专利号:US-10266565-B2 优先权日:2011-04-12 标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN 权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.
专利号:US-8637695-B2 优先权日:2011-12-30 标 题:Synthesis of organohalosilane monomers from conventionally uncleavable Direct Process Residue 发明人:LEWIS KENRICK MARTIN; NEELY JOHN DAVID 权利人:LEWIS KENRICK MARTIN; NEELY JOHN DAVID; MOMENTIVE PERFORMANCE MAT INC 摘要:Disclosed herein is a catalytic process for the synthesis of organohalosilane monomers from tetraorganodihalodisilanes and other compounds that are not cleaved during the conventional hydrochlorination of Direct Process Residue. The process is characterized by the use of a catalyst containing (1) one or more heterocyclic amines and/or one or more heterocyclic ammonium halides, and (2) one or more quaternary Group 15 onium compounds.
专利号:US-7767826-B2 优先权日:2007-10-05 标题 :Process for the synthesis of L-(+)-ergothioneine 发明人:TRAMPOTA MIROSLAV 权利人:PHARMATECH INTERNATIONAL INC 摘要:This invention relates to a novel process for the preparation of optically pure L-(+)-ergothioneine. The process for the chemical synthesis of L-ergothioneine comprises steps which consist of reacting L-histidine alkyl ester with an acid halide, chloroformate or pyrocarbonate in the presence of a base, hydrolysis of the alkyl-(S,Z)-2,4,5-triamidopent-4-enoate to obtain a (S)-alkyl 2,5-diamido-4-oxopentanoate, acid catalyzed hydrolysis of the (S)-alkyl 2,5-diamido-4-oxopentanoate followed by reaction with a metal thiocyanate to obtain the thiohistidine, protection of the sulfur of thiohistidine as the tert-butyl thioether, dialkylation of the primary amine to obtain a tertiary amine, quaternization of the tertiary amine, and removal of the protecting group to obtain the desired (S)-3-(2-mercapto-1H-imidazol-5-yl)-2-(trialkylammonio)propanoate (I). This process affords a better yield and is capable of practical application at large scale.
专利号:US-6395894-B2 优先权日:1998-04-16 标 题 :Process for the synthesis of carbapenem intermidiates, and compounds produced 发明人:PYE PHILIP J; REIDER PAUL J; ROSSEN KAI; VOLANTE RALPH P 摘要:A process of synthesizing a compound of structural formula 6is disclosed wherein R1 represents H or a suitable protecting group for an alcohol; R2 represents a benzyl, C1-6 alkyl or aryl; Y represents C1-3 alkyl, O, NH or S; X represents O, NH, or S and R5 represents a carboxy protecting group, comprising reacting a compound of formula 5:wherein R1, R2, R5, X and Y are as previously described with a phosphite or phosphonite reagent to produce a compound of formula 6. Further disclosed is an efficient method for the synthesis of a compound of formula 2:which comprises reacting a 4-acyl-2-azetidinone with a titanium, zirconium or hafnium enolate of a 1-hydroxy-2-butanone derivative.
专利号:US-4895939-A 优先权日:1986-02-24 标题:High percentage β-yield synthesis of carbapenem intermediates 发明人:MARTEL ALAIN; DARIS JEAN-PAUL; CORBEIL JACQUES 权利人:BRISTOL MYERS CO 摘要:Disclosed herein is a novel high beta -yield producing novel intermediates of the formula where R4 is useful in the synthesis of 1- beta -alkyl carbapenems.
专利号:US-2002147331-A1 优先权日:2001-02-02 标题:Methods for synthesis of oligonucleotides 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH 摘要:The present invention is directed to improved methods and compositions for synthesis of oligonucleotides and other phosphorus-linked oligomers, without the need for phosphoryl protecting groups. The methods involve the reaction of nucleoside phosphoramidites with a support-bound oligomer having one or more unprotected phosphorus-containing internucleoside linkages in the presence of a neutralizing agent.
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合成参考文献
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