2,3-二溴丁二酸二甲酯置于羟基脲,Potassium Tert-Butylate体系中,用 甲醇 用作溶剂,化学反应 17.0H,以66.3%的收率获得3-羟基异恶唑-5-甲酸甲酯 参考文献:Process Research And Development Of An Enantiomerically Enriched Allyic Amine,One Of The Key Intermediates For The Manufacture Of Synthetic Tetracyclines 标题:Process Research And Development Of An Enantiomerically Enriched Allyic Amine,One Of The Key Intermediates For The Manufacture Of Synthetic Tetracyclines 摘要:A Robust,Cost-Effective,And High Yielding Manufacturing Process For Enantiomerically Enriched (S)-Allylic Amine 3,A Key Intermediate For Fully Synthetic Tetracyclines Have Been Developed. Two-Novel And Scalable Asymmetric Vinylations Resulting High-To-Excellent Stereoselectivity Have Been Developed For The Key Step. The Final Product Is Purified By An Efficient Crystallization Of A L-Tartaric Salt. The Process Described Has Been Used To Manufacture Similar To 350 Kg Of The Tartaric Salt Of 3 With 99.0% Ee In 8 Steps (35% Overall Yield) From Cheap And Readily Available Dimethyl Maleate. Doi:10.1021/acs.Oprd.5B00274
专利信息
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-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-2018230111-A1 优先权日:2004-05-21 标 题:Synthesis of tetracyclines and analogues thereof
专利号:US-2010120784-A1 优先权日:2007-04-20 标题 :Novel heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:LACHANCE NICOLAS; LI CHUN SING; LECLERC JEAN-PHILPPE; RAMTOHUL YEEMAN K 权利人:LACHANCE NICOLAS; LI CHUN SING; LECLERC JEAN-PHILPPE; RAMTOHUL YEEMAN K 摘要:Heteroaromatic compounds of structural formula (I) or a pharmaceutically acceptable salt thereof, wherein W is a substituted heteroaryl, X and Y are each independently a bond, —O—, —S—, —S(O)—, —S(O) 2 —, —NR 6 —, —C(O)—, —C(CH 3 )(OH)— or —C(CH 3 )â•?CH—, u (I) is an integer from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis, obesity, Type 2 diabetes, insulin resistance, hyperglycemia, Metabolic Syndrome, neurological disease, cancer, and liver steatosis
专利号:US-8598148-B2 优先权日:2004-05-21 标题:Synthesis of tetracyclines and analogues thereof
专利号:US-2010130451-A1 优先权日:2006-04-07 标 题:Synthesis of tetracyclines and analogues thereof