CAS: 199463-33-7; N-(4-Fluorophenyl)-4,5-Dimethyl-6-(1-Methyl-3,4-Dihydroisoquinolin-2(1H)-yl)Pyrimidin-2-Amine

上下游产品

2-Chloro-5,6-Dimethyl-4-(1-Methyl-1,2,3,4-Tetrahydroisoquinolin-2-yl)Pyrimidine 178308-12-8

2,4-二氯-5,6-二甲基嘧啶,1-甲基-1,2,3,4-四氢异喹啉置于双(三甲基硅烷基)氨基钾,三乙胺体系中,用 四氢呋喃,N,N-二甲基甲酰胺 用作溶剂,化学反应 16.0H,反应生成盐酸瑞伐拉赞
参考文献:具有抗癌活性的n-杂芳基胺的合成:N-杂芳基烷基醚与胺的亲核胺化作用.
标题:具有抗癌活性的n-杂芳基胺的合成:N-杂芳基烷基醚与胺的亲核胺化作用.
摘要:描述了n-杂芳基烷基醚与各种胺的温和胺化方案.通过使用简单易用的碱基作为启动子通过c-o键裂解来实现这种转化,从而提供了一种新的胺化策略来使用多种抗癌活性化合物.出色的官能团兼容性,可扩展性,广泛的底物范围以及多种药物的容易衍生化,突出了这项工作.
Doi:10.1021/acs.Orglett.9B01711

专利信息

专利号:US-2008280855-A1
优先权日:2005-06-22
标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles
发明人：CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO
权利人:NYCOMED GMBH
摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.

专利号:WO-02088088-A9
优先权日:2001-04-27
标题 :Process for preparing 1-methyl-1,2,3,4-tetrahydroisoquinoline or a salt thereof
发明人：BREEN GARY FRANCIS; FORTH MICHAEL ANTHONY; POPKIN MATTHEW EDWARD
权利人:SB PHARMCO INC; BREEN GARY FRANCIS; FORTH MICHAEL ANTHONY; POPKIN MATTHEW EDWARD
摘要:The invention provides a process for preparing 1-methyl-1,2,3,4-tetrahydroisoquinoline of formula (A), or a salt thereof, the process comprising: (i) reacting N-(2-chloroethyl)-α-methylbenzylamine of formula (B), or a salt thereof, with a Lewis acid such as AlCl3, and (ii) causing or allowing cyclisation to 1-methyl-1,2,3,4-tetrahydroisoquinoline. The invention also provides a process for preparing 1-methyl-1,2,3,4-tetrahydroisoquinoline of formula (A), or a salt thereof, the process comprising: (i) reacting a N-(2-haloethyl)-α-methylbenzylamine, or a salt thereof, with a Lewis acid and (ii) causing or allowing cyclisation to 1-methyl-1,2,3,4-tetrahydroisoquinoline at a temperature of ≤130°C. The use of N-(2-chloroethyl)-α-methylbenzylamine and/or lower cyclisation temperatures decreases the amount of certain impurities formed in the reaction. In other aspects of the invention, the 1-methyl-1,2,3,4-tetrahydroisoquinoline can be used in the synthesis of 5,6-dimethyl-2-(4-fluorophenylamino)-4-(1-methyl-1,2,3,4-tetrahydroisoquinolin-2-yl)pyrimidine (SB 641257, YH1885), a pharmaceutically active reversible proton pump inhibitor.

专利号:CN-114616340-A
优先权日:2019-07-09
标题 :Process for the synthesis of anticoagulant polysaccharides

专利号:CN-118978468-A
优先权日:2024-07-31
标 题 :Synthesis method of voronoi fumarate intermediate

专利号:CN-119798142-A
优先权日:2025-01-15
标 题 :Asymmetric catalytic synthesis method of chiral 3-aminopiperidine and derivative thereof