专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-8012901-B1 优先权日:2006-08-30 标 题 :Method of synthesizing enantiopure mexiletine analogues and novel β-thiophenoxy and pyridyl ethers 发明人:ORTIZ-MARCIALES MARGARITA; HUANG KUN; STEPANENKO VIATCHESLAV; DE JESUS MELVIN; CORREA WILDELIZ 权利人:ORTIZ-MARCIALES MARGARITA; HUANG KUN; STEPANENKO VIATCHESLAV; DE JESUS MELVIN; CORREA WILDELIZ 摘要:A practical and efficient procedure for the enantioselective synthesis of mexiletine analogues using 10% of a novel spiroborate ester as chirality transfer agent is presented. A variety of mexiletine analogues were prepared with excellent enantioselectivities (91-97% ee) in good yield from readily available starting materials. The developed methodology was also successfully applied for the synthesis of novel β-amino ethers containing thiophenyl and pyridyl fragments.
专利号:US-7884125-B2 优先权日:2008-04-30 标 题:Straightforward entry to 7-azabicyclo[2.2.1]heptane-1-carbonitriles and subsequent synthesis of epibatidine analogues 发明人:STEVENS CHRISTIAN; HEUGEBAERT THOMAS 权利人:UNIV GENT 摘要:The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction.
专利号:US-2015158809-A9 优先权日:2013-02-26 标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds 发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P 权利人:XENOPORT INC 摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.
专利号:US-5565573-A 优先权日:1993-11-12 标 题:Synthesis of epibatidine and analogs thereof 发明人:LAROCK RICHARD C 权利人:UNIV IOWA STATE RES FOUND INC 摘要:The present invention provides a method to prepare epibatidine or an analog thereof comprising reacting a bicyclic olefin or diene, such as an azanorbornene, with an aryl or heteroaryl halide or triflate in the presence of a catalytic amount of Pd(O) and a formate salt.
专利号:US-8252930-B2 优先权日:2006-07-06 标 题:Azaindole derivatives with a combination of partial nicotinic acetyl-choline receptor agonism and dopamine reuptake inhibition 发明人:STOIT AXEL; COOLEN HEIN K A C; VAN DER NEUT MARTINA A W; KRUSE CORNELIS G 权利人:STOIT AXEL; COOLEN HEIN K A C; VAN DER NEUT MARTINA A W; KRUSE CORNELIS G; SOLVAY PHARM BV 摘要:Azaindole derivatives of formula (I): n nwherein the symbols have the meanings given in the specification, are described. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, for example, their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.
参考标题:The Amino Thiourea-Catalyzed Asymmetric Nucleophilic Reactions 作者:Yoshiji Takemoto,Hideto Miyabe 摘要:Bifunctional Amino Thiourea-Catalyzed Asymmetric Additions Of Several Nucleophiles Into Electron-Deficient Unsaturated Compounds Such As Nitroolefins, , -Unsaturated Imides, Imines, And Azodicarboxylates Are Described. We Discovered That Bifunctional Thioureas Bearing A Tertiary Amino Group Significantly Accelerated Several Nucleophilic Addition Reactions Of Active Methylene Compounds To Electron-Deficient Double Bonds. In These Reactions, A Strong Hydrogen-Bonding Ability Of The Thiourea Moiety As Well As An Appropriate Brønsted Basicity Of The Tertiary Amine Is Crucial For High Enantioselectivity. This Dual Activation Of Both Nucleophiles And Electrophiles By The Bifunctional Thiourea Expanded The Applicability Of The Thiourea-Catalyzed Enantioselective Reaction. In Addition, These Organocatalyzed Asymmetric Reactions Were Successfully Applied To The Concise Asymmetric Synthesis Of Natural Products And Medicinal Candidates Such As Epibatidine, Baclofen, And Cp-99,994.
合成参考文献
参考文献:10.1016/j.jmgm.2011.06.008 摘要:Taly A, Colas C, Malliavin T, Blondel A, Nilges M, Corringer P, Joseph D. Discrimination of agonists versus antagonists of nicotinic ligands based on docking onto AChBP structures. Journal of Molecular Graphics and Modelling. 2011 Sep;30():100–9. doi: 10.1016/j.jmgm.2011.06.008.