专利号:WO-2025104624-A1 优先权日:2023-11-14 标题 :Synthesis of 1,5-anhydro-3-({5-chloro-4-[4-fluoro-2-(2-hydroxypropan-2-yl)-1-(propan-2-yl)-1h-benzimidazol-6-yl]pyrimidin-2-yl}amino)-2,3-dideoxy-d-threo-pentitol 发明人:ALEXANDER KATY LOUISE; ANSARI ZARRIN FAZAL KHADIJA; DANIELS DAVID SYDNEY BERNARD; HASSEL LUKE HARRY; KEEN STEPHEN PHILIP; SCOTT JEREMY PETER; SCOTT REUBEN JOHN; SIMMONS JOHATHAN ANDREW; STOLL EMMA LOUISE; TRINDADE ALEXANDRE FONSECA; VICINI ANNA CHIARA 权利人:PFIZER 摘要:This disclosure relates novel methods to prepare 1,5-anhydro-3-({5-chloro-4-[4- fluoro-2-(2-hydroxypropan-2-yl)-1-(propan-2-yl)-1H-benzimidazol-6-yl]pyrimidin-2- yl}amino)-2,3-dideoxy-D-threo-pentitol, and hydrates and stereoisomers thereof, as well as intermediates, including solid forms of the intermediates, useful for the preparation of such compounds and the synthesis of said intermediates.
专利号:US-5200514-A 优先权日:1990-01-19 标 题 :Synthesis of 2'-deoxypyrimidine nucleosides 发明人:CHU CHUNG K 权利人:UNIV GEORGIA RES FOUND 摘要:A method for the preparation of 2'-deoxynucleosides and 2',3'-dideoxy-2',3'-didehydronucleosides that includes the step of reacting a nucleoside having hydroxyl groups in the 2' and 3' positions with a mixture of acyl bromide or chloride and HX, wherein X is Br or Cl, at moderate temperature, to give a haloacyl nucleoside derivative that can be deprotected and reduced to form the desired compound.
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-2009118296-A1 优先权日:2005-07-20 标 题:Heteroaromatic Compounds As Inhibitors Of Stearoyl-Coenzyme A Delta-9 Desaturase 发明人:BLACK CAMERON; DESCHENES DENIS; GAGNON MARC; LACHANCE NICOLAS; LEBLANC YVES; LEGER SERGE; LI CHUN SING; OBALLA RENATA M 权利人:MERCK FROSST CANADA LTD 摘要:Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; lipid disorders; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and fatty liver disease.
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:US-2005250946-A1 优先权日:2001-03-01 标 题 :Method for the synthesis of 2',3'-dideoxy-2',3'-didehydronucleosides
摘要:Kelly, C. B.; Matsui, J. K.; Phelan, J. P.; Gutiérrez Bonet, Á.; Lang, S. B.; Molander, G. A., Science of Synthesis: Photocatalysis in Organic Synthesis, (2018) 1, 347.