LU-420627(sodium salt), BSF-420627(sodium salt), LU-302872
Chemical Name: 3-[2-(3,4-Dimethoxyphenyl)ethoxy]-2(S)-(4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid
CAS No. 204267-34-5
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:The esterification of 2(S)-hydroxy-3-methoxy-3,3-diphenylpropionic acid (I) with NaOMe and dimethyl sulfate gives the methyl ester (II),which is submitted to and acid (TsOH) catalyzed transetherification with 2-(3,4-dimethoxyphenyl)ethanol (III) to yield 3-[2-(3,4-dimethoxyphenyl)ethoxy-2(S)-hydroxy-3,3-diphenylpropionic acid methyl ester (IV).The hydrolysis of (IV) with KOH in methanol affords the corresponding free acid (V),which is finally condensed with 4,6-dimethyl-2-(methylsulfonyl)pyrimidine (VI) by means of lithium amide in DMF.
📌 参考资料/链接：
参考文献标题:Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2-(4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872),a novel orally active mixed ETA/ETB receptor antagonist
文献作者:Amberg,W.; Hergenr鰀er,S.; Hillen,H.; Jansen,R.; Kettschau,G.; Kling,A.; Klinge,D.; Raschack,M.; Riechers,H.; Unger,L.
参考来源:J Med Chem 1999,42(16),3026