D-2',3'-O-Thiocarbonylene-5'-O-Tert-Butyldimethylsilyl Inosine置于四丁基氟化铵,亚磷酸三乙酯体系中,用 四氢呋喃 作为反应溶剂,化学反应 0.5H,反应生成 2',3'-双脱氧双脱氢肌苷 参考文献:General Syntheses Of 2',3'-Dideoxynucleosides And 2',3'-Didehydro-2',3'-Dideoxynucleosides 标题:General Syntheses Of 2',3'-Dideoxynucleosides And 2',3'-Didehydro-2',3'-Dideoxynucleosides 摘要: DOI:10.1021/jo00270A036
专利号:US-11858953-B2 优先权日:2018-04-04 标 题:Compositions and methods for synthesis of phosphorylated molecules 发明人:CHAPUT JOHN; LIAO JEN-YU; BALA SAIKAT 权利人:UNIV CALIFORNIA 摘要:The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.
专利号:US-6927291-B2 优先权日:2001-03-01 标 题:Method for the synthesis of 2′,3′-dideoxy-2′,3′-didehydronucleosides 发明人:JIN FUQIANG; CONFALONE PASQUALE N 权利人:PHARMASSET LTD 摘要:An efficient synthetic route to antiviral 2′,3′-dideoxy-2′,3′-didehydro-nucleosides, such as 2′,3′-dideoxy and 2′- or 3′-deoxyribo-nucleoside analogs, from available precursors is disclosed, with the option of introducing functionality as needed. In one embodiment, a method for the preparation of β-D and β-L-2′,3′-dideoxy-2′,3′-didehydro-nucleosides is described that includes: activating a compound of structure (1) n n nwherein B is a pyrimidine or purine base and Y is O, S or CH 2 with an acyl halide of the formula X—C(â•?O)R 1 , X—C(â•?O)C(R 1 ) 2 OC(â•?O)R 1 or X—C(â•?O)OR 1 (wherein X is a halogen, and each R 1 is independently hydrogen, lower alkyl, alkyl, aryl or phenyl); reducing the resulting compound with a reducing agent to form a 2′,3′-dideoxy-2′,3′-didehydro-nucleoside; and optionally deprotecting the nucleoside. The haloacylation of the first step can form the 2′-acyl-3′-halonucleoside, the 3′-acyl-2′-halonucleoside, or a mixture thereof.
专利号:US-2020239500-A1 优先权日:2018-04-04 标 题 :Compositions and Methods for Synthesis of Phosphorylated Molecules
专利号:CA-2439836-A1 优先权日:2001-03-01 标 题 :Method for the synthesis of 2',3'-dideoxy-2',3'-didehydronucleosides
专利号:ZA-200306739-B 优先权日:2001-03-01 标题 :Method for the synthesis of 2',3'-dideoxy-2',3'-didehydro-nucleosides.
专利号:US-2005250946-A1 优先权日:2001-03-01 标 题 :Method for the synthesis of 2',3'-dideoxy-2',3'-didehydronucleosides
参考文献:10.1016/0006-2952(88)90383-8 摘要:Chu CK, Schinazi RF, Arnold BH, Cannon DL, Doboszewski B, Bhadti VB, Gu ZP. Comparative activity of 2',3'-saturated and unsaturated pyrimidine and purine nucleosides against human immunodeficiency virus type 1 in peripheral blood mononuclear cells. Biochem Pharmacol. 1988 Oct 01;37(19):3543–8. doi: 10.1016/0006-2952(88)90383-8.