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2(或3)-甲基及2(或3)-(N-哌啶甲(扌牚))-酪氨酸的合成
引用本文:任云峯,缪淑如. 2(或3)-甲基及2(或3)-(N-哌啶甲(扌牚))-酪氨酸的合成[J]. 药学学报, 1965, 12(3): 205-208
作者姓名:任云峯  缪淑如
作者单位:中国科学院药物研究所,中国科学院药物研究所 上海合成橡胶研究所
摘    要:交感神经的兴奋导致血压升高,而去甲肾上腺素是传递交感神经兴奋的化学介质.去甲肾上腺素系从酪氨酸在体内经过一系列生化反应而得,若干与酪氨酸代谢产物有关的类似物如α-甲基儿茶酚丙氨酸(Ⅰ)、α-甲基间酪氨酸(Ⅱ)等在动物试验中有明显的生理活性,临床上亦具有明显的降压作用.作者拟从对抗去甲肾上腺素的形成出发,合成若干酪氨酸的类似物,以寻找降低血压药物.从酪氨酸变成去甲肾上腺素的代谢

收稿时间:1964-10-27

THE PREPARATION OF 2(OR 3)-METHYL-AND 2(OR 3)-PIPERUDINYLTYROSINES
JEN YUN-FENG AND MEAU SHU-RU. THE PREPARATION OF 2(OR 3)-METHYL-AND 2(OR 3)-PIPERUDINYLTYROSINES[J]. Acta pharmaceutica Sinica, 1965, 12(3): 205-208
Authors:JEN YUN-FENG AND MEAU SHU-RU
Abstract:Nor-adrenaline is derived from tyrosine through a series of biochemical reactions, and certain related analogues (Ⅱ,Ⅲ) are potent in the treatment of hypertension. In order to find the compounds which may interfere with the biosynthesis of nor-adrenaline, several tyrosine analogues (Ⅳ,Ⅴ,Ⅵ, and Ⅶ) were synthesized. But none of these compounds are active. The above compounds were prepared by condensation of diethyl 2(or 3)-bromo- methyl-4-acetoxybenzyl-formamidomalonate with excess piperidine and subsequent hydro- lysis of the condensation products (Ⅸ,Ⅹ) and diethyl 2(or 3)-methyl-4-hydroxybenzyl- formamidomalonate with concentrated hydrochloric acid.
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