专利号:US-2009099061-A1 优先权日:2006-01-27 标 题:Synthesis of carotenoid analogs or derivatives with improved antioxidant characteristics 发明人:FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F 权利人:FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F 摘要:A method is described for synthesizing and administering carotenoid compounds with improved antioxidant characteristics. In some embodiments, extension or improvement of conjugation may be employed in structural modification of carotenoids. In other embodiments, reduction of ring/chain steric hindrance may improve the lambda max, and hence, the overall antioxidant capability, of particular compounds. In other embodiments, introduction and/or increase in synthetic handles for conjugation may improve the stoichiometric ratios of conjugating moieties to the polyene backbone. The methods may be used to improve natural and/or synthetic compounds for medicinal application in the treatment of disease.
专利号:US-5137660-A 优先权日:1991-03-15 标题:Regioselective synthesis of 1,3-disubstituted glycerides 发明人:MAZUR ADAM W; HILER II GEORGE D 权利人:PROCTER & GAMBLE 摘要:A process for the selective esterification of glycerol and 1-glyceryl derivatives to 1,3-disubstituted glycerides is disclosed. This process uses a water immiscible solvent, either a hydrocarbon or halogenated hydrocarbon, a 1,3-lipase and fatty acid anhydrides. This reaction mixture selectively esterifies the primary alcohol groups of glycerol or glycerol derivatives. The preferred derivatives of glycerol are alkyl ethers, alkyl phosphates, phospholipids, alkyl and diaklyl phosphates, and sugar glycosides.
专利号:US-3998888-A 优先权日:1975-11-12 标 题:Synthesis of sulfonyl peroxides 发明人:MANNER JAMES A 权利人:PPG INDUSTRIES INC 摘要:Sulfonyl peroxides represented by the formula ##STR1## wherein R and R' independently are alkyl, cycloalkyl, or substituted alkyl or cycloalkyl groups having 1 to 20 carbons, are prepared in a liquid reaction phase by the sulfoxidation of an alkane or cycloalkane reactant with SO 2 and O 2 and acylation of the sulfoxidation product with a carboxylic acid anhydride. In the practice of this invention, an inert, immiscible organic solvent for the sulfonyl peroxide is introduced into the liquid reaction phase to dissolve the peroxide as it is formed and to produce a lower crude product phase containing the sulfonyl peroxide already dissolved in the inert solvent.
专利号:US-6544952-B1 优先权日:1994-03-15 标 题:Synthesis of glycoconjugates of the globo-H epitope and uses thereof 发明人:DANISHEFSKY SAMUEL J; LIVINGSTON PHILIP O; RAGUPATHI GOVINDASWAMI; KIM IN JONG; SCHER HOWARD; SLOVIN SUSAN 权利人:SLOAN KETTERING INST CANCER 摘要:The present invention provides a method of synthesizing a compound having the structure:as well as other related glycoconjugates useful as vaccines for inducing antibodies to epithelial cancer cells in an adjuvant therapy therefore, and in a method for preventing recurrence of epithelial cancer. The present invention also provides a vaccine comprising an amount of the compound described above effective to prevent the recurrence of cancer in a subject.
专利号:US-8940749-B2 优先权日:2011-05-31 标题:Preparation of 3-[2-[4-((6-fluoro-1, 2-benzisoxazol-3-yl)-l-piperidinyl)-6, 7, 8, 9-tetrahydor-9-hydroxy-2-methyl-4H-pyrido[ 1, 2-A]-pyrimidin-4-one(paliperidone) and paliperidone palmitate 发明人:DAVULURI RAMAMOHAN RAO; PONNAIAH RAVI; NEELA PRAVEEN KUMAR; BATTHINI GURUSWAMY; VENKATA NARASIMHARAO TELAGAREDDY; RAVANABABU KOSIREDDY; SUDHEER KALLEPALLY 权利人:DAVULURI RAMAMOHAN RAO; PONNAIAH RAVI; NEELA PRAVEEN KUMAR; BATTHINI GURUSWAMY; VENKATA NARASIMHARAO TELAGAREDDY; RAVANABABU KOSIREDDY; SUDHEER KALLEPALLY 摘要:An improved process for the synthesis of 3-[2-[4-((6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]-pyrimidin-4-one (Paliperidone) and Paliperidone Palmitate through a novel intermediate (2-Chloroethyl)-6,7,8,9-tetrahydro-2-methyl-9-hydroxy-4H-pyrido [1,2-a]pyrimidine-4-one Palmitate ester.
专利号:US-8884001-B2 优先权日:2008-05-08 标题:Preparation of intermediates useful in the synthesis of 2′-cyano-2′-deoxy-N4-palmi-toyl-1-β-D-arabinofuranosylcytosine 发明人:WOOD GAVIN; WESTWOOD ROBERT; Murofushi tsuyoshi; NUMAGAMI EIJI; TAKITA TAKASHI 权利人:WOOD GAVIN; WESTWOOD ROBERT; Murofushi tsuyoshi; NUMAGAMI EIJI; TAKITA TAKASHI; CYCLACEL LTD 摘要:The present invention relates to a process for preparing a compound of formula 682-4, said process comprising the steps of: (i) converting a compound of formula 682-1 into a compound of formula 682-2; (ii) converting said compound of formula 682-2′ into a compound of formula 682-3; and (iii) converting said compound of formula 682-3 into a compound of formula 682-4. Further aspects of the invention relate to the use of the above process in the preparation of 2′-cyano-2′-deoxy-N 4 -palmitoyl-1-β-D-arabmofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.
1: Lee S, Shin H, Bae J, Lee T, Kim M, Jeon HB, Lee KH, Yoo HY, Park C. Enhanced Enzymatic Synthesis of Puerarin Palmitate with Different Acyl Donors for Lipid Solubility Improvement. Int J Mol Sci. 2024 Jan 5;25(2):709. doi: 10.3390/ijms25020709. 2: Trabelsi I, Essid K, Frikha MH. Esterification of Mixed Carboxylic-fatty Anhydrides Using Amberlyst-15 as Heterogeneous Catalyst. J Oleo Sci. 2017;66(7):667-676. doi: 10.5650/jos.ess17008. 28(23):2605-16. doi: 10.1002/rcm.7057. 20(10):1531-7. doi: 10.1002/rcm.2501. 3(2):152-60. doi: 10.1021/mp050010c. 265(1-2):104-6. doi: 10.1016/0014-5793(90)80894-o. 21(11):2765-73. doi: 10.1021/bi00540a029.
合成参考文献
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