专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:WO-2021038581-A1 优先权日:2019-08-30 标题 :A one step synthesis of 2-substituted benzo[b]thiophenes 发明人:SEKAR GOVINDASAMY; POONGUZHALI ELAMVAZHUTHI 权利人:INDIAN INST TECH MADRAS 摘要:The invention pertains to a one step synthesis of 2-substituted benzo[ b ]thiophene of general formula wherein the synthesis of 2-substituted benzo[ b ]thiophenes is by reacting the starting materials substituted or unsubstituted 2-halogenobenzaldehyde and substituted or unsubstituted acetyl/phenacyl bromide with a catalyst, a sulphur source and phase transfer catalyst in an aqueous medium with atmospheric air and at temperature in the range of 25°C-30°C.
专利号:US-9597327-B2 优先权日:2005-05-25 标 题:Synthesis of (R)-N-methylnaltrexone 发明人:DOSHAN HAROLD D; PEREZ JULIO 权利人:PROGENICS PHARM INC 摘要:This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use.
专利号:US-2005014954-A1 优先权日:2001-11-22 标 题:Pyrrole synthesis 发明人:OHRLEIN REINHOLD; BAISCH GABRIELE 摘要:The invention relates to a novel process for the preparation of N-substituted pyrroles, especially of formula (V), wherein the radicals are as defined in the description, by intermolecular aza-Wittig reaction starting from organic azides and 1,4-dioxo compounds. The invention relates also to novel iminophosphorane intermediates for this synthesis. The resulting pyrroles are useful, for example, in the organic synthesis of pharmaceuticals or other active substances and chemicals.
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-8026383-B2 优先权日:2001-07-06 标题:Process for the preparation of intermediates useful in the synthesis of statin derivatives 发明人:OEHRLEIN REINHOLD; BAISCH GABRIELE; END NICOLE; BURKHARDT STEPHAN; STUDER MARTIN 权利人:BASF SE 摘要:The invention relates to novel synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I n nwherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or —N(CH 3 )OCH 3 , R a is a hydroxy-protecting group and R b is a carboxy-protecting group, and, as well as to the compound of formula I, to further new intermediates and methods for their preparation by Friedel-Crafts acylation.
参考标题:Palladium-Catalyzed Carbonylation Of 2-Bromoanilines With 2-Formylbenzoic Acid And 2-Halobenzaldehydes: Efficient Synthesis Of Functionalized Isoindolinones 作者:Kishore Natte,Jianbin Chen,Haoquan Li,Helfried Neumann,Matthias Beller,Xiao-Feng Wu |发布日期:2014.10.27 摘要:Versatile Method For The Synthesis Of Functionalized Isoindolinones Is Reported. Various 2‐bromoanilines Undergo Palladium‐catalyzed Carbonylation With 2‐formylbenzoic Acid Under A Convenient And Mild Procedure To Give Good To Excellent Yields Of The Corresponding Isoindolinones. Additionally, 2‐halobenzaldehydes Can Be Applied As Substrates In Palladium‐catalyzed Double‐carbonylation To Provide Identical
合成参考文献
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