Chemical Name: N-(5-Chloro-3-methoxypyrazin-2-yl)-5-(dimethylamino)naphthalene-1-sulfonamide
CAS No. 173253-74-2
项目整合开发状态: Preclinical
项目研究机构: AstraZeneca (Originator)
合成路线:Bromination of 2-amino-5-chloropyrazine (I) with bromine in chloroform-pyridine provided bromopyrazine (II).Then,reaction with sodium methoxide in refluxing methanol afforded methyl ether (III).Finally,condensation of (III) with dansyl chloride (IV) in the presence of NaH in dimethoxyethane yielded the corresponding sulfonamide.
📄 详细内容
合成路线:Bromination of 2-amino-5-chloropyrazine (I) with bromine in chloroform-pyridine provided bromopyrazine (II).Then,reaction with sodium methoxide in refluxing methanol afforded methyl ether (III).Finally,condensation of (III) with dansyl chloride (IV) in the presence of NaH in dimethoxyethane yielded the corresponding sulfonamide.
参考文献标题:New non-peptide endothelin-A receptor antagonists: Synthesis,biological properties,and structure-activity relationships of 5-(dimethylamino)-N-pyridyl-,-N-pyrimidinyl-,-N-pyridazinyl-,and -N-pyrazinyl-1-naphthalenesulfonamides
文献作者:Bradbury,R.H.; Bath,C.; Butlin,R.J.; Dennis,M.; Heys,C.; Hunt,S.J.; James,R.; Mortlock,A.A.; Sumner,N.F.; Tang,E.K.; Telford,B.; Whiting,E.; Wilson,C.
参考来源:J Med Chem 1997,40(6),996