专利号:US-11053227-B2 优先权日:2017-12-20 标 题:Process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction and novel synthesis intermediates 发明人:COLLI CORRADO; BERTOLINI GIORGIO; SADA MARA; GARIS FARIS; NISIC FILIPPO; BIANCHI ALDO; BIAGGI CINZIA; DI FABIO ROMANO; RONZONI SILVANO; BERTUOLO STEFANIA; PRANDI ADOLFO; MAIORANA STEFANO 权利人:OLON SPA 摘要:Subject-matter of the present invention is a process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction of the corresponding beta-amino ketones. Subject-matter of the invention are also said novel synthesis intermediates and the use thereof in the preparation of active pharmaceutical ingredients, among which vilanterol and the salts thereof.
专利号:US-11912647-B2 优先权日:2020-05-22 标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation 发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS 权利人:UNIV GEORGIA 摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
专利号:US-4190579-A 优先权日:1977-12-29 标题:Synthesis of beta-lactams from azetidine carboxylic acid esters 发明人:LIPSHUTZ BRUCE H; WASSERMAN HARRY H; WU JAMES S 权利人:RESEARCH CORP 摘要:Azetidine carboxylic acid esters are converted into enol silyl ethers which, as enamino ketene acetals, undergo ready oxidative cleavage of the ethylenically unsaturated double bond, e.g. by dye-sensitized photo-oxygenation, to form beta-lactams. The beta-lactams and substitution products thereof are useful intermediates in the synthesis of biologically active lactams.
专利号:US-9023626-B2 优先权日:2007-09-20 标 题:Methods for the synthesis of fatty diacids by the metathesis of unsaturated diacids obtained by fermentation of natural fatty acids 发明人:DUBOIS JEAN-LUC 权利人:DUBOIS JEAN-LUC; ARKEMA FRANCE 摘要:The invention relates to a method for the synthesis of diacids of general formula ROOC—(CH 2 ) n —(CHâ•?CH) a —(CH 2 ) m COOR 1 in which n and m are identical or different and each represent an integer such that their sum is between 6 and 15, a is an index of 0 or 1, and R and R 1 are H or an alkyl radical with 1 to 4 carbon atoms, from long-chain mono-unsaturated natural fatty acids or esters having at least 10 adjacent carbon atoms per molecule of the general formula CH 3 —(CH 2 ) p —CHâ•?CH—(CH 2 ) q —COOR, p and q, being identical or different and representing indices between 2 and 11, wherein said method comprises the first step of oxidizing by fermentation said natural fatty acid or ester, using a microorganism, such as a bacterium, a yeast, or a fungus, into at least one unsaturated dicarboxylic acid or dicarboxylate, the second step of submitting the product from the first step to a metathesis crossed with a compound of formula R 2 OOC—(CH 2 ) x —CHâ•?CH—R 3 , in which R 2 is H or an alkyl radical with 1 to 4 carbon atoms, x is 0 or 1 or 2, and R 3 is H, CH 3 or COOR 2 , in order to obtain the unsaturated compound of formula ROOC—(CH 2 ) q —CHâ•?CH—(CH 2 ) x —COOR 2 , and the third optional step of converting the usaturated compound into a saturated compound by hydrogenation of the double bond.
专利号:US-6384228-B2 优先权日:1998-05-26 标题 :Method for synthesis of halopyridyl-azacyclopentane derivative and intermediate thereof 发明人:NODE MANABU; NAKAMURA DAISAKU; FUJIWARA TOSHIO; ICHIHASHI SHOGO 权利人:NIHON MEDIPHYSICS CO LTD 摘要:The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optically active acetonedicarboxylic acid ester derivative and then proceeding through a 7-azabicyclo[2.2.1]heptane derivative to obtain the objective product.
专利号:US-8940923-B2 优先权日:2007-06-13 标题:Method for the synthesis of diacids or diesters from natural fatty acids and/or esters 发明人:DUBOIS JEAN-LUC 权利人:ARKEMA FRANCE 摘要:Disclosed herein a process for the synthesis of diacids or diesters of general formula ROOC—(CH 2 )x-COOR, in which n represents an integer between 5 and 14 and R is either H or an alkyl radical of 1 to 4 carbon atoms, starting from long-chain natural monounsaturated fatty acids or esters comprising at least 10 adjacent carbon atoms per molecule, of formula CH 3 —(CH 2 )n-CHR 1 —CH 2 —CHâ•?CH—(CH 2 )p-COOR, in which R represents H or an alkyl radical comprising from 1 to 4 carbon atoms, R 1 is either H or OH, and n and p, which are identical or different, are indices between 2 and 11.
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合成参考文献
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