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    • 5. 发明授权
    • Method of producing DAI from DOPA, using one reaction vessel
    • 使用一个反应容器从DOPA生产DAI的方法
    • US5486619A
    • 1996-01-23
    • US235763
    • 1994-04-29
    • Gottfried WenkeYuh-Guo PanMu-Ill LimLinas Stasaitis
    • Gottfried WenkeYuh-Guo PanMu-Ill LimLinas Stasaitis
    • C07D209/08
    • C07D209/08
    • A method of producing and isolating 5,6-diacetoxyindole (DAI) in a single reaction vessel comprising the following steps:(a) preparing a first solution comprising dopa, water and a solubilizing agent selected from the group consisting of an acid having a pk.sub.a value equal to or less than 4 and a first base having a pk.sub.b value equal to or greater than 10;(b) preparing a second solution comprising an oxidant, a buffer and water;(c) mixing the first and second solutions to form a combined solution which is rendered oxygen-free and has a pH of from about 6 to about 9;(d) stirring the combined solution in an inert atmosphere until 5,6-dihydroxyindole (DHI) is substantially completely formed;(e) adding a derivatizing agent and a second base to the combined solution to form a final solution;(f) stirring the final solution until the DHI is substantially fully consumed;(g) cooling the final solution to precipitate DAI;(h) isolating the precipitated DAI.
    • 一种在单个反应容器中生产和分离5,6-二乙酰氧基吲哚(DAI)的方法,包括以下步骤:(a)制备包含多巴,水和增溶剂的第一溶液,所述第一溶液选自具有pka 值等于或小于4,以及pkb值等于或大于10的第一碱基; (b)制备包含氧化剂,缓冲剂和水的第二溶液; (c)混合第一和第二溶液以形成无氧的并具有约6至约9的pH的组合溶液; (d)在惰性气氛中搅拌合并的溶液直到5,6-二羟基吲哚(DHI)基本上完全形成; (e)向组合溶液中加入衍生剂和第二碱以形成最终溶液; (f)搅拌最终溶液直到DHI基本上完全消耗; (g)冷却最终溶液以沉淀DAI; (h)分离析出的DAI。