专利号:US-9994508-B2 优先权日:2012-12-11 标 题:Versatile and functionalised intermediates for the synthesis of vitamin D and novel vitamin D derivatives 发明人:LOPEZ PEREZ BORJA; SIGUEIRO PONTE RITA; MAESTRO SAAVEDRA MIGUEL A; MOURINO MOSQUERA ANTONIO 权利人:ENDOTHERM GMBH 摘要:Novel intermediates for the complete synthesis of vitamin D are provided that allow a great versatility of functional groups in the final vitamin derivatives. Vitamin derivatives that are epimeric in position 3 and vitamin derivatives with a wide range of functionalities in position 18, including compounds with isotopic labelling are provided.
专利号:US-6048991-A 优先权日:1990-11-16 标题:Preparation of epoxides 发明人:HAERMELING DIETER 权利人:BASF AG 摘要:Alpha-hydroxy-epoxides of alpha-alkoxy-epoxides of the formula IV ##STR1## in which the substituents have the following meanings: R 7 , R 8 , R 9 , R 10 , R 11 are independently hydrogen, C 1 -C 20 -alkyl, C 3 -C 12 -cycloalkyl, C 4 -C 20 -cycloalkylalkyl, C 1 -C 20 -hydroxy-alkyl, a heterocyclic ring, or an aryl or C 7 -C 20 -arylalkyl group optionally substituted by C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, halogen, C 1 -C 4 -haloalkyl, C 1 -C 4 -halo-alkoxy, phenyl, phenoxy, halophenyl, halophenoxy, carboxy, C 2 -C 8 -alkoxycarbonyl, or cyano, or R 7 and R 8 or R 7 and R 9 or R 7 and R 10 or R 9 and R 10 or R 10 and R 11 together form a (CH 2 ) n group in which n is an integer from 1 to 10 and which may be optionally substituted by C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, and/or halogen, and n R 12 is hydrogen, C 1 -C 8 -alkyl, or benzyl, n provided that R 10 is not hydrogen, methyl, ethyl, propyl, or cyclohexyl when R 7 , R 8 , R 9 , or R 11 is hydrogen, that R 7 is not methyl when R 8 is methyl or phenyl and R 9 , R 10 , or R 11 is hydrogen, that R 7 is not methyl when R 8 , R 9 , R 10 , or R 11 is hydrogen and R 12 is ethyl, that R 7 is not phenyl or hexyl when R 8 , R 9 , R 10 , or R 11 is hydrogen, that R 9 is not methyl when R 7 , R 8 , R 10 , or R 11 is hydrogen, that R 10 and R 11 are not methyl when R 7 , R 8 , or R 9 is hydrogen, and that R 7 and R 10 do not together form an unsubstituted cycloalkyl when R 8 , R 9 , or R 11 is hydrogen. The epoxides of the above formula serve as intermediates for the synthesis of, inter alia, perfumes, plant protectants and polymers.
专利号:WO-0112791-A1 优先权日:1999-08-12 标 题 :Dna shuffling of dioxygenase genes for production of industrial chemicals 发明人:SELIFONOV SERGEY A; NEWMAN LISA M 权利人:MAXYGEN INC; SELIFONOV SERGEY A; NEWMAN LISA M 摘要:This invention provides improved polypeptides, including dioxygenases, dehydrogenases, ligases and transferases that are useful for the biocatalytic synthesis of compounds such as α-hydroxycarboxylic acids, and aryl- and alkyl-hydroxy and carboxylic acid compounds. The polypeptides provided herein are improved in properties such as regioselectivity, enzymatic activity, stereospecificity, and the like. Methods for obtaining recombinant polynucleotides that encode these improved polypeptides are also provided, as are organisms that express the polypeptides and are thus useful for carrying out said biocatalytic syntheses. Also provided by the invention are methods for increasing said solvent resistance of organisms that are used in the synthetic methods.
专利号:US-4301129-A 优先权日:1978-09-18 标题 :Synthesis of NaBH3 CN and related compounds 发明人:WADE ROBERT C; HUI BENJAMIN C 权利人:THIOKOL CORP 摘要:A process for the preparation of compounds of the formula RBH 3 CN wherein R is an alkali metal, a quaternary ammonium radical or a phosphonium radical wherein a compound of the formula RCN is treated with a stoichiometric amount or slightly less than a stoichiometric amount of a BH 3 donor is described. The final products are useful as hydrolysis stable reductants and as synthetic intermediates.
专利号:US-9533959-B2 优先权日:2013-10-07 标 题:Methods of regioselective synthesis of 2,4-disubstituted pyrimidines 发明人:CHARRIER JEAN-DAMIEN; O'DONNELL MICHAEL EDWARD 权利人:VERTEX PHARMA 摘要:The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.
专利号:US-10954265-B2 优先权日:2016-10-14 标 题 :Structures and mechanism for the design of highly potent glucocorticoids 发明人:XU HUAQIANG ERIC; HE YUANZHENG 权利人:VAN ANDEL RES INSTITUTE 摘要:The present invention relates to novel glucocorticoid compounds. The invention also relates to methods of using these compounds, the synthesis of these compounds, and to compositions and formulations comprising the glucocorticoid compounds, and uses thereof.
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合成参考文献
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