首页> 外国专利> Procedure for obtaining a Derivative of 11 - (4 - (1-piperazinyl) dibenz (B, f) (1.4) thiazepine.

Procedure for obtaining a Derivative of 11 - (4 - (1-piperazinyl) dibenz (B, f) (1.4) thiazepine.

机译:获得11-(4-(1-哌嗪基)dibenz(B,f)(1.4)噻嗪类衍生物的步骤。

摘要

Procedure for obtaining a Derivative of 11 - (4) - 1-piperazinyl) dibenzo [B, F] [1,4] thiazepine, fu00f3rmu00fala general I, which means Hydrogen or a Group - (CH2) 2 - Oh group or a - (CH2) 2 - or - (CH2 2 - Oh), or a Salt thereof, comprises a step in which REACT with 10h - Dibenzo [B, F] [1,4] thiazepin-11 - ona, a Derivative of piperazineIn the presence of a Titanium alkoxide, of General formula ti (OR) 4, where r is an alkyl group, linear or branched, one to eight carbon ATOMS, to obtain the Derivative of formula (i) or a Salt thereof.In the case that a is - (CH2) 2 - or - (CH2) 2 - Oh, then the Derivative of piperazine is 1 - (2 - (2-hydroxyethoxy) ethyl) piperazine derivative 11 - (4 - 1-piperazinyl) dibenzo [B, F] [1,4] thiazepine is quetiapine (11 - (4 - (2 - (2-hydroxyethoxy) ethyl) - 1-piperazinyl) dibenzo [B, F] [1,4] thiazepine).The procedure may include an additional stage of reaction of Quetiapine with fumaric acid to obtain Quetiapine hemifumarate.
机译:获得11-(4)-1-哌嗪基)二苯并[B,F] [1,4]噻氮平,f u00f3rm u00fala通式I的衍生物的步骤,其中I表示氢或基团-(CH2)2-哦基团或-(CH 2)2-或-(CH 2 2-Oh)或其盐包括以下步骤:其中与10h-二苯并[B,F] [1,4]噻嗪11-11-ona,a哌嗪的衍生物在通式为ti(OR)4的钛醇盐的存在下,其中r为直链或支链的烷基,具有1至8个碳原子的ATOMS,以获得式(i)的衍生物或其盐。在a为-(CH2)2-或-(CH2)2-欧姆的情况下,哌嗪衍生物为1-(2-(2-羟基乙氧基)乙基)哌嗪衍生物11-(4-1-哌嗪基)二苯并[B,F] [1,4]硫氮平为喹硫平(11-(4-(2--(2-羟基乙氧基)乙基)-1-哌嗪基)二苯并[B,F] [1,4]硫氮平)。程序可能包括奎硫平与富马酸反应的另一个阶段,以得到喹硫平半富马酸盐。

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