首页> 外国专利> A PROCEDURE FOR THE PREPARATION OF 1-(2-(5- DIMETHYLAMINOMETHYL-2-(FURYLMETHYLTHIO)-ETHYL))-AMINO-1-M543ETHYLAMINO-2-NITRO ETHYLENE HYDROCHLORIDE USING FORMULA (I).

A PROCEDURE FOR THE PREPARATION OF 1-(2-(5- DIMETHYLAMINOMETHYL-2-(FURYLMETHYLTHIO)-ETHYL))-AMINO-1-M543ETHYLAMINO-2-NITRO ETHYLENE HYDROCHLORIDE USING FORMULA (I).

机译:使用式(I)制备1-(2-(5-二甲基亚氨基甲基-2-(氟代甲基乙基)-乙基))-氨基-1-M <543>乙基氨基-2-硝基乙烯氢氯化物的方法。

摘要

The invention relates to a process for preparing the hydrochloride of 1-(2-(5-[dimethylaminomethyl]-2- [furylmethylthio]ethyl))amino-1-[methylamino]-2- nitroethylene of the formula I and is characterized in that the hydrochloride of 5-[dimethylaminomethyl]furfuryl alcohol of the formula IV is reacted with cysteamine hydrochloride at temperatures between 50 degree C and 100 degree C in the absence of solvents - preferably in the presence of a catalytic amount of from 10 to 20 mol% of mineral acid and, where appropriate, in the presence of 5 to 10 mol% of an organic acid with a pKa of 0 to 2 or in the presence of a catalytic amount of 2 to 10 mol% of amounts, which are catalytic under the reaction conditions, of mineral acid, and possibly compounds which release organic acids with a pKa of 0 - 2, the dihydrochloride, formed in this way, of the base of the formula II is removed and the monohydrochloride of the base of the formula II is liberated therefrom with an inorganic base and is - where appropriate after intermediate isolation - reacted with 1-[methylthio]-1- [methylamino]-2-nitroethylene of the formula III at temperatures between 40 degree C and 80 degree C, and the hydrochloride thus obtained, of the base of the formula I is removed.
机译:本发明涉及一种制备式I的1-(2-(5- [二甲基氨基甲基] -2- [呋喃基甲硫基]乙基)氨基-1- [甲基氨基] -2-硝基乙烯的盐酸盐的方法,其特征在于式IV的5- [二甲基氨基甲基]糠醇的盐酸盐与半胱胺盐酸盐在50°C至100°C的温度下在无溶剂存在下反应-优选在催化量为10至20 mol的条件下反应%的无机酸,以及在合适的情况下,在5至10 mol%的pKa为0至2的有机酸的存在下,或在2至10 mol%的催化量的存在下,在在无机酸的反应条件下,以及可能以pKa为0-2释放有机酸的化合物的反应条件下,将式II的碱以此方式形成的二盐酸盐除去,式II的碱的一盐酸盐用无机碱从中解放出来,并且-w在中间分离后这里合适的是在40℃至80℃的温度下与式III的1- [甲硫基] -1- [甲基氨基] -2-硝基乙烯反应,并由此制得盐酸盐,我被删除了。

著录项

  • 公开/公告号AR242029A1

    专利类型

  • 公开/公告日1993-02-26

    原文格式PDF

  • 申请/专利权人 RICHTER GEDEON VEGYESZETI GYAR R.T.;

    申请/专利号AR19840297205

  • 发明设计人

    申请日1984-07-13

  • 分类号C07D307/52;A61K31/34;

  • 国家 AR

  • 入库时间 2022-08-22 05:12:40

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