3-Methyl-1-Phenyl-3-Phospholene置于1,8-二氮杂双环[5.4.0]十一碳-7-烯体系中,用 四氢呋喃,甲苯 用作溶剂,化学反应 9.0H,反应生成肉桂酸甲酯 参考文献:Keglevich,Gyoergy; Forintos,Henrietta; Ujvari,Aniko,Journal Of Chemical Research,2005,# 4,P. 215-217 标题:Keglevich,Gyoergy; Forintos,Henrietta; Ujvari,Aniko,Journal Of Chemical Research,2005,# 4,P. 215-217
专利信息
专利号:US-7816544-B2 优先权日:2004-03-23 标 题:Synthesis of rocaglamide natural products via photochemical generation of oxidopyrylium species 发明人:JONES II GUILFORD; GERARD BAUDOUIN; PORCO JR JOHN A 权利人:UNIV BOSTON 摘要:The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
专利号:US-8404088-B2 优先权日:2006-05-22 标 题:Asymmetric synthesis of rocaglamides via enantioselective photocycloaddition mediated by chiral bronsted acids 发明人:PORCO JR JOHN A; GERARD BAUDOUIN 权利人:PORCO JR JOHN A; GERARD BAUDOUIN; UNIV BOSTON 摘要:The present invention provides a new strategies for the synthesis of compounds of the rocaglamide family and related natural products. The synthetic approach generally involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by an enantioselective 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile in the presence of a TADDOL derivative. This approach can be used for the formation of adducts containing an aglain core structure. Methods of the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
专利号:US-7598291-B2 优先权日:2004-09-02 标题 :Methods and compositions for enhancing collagen and proteoglycan synthesis in the skin 发明人:NIMNI MARCEL; HAN BO 权利人:NIMNI MARCEL; HAN BO 摘要:A composition for application to the skin can stimulate the in vivo synthesis of collagen and proteoglycans and improve the appearance of the skin, increasing its elasticity and fullness. In general, a composition according to the present invention comprises: (1) an antioxidant compound in a quantity sufficient to enhance collagen synthesis in the skin; (2) an organic penetrant in which the antioxidant compound is soluble in a sufficient quantity that a concentration of the antioxidant compound sufficient to enhance collagen synthesis can be applied topically and penetrate the skin; (3) a mixture of essential amino acids; (4) a supplemental source of sulfur; and (5) a topical pharmaceutically acceptable carrier. The antioxidant compound can be lipoic acid, a lipoic acid analogue or derivative, a bioflavonoid, a constituent of ginkgo, or an isoflavone. The organic penetrant is preferably benzyl alcohol. Other ingredients, such as esters of tocopherol and ascorbic acid, can be included.
专利号:US-2010160244-A1 优先权日:2004-09-02 标 题 :Methods and compositions for enhancing collagen, proteoglycan, and glutathione synthesis in the skin 发明人:NIMNI MARCEL; HAN BO 权利人:NIMNI MARCEL; HAN BO 摘要:A composition for application to the skin can stimulate the in vivo synthesis of collagen and proteoglycans and improve the appearance of the skin, increasing its elasticity and fullness. In general, a composition according to the present invention comprises: (1) an antioxidant compound in a quantity sufficient to enhance collagen synthesis in the skin; (2) an organic penetrant in which the antioxidant compound is soluble in a sufficient quantity that a concentration of the antioxidant compound sufficient to enhance collagen synthesis can be applied topically and penetrate the skin; (3) a mixture of essential amino acids or hydrolyzed whey protein; (4) a supplemental source of sulfur; and (5) a topical pharmaceutically acceptable carrier. The antioxidant compound can be lipoic acid or a lipoic acid analogue or derivative. The organic penetrant is preferably benzyl alcohol. Other ingredients, such as esters of tocopherol and ascorbic acid, can be included.
专利号:US-2012178961-A1 优先权日:2009-07-02 标题:Bio-derived olefin synthesis 发明人:SANDERS JOHAN PIETER MARINUS; VAN HAVEREN JACOBUS; SCOTT ELINOR; VAN ES DANIEL STEPHAN; LE NOTRE JEROME; SPEKREIJSE JURJEN 权利人:SANDERS JOHAN PIETER MARINUS; VAN HAVEREN JACOBUS; SCOTT ELINOR; VAN ES DANIEL STEPHAN; LE NOTRE JEROME; SPEKREIJSE JURJEN; UNIV WAGENINGEN; STICHTING DIENST LANDBOUWKUNDI 摘要:Disclosed is a method for the combined synthesis of at least two vinylic monomers, at least one of which being an acrylic compound, comprising subjecting a monoconjugated alkene-1-carboxylic compound to reaction with a C 2 -C 4 alkene under conditions of olefin cross-metathesis. The invention is particularly useful for extracting value from protein side streams. Upon protein hydrolysis, suitable amino acids (preferably phenylalanine or tyrosine) are subjected to reductive amination so as to form the corresponding alkene-1-carboxylic acid. Preferably after esterification and separation, this is used in cross-metathesis for the concomitant production of styrene resp. hydroxy styrene, and acrylates. The invention is applicable more widely, to the synthesis of olefins on the basis of carbohydrates, naturally occurring phenolic components, natural protein resources, or amino acids obtained from fermentations.
专利号:WO-2016088138-A1 优先权日:2014-12-01 标题 :Diphenyloxiranes, process for preparation thereof, and its use in an enantioselective synthesis of (+)-sertraline 发明人:SURYAVANSHI GURUNATH MALLAPPA; SUDALAI ARUMUGAM; KAMBLE ROHIT BALKRISHNA 权利人:COUNCIL SCIENT IND RES 摘要:The present invention discloses substituted diphenyloxiranes and process for synthesis thereof. The present invention also provides a process for production of enantiomerically pure anti-3,3' -diphenylmethyloxirane and anti-3,3'- diphenylpropan- 1,2-diol from racemic anti-3,3' -diphenylmethyloxirane using hydrolytic kinetic resolution. Further it provides a process for preparation of enantioselective (+)- Sertraline from anti-3,3' -diphenylpropan-1,2-diol.
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合成参考文献
摘要:Takeda, T.; Tsubouchi, A., Science of Synthesis, (2009) 46, 63. 摘要:Petasis, N. A., Science of Synthesis, (2010) 47, 171. 摘要:Petasis, N. A., Science of Synthesis, (2010) 47, 185. 摘要:Fringuelli, F.; Piermatti, O.; Pizzo, F.; Vaccaro, L., Science of Synthesis, (2010) 47, 591. 摘要:Takeda, T.; Tsubouchi, A., Science of Synthesis, (2009) 46, 69.