血管活性肽P6A类似物的合成

Synthesis of analogue of P6A

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

Key words:  P6A  analogoue  1-(4-formamido)butyryl-4-［3-(4-formamido)butyryl］benzylpiperazin

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.

Abstract:

To obtain a stable and effective analogoue of P6A as an anti-thrombus drug．［Methods］ 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］benzyl piperazine．［Results］ The structure of the target product was characterized by H-NMR and MS． ［Conclusion］ The target compound can be synthesized by the designed method．