BMS-379224
Chemical Name: 2(R)-[4-(4-Cyanophenyl)thiazol-2-yl]-1(R)-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-ylmethyl)propoxymethyl dihydrogen phosphate disodium salt
项目整合开发状态: Phase I
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:The condensation of BMS-207147 (I) with phosphoric acid di-tert-butyl chloromethyl triester (II) by means of NaH in THF gives the phosphoric triester (III),which is finally hydrolyzed with TFA in dichloromethane and treated with Na2CO3 to provide the target disodium salt.
📌 参考资料/链接：
参考文献标题:Water soluble prodrugs of azole cpds.
文献作者:Hudyma,T.W.; Golik,J.; Ueda,Y.; Chen,C.-P.; Matiskella,J.D.(Bristol-Myers Squibb Co.)
参考来源:EP 1284737; US 6362172; WO 0152852
📄 详细内容
合成路线:The condensation of BMS-207147 (I) with phosphoric acid di-tert-butyl chloromethyl triester (II) by means of NaH in THF gives the phosphoric triester (III),which is finally hydrolyzed with TFA in dichloromethane and treated with Na2CO3 to provide the target disodium salt.
参考文献标题:BMS-379224,a water-soluble prodrug of ravuconazole
文献作者:Ueda,Y.; Barbour,N.; Bronson,J.J.; et al.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-817