专利号:US-8987504-B2 优先权日:2010-06-18 标题 :Aminohydroxylation of alkenes 发明人:MEE SIMON PETER HAROLD; LUXENBURGER ANDREAS; HARRIS LAWRENCE DANIEL 权利人:MEE SIMON PETER HAROLD; LUXENBURGER ANDREAS; HARRIS LAWRENCE DANIEL; VICTORIA LINK LTD 摘要:The invention relates to a process for the aminohydroxylation of alkenes using N-oxycarbamate reagents, e.g. N-acyloxycarbamate, N-alkyloxycarbonyloxycarbamate and N-aralkoxycarbonyloxycarbamate reagents. The invention particularly relates to an intermolecular aminohydroxylation reaction that can be carried out in the absence of added base. The invention also relates to novel N-oxycarbamate reagents that are stable crystalline materials. The process of the invention is useful in the synthesis of compounds having a vicinal amino alcohol moiety, such as biologically active compounds.
专利号:US-8530689-B2 优先权日:2008-05-05 标 题 :Processes for the preparation of biphenyl compounds 发明人:PERCEC VIRGIL; ROSEN BRAD MATTHEW; WILSON DANIELA A; WILSON CHRISTOPHER J 权利人:PERCEC VIRGIL; ROSEN BRAD MATTHEW; WILSON DANIELA A; WILSON CHRISTOPHER J; UNIV PENNSYLVANIA 摘要:The invention concerns processes for the synthesis of a compound of the formula: wherein: R 1 and R 2 are each, independently, C 1 -C 12 alkyl, CO 2 R 3 , OR 4 , R 5 (OR 6 ), or C 6 -C 18 aryl; R 3 -R 6 are each, independently, C 1 -C 12 alkyl or C 6 -C 12 aryl; and n and m are each, independently, O or an integer from 1-5; said process comprising:—contacting a compound of the formula H0-R 7 -0H with BH 3 and a compound of the formula in the presence of a nickel-containing catalyst to produce a first product, where R 7 is a C 2 -C 12 hydrocarbon group and X is a halogen, OMs or OTs;—contacting the first product in situ with a compound of the formula: in the presence of a nickel-containing catalyst to produce a compound of formula I, where Z is a halogen.
专利号:WO-2014027658-A1 优先权日:2012-08-13 标题 :INTERMEDIATE FOR SYNTHESIS OF 1-(2-DEOXY-2-FLUORO-4-THIO-β-D-ARABINOFURANOSYL) CYTOSINE, INTERMEDIATE FOR SYNTHESIS OF THIONUCLEOSIDE, AND METHODS FOR PRODUCING THESE INTERMEDIATES
专利号:ES-2718307-T3 优先权日:2012-08-13 标题 :Intermediate for the synthesis of 1- (2-deoxy-2-fluoro-4-thio-beta-d-arabinofuranosyl) cytosine, intermediate for the synthesis of thionucleoside and methods to produce these intermediates
专利号:US-2010035867-A1 优先权日:2006-07-11 标 题 :Inhibitors of Cyclic Nucleotide Synthesis and Their Use for Therapy of Various Diseases 发明人:GUERRANT RICHARD L; KOTS ALEXANDER Y; MURAD FERID; CHOI BYUNG-KWON 权利人:GUERRANT RICHARD L; KOTS ALEXANDER Y; MURAD FERID; CHOI BYUNG-KWON 摘要:We disclose a method of inhibiting activity of adenylyl cyclase or guanylyl cyclase in a mammal by administering to the mammal an amount of a composition effective to inhibit the activity, wherein the composition contains at least one compound selected from the group consisting of structural formulae (Ia) and (Ib) and salts thereof, wherein R1 is —H or has the structure —C(â•?O)R8; R2 is â•?O or has the structure —OC(â•?O)R9; and R3, R4, R5, R6, and R7 are each independently selected from the group consisting of —H, —NO 2 , formula (I), -halogen, —OC(â•?O)R9, —OR9, —OH, —R8OH, —CH 3 , —OC(â•?O)CH 2 Ph, formulae (II), (III), (IV), —OPh, —CF 3 , —R8, —C(â•?O)OR9, -Ph, —R8Ph, formulae (V), (VI), (VII), (VIII), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), (XVII), (XVIII), (XIX), (XX), and (XXI), wherein each R8 is independently a linear or branched hydrocarbon group having from 1 to 4 carbon atoms and each R9 is independently a hydrocarbon group having from 1 to 2 carbon atoms. Administering the composition can be used to treat a disease in a mammal mediated by activity of adenylyl cyclase or guanylyl cyclase and effected by a toxin produced by a pathogenic organism or to reduce cyclic AMP or cyclic GMP levels in a mammal in need of reduction thereof. The composition can also be administered to mammalian cells in vitro. The above methods of inhibiting activity of adenylyl cyclase or guanylyl cyclase and treating diseases via such inhibition can be effective without prolonged treatment, have reversible effects, have low or no toxicity, are highly potent, are unlikely to have side effects, do not act on purinergic recptors, or can negate pathogenic toxins independently of whether the pathogenic organism survives.
专利号:US-2023174496-A1 优先权日:2020-05-06 标 题:Synthesis of Vinylic Protected Alcohol Intermediates
[参考文献]: C Hignite, Et Al. Drugs And Drug Metabolites As Environmental Contaminants: Chlorophenoxyisobutyrate And Salicyclic Acid In Sewage Water Effluent. Life Sci. 1977 Jan 15;20(2):337-41.
合成参考文献
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