专利号:US-6815214-B2 优先权日:2000-12-29 标 题 :Pharmaceutical uses and synthesis of diketopiperazines 发明人:BOYCE JIM P; HOWBERT J JEFFRY; TABONE JOHN C 权利人:CELLTECH R & D INC 摘要:The synthesis of novel diketopiperazines, their use in inhibiting cellular events such as those involving NFK-α, NFK-β and in the treatment of inflammation events, a combinatorial library of diverse diketopiperazines and process for their synthesis as a library and as individual compounds. In particular novel diketopiperazines are disclosed including their synthesis and use in cellular events such as activation of the transcription factor, nuclear factor, TNF-α, TNF-β and also apoptosis.
专利号:US-4898952-A 优先权日:1987-05-29 标 题 :Regioselective synthesis of a 1,5-disubstituted pyrazole 发明人:MURRAY WILLIAM V; WACHTER MICHAEL P 权利人:ORTHO PHARMA CORP 摘要:A highly regioselective synthesis of pyrazoles from a mono-substituted hydrazine and a beta -dicarbonyl compound wherein a carboxylic acid moiety is present on the substituent attached to one of the carbonyls. For example, compounds of the formula (I) are formed in marked preference to isomers of formula (IV): (I) (IV)
专利号:US-10882884-B2 优先权日:2016-05-18 标题:Stereoselective synthesis of phosphorothioate oligoribonucleotides 发明人:HALL JONATHAN; LI MEILING 权利人:ETH ZUERICH 摘要:The present invention relates to chiral phosphoramidites represented by formula (Ia) or formula (Ib) n n n n n n n n n n n n as novel monomers for the synthesis of stereodefined phosphorothioate MOE oligonucleotides. Furthermore, the present invention relates to a method for synthesizing stereodefined phosphorothioate MOE oligonucleotides using said novel chiral phosphoramidites.
专利号:WO-2024163644-A1 优先权日:2023-02-01 标题:Belt reactor manufacturing process for oligomer synthesis 发明人:KELLER KARSTEN; HILLEBRAND ROMAN 权利人:ARROWHEAD PHARMACEUTICALS INC 摘要:A method and apparatus for synthesis of oligomers such as oligonucleotides and peptides are disclosed. The method employs a device including at least one deprotection station to carry out a step of deprotection, at least one coupling station to carry out a step of coupling, optionally, one or more oxidation and/or thiolation stations to carry out a step of oxidation or thiolation, optionally, one or more capping stations to carry out a step of capping, and, optionally, one or more washing stations to carry out a step of washing. A plurality of solid phase material for oligomer synthesis is moved to the stations via a conveyor device, wherein a fluid delivery device acts upon said solid phase material to produce an oligomer.
专利号:US-6492136-B1 优先权日:1995-12-07 标题 :Solid phase organic synthesis 发明人:FLITSCH SABINE LAHJA; TURNER NICHOLAS JOHN 权利人:GENZYME LTD 摘要:A method of synthesis of a material corresponding to the general formula:characterized in that it comprises a material corresponding to the following general formula:being cleaved as indicated enzymatically or non-enzymatically using acid catalysis in the presence of a nucleophile, wherein: R1 represents a group providing the site for exo-enzyme or acid hydrolysis; R2 represents an intermediate linked to a solid support; R3 represents a carbohydrate, (oligo-)saccharide, (glyco-)peptide, (glyco-)lipid or an organic molecule which is at least one of heterocyclic and aromatic in structure; X represents O, N(H), N(R''), C(O)O, S, C(O)N(H) or C(O)N(R''), R'' being a non-interfering group; and Support represents a solid support.
专利号:US-7329760-B2 优先权日:2002-04-05 标题 :CC-1065 analog synthesis 发明人:ZHAO ROBERT YONGXIN; CHARI RAVI V J 权利人:IMMUNOGEN INC 摘要:Improved synthesis of seco(−)CBI (5-hydroxy-3-amino-1-[S]-(chloromethyl)-1,2-dihydro-3H-benz(e)indole): n nand improved syntheses therefrom of a wide variety of CC-1065 analogs that comprise a cyclopropabenzidole (CBI) alkylating moiety, and which are collectively DC1 and its derivatives, for the synthesis of cell-targeted therapeutic agents.
参考标题:Zirconium-Hydride-Catalyzed Site-Selective Hydroboration Of Amides For The Synthesis Of Amines: Mechanism, Scope, And Application 作者:Bo Han,Jiong Zhang,Haijun Jiao,Lipeng Wu |发布日期:2021.11 摘要:Diverse Amines. Various Readily Reducible Functional Groups, Such As Esters, Alkynes, And Alkenes, Were Well Tolerated. Furthermore, The Methodology Was Extended To The Synthesis Of Bio- And Drug-Derived Amines. Detailed Mechanistic Studies Revealed A Reaction Pathway Entailing Aldehyde And Amido Complex Formation Via An Unusual C-N Bond Cleavage-Reformation Process, Followed By C-O Bond Cleavage.
合成参考文献
摘要:Grimmer, J.; Krieg, S.-C.; Manolikakes, G., Science of Synthesis Knowledge Updates, (2021) 1, 241. 摘要:Besson, M.; Pinel, C., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 2, 281. 摘要:Huang, J.; Ma, D., Science of Synthesis: Special Topics, (2022) 1, 15.