CAS: 2013-58-3; Meclocycline

上下游产品

土霉素 Oxytetracycline 79-57-2
四环素 Tetracycline 60-54-8

📜土霉素置于二甲胺,次氯酸叔丁酯体系中,用 甲醇 用作溶剂,以96.7 %的收率获得氯甲烯土霉素
参考文献:一种n-氯代土霉素的合成方法
标题:一种n-氯代土霉素的合成方法
摘要:本发明提供了一种n‑氯代土霉素的合成方法,其解决了现有n‑氯代土霉素的合成伴有大量的人力投入以及固废产生的技术问题,其包括如下步骤:(1)将装有温度计,搅拌器的四口烧瓶置于冷冻机中,加入甲醇,降温;(2)降到‑15~‑10oc后,加入土霉素,搅拌;(3)先滴加助剂,后滴加次氯酸叔丁酯,保温继续反应1~1.5H;其中,助剂为二甲胺,一甲胺或无水乙酸钠溶液,次氯酸叔丁酯的加入量为土霉素的1.5当量;(4)过滤,滤饼用冷甲醇漂洗,之后旋蒸干燥,得到n‑氯代土霉素.可广泛应用于化合物制备技术领域.

专利信息

专利号:US-9982005-B2
优先权日:2013-04-04
标 题 :Macrolides and methods of their preparation and use
发明人：MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG
权利人:HARVARD COLLEGE
摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.

专利号:US-11466046-B2
优先权日:2014-10-08
标题 :14-membered ketolides and methods of their preparation and use
发明人：MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG
权利人:HARVARD COLLEGE
摘要:Provided herein are methods of preparing new 14-membered ketolides via coupling of an eastern and western half moiety, followed by macrocyclization, and optional functionalization. Intermediates in the synthesis of these ketolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using these ketolides are also provided.

专利号:WO-2025128098-A1
优先权日:2023-12-13
标 题 :Solid oral dosage forms, kits, and methods of using the same
发明人：LI YING; LANGER ROBERT; TRAVERSO CARLO
权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

专利号:US-9693999-B2
优先权日:2011-01-26
标题:Small molecule RNase inhibitors and methods of use
发明人：DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE
权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education
摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.

专利号:US-10472663-B2
优先权日:2015-01-21
标 题:Procedure for the rapid determination of bacterial susceptibility to antibiotics that inhibit protein synthesis
发明人：FERNÃ?NDEZ GARCÃ?A JOSÉ LUIS; GOSÃ?LVEZ BERENGUER JAIME; BOU ARÉVALO GERMÃ?N; TAMAYO NOVAS MARIA; SANTISO BRANDARIZ REBECA; OTERO FARIÑA FÃ?TIMA MARÃ?A
权利人:ABM TECH LLC
摘要:The present invention relates to a method for the rapid evaluation of bacterial susceptibility or non-susceptibility of bacteria to antibiotics that inhibit protein synthesis. The rationale is to identify bacterial responses that depend or are influenced by protein synthesis. If this response is prevented or reduced by the antibiotic that inhibits the protein synthesis, the bacteria are susceptible to this antibiotic. Otherwise, if the response keeps similar despite the incubation with the antibiotic, the bacteria are not susceptible or resistant to this antibiotic. These responses could be determined at the DNA lev-el, cell wall level, morphological level or any other experimental approach, including metabolic, bio-chemical, physiological or genetic processes.

专利号:WO-2009056955-A1
优先权日:2007-10-30
标题 :Amine-bearing phospholipids (abps), their synthesis and use
发明人：ZUMBUEHL ANDREAS
权利人:UNIV BASEL; ZUMBUEHL ANDREAS
摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.