📜(1S,2S)-2-羟基-3-环戊烯-1-甲醇置于四(三苯基膦)钯 三乙胺体系中,用 四氢呋喃,乙醇,二氯甲烷,二甲基亚砜 用作溶剂,化学反应 8.0H,反应生成Ent-阿巴卡韦 参考文献:Practical Enantiodivergent Syntheses Of Both Enantiomers Of Carbovir,1592U89 And Six-Membered Ring Analogues 标题:Practical Enantiodivergent Syntheses Of Both Enantiomers Of Carbovir,1592U89 And Six-Membered Ring Analogues 摘要:羟基内酯 4A-B(均可通过生物催化过程获得光学纯品)已被用于制备卡巴韦,1592U89 及其六元环类似物. Doi:10.1039/a708261D
专利号:US-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
专利号:WO-2005105153-A1 优先权日:2004-04-30 标 题 :Hydroxyalkyl derivatives of biologically active compounds 发明人:DESHPANDE JAYANT VENKATESH; KADAM VAISHALI MADHUKAR; GUPTE VANDANA SANDEEP; RANBHAN KAMLESH JAYANTILAL 权利人:KOPRAN RES LAB LTD; DESHPANDE JAYANT VENKATESH; KADAM VAISHALI MADHUKAR; GUPTE VANDANA SANDEEP; RANBHAN KAMLESH JAYANTILAL 摘要:Hydroxyalkyl derivatives of biologically active compounds represented by the formula VII wherein R2 = H, CI-12 alkyl, C6-12 aryl, or -OH and D = Biologically active agent having functional groups such as Formula (a) epoxy or aziridine and Z' = Formula (b) L= spacer comprising (un)substituted alkyl, hydroxyalkyl or alkoxy alkyl with the condition that the carbon chain length contains 2 to 6 carbon atoms when Z' = Formula (c) and pharmaceutically acceptable acid addition salts and enantiomers thereof Also process for the synthesis of compounds of the Formula VII and pharmaceutically acceptable acid addition salts and enantiomers thereof comprising condensation of the biologically active agents having functional groups such as Formula (d) epoxy or azifidine with substituted alkyl derivatives under alkaline conditions, at 20 - 80°C, in an organic solvent.
专利号:US-2010204463-A1 优先权日:2007-08-07 标题 :Preparation Of Synthetic Nucleosides via Pi-Allyl Transition Metal Complex Formation 发明人:LIOTTA DENNIS C; LI YONGFENG 权利人:LIOTTA DENNIS C; LI YONGFENG 摘要:This invention provides highly regioselective and stereoselective processes for preparing synthetic nucleosides. A process for the preparation of synthetic nucleosides is provided that comprises a) preparing a bicycloamide derivative, b) reacting the bicycloamide derivative with a nucleic acid base or heterocyclic base or salt thereof in the presence of a transition metal catalyst to form a cyclopentenecarboxamide, and c) cleaving a carboxamide group from the cyclopentenecarboxamide to form the synthetic nucleoside. The processes according to the invention can be used for the synthesis of a variety of anti-viral agents, including Abacavir, Carbovir, and Entecavir, as well as derivatives thereof.
专利号:US-9994550-B2 优先权日:2014-01-07 标题 :Heterocyclic modulators of lipid synthesis for use against cancer and viral infections 发明人:WAGMAN ALLAN S; JOHNSON RUSSELL J; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; DUKE GREG; OHOL-GUPTA YAMINI; HEUER TIMOTHY; O'FARRELL MARIE 权利人:3 V BIOSCIENCES INC 摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by dysregulation of a fatty acid synthase pathway by the administration of such compounds.
专利号:US-2024400552-A1 优先权日:2016-11-11 标题 :Heterocyclic modulators of lipid synthesis 发明人:BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S 权利人:SAGIMET BIOSCIENCES INC 摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by dysregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).
专利号:US-11622968-B2 优先权日:2011-03-08 标 题:Heterocyclic modulators of lipid synthesis 发明人:BUCKLEY DOUGLAS; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S 权利人:SAGIMET BIOSCIENCES INC 摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).
参考文献:10.1021/bi0121858 摘要:Ray AS, Yang Z, Shi J, Hobbs A, Schinazi RF, Chu CK, Anderson KS. Insights into the molecular mechanism of inhibition and drug resistance for HIV-1 RT with carbovir triphosphate. Biochemistry. 2002 Apr 23;41(16):5150–62. doi: 10.1021/bi0121858. 参考文献:10.2174/1874120701004010041|10.2174/1874613601004010041|10.2174/1874613601004020041 摘要:Satyanarayana K, Srivastava S. Patent Pooling for Promoting Access to Antiretroviral Drugs (ARVs) - A Strategic Option for India. Open AIDS J. 2010 Jan 19;4():41–53.