CAS: 100403-24-5; Pdrn

专利信息

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-2005250946-A1
优先权日:2001-03-01
标 题 :Method for the synthesis of 2',3'-dideoxy-2',3'-didehydronucleosides

专利号:US-2002198224-A1
优先权日:2001-03-01
标 题:Method for the synthesis of 2',3'-dideoxy-2',3'-didehydronucleosides

专利号:WO-02070533-A2
优先权日:2001-03-01
标题 :Method for the synthesis of 2',3'-dideoxy-2',3'-didehydronucleosides