CAS: 10118-90-8; (4S,4As,5Ar,12As)-4,7-Bis(Dimethylamino)-3,10,12,12A-Tetrahydroxy-1,11-Dioxo-1,4,4A,5,5A,6,11,12A-Octahydrotetracene-2-Carboxamide

上下游产品

CAS号13614-98-7 盐酸米诺环素 | CAS号993-50-0 (二甲基氨基)三甲基锡 | CAS号113164-67-3 7-iodosancycline | CAS号149934-19-0 9-Animomin°Cycline

3,10,12,12A-Tetraacetylminocycline置于甲醇,Lithium Hydroxide体系中,化学反应 2.0H,以93%的收率获得米诺环素
参考文献:一种盐酸米诺环素的合成方法
标题:一种盐酸米诺环素的合成方法
摘要:本发明公开一种盐酸米诺环素的制备方法,其特征在于:以盐酸去甲基金霉素为起始原料,经过脱羟基反应得到6‑脱氧‑6‑去甲基金霉素(简称中间体i),中间体i经过乙酰基保护得到3,10,12,12A‑四乙酰基‑6‑脱氧‑6‑去甲基金霉素(简称中间体ii),中间体ii经过buchwald‑hartwig反应得到3,10,12,12A‑四乙酰基米诺环素(简称中间体iii),中间体iii经过水解得到米诺环素游离碱(简称中间体iv),中间体iv经过成盐得到盐酸米诺环素.本发明避免了传统盐酸米诺环素合成过程中使用的硝化,重氮化,偶氮化反应,降低了生产过程中的危险因素,操作简单,避免了环境污染,具有工业化生产的前景.

专利信息

专利号:WO-2012047907-A9
优先权日:2010-10-04
标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto
发明人：MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN
权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN
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 a wide variety of substituents at position 5 of the tetracycline ring system.

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-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-2024197774-A1
优先权日:2021-04-16
标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles
发明人：LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO
权利人:UNIV TEXAS
摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.