网站主页>>>项目整合精选>>>项目整合精选>>>Posatirelin, pAad-Leu-Pro-NH2, RGH-2202, Pyladox

Posatirelin, pAad-Leu-Pro-NH2, RGH-2202, Pyladox

泊替瑞林Chemical Name: N-[6-Oxopiperidin-2(S)-ylcarbonyl]-L-leucyl-L-prolinamide
CAS No. 78664-73-0
项目整合开发状态: Discontinued
项目研究机构: Gedeon Richter (Originator), Dainippon Pharmaceutical (Licensee)
合成路线:a) N-Protected L-Leucine activated as the pentafluorophenyl ester (I) is coupled with L-prolinamide (II),and the resulting dipeptide (III) is deprotected te (IV) and coupled with L-pyro-2-aminoadipic acid pentatluorophenyl ester (V) to give RGH-2202.

合成路线:b) Large scale preparation of L-pyro-2-aminoadipic acid (IX) is accomplished by oxidation of the N-protected L-lysine derivative (VI) with KMnO4 followed by deprotection to (VIII) and cyclization.
📌 参考资料/链接:
参考文献标题:RGH-2202
文献作者:N骻r醖i,M.
参考来源:Drugs Fut 1988,13(5),420

📄 详细内容


合成路线:a) N-Protected L-Leucine activated as the pentafluorophenyl ester (I) is coupled with L-prolinamide (II),and the resulting dipeptide (III) is deprotected te (IV) and coupled with L-pyro-2-aminoadipic acid pentatluorophenyl ester (V) to give RGH-2202.

合成路线:b) Large scale preparation of L-pyro-2-aminoadipic acid (IX) is accomplished by oxidation of the N-protected L-lysine derivative (VI) with KMnO4 followed by deprotection to (VIII) and cyclization.

参考文献标题:Synthesis of thyrotropin releasing hormone analogu
文献作者:Szirtes,T.; Kisfaludy,L.; P醠osi,?; Szporny,L.
参考来源:J Med Chem 1984,27741


合成路线:a) N-Protected L-Leucine activated as the pentafluorophenyl ester (I) is coupled with L-prolinamide (II),and the resulting dipeptide (III) is deprotected te (IV) and coupled with L-pyro-2-aminoadipic acid pentatluorophenyl ester (V) to give RGH-2202.

合成路线:b) Large scale preparation of L-pyro-2-aminoadipic acid (IX) is accomplished by oxidation of the N-protected L-lysine derivative (VI) with KMnO4 followed by deprotection to (VIII) and cyclization.
参考文献标题:Synthesis of thyrotropin-releasing hormone analogu
文献作者:Szirtes,T.; Kisfaludy,L.; P醠osi,?; Szporny,L.
参考来源:J Med Chem 1986,291654


产品链接: CAS No. 78664-73-0››