Pifatidine, Roxatidine acetate hydrochloride, Hoe-760, TZU-0460, Gastralgin, Roxit, Altat, Xarcin-药物合成数据库

【药物名称】Pifatidine, Roxatidine acetate hydrochloride, Hoe-760, TZU-0460, Gastralgin, Roxit, Altat, Xarcin

化学结构式(Chemical Structure):

参考文献No.	46470
标题:	Antiulcer phenoxypropylamine derivatives
作者:	Shibata, K.; et al. (Teikoku Hormone Manufacturing Co., Ltd.)
来源:	EP 0024510; JP 81115750; US 4293557

合成路线图解说明: The reductocondensation of piperidine (I) with 3-hydroxybenzaldehyde (II) by means of sodium borohydride in ethanol gives 3-(1-piperidylmethyl)phenol (III), which is then condensed with N-(3-bromopropyl)phthalimide (IV) by means of NaH in DMF yielding N-[3-[3-(1-piperidylmethyl)phenoxy]propyl]phthalimide (V). The hydrolysis of (V) with hydrazine in ethanol affords 3-[3-(1-piperidylmethyl)phenoxy]propylamine (VI), which is acylated with hydroxyacetic acid (VII) at 200 C giving N-[3-[3-(1-piperidylmethyl)phenoxy]propyl]hydroxyacetamide (VIII). Finally, this compound is acetylated with acetic anhydride at 100 C.

参考文献No.	50870
标题:	TZU-0460
作者:	Casta馿r, J.; Serradell, M.N.
来源:	Drugs Fut 1985,10(12),995

合成路线图解说明: The reductocondensation of piperidine (I) with 3-hydroxybenzaldehyde (II) by means of sodium borohydride in ethanol gives 3-(1-piperidylmethyl)phenol (III), which is then condensed with N-(3-bromopropyl)phthalimide (IV) by means of NaH in DMF yielding N-[3-[3-(1-piperidylmethyl)phenoxy]propyl]phthalimide (V). The hydrolysis of (V) with hydrazine in ethanol affords 3-[3-(1-piperidylmethyl)phenoxy]propylamine (VI), which is acylated with hydroxyacetic acid (VII) at 200 C giving N-[3-[3-(1-piperidylmethyl)phenoxy]propyl]hydroxyacetamide (VIII). Finally, this compound is acetylated with acetic anhydride at 100 C.