clarithromycinformaldehyd6-O-methyl-N-demethylerythromycin A 9-oxime60H86N2O17C60H86N2O17clarithromycin9-(benzylideneamino)-9-deoxo-12-deoxy-9,12-epoxy-6-O-methylerythromycin A6-methoxyerythromycin A 9-oxime
专利号:WO-9928333-A1 优先权日:1997-12-01 标题 :Chemical synthesis of 6-o-alkyl erythromycin c 发明人:MONTGOMERY STEPHEN H; IVES MICHAEL D; LIU JIH-HUA 权利人:ABBOTT LAB 摘要:A process of preparing a 6-O-alkyl derivative of erythromycin C is provided. The process includes the steps of protecting the 2',4'- and 9-oxime hydroxyls with acetyl and ketal protecting groups, alkylating the 6-hydroxyl, removing the protecting groups and deoximating. Intermediates used in the process are also provided.
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:WO-0112817-A1 优先权日:1999-08-12 标题:Evolution and use of enzymes for combinathorial and medicinal chemistry 发明人:KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL 权利人:MAXYGEN INC; LIU LU; KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL 摘要:This invention provides libraries of recombinant derivatizing enzymes that are useful for biocatalytic synthesis of derivatives oforganic molecules, including lead compounds for pharmaceutical use. The recombinant derivatizing enzymes catalyze reactions such as modification or replacement of functional groups on the organicmolecules, or addition of chemical moieties onto preexisting functional groups. The use of recombinant enzyme libraries enables one to obtain enzymes that catalyze the formation of organic molecule derivatives that could not otherwise be made using only naturally occurring enzymes.
专利号:AU-1528299-A 优先权日:1997-12-01 标 题 :Chemical synthesis of 6-o-alkyl erythromycin c
专利号:AU-1416699-A 优先权日:1997-11-17 标题 :Chemical synthesis of 6-o-alkyl erythromycin a
专利号:EP-1036084-A1 优先权日:1997-12-01 标 题 :Chemical synthesis of 6-o-alkyl erythromycin c
参考文献:10.1016/j.ejmech.2017.03.056 摘要:Koštrun S, Munic Kos V, Matanović Škugor M, Palej Jakopović I, Malnar I, Dragojević S, Ralić J, Alihodžić S. Around the macrolide – Impact of 3D structure of macrocycles on lipophilicity and cellular accumulation. European Journal of Medicinal Chemistry. 2017 Jun;133():351–64. doi: 10.1016/j.ejmech.2017.03.056.