Ro-23-9424/001(monoNa salt, diH2O), Ro-23-9424
5-硫-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸,7-[[(2Z)-(2-氨基-4-噻噻醇)(甲氧基亚胺基)乙酰]氨基]-3-[[[[6,8-二氟-1-(2-氟乙基)-1,4-二氢-7-(4-甲基-1-吡嗪基)-4-氧基-3-喹啉基]氧基]甲基]-8-氧基,(6R,7R)-(9CI)Chemical Name: [6R-[6alpha,7beta(Z)]]-7-[2-(2-Aminothiazol-4-yl)-2-(methoxyimino)acetamido]-3-[6,8-difluoro-1-(2-fluoroethyl)-1,4-dihydro-7-(4-methylpiperazin-1-yl)-4-oxoquinolin-3-ylcarbonyloxymethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid dihydrochloride; (6R,7R)-7-[2-(2-Aminothiazol-4-yl)-2(Z)-(methoxyimino)acetamido]-3-(6,8-difluoro-1-(2-fluoroethyl)-7-(4-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinolin-3-ylcarbonyloxymethyl)-3-cephem-4-carboxylic acid dihydrochloride
CAS No. 115622-58-7 (free base), 115699-46-2 (free base, Na salt)
项目整合开发状态: Phase II
项目研究机构: Roche (Originator)
合成路线:Displacement of iodide from the protected cephalosporin (I),with the potassium salt of fleroxacin (II) results in joining of the two fragments via an ester bond.Removal of protecting groups with trifluoroacetic acid in nitromethane followed by treatment with hydrochloric acid in acetone/water yields Ro 23-9424.
📌 参考资料/链接:
参考文献标题:Cephalosporin 3'-quinolone esters with a dual mode of action
文献作者:Albrecht,H.A.; Beskid,G.; Chan,K.-K.; Christenson,J.G.; Cleeland,R.; Deitcher,K.H.; Georgopapadakou,N.H.; Keith,D.D.; Pruess,D.L.; Sepinwall,J.; et al.
参考来源:J Med Chem 1990,33(1),77-86
📄 详细内容
合成路线:Displacement of iodide from the protected cephalosporin (I),with the potassium salt of fleroxacin (II) results in joining of the two fragments via an ester bond.Removal of protecting groups with trifluoroacetic acid in nitromethane followed by treatment with hydrochloric acid in acetone/water yields Ro 23-9424.
参考文献标题:Ro 23-9424
文献作者:Christenson,J.G.; Squires,E.
参考来源:Drugs Fut 1991,16(7),620
产品链接: CAS No. 115622-58-7››