RWJ-38063-药物合成数据库

【药物名称】RWJ-38063

化学结构式(Chemical Structure):

参考文献No.	37794
标题:	Arylsubstd. piperazines useful in the treatment of benign prostatic hyperplasia
作者:	Mulcahy, L.; Pulito, V.; Villani, F.; Li, X.; Murray, W.; Maryanoff, C.; Jolliffe, L.; Reitz, A. (Ortho-McNeil Pharmaceutical, Inc.)
来源:	EP 0984777; US 6071915; WO 9851298

合成路线图解说明: The intermediate amine (IV) was prepared by alkylation of N-(2-isopropoxyphenyl)piperazine (I) with N-(2-bromoethyl)phthalimide (II), followed by removal of the phthaloyl group upon treatment with methylhydrazine.

合成路线图解说明: Alkylation of delta-valerolactam (V) with tert-butyl bromoacetate in the presence of NaH provided (VI). Subsequent tert-butyl ester cleavage by means of trifluoroacetic acid furnished 2-(2-oxopiperidin-1-yl)acetic acid (VII), which was finally coupled with amine (IV) to afford the title amide.

参考文献No.	581812
标题:	Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists
作者:	Li, X.; Murray, W.V.; Jolliffe, L.; Pulito, V.
来源:	Bioorg Med Chem Lett 2000,10(10),1093

合成路线图解说明: The intermediate amine (IV) was prepared by alkylation of N-(2-isopropoxyphenyl)piperazine (I) with N-(2-bromoethyl)phthalimide (II), followed by removal of the phthaloyl group upon treatment with methylhydrazine.

合成路线图解说明: Alkylation of delta-valerolactam (V) with tert-butyl bromoacetate in the presence of NaH provided (VI). Subsequent tert-butyl ester cleavage by means of trifluoroacetic acid furnished 2-(2-oxopiperidin-1-yl)acetic acid (VII), which was finally coupled with amine (IV) to afford the title amide.