N-(2-Tetrahydropyran-2-Yloxy-Ethyl)-Phthalimide置于indium(Iii) Triflate体系中,用 甲醇,水 作为反应溶剂,化学反应 7.0H,以81%的收率获得产物n-羟乙基酞酰亚胺 参考文献:A Fast And Practical Approach To Tetrahydropyranylation And Depyranylation Of Alcohols Using Indium Triflate 标题:A Fast And Practical Approach To Tetrahydropyranylation And Depyranylation Of Alcohols Using Indium Triflate 摘要:Indium Triflate-Mediated Tetrahydropyranylation Of Alcohols In Dichloromethane And Depyranylation Of These Products In Aqueous Methanol Utilizing The Same Reagent But Different Molar Ratio Is Described. In Addition,Indium Triflate-Promoted Conversion Of Tetrahydropyran Ethers To Their Corresponding Acetates Has Also Been Described. (C) 2002 Elsevier Science Ltd. All Rights Reserved. DOI:10.1016/s0040-4039(02)01864-6
专利号:US-8536375-B2 优先权日:2008-12-22 标题:Synthesis of obtaining modified polyethylene glycol intermediates 发明人:ENGELL TORGRIM 权利人:ENGELL TORGRIM; GE HEALTHCARE LTD 摘要:The present invention provides novel and more efficient synthesis's for obtaining an intermediate in the synthesis of obtaining a protecting group aminoxy PEG linker.
专利号:US-5696246-A 优先权日:1995-05-16 标题 :Process for the specific synthesis of β-glycosidically linked N-acetylpyranoside derivatives 发明人:SCHMIDT WOLFGANG; KRETZSCHMAR GERHARD 权利人:HOECHST AG 摘要:A process for the stereospecific synthesis of β-glycosidically linked N-acetylglucosamine derivatives is provided, wherein a protected α-(N-acetyl-2-amino-2-deoxy)-β-pyranosyl halide is coupled to a glycosyl acceptor using zinc chloride and a 4,4'-dialkoxytriphenylmethyl halide as catalysts.
专利号:US-2009326223-A1 优先权日:2006-07-18 标题 :Synthesis of 2-amino-substituted 4-oxo-4h-chromen-8.yl-trifluoro-methanesulfonic acid esters 发明人:GRIFFIN ROGER JOHN; HARDCASTLE IAN ROBERT; DESAGE-EL MURR MARINE; RODRIGUEZ-ARISTEGUI SONSOLES; GOLDING BERNARD THOMAS 权利人:GRIFFIN ROGER JOHN; HARDCASTLE IAN ROBERT; DESAGE-EL MURR MARINE; RODRIGUEZ-ARISTEGUI SONSOLES; GOLDING BERNARD THOMAS 摘要:A method of synthesising a compound of formula (I): wherein R N1 and R N2 are independently selected from hydrogen, an optionally substituted C 1-7 alkyl group, C 3-20 heterocyclyl group, or C 5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; from a compound of formula (III): comprising the steps of: (a) removing the allyl group from the compound of formula (III) with appropriate reaction conditions to yield a compound of formula (II): and (b) reacting the compound of formula (II) with a triflating agent to yield a compound of formula (I).
专利号:WO-2004058711-A1 优先权日:2002-12-30 标 题 :Isolation of dihydropyridine derivative and preparation salts thereof 发明人:ASLAN TUNCER; ADIYAMAN MUSTAFA; YURDAKUL AYCIL; SAHPAZ FILIZ; OZARSLAN EVREN A; GUNER DIDEM; RIDVANOGLU NURTEN 权利人:EOS ECZACIBASI OZGUN KIMYASAL; ASLAN TUNCER; ADIYAMAN MUSTAFA; YURDAKUL AYCIL; SAHPAZ FILIZ; OZARSLAN EVREN A; GUNER DIDEM; RIDVANOGLU NURTEN 摘要:The title compound is isolated in pure form by using a crystallization process and converted to its pharmaceutically acceptable salts. The crystallization process affects stability and purity of the amlodipine salts. All known impurities and one unknown impurity, which forms during the synthesis of the amlodipine salts, were isolated, characterized, and synthesized. A new method allowing the quantitative HPLC analysis of all related impurities of amlodipine salts in a single chromatogram was developed.
专利号:WO-9925689-A1 优先权日:1997-11-14 标题 :Process for the preparation of acetal derivatives of 1,4-dihydropyridines 发明人:KARUP GUNNAR LEO; PREIKSCHAT HERBERT FRITZ; PEDERSEN SOEREN BOLS 权利人:GEA FARMACEUTISK FABRIK AS; KARUP GUNNAR LEO; PREIKSCHAT HERBERT FRITZ; PEDERSEN SOEREN BOLS 摘要:A process for the preparation of 1,4-dihydropyridine acetal derivatives of formula (II) wherein R1 each, independently, represents H, Cl or CF¿3; R?2 represents H, C¿1?-C5 alkyl, C3-C6 cycloalkyl or aralkyl; R?3 and R4¿ which may be the same or different, represent C¿1?-C5 alkyl, C3-C6 cycloalkyl, aralkyl or together represent -(CH2)m-, wherein m is 2 or 3, and n is 1 or 2, wherein the 1,4-dihydropyridine ring structure is formed by a Hantzsch synthesis carried out in one or more steps using a compound containing a group of formula (a); wherein R?3 and R4¿ have the same meanings as defined above, as one of the reactants in the Hantzsch condensation, is described. The Hantzsch synthesis, or at least one step thereof, is carried out in a solvent, which is capable of forming an azeotrope with water, under azeotropic removal of water of reaction. The compounds of formula (II) are useful as intermediates for the preparation of pharmaceutically active 1,4-dihydropyridines and other intermediates of use for such purpose.
专利号:US-6956131-B2 优先权日:2000-04-13 标 题 :2-amino-3, 4 heptenoic compounds useful as nitric oxide synthase inhibitors 发明人:PITZELE BARNETT S; SIKORSKI JAMES A; WEBBER RONALD KEITH 权利人:PHARMACIA CORP 摘要:The present invention is directed to a compound of formula I: n n nor a pharmaceutically acceptable salt thereof, wherein:n R 2 is selected from the group consisting of H and methyl; and R 2 is selected from the group consisting of H and methyl.n nThe compounds possess useful nitric oxide synthetase inhibiting activity, and are expected to be useful in the treatment or prophylaxis of a disease or condition in which the synthesis or over synthesis of nitric oxide forms a contributory part.