专利号:US-8198465-B2 优先权日:2005-10-17 标 题 :3-alkyl-5- (4-alkyl-5-oxo-tetrahydrofutran-2-yl) pyrrolidin-2-one derivatives as intermediates in the synthesis of renin inhibitors 发明人:SEDELMEIER GOTTFRIED; GRIMLER DOMINIQUE; ACEMOGLU MURAT 权利人:SEDELMEIER GOTTFRIED; GRIMLER DOMINIQUE; ACEMOGLU MURAT; NOVARTIS AG 摘要:The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula II, n nor a salt thereof, and a compound of formula VIn n nor a salt thereof, wherein R 3 and R 4 as well as Act are as defined in the specification, and processes of manufacturing these.n n Additionally transformation of compounds (VI) with metallo organic compounds (VII) give rise to the new compounds (VIII) which are direct precursors for the preparation of Aliskiren.
专利号:US-8785629-B2 优先权日:2009-06-18 标题 :Phosphonates synthons for the synthesis of phosphonates derivatives showing better bioavailability 发明人:AGROFOGLIO LUIGI A; ROY VINCENT; PRADERE UGO 权利人:AGROFOGLIO LUIGI A; ROY VINCENT; PRADERE UGO; CENTRE NAT RECH SCIENT; UNIV ORLEANS 摘要:Synthons for the synthesis of phosphonates prodrugs POM and POC, especially for direct Cross Metathesis.
专利号:US-6310180-B1 优先权日:1993-06-21 标 题 :Method for synthesis of proteins 发明人:TAM JAMES P 权利人:UNIV VANDERBILT 摘要:A method for peptide synthesis is disclosed that requires neither protecting groups nor activation of the C-α carboxyl groups. The method comprises ligating a first molecule to a second molecule by promoting the orthogonal coupling of the molecules to each other. In an aspect of this method, an acyl-type reaction occurs between the molecules. The method contemplates the joining of molecules of variant size to each other, as well as the coupling of multiple identical molecules. The invention also covers the ligation of unprotected peptide, proteins or nonpeptide segments to prepare therapeutic products and synthetic vaccines with linear, circularized, or branched backbone structures, as well as the site-specific modification of peptides or proteins by lipidation and pegylation.
专利号:US-7205399-B1 优先权日:2001-07-06 标 题 :Methods and reagents for oligonucleotide synthesis 发明人:VARGEESE CHANDRA; WANG WEIMIN 权利人:SIRNA THERAPEUTICS INC 摘要:The present invention features novel compositions, linkers, derivatized solid supports, and methods for the efficient solid phase synthesis of oligonucleotides, including RNA, DNA, RNA-DNA chimeras, and analogs thereof.
专利号:US-4052413-A 优先权日:1974-06-24 标 题:Stereospecific total steroidal synthesis via substituted c/d-trans indanones 发明人:HAJOS ZOLTAN GEORGE 权利人:HOFFMANN LA ROCHE 摘要:Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##STR1## WHEREIN M IS AN INTEGER HAVING A VALUE OF 1 OR 2; R 4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR 2 ) and carbonyl; R 8 when taken alone is hydrogen; R 9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R 8 when taken alone is hydrogen; R 9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R 2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxy-benzoyl, trifluoroacetyl and camphorsulfonyl n And reacting them in the case where R 8 and R 9 taken together are methylene or R 8 is hydrogen and R 9 is methylene-X with β-keto esters and other analogs of the formula ##STR2## wherein R 6 is selected from the group consisting of ##STR3## and lower alkyl; R 7 is lower alkyl; R 15 is selected from the group consisting of oxo, lower alkylenedioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R 25 and R 26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.
专利号:US-9505719-B2 优先权日:2010-06-30 标 题 :Synthesis and use of kinase inhibitors 发明人:LEI YIXIONG; BEHRENS CARL HENRY; LI HUI-YIN; SUN CONNIE L 权利人:VERASTEM INC 摘要:An improved synthesis of a class of inhibitor of Focal Adhesion Kinase (FAK) is provided, wherein use of an expensive palladium-based catalyst is reduced and reaction yields and product purities are improved. Two key reactions of coupling of aryl halides with anilines are optimized with the surprising discovery that the palladium-based catalyst can be dispensed with entirely in one of the reactions. The invention also provides the use of the FAK-inhibitory compounds in the treatment of inflammatory and immune disorders and of arthritis.
1: Ishikawa W, Sato S. Mechanical Interatomic Bond Formation in Ethanol and Methanol-Ethanol Mixture by Laser-Driven Shock Waves. Chemphyschem. 2024 May 7:e202400164. doi: 10.1002/cphc.202400164. Epub ahead of print.
合成参考文献
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