DF-1601A
Chemical Name: 5-(tert-Butoxycarbonylamino)-2-carboxy-2-(tetrahydropyran-4-yloxy)pentanoic acid lithium salt; 2-[3-(tert-Butoxycarbonylamino)propyl]-2-(tetrahydropyran-4-yloxy)propanedioic acid lithium salt
CAS No. 196088-28-5, 196088-29-6 (free acid)
项目整合开发状态: Preclinical
项目研究机构: Domp?(Originator)
合成路线:Diethyl diazomalonate (III) was prepared by reaction of diethyl malonate (I) with p-tosyl azide (II) in the presence of Et3N.Subsequent coupling of (II) with 4-hydroxytetrahydropyran (IV) using dirhodium tetraacetate as the catalyst afforded ether (V).Alkylation of (V) with 3-(tert-butoxycarbonylamino)propyl bromide (VI) yielded adduct (VII).Finally,hydrolysis of ester groups of (VII) employing LiOH furnished the title dicarboxylic acid lithium salt.
📌 参考资料/链接:
参考文献标题:Geminal carboxylic acids and esters thereof pharmaceutical formulations containing them useful in the treatment of bone dysmetabolism
文献作者:Fiorentino,S.; Allegretti,M.; Mantovanini,M.; Clavenna,G.; Caselli,G.; Gandolfi,C.A.(Domp?Farmaceutici SpA)
参考来源:EP 0792878; US 5908863