ILX-295501, LY-295501

5-苯呋喃磺酰胺,N-[[(3,4-二氯苯基)氨基]-2,3-二氢-Chemical Name: 1-(3,4-Dichlorophenyl)-3-(2,3-dihydrobenzofuran-5-ylsulfonyl)urea; N1-(3,4-Dichlorophenyl)-N2-(2,3-dihydrobenzofuran-5-ylsulfonyl)urea
CAS No. 150869-74-2
项目整合开发状态: Phase II
项目研究机构: Lilly (Originator), Ilex Oncology (Codevelopment)
合成路线:Electrophilic sulfonation of 2,3-dihydrobenzofuran (I) using sulfur trioxide-dimethylformamide complex produced sulfonic acid (II),which was subsequently converted into the sulfonyl chloride (III) by chlorination with SOCl2.Reaction of sulfonyl chloride (III) with a solution of ammonia in cold dichloroethane gave rise to the sulfonamide (IV).This was subsequently condensed with 3,4-dichlophenyl isocyanate (V) to furnish the target sulfonyl urea
📌 参考资料/链接:
参考文献标题:Synthesis of bicyclic aromatic sulfonic acids,sulfonyl chlorides and sulfonamides
文献作者:Tao,E.V.-P.; Miller,W.D.(Eli Lilly and Company)
参考来源:EP 0583960

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