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L-谷氨酸置于palladium On Activated Charcoal 乙二胺四乙酸,硫酸,水,氢气,Copper(II) Sulfate,三乙胺体系中,用 1,4-二氧六环,乙醇,苯 用作溶剂,化学反应 6.0H,反应生成Boc-L-谷氨酸-1-叔丁酯
参考文献:嘧啶-4-基取代的α-氨基酸的合成.炔基酮的通用方法
标题:嘧啶-4-基取代的α-氨基酸的合成.炔基酮的通用方法
摘要:Am与α-氨基酸炔基酮的反应显示出是嘧啶-4-基取代的α-氨基酸的通用途径.该途径也适用于平行合成方法,并允许形成一定范围的嘧啶-4-基取代的α-氨基酸,包括天然存在的α-氨基酸l-山thy碱4.
Doi:10.1039/a806741D

专利信息

专利号:US-2004101523-A1
优先权日:1989-07-27
标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension
发明人：REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
权利人:SEARLE & CO
摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.

专利号:WO-2014150909-A1
优先权日:2013-03-15
标 题:Lysine isotopologues, compositions comprising the same and methods of synthesis