CAS: 1393813-42-7; N-[5-(4-Bromophenyl)-6-Chloro-4-Pyrimidinyl]-N'-Propylsulfamide

相似化合物

146533-41-7 441797-83-7 2365406-85-3

4-溴苯乙酸甲酯置于lithium Amide,Sodium Methylate,三氯氧磷体系中,用 四氢呋喃,甲醇,二甲基亚砜 用作溶剂,化学反应 3.0H,反应生成N-[5-(4-溴苯基)-6-氯-4-嘧啶基]-N'-丙基氨基磺酰胺
参考文献:通过锂酰胺介导的亲核取代反应合成内皮素受体拮抗剂macitentan的改进的单锅法
标题:通过锂酰胺介导的亲核取代反应合成内皮素受体拮抗剂macitentan的改进的单锅法
摘要:摘要描述了从5-(4-溴苯基)-4,6-二氯嘧啶开始的内皮素受体拮抗剂macitentan的改进,简单,有效和可伸缩合成,总收率约为62%. 图形概要
Doi:10.1007/s00706-017-2098-2

专利信息

专利号:US-11667610-B2
优先权日:2016-09-28
标题:Method for preparing Macitentan and intermediate compound thereof
发明人：JIA QIANG; MA CHI; YANG ZHENGWEI; YANG JINJIN
权利人:SEASONS BIOTECHNOLOGY TAIZHOU CO LTD
摘要:The present invention relates to technical field of chemical synthesis of drugs, and provides a preparation method of Macitentan and intermediate compound thereof. Adding THF solution containing compound II and 5-bromo-2-chloropyrimidine slowly into THF solution containing base to react, or adding THF solution containing compound II and THF solution containing 5-bromo-2-chloropyrimidine slowly at the same time into THF solution containing base to react and obtain Macitentan (shown as compound I), wherein the base is selected from sodium hydride, potassium hydride, lithium hydride or lithium bis(trimethylsilyl)amide. The selectivity of the preparation method is very good, which is suitable for industrial production. The obtained product Macitentan has good quality and high yield. And the product compound II also has good quality and high yield, its HPLC purity is up to 99.0%, the content of impurity A is less than 0.20%, the content of impurity B is less than 0.25%.