RP-67580-药物合成数据库

【药物名称】RP-67580

化学结构式(Chemical Structure):

参考文献No.	169663
标题:	Synthesis of RP-67,580, a new potent nonpeptide substance P antagonist
作者:	Peyronel, J.-F.; et al.
来源:	Bioorg Med Chem Lett 1992,2(1),37

合成路线图解说明: The cyclization of 4,4-diphenyl-2-cyclohexen-1-one (I) with N-benzyl-N-(butoxymethyl)-N-(trimethylsilylmethyl)amine (II) gives 2-benzyl-7,7-diphenylperhydroisoindol-4-one (III), which is debenzylated by hydrogenation with H2 over Pd/C to afford 7,7-diphenylperhydroisoindol-4-one (IV). The optical resolution of (IV) yields the desired enantiomer, which is finally condensed with 2-(2-methoxyphenyl)acetimidic acid ethyl ester tetrafluoroborate (V).

参考文献No.	194882
标题:	Substance P antagonists
作者:	Lowe, J.A. III
来源:	Drugs Fut 1992,17(12),1115

合成路线图解说明: The cyclization of 4,4-diphenyl-2-cyclohexen-1-one (I) with N-benzyl-N-(butoxymethyl)-N-(trimethylsilylmethyl)amine (II) gives 2-benzyl-7,7-diphenylperhydroisoindol-4-one (III), which is debenzylated by hydrogenation with H2 over Pd/C to afford 7,7-diphenylperhydroisoindol-4-one (IV). The optical resolution of (IV) yields the desired enantiomer, which is finally condensed with 2-(2-methoxyphenyl)acetimidic acid ethyl ester tetrafluoroborate (V).