CAS: 77668-42-9; 2,3-Dichlorobenzoyl Cyanide

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CAS号2905-60-4 2,3－二氯苯甲酰氯 | CAS号143-33-9 氰化钠 | CAS号544-92-3 氰化亚铜 | CAS号50-45-3 2,3-二氯苯甲酸 | CAS号84057-84-1 拉莫三嗪 | CAS号84689-20-3 2-(2,3-二氯苯基)-2-...

2,3-二氯苯甲酸置于氯化亚砜,十六烷基三甲基溴化铵体系中,用 甲苯 作为反应溶剂,化学反应 14.0H,反应生成 2,3-二氯苯甲酰腈
参考文献:2,3-二氯苯甲酰氯氰化反应的多种催化体系评价:在拉莫三嗪的合成中的应用
标题:2,3-二氯苯甲酰氯氰化反应的多种催化体系评价:在拉莫三嗪的合成中的应用
摘要:2,3-二氯苯甲酰氰是合成拉莫三嗪的关键中间体.描述了各种催化体系用于氰化2,3-二氯苯甲酰氯氰化的评估.高通量实验确定了影响必要化学反应的许多条件,包括胺碱和相转移催化剂,以及使用乙腈作为极性助溶剂的无催化剂条件.新型催化剂cubr 2通过在高通量筛选实验中考虑到cu(i)的可能氧化来确定.发现cucn是实现清洁转化的最佳氰化物来源.然而,在许多条件下,Cucn的溶解度是限制反应速率的主要因素.通过使用乙腈作作为反应溶剂来提高cucn的溶解度,即使在没有测试的催化剂的情况下,也可以提高反应速率,但是产物的分离非常复杂.在没有乙腈助溶剂的情况下,相转移催化剂(如四丁基溴化铵(tbabr))是有效的.但是,由于cucn固体的意外团聚,Tbabr的使用导致每次运行的反应曲线不一致.改用十六烷基三甲基溴化铵(ctab)减轻了这种结块现象,从而导致了始终如一的反应性.
DOI:10.1021/acs.Oprd.7B00262

专利信息

专利号:US-7390899-B2
优先权日:2002-09-20
标 题:Process for the synthesis of high purity 3,5-diamino-6-(2,3-dichlorophenyl) (1,2,4-triazine)
发明人：NEU JOZSEF; GIZUR TIBOR; TOERLEY JOZSEF; CSABAI JANOS; VEGH FERENC; KALVIN PETER; TARKANYI GABOR
权利人:RICHTER GEDEON VEGYESZET
摘要:The present invention relates to a new process for the synthesis of high purity 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine of formula (I) using 2,3-dichlorobenzoyl cyanide and an aminoguanidine salt as starting materials. 2,3-dichlorobenzoyl cyanide is reacted with 1-2 mol equivalent of aminoguanidine salt in 3-6 mol equivalent of methanesulfonic acid, then the obtained adduct of formula (IV) is transformed without isolation into the product with magnesium oxide. In given case the obtained crude product can be recrystallized from a proper organic solvent

专利号:WO-2007069265-A1
优先权日:2005-12-12
标 题 :A novel process for the synthesis of lamotrigine and its intermediate
发明人：RAMAKRISHNAN ARUL; BHUSHAN VASANT DABHOLKAR; DINESH B DEORE
权利人:UNICHEM LAB LTD; RAMAKRISHNAN ARUL; BHUSHAN VASANT DABHOLKAR; DINESH B DEORE
摘要:This invention discloses a process for the preparation of 3,5-Diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine of a formula (I), commonly known as Lamotrigine which comprises the step of reacting aminoguanidine bicarbonarte and 2,3- dichlorobenzocynide with a reagent prepared by dissolving phosphorus pentoxide and methane sulfonic acid, to produce a novel intermediate 2-(2,3-dichlorophenyl)-2-(aminoguanidine)-acetonitrile monomesylate which is further cyclized to lamotrigine without basification.

专利号:US-2006178511-A1
优先权日:2002-09-20
标题:Process for the synthesis of high purity3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine

专利号:CA-2498761-A1
优先权日:2002-09-20
标 题 :New process for the synthesis of high purity 3,5-diamino-6-(2, 3-dichlorophenyl)-1,2,4-triazine

专利号:EP-1539720-A1
优先权日:2002-09-20
标题:New process for the synthesis of high purity 3,5-diamino-6-(2, 3-dichlorophenyl)-1,2,4-triazine

专利号:EP-1539720-B1
优先权日:2002-09-20
标题 :New process for the synthesis of high purity 3,5-diamino-6-(2, 3-dichlorophenyl)-1,2,4-triazine