二氢-3-(异十二碳烯基)呋喃-2,5-二酮置于aspergillus Niger Lipase As Amano体系中,用 二甲基亚砜 作为反应溶剂,化学反应 4.0H,反应生成 3-苯基苯甲酸 参考文献:Characterization Of Chemo-And Regioselectivity In Enzyme-Catalyzed Consecutive Hydrolytic Deprotection Of Methyl Acetyl Derivatives Of 1-β-O-Acyl Glucuronides 标题:Characterization Of Chemo-And Regioselectivity In Enzyme-Catalyzed Consecutive Hydrolytic Deprotection Of Methyl Acetyl Derivatives Of 1-β-O-Acyl Glucuronides 摘要:Methyl Acetyl Derivatives Of 1-Beta-O-(O-,M-,Or P-Phenyl)Benzoyl Glucuronides 2A-C Are Fully Deprotected By A One-Pot Consecutive Enzyme-Catalyzed Hydrolytic Reaction To Afford 4A-C,Without Isolation Of The O-Deacetylated Derivatives 3A-C. A Lipase As Amano From Aspergillus Niger (Las) And A Carboxylesterase From Streptomyces Rochei (Csr) Showed High Chemoselectivity Toward The O-Deacetylation Of The O-And M-Isomers,Respectively. Chemoselective O-Deacetylation Of The P-Isomer Was Promoted Only In The Presence Of Both Enzymes. A Lipase Type B From Candida Antarctica (Calb) Was Effective For The Subsequent Enzymatic Hydrolysis Of The Methyl Esters Of 3A-C. Las Exhibited Also Regioselective 3-O-Deacetylation Activity To Afford The Corresponding 2,4-Di-O-Acetyl Intermediates 5A-C,For Which Csr Showed Higher O-Deacetylation Activity Than That For 2A-C. In Kinetic Studies Using P-Nitrophenyl Ester Substrates,Las Exhibited A Broader Acyl Preference,The octanoyl Ester Being Most Effectively Hydrolysed,Whereas Csr Exhibited The Highest Hydrolytic Activity Toward The Acetyl Ester. Las And Csr Play Complementary As Well As Synergistic Roles In The O-Deacetylation Of 2 Bearing R Groups Of Different Steric Bulkiness. (C) 2011 Elsevier B.V. All Rights Reserved. DOI:10.1016/j.Molcatb.2010.12.014
专利号:US-8188113-B2 优先权日:2006-09-14 标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC 摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
专利号:US-5728366-A 优先权日:1994-04-29 标 题:Two powder synthesis of hydrotalcite and hydrotalcite-like compounds with monovalent organic anions 发明人:MARTIN EDWARD S; STINSON JOHN M; CEDRO III VITO; HORN JR WILLIAM E 权利人:ALUMINUM CO OF AMERICA 摘要:There is provided a method for making monovalent organic anion-intercalated hydrotalcite-like materials by first reacting a magnesium-containing powder and a transition alumina powder in a carboxylic acid-free, aqueous suspension to form a meixnerite intermediate. This intermediate is then contacted with a monovalent organic anion to form a hydrotalcite-like material. The latter is then separated from the suspension. Representative materials include a stearate-, acetate- or benzoate-intercalated hydrotalcite-like material.
专利号:US-8114993-B2 优先权日:2007-02-06 标题:Use of aryl chlorides in palladium-catalyzed C-H bond functionalization 发明人:DAUGULIS OLAFS; CHIONG HENDRICH 权利人:DAUGULIS OLAFS; CHIONG HENDRICH; UNIV HOUSTON SYSTEM 摘要:A one-step method for efficiently converting carbon-hydrogen bonds into carbon-carbon bonds using chloroarenes and palladium catalysts is disclosed. This method allows faster introduction of complex molecular entities, a process that would otherwise require many more steps. This invention is particularly relevant for the organic synthesis of complex molecules such as, but not limited to, pharmacophores.
专利号:WO-2013049605-A1 优先权日:2011-09-28 标题 :Processes for the preparation of an intermediate in the synthesis of eltrombopag 发明人:AVDAGIC AMIR; BARAN PHIL S 权利人:ASSIA CHEM IND LTD; TEVA PHARMACEUTICAL USA INC 摘要:3'-Amino-2'-hydroxybiphenyl-3-carboxylic acid (BPCA) and related compounds have been prepared using compounds such as: wherein R 1 is -H, -Cl or -F; R 2 is -Br or -I; and R 3 is -H or -N0 2 . BPCA is useful, for example, in the preparation of Eltrombopag.
专利号:US-5728365-A 优先权日:1994-04-29 标 题:Two powder synthesis of hydrotalcite and hydrotalcite-like compounds with divalent inorganic anions 发明人:MARTIN EDWARD S; STINSON JOHN M; CEDRO III VITO; HORN JR WILLIAM E 权利人:ALUMINUM CO OF AMERICA 摘要:There is provided a method for making a divalent inorganic anion-intercalated hydrotalcite-like material by first reacting a magnesium-containing powder and a transition alumina powder in a carboxylic acid-free aqueous suspension to form a meixnerite intermediate. This intermediate is then contacted with a divalent inorganic anion, in its acid, acid salt or ammonium salt form, to make a hydrotalcite-like material. The latter is then separated from the suspension. Representative materials include a sulfate- and metavanadate-intercalated hydrotalcite-like material.
专利号:US-5776424-A 优先权日:1994-04-29 标题 :Two powder synthesis of hydrotalcite and hydrotalcite-like compounds with monovalen inorganic anions 发明人:MARTIN EDWARD S; STINSON JOHN M; CEDRO III VITO; HORN JR WILLIAM E 权利人:ALUMINUM CO OF AMERICA 摘要:There is provided a method for making a monovalent inorganic anion-intercalated hydrotalcite-like material by first reacting a magnesium-containing powder and a transition alumina powder in a carboxylic acid-free, aqueous suspension to form a meixnerite intermediate. This intermediate is then contacted with a monovalent inorganic anion, in its acid or soluble salt form, to make a hydrotalcite-like material. The latter is then separated from the suspension. Representative materials include a bromide-, chloride-, nitrate- or vanadate-intercalated, hydrotalcite-like material.