CAS: 29256-90-4; Cyclohexanediamine

专利信息

专利号:WO-9837078-A1
优先权日:1997-02-20
标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:WO-9740025-A1
优先权日:1996-04-19
标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA
摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-6207858-B1
优先权日:1999-03-03
标 题 :Regioselective synthesis of DTPA derivatives
发明人：CHINN PAUL; GYORKOS ALBERT; LABARRE MICHAEL J; RUHL STEVE; RYSKAMP THOMAS
权利人:IDEC PHARMA CORP
摘要:The present invention provides a process for high yield regioselective synthesis of DTPA derivatives that eliminates the need for ion exchange chromotographic separation of intermediates. Moreover, as this process yields a single regioisomer of the chelate, it provides for the regiospecific synthesis of desired chelates useful as radiolabeling agents.

专利号:US-7759492-B2
优先权日:2004-08-20
标 题:Enantioselective synthesis of 13-oxotricyclo[8.2.1.0.3,8] trideca-3(8),4,6-triene-5-carboxylates
发明人：KEEN STEPHEN PHILIP; OLIVER STEVEN FRASER; STEWART GAVIN WILLIAM
权利人:MERCK SHARP & DOHME
摘要:An enantioselective route to compounds of formula I is disclosed: n n n n n n n n n n The compounds of formula I are key intermediates in the synthesis of compounds useful in treatment of Alzheimer's disease.

专利号:WO-03050105-A2
优先权日:2001-12-10
标题 :Catalytic asymmetric synthesis of optically active compounds
发明人：HALLAND NIS; JOERGENSEN KARL ANKER; HANSEN TORE
权利人:CHEMINOVA AS; HALLAND NIS; JOERGENSEN KARL ANKER; HANSEN TORE
摘要:A one step catalytic asymmetric process for the synthesis of an optically active compound of formula la or lb wherein R is selected from C1-7 alkyl, C1-7 haloalkyl, C1-7 alkoxy, C1-7 haloalkoxy, halogen and hydroxy; R3 is H or C1-4 alkyl; R4 is selected from H, C1-7 alkyl, C1-7 haloalkyl, C1-7 alkoxy, COOH, CO-C1-7 alkoxy and an optionally substituted aryl or heterocycle; AR represents C1-7 alkyl, optionally substituted aryl, an optionally substituted heterocycle or AR and R4 may be bridged together forming part of a ring system; X is O or S; m is a number between 0-4; comprising the step of reacting a compound of the formula 2 with a compound of formula 3 in the presence of a catalytic amount of a chiral nitrogen containing organic compound.

专利号:US-9006425-B2
优先权日:2009-03-18
标题:Aluminum complexes and their use in the synthesis of cyclic carbonates
发明人：NORTH MICHAEL
权利人:NORTH MICHAEL; UNIV YORK
摘要:Dimeric aluminum catalysts of formula I: and their use in catalyzing the synthesis of cyclic carbonates from epoxides and carbon dioxide.