RPR-101511A, -Drug Synthesis Database

【结构式】

【药物名称】RPR-101511A

【化学名称】6,7-Dimethoxy-2-(3-thienyl)quinoxaline hydrochloride

【CA登记号】146847-57-6

【分子式】C₁₄H₁₃ClN₂O₂S

【分子量】308.78891

【开发单位】Aventis Pharma (Originator)

【药理作用】CARDIOVASCULAR DRUGS, Restenosis Treatment of, Treatment of Disorders of the Coronary Arteries and Atherosclerosis, Tyrosine Kinase Inhibitors

合成路线1

Oxidation of 3-acetylthiophene (I) with selenium dioxide in refluxing dioxan provided 3-thienylglyoxaldehyde hydrate (II). This was then condensed with 4,5-dimethoxy-1,2-phenylenediamine (III) in boiling EtOH to produce the target quinoxaline, which was finally isolated as the hydrochloride salt.

参考文献中间体

【1】 Myers, M.R.; Maguirre, M.P.; Spada, A.P.; Persons, P.E. (Aventis Pharmaceuticals, Inc.); Bis mono- and bicyclic aryl and heteroaryl cpds. which inhibit EGF and/or PDGF receptor tyrosine kinase. US 5480883 .

中间体序号	中间体编号	品名	CAS号	分子式	供应商	用于合成
(I)	34619	1-(3-thienyl)-1-ethanone	1468-83-3	C₆H₆OS	详情	详情
(II)	34620	2,2-dihydroxy-1-(3-thienyl)-1-ethanone		C₆H₆O₃S	详情	详情
(III)	34621	4,5-dimethoxy-1,2-benzenediamine; 2-amino-4,5-dimethoxyphenylamine		C₈H₁₂N₂O₂	详情	详情

Extended Information

Drug NewChemical Entity Original Patent(1)