专利号:US-10308588-B2 优先权日:2014-12-15 标 题 :Synthesis of amides and amines from aldehydes or ketones by heterogeneous metal catalysis 发明人:CÓRDOVA ARMANDO; PALO-NIETO CARLOS; AFEWERKI SAMSON 权利人:ORGANOFUEL SWEDEN AB 摘要:A mild and efficient synthesis of primary amines and amides from aldehydes or ketones using a heterogeneous metal catalyst and amine donor is disclosed. The initial heterogeneous metal-catalyzed reaction between the carbonyl and the amine donor components is followed by the addition of a suitable acylating agent component in one-pot, thus providing a catalytic one-pot three-component synthesis of amides. Integration of enzyme catalysis allows for eco-friendly one-pot co-catalytic synthesis of amides from aldehyde and ketone substrates, respectively. The process can be applied to asymmetric synthesis or to the co-catalytic one-pot three-component synthesis of capsaicin and its analogues from vanillin or vanillyl alcohol. A co-catalytic reductive amination/dynamic kinetic resolution (dkr) relay sequence for the asymmetric synthesis of optically active amides from ketones is disclosed. Implementation of a catalytic reductive amination/kinetic resolution (kr) relay sequence produces the corresponding optically active amide product and optical active primary amine product with the opposite stereochemistry from the starting ketones.
专利号:US-9085538-B2 优先权日:2010-07-26 标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof 发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO 权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS 摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
专利号:US-4871873-A 优先权日:1988-03-18 标 题:Process for synthesis of arylglyoxal arylimines 发明人:DESMOND RICHARD; MILLS SANDER G; VOLANTE RALPH P; SHINKAI ICHIRO 权利人:MERCK & CO INC 摘要:A process for producing arylglyoxal arylimine intermediates, by the DMSO/HBr oxidation of arylmethylketones. The imine compounds are intermediates in the synthesis of carbapenem antibiotics, i.e. imipenem.
专利号:US-6096883-A 优先权日:1996-05-31 标 题 :3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones 发明人:WU GEORGE G; CHEN XING; WONG YEE-SHING; SCHUMACHER DORIS P; STEINMAN MARTIN 权利人:SCHERING CORP 摘要:The invention relates to intermediates of the formulae ##STR1## said intermediates being useful in a process for producing a compound of the formula ##STR2## wherein Bn is benzyl and R 1 , 2 and R 3 are as defined in the specification,
专利号:US-2023212216-A1 优先权日:2019-12-20 标 题:Synthesis of lactone derivatives and their use in the modification of proteins 发明人:MORRIS ALEXANDER REDFERN; SUTOV GRIGORIJ; BRUNE KARL DIETRICH 权利人:GENIE BIOTECH UK LTD 摘要:Site-specific modifications of proteins are desirable in biotechnological applications such as biopharmaceuticals, immunotherapy, vaccines, and are useful in chemical biology. Gluconoylation is a non-enzymatic, covalent, post-translational modification commonly observed on N-terminal His-Tags bearing proteins. We synthesized glucono-1,5-lactone derivatives, including azido variants for selective acylation. High yield acylation is achieved by simply mixing derivatives with target protein amidst diverse conditions of temperatures, aqueous buffers, excipients, or complex cell lysate.
专利号:US-2024239805-A1 优先权日:2022-12-16 标 题:Aza-yang cyclization-buchner aromatic ring expansion: collective synthesis of cycloheptatriene-containing azetidine lactones 发明人:SINGH MANVENDRA PAL; BOSKOVIC ZARKO; GASKINS BRYCE 权利人:UNIV KANSAS 摘要:The present disclosure is directed to a compound of Formula I, Formula II, Formula III, Formula IV, or Formula Vor a pharmaceutically acceptable salt and/or solvate thereof.