专利号:US-7064122-B2 优先权日:2001-12-20 标题:Pancreatic lipase inhibitor compounds, their synthesis and use 发明人:WITTER DAVID; CASTELHANO ARLINDO 权利人:OSI PHARM INC 摘要:The subject invention features compounds having the structure: n n nwherein X is O, S, CH 2 or NR 5 ; Y is O or S; R 1 is H, substituted or unsubstituted C 1 -C 15 alkyl, C 1 -C 8 alkylaryl, —C(O)OR 4 , —C(O)NR 4 R 5 , —CR 6 R 6′ OR 4 , —CR 6 R 6′ OC(O)R 4 , —CR 6 R 6′ OC(O)NHR 7 , —C(O)NR 10 R 11 , —C(O)NR 8 R 9 NR 8 R 9 , —N(R 5 )C(O)NHR 5 , or CH 2 R 4 ; R 2 is a substituted or unsubstituted, straight chain C 1 —C 30 alkyl or branched C 3 -C 30 alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R 3 is H or substituted or unsubstituted C 1 -C 6 alkyl or C 3 -C 10 cycloalkyl; R 4 is H or a substituted or unsubstituted, straight chain or branched, C 6 -C 30 alkyl, aryl, —CH 2 -aryl, aryl —C 1 -C 15 alkyl, heteroaryl-C 1 -C 15 alkyl or C 3 -C 10 cycloalkyl; R 5 is H or a substituted or unsubstituted, straight chain or branched, C 6 -C 30 alkyl, aryl C 1 -C 30 alkyl, heteroarylalkyl or cycloalkyl; R 6 and R 6′ are each independently H, substituted or unsubstituted C 1 -C 6 alkyl, dialkyl or C 3 -C 10 cycloalkyl or together form a 3-7 membered ring system; R 7 is H or substituted or unsubstituted C 1 -C 12 alkyl or C 3 -C 10 cycloalkyl; R 8 and R 9 are each independently H, substituted or unsubstituted C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 alkylaryl, or NR 8 R 9 together form a substituted piperazine or piperidine ring or a dihydro-1H-isoquinoline ring system, or a specific enantiomer thereof, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating diabetes or obesity by administering a therapeutically effective amount of the compounds of the invention.
专利号:MX-PA04005863-A 优先权日:2001-12-20 标 题 :INHIBITING COMPOUNDS OF PANCREATIC LIPASE, ITS SYNTHESIS AND USE.
参考标题:Copper-Catalyzed Multicomponent Reaction: Synthesis Of 4-Arylsulfonylimino-4,5-Dihydrofuran Derivatives 作者:Yongjia Shang,Kai Ju,Xinwei He,Jinsong Hu,Shuyan Yu,Min Zhang,Kaisheng Liao,Lifen Wang,Ping Zhang |发布日期:2010.8.20 摘要:A Series Of 4-Arylsulfonylimino-4,5-Dihydrofurans (14 Examples) Were Efficiently Synthesized In Good To Excellent Yields By Using The Copper-Catalyzed Three-Component Reaction Between Sulfonyl Azides, Phenylacetylene, And β-Ketoesters In Tetrahydrofuran (Thf) At 40 °C For 8 H In The Presence Of Triethylamine (Tea). A Plausible Mechanism For This Process Is Proposed.
合成参考文献
摘要:Chemla, F.; Ferreira, F.; Pérez-Luna, A., Science of Synthesis Knowledge Updates, (2012) 1, 461.