Montirelin, CNK-602A, PS-24, CG-3703
孟替瑞林 孟替瑞林 Chemical Name: N-[[(3R,6R)-6-Methyl-5-oxo-3-thiomorpholinyl]carbonyl]-L-histidyl-L-prolinamide
CAS No. 90243-66-6, 62305-91-3 (undefined stereoch.)
项目整合开发状态: Phase III
项目研究机构: Gr黱enthal (Originator), Nippon Shinyaku (Licensee)
合成路线:The synthesis of thyrotropin releasing hormone (TRH) analogues is described as follows:The reduction of N-benzyloxycarbonylprolinamide (I) with H2 over Pd/C in methanol gives prolinamide (II),which is condensed with N-benzyloxy-carbonylhistidyl hydrazide (III) by means of NaNO2 - HCl in ethyl acetate yielding N-benzyloxycarbonylhistidylprolinamide (IV).The hydrolysis of (IV) with HBr in acetic acid affords histidylprolinamide (V),which is finally condensed with 6-methyl-5-oxothiomorpholinyl-3-carboxylic acid (VI) by means of 1-hydroxybenzotriazole,dicyclohexylcarbodiimide and triethylamine in DMF.
📌 参考资料/链接：
参考文献标题:CG-3703
文献作者:Pento,J.T.
参考来源:Drugs Fut 1983,8(12),1007
📄 详细内容
合成路线:The synthesis of thyrotropin releasing hormone (TRH) analogues is described as follows:The reduction of N-benzyloxycarbonylprolinamide (I) with H2 over Pd/C in methanol gives prolinamide (II),which is condensed with N-benzyloxy-carbonylhistidyl hydrazide (III) by means of NaNO2 - HCl in ethyl acetate yielding N-benzyloxycarbonylhistidylprolinamide (IV).The hydrolysis of (IV) with HBr in acetic acid affords histidylprolinamide (V),which is finally condensed with 6-methyl-5-oxothiomorpholinyl-3-carboxylic acid (VI) by means of 1-hydroxybenzotriazole,dicyclohexylcarbodiimide and triethylamine in DMF.
参考文献标题:
文献作者:
参考来源:US 4045556
合成路线:The synthesis of thyrotropin releasing hormone (TRH) analogues is described as follows:The reduction of N-benzyloxycarbonylprolinamide (I) with H2 over Pd/C in methanol gives prolinamide (II),which is condensed with N-benzyloxy-carbonylhistidyl hydrazide (III) by means of NaNO2 - HCl in ethyl acetate yielding N-benzyloxycarbonylhistidylprolinamide (IV).The hydrolysis of (IV) with HBr in acetic acid affords histidylprolinamide (V),which is finally condensed with 6-methyl-5-oxothiomorpholinyl-3-carboxylic acid (VI) by means of 1-hydroxybenzotriazole,dicyclohexylcarbodiimide and triethylamine in DMF.
参考文献标题:Synthesis of a series of residue 1-(pyroglutamic acid) analogs of thyrotropin releasing hormone
文献作者:Goren,H.J.; Bauce,L.G.
参考来源:Intl J Pept Protein Res 1979,14216-226
产品链接: CAS No. 90243-66-6›› 产品链接: CAS No.62305-91-3››