryl]benzylpiperazine. The structure of the target product was characterized by H-NMR and MS. [Conclusion] The target compound can be synthesized by the designed method.

关 键 词：P6A 结构类似物 1-(4-甲酰氨基)丁酰基-4-[3-(4-甲酰氨基)丁酰基]苄基哌嗪 

分 类 号：R914[医药卫生—药物化学]