专利号:US-9266863-B2 优先权日:2010-03-30 标题 :Process for the synthesis of azacitidine and decitabine 发明人:DE FERRA LORENZO; ZENONI MAURIZIO; TURCHETTA STEFANO; ANIBALDI MAURO; AMMIRATI ETTORE; BRANDI PAOLO; BERARDI GIORGIO 权利人:DE FERRA LORENZO; ZENONI MAURIZIO; TURCHETTA STEFANO; ANIBALDI MAURO; AMMIRATI ETTORE; BRANDI PAOLO; BERARDI GIORGIO; CHEMI SPA 摘要:Described herein is a process for the synthesis of azacitidine or decitabine, comprising the silylation of azacytosine in the presence of N,O-bis-trimethylsilyl-trifluoroacetamide. Such reaction is performed in an organic solvent, preferably aprotic, even more preferably selected from among dichloromethane, dichloroethane and/or acetonitrile. According to a further aspect of the process, 2 to 3 moles of N,O-bis-trimethylsilyl-trifluoroacetamide are used per mole of azacytosine, preferably from 2.2 to 2.5.
专利号:US-11629163-B2 优先权日:2017-06-30 标题:Methods of synthesizing nicotinamide riboside 发明人:MARCOTULLI ERIC; ALMINANA DAN; DELLINGER RYAN; MORRIS MARK; THAMATAM RAJESH 权利人:ELYSIUM HEALTH INC 摘要:Provided herein are efficient and scalable methods for the synthesis of nicotinamide riboside from riboside triacetate. Also provided are compositions comprising nicotinamide riboside, and therapeutic methods employing nicotinamide riboside.
专利号:US-4914233-A 优先权日:1988-03-01 标题:Synthesis of beta-thymidine 发明人:FRESKOS JOHN N; SENARATNE K PUSHPANANDA A 权利人:ETHYL CORP 摘要:A process is provided in which a mixture of alpha- and beta-anomers is converted selectively to the desired beta-thymidine. The process involves the following steps: (a) converting a mixture of alpha- and beta-anomers of tetra-O-acylribofuranose to tri-O-acyl-β-ribothymidine; (b) converting tri-O-acyl-β-ribothymidine to β-ribothymidine; (c) converting β-ribothymidine to 2,2'-anhydro-β-thymidine; (d) converting 2,2'-anhydro-β-thymidine to 2'-halo-2'-deoxy-5-methyluridine; and (e) converting 2'-halo-2'-deoxy-5-methyluridine to beta-thymidine. The mixture of alpha- and beta-anomers of tetra-O-acylribofuranose may be produced by any suitable procedure such as by converting lower alkyl ribofuranoside to the tetra-O-acylribofuranose mixture. The lower alkyl ribofuranosides may in turn be produced by various methods. However, a desirable way of effecting this conversion involves use of D-ribose as the starting material which is converted to the lower alkyl ribofuranoside.
专利号:US-2004186283-A1 优先权日:2003-03-17 标题:Synthesis of 5-azacytidine
专利号:US-7399754-B2 优先权日:2005-06-16 标 题:N2-quinoline or isoquinoline substituted purine derivatives 发明人:WU ZHANGGUI 权利人:WU ZHANGGUI 摘要:Novel compound having the following formula: n nwherein W represents a hydrogen, an optionally substituted C 1-6 alkyl, an optionally substituted C 3-6 cycloalkyl, or an optionally substituted C 1-6 haloalkyl, Y represents a hydrogen, or a saccharide, Q represents a quinoline or isoquinoline. Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same.
专利号:EP-1600451-A2 优先权日:1999-11-12 标题 :Synthesis of 2'-deoxy-l-nucleosides