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项目整合精选>>>Azithromycin, DCH3, XZ-450, CP-62993, Zentavion, Toraseptol, Vinzam, Zithromac, Zitromax Avium 600, Zitromax, Zithromax, Sumamed
Azithromycin, DCH3, XZ-450, CP-62993, Zentavion, Toraseptol, Vinzam, Zithromac, Zitromax Avium 600, Zitromax, Zithromax, Sumamed
阿奇霉素阿奇霉素二水合物Chemical Name: 9-Deoxo-9a-aza-9a-methyl-9a-homoerythromycin A ; [2R-(2R*,3S*,4R*,5R*,8R*,10R*,11R*,12S*,13S*,14R*)]-13-[(2,6-Dideoxy-3C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,6,8,10,12,14-heptamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl]oxy]-1-oxa-6-azacyclopentadecan-15-one
CAS No. 83905-01-5, 90581-31-0 (diHCl), 117772-70-0 (dihydrate), 90581-30-9 (monoHCl)
项目整合开发状态: Launched-1988
项目研究机构: Pfizer (Orphan Drug), Pliva (Originator), Almirall Prodesfarma (Licensee), Pfizer (Licensee), Vita (Licensee)
合成路线:This compound can be obtained by two different ways:1) The oxidation of 9-deoxo-9a-aza-9a-homoerythromycin A (I) with 30% H2O2 in methanol gives the N-hydroxy-9-deoxo-9a-aza-9a-homoerythromycin A N'-oxide (II),which is methylated with ICH3 and K2CO3 in dichloromethane to afford N-methyl-9-deoxo-9a-aza-9a-homoerythromycin A bis(N-oxide) (III).Finally,this compound is reduced with H2 over Pd/C in ethanol.2) By methylation of 9-deoxo-9a-aza-9a-homoerythromycin A (I) with formaldehyde and formic acid in CHCl3.
📌 参考资料/链接：
参考文献标题:N-Methyl 11-aza-10-deoxo-10-dihydroerythromycin A,intermediates therefor
文献作者:Bright,G.M.(Pfizer Inc.)
参考来源:EP 0101186; JP 1193292; US 4474768
📄 详细内容
合成路线:This compound can be obtained by two different ways:1) The oxidation of 9-deoxo-9a-aza-9a-homoerythromycin A (I) with 30% H2O2 in methanol gives the N-hydroxy-9-deoxo-9a-aza-9a-homoerythromycin A N'-oxide (II),which is methylated with ICH3 and K2CO3 in dichloromethane to afford N-methyl-9-deoxo-9a-aza-9a-homoerythromycin A bis(N-oxide) (III).Finally,this compound is reduced with H2 over Pd/C in ethanol.2) By methylation of 9-deoxo-9a-aza-9a-homoerythromycin A (I) with formaldehyde and formic acid in CHCl3.
参考文献标题:11-Methyl-11-aza-4-O-cladinosyl-6-O-desosaminyl-15-ethyl-7,13,14-trihydroxy-3,5,7,9,12,14-hexamethyl-oxacyclopentadecane-2-one and derivatives thereof
文献作者:Djokic,S.; Kobrehel,G.(Pliva Pharmaceutical,Chem.,Food & Cosmetic Ind.,Inc.)
参考来源:BE 0892357
合成路线:This compound can be obtained by two different ways:1) The oxidation of 9-deoxo-9a-aza-9a-homoerythromycin A (I) with 30% H2O2 in methanol gives the N-hydroxy-9-deoxo-9a-aza-9a-homoerythromycin A N'-oxide (II),which is methylated with ICH3 and K2CO3 in dichloromethane to afford N-methyl-9-deoxo-9a-aza-9a-homoerythromycin A bis(N-oxide) (III).Finally,this compound is reduced with H2 over Pd/C in ethanol.2) By methylation of 9-deoxo-9a-aza-9a-homoerythromycin A (I) with formaldehyde and formic acid in CHCl3.
参考文献标题:Azithromycin
文献作者:Castar,J.; Serradell,M.N.
参考来源:Drugs Fut 1988,13(1),9
产品链接: CAS No. 83905-01-5›› 产品链接: CAS No.117772-70-0››