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-2016207894-A1 优先权日:2013-10-17 标 题:Synthesis of Diacids, Dialdehydes, or Diamines from THF-Diols 发明人:STENSRUD KENNETH 权利人:ARCHER DANIELS MIDLAND CO 摘要:A simple and elegant chemical process for the synthesis of oxygenated products, such as acids and aldehydes, or other derivative products, such as amines and nitriles, of cyclic bifunctional molecules made from renewable, bio-based sources such as HMF and/or its reduction product, 2,5-bis(hydroxymethyl)-tetrahydrofuran (bHMTHF) is described. In general, the process involves: a) generating a tetrahydrofuran-2,5-diyl-bis(methylene)-bis(sulfonate) from bHMTHFs using a sulfonate; b) displacing nucleophilically at least a sulfonate leaving group from the tetrahydrofuran-2,5-diyl-bis(methylene)-bis(sulfonate) to form a THF-dinitrile; and either c) oxidizing the THF-dinitrile with an acid having a pKa of ≦0 to generate a di-acid, or d) reducing partially the THF-dinitrile to generate a di-aldehyde, or e) reducing fully the THF-dinitrile to generate a di-amine.
专利号:US-9346743-B2 优先权日:2012-10-15 标题 :Processes for the synthesis of 2-amino-4,6-dimethoxybenzamide and other benzamide compounds 发明人:THAKKAR AMIT; ZEILER ANDREW G; SKUFCA ANTHONY F; SPRINGER JAMES J; ASSINK BRYCE KELLY; LOZANOV MARIO E 权利人:ALBEMARLE CORP 摘要:This invention provides a method for the synthesis of a 2-amino-4,6-dimethoxybenzamide and other benzamides of Compound I: wherein R 1 , R 2 , R 3 , and R 4 each independently represent a hydrogen, a C 1 -C 6 alkyl, or a C 1 -C 6 alkoxy; and wherein R 6 and R 7 each independently represent a hydrogen, a C 1 -C 6 alkyl, a protecting group, or a directing group.
专利号:WO-2015177083-A1 优先权日:2014-05-19 标题 :STEREOSELECTIVE SYNTHESIS OF INTERMEDIATES IN THE PREPARATION OF ß-C-ARYLGLUCOSIDES 发明人:ZUPANCIC BORUT; SELIC LOVRO; CUSAK ANJA; RICHTER FRANK 权利人:LEK PHARMACEUTICALS 摘要:The invention belongs to the fields of pharmaceutical industry, and particularly to an improved stereoselective synthesis of intermediate compounds for the preparation of gliflozins, for example canagliflozin or structurally similar gliflozins. Gliflozins, such as canagliflozin, dapagliflozin, empagliflozin, or ipragliflozin, inhibit the sodium-dependent glucose cotransporter 2 (SGLT2) in the kidney and as such are useful in the treatment of type-2 diabetes.
专利号:US-6686485-B2 优先权日:2001-04-19 标题:Synthesis of coenzyme Q10, ubiquinone 发明人:WEST DANIEL DAVID 摘要:Processes for the stereospecific synthesis of coenzyme Q10, ubiquinone, are disclosed; a semi synthetic procedure using solanesol derived from tobacco waste as the starting material. The process of the invention results in high yields of isometrically useful compositions containing the optically pure isomers.
专利号:US-9611206-B2 优先权日:2011-03-02 标题:Synthesis of intermediate for treprostinil production 发明人:SHARMA VIJAY 权利人:UNITED THERAPEUTICS CORP 摘要:The compound according to Formula I is an intermediate in the synthesis of prostacylin analogs. The present invention provides an efficient method for synthesizing a Formula I compound.