CAS: 76801-85-9; (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-11-(((2S,3R,4S,6R)-4-(Dimethylamino)-3-Hydroxy-6-Methyltetrahydro-2H-Pyran-2-yl)Oxy)-2-Ethyl-3,4,10-Trihydroxy-13-(((2R,4R,5S,6S)-5-Hydroxy-4-Methoxy-4,6-Dimethyltetrahydro-2H-Pyran-2-yl)Oxy)-3,5,8,10,12,14-Hexamethyl-

上下游产品

阿奇霉素 Zithromax(R) 83905-01-5
红霉素 Erythromycin 114-07-8
Erythromycin A 9-(E)-Oxime 111321-02-9
红霉素a肟 Erythromycin A Oxime 13127-18-9
9-Deoxo-6-Deoxy-6,9-Epoxy-9,9A-Didehydro-9A-Aza-Homoerythromycin A 342371-84-0
Erythromycin A 6,9-Imino Ether

硫氰酸红霉素置于钾硼氢,磷酸,盐酸羟胺,碳酸氢钠,三乙胺,对甲苯磺酰氯体系中,用 甲醇,水,丙酮 作为反应溶剂,化学反应 67.0H,反应生成 阿奇霉素 A
参考文献:一种去甲阿奇霉素的制备方法
标题:一种去甲阿奇霉素的制备方法
摘要:本发明公开了一种去甲阿奇霉素的制备方法,涉及大环内酯类抗生素制备技术领域.红霉素a 6,9‑亚胺醚在水中,0oc‑室温,Ph 7.0‑9.0下,用还原试剂硼氢化钠或硼氢化钾还原;之后在有机溶剂和水存在下,0oc‑室温,Ph 2.0‑3.5下,进行连续水解;再将连续水解两相反应液加入碱性水溶液中,调节ph>=12,搅拌,分层,弃去水相;有机溶剂为二氯甲烷,氯仿,1,2‑二氯甲烷,乙酸乙酯或乙酸丁酯;连续水解的最后一次水解反应结束后,分层,水相直接加入碱性水溶液中,调节ph>=12,搅拌,析出去甲阿奇霉素.本方法提高了还原剂利用率,可以控制硼酸酯的逆反应,减少不必要的分离过程,得到高质量去甲阿奇霉素.

专利信息

专利号:US-2004266997-A1
优先权日:2003-03-25
标题:Degradation products of azithromycin, and methods for their indentification
发明人：PESACHOVICH MICHAEL; ISAACS SARAH; SINGER CLAUDE; SCHWARTZ EDUARD; BERGER EDIT
权利人:PESACHOVICH MICHAEL; ISAACS SARAH; SINGER CLAUDE; SCHWARTZ EDUARD; BERGER EDIT
摘要:The invention is directed to degradation products of azithromycin, methods for the preparation and identification of the degradation products which may be produced during storage and/or synthesis of azithromycin.

专利号:US-7358367-B2
优先权日:2002-09-27
标题:Present invention relates to the new 3-decladinosyl derivatives of 9-deoxo-9a-aza9a-homoerythromycin a 9a, 11-cyclic carbamates
发明人：FAJDETIC ANDREA; KOBREHEL GABRIJELA; LAZAREVSKI GORJANA; MUTAK STJEPAN
权利人:GLAXOSMITHKLINE ZAGREB
摘要:The present invention relates to the new 3-decladinosyl derivatives of 9-de-oxo-9a-aza9a-homoerythromycin A 9a,11-cyclic carbamate of the general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, wherein R 1 individually stands for hydrogen, hydroxyl or a group of the formula (II), wherein X individually stands for C 1 -C 6 alkyl group, C 2 -C 6 alkenyl group or X individually stands for C 1 -C 6 alkyl group with at least one incorporated O, S or N atom or X individually stands for (CH 2 ) n —Ar or X individually stands for (CH 2 ) n -heterocycloalkyl, wherein (CH 2 ) n individually stands for alkyl, wherein n is 1-10, with or without incorporated atom O, S or N, wherein Ar individually stands for 5-10-membered monocyclic or bycyclic aromatic ring with 0-3 atom O, S or N, unsubstituted or substituted with 1-3 group, which are selected independently from halogen, OH, OMe, NO 2 , NH 2 , amino-C 1 -C 3 alkyl or amino-C 1 -C 3 dialkyl, CN, SO 2 NH 2 , C 1 -C 3 alkyl, and heterocycloalkyl stands for unaromatic, partially or completely saturated 3-10-membered monocyclic or bicyclic ring system, which includes 3-8-membered monocyclic or bicyclic ring, which includes 6-membered aromatic or heteroaromatic ring connected with a unaromatic ring with or without incorporated O, S or N atom, unsubstituted or substituted with 1-4 group, which are selected independently from halogen, OH, OMe, NO 2 , NH 2 , amino-C 1 -C 3 alkyl or amino-C 1 -C 3 dialkyl, CN, SO 2 NH 2 , C 1 C 3 alkil, —C(O)—, COOH or R 1 together with R 2 stands for ketone, R 2 individually stands for hydrogen or together with R 1 stands for ketone or together with R 3 stands for ether, R 3 individually stands for hydroxyl, a group of the formula —OX or together with R 2 stands for ether, R 4 individually stands for hydrogen, C 1 -C 4 alkyl group or C 2 -C 4 alkenyl group, and R 5 individually stands for hydrogen or hydroxyl protected group, to intermediates for synthesis of other macrolide compounds with antibacterial activity, to the process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to the process for the preparation of pharmaceutical compositions, as well as the use of pharmaceutical compositions for treating bacterial infections

专利号:US-6369035-B1
优先权日:1997-10-16
标 题:3,6-hemiketals from the class of 9A-azalides
发明人：KOBREHEL GABRIJELA; LAZAREVSKI GORJANA; VINKOVIC MLADEN
权利人:PLIVA FARMACEUTSKA INDUSTRJA D
摘要:The invention relates to novel compounds from the class of macrolide antibiotics. Particularly, the invention relates to novel 3,6-heiketals from the class of 9a-azalides, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for their preparation and to the use thereof as antibiotics or as intermediates for the synthesis of other macrolide antibiotics.

专利号:US-5869629-A
优先权日:1996-07-11
标题 :Synthesis of 9-deoxo-9a-aza-11,12-deoxy-9a-methyl-9a-homoerythromycin A 11,12 Hydrogenorthoborate dihydrate and a process for the preparation of azitromicin dihydrate
发明人：BAYOD JASANDA D MIGUEL SANTOS; FERNANDEZ GONZALEZ D JOSERAMON
权利人:ASTURPHARMA S A
摘要:The preparation of azitromycin dihydrate from 9-deoxo-9a-aza-11,12-deoxy-9a-methyl-9a-homoerythromycin A 11,12-hydrogenorthoborate, obtained by a step by step process starting from 9-deoxo-6-deoxy-6,9-epoxy-9,9a-dihydro-9a-azahomoerythromycin A is a process which takes place under mild conditions and with good yields.

专利号:US-4526889-A
优先权日:1982-11-15
标 题 :Epimeric azahomoerythromycin A derivative, intermediates and method of use
发明人：BRIGHT GENE M
权利人:PFIZER
摘要:Antibacterial 4''-epi-9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A, pharmaceutically-acceptable salts thereof, pharmaceutical compositions comprising antibacterially-effective amounts thereof, a method of treatment of bacterial infections with antibacterially effective amounts thereof, and intermediates for the synthesis thereof from erythromycin A.

专利号:EP-0827965-A2
优先权日:1996-07-11
标 题:Synthesis of 9-deoxo- 9a-aza 11,12-deoxy- 9a-methyl-9a-homoerythromycin A 11,12- hydrogenorthoborate dihydrate