CAS: 808-26-4; (4S,4As,5Ar,12As)-4-(Dimethylamino)-3,10,12,12A-Tetrahydroxy-1,11-Dioxo-1,4,4A,5,5A,6,11,12A-Octahydrotetracene-2-Carboxamide

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CAS号5679-00-5 7-二去甲基米诺环素

地美环素置于10% Rhodium On Carbon,氢气,对甲苯磺酸体系中,用 甲醇 作为反应溶剂,20.0 °C,2.5 Mpa 条件下,反应 15.0H,以88%的收率获得产物山环素
参考文献:一种山环素的制备方法
标题:一种山环素的制备方法
摘要:本发明公开了一种山环素的制备方法,其包括下列步骤:醇和酸的混合溶剂中,氢气环境下,在催化剂的作用下,将化合物i进行反应,得到化合物ii即可;所述的醇为c1~c6的醇;所述的酸为硫酸,氢溴酸,甲磺酸,对甲苯磺酸,高氯酸和重量百分比为85%磷酸中的一种或多种.本发明的制备方法收率高,反应副产物少,纯度高,工艺过程简捷,后处理简单,溶剂和催化剂能够回收,环保压力小,成本低廉,适合于工业化生产.

专利信息

专利号:US-9688644-B2
优先权日:2009-04-30
标 题 :Synthesis of Tetracyclines and intermediates thereto
发明人：MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M
权利人:HARVARD COLLEGE
摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.

专利号:US-9884830-B2
优先权日:2004-05-21
标题 :Synthesis of tetracyclines and analogues thereof
发明人：MYERS ANDREW G; CHAREST MARK G; LERNER CHRISTIAN D; BRUBAKER JASON D; SIEGEL DIONICIO R
权利人:HARVARD COLLEGE
摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

专利号:US-8907104-B2
优先权日:2006-10-11
标 题 :Synthesis of enone intermediate
发明人：MYERS ANDREW G; BRUBAKER JASON D
权利人:HARVARD COLLEGE
摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.

专利号:US-8486921-B2
优先权日:2006-04-07
标 题:Synthesis of tetracyclines and analogues thereof
发明人：MYERS ANDREW G; BRUBAKER JASON D; SUN CUIXIANG; WANG QIU
权利人:MYERS ANDREW G; BRUBAKER JASON D; SUN CUIXIANG; WANG QIU; HARVARD COLLEGE
摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetra-cycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-pro liferative agents in the treatment of diseases of humans or other animals.

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.