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-6828466-B2 优先权日:2002-07-19 标题:Process for the synthesis of phenols from arenes 发明人:MALECZKA JR ROBERT E; SMITH III MILTON R; HOLMES DANIEL; SHI FENG 权利人:UNIV MICHIGAN STATE 摘要:A process to synthesize substituted phenols such as those of the general formula RR'R''Ar(OH) wherein R, R', and R'' are each independently hydrogen or any group which does not interfere in the process for synthesizing the substituted phenol including, but not limited to, halo, alkyl, alkoxy, carboxylic ester, amine, amide; and Ar is any variety of aryl or hetroaryl by means of oxidation of substituted arylboronic esters is described. In particular, a metal-catalyzed C-H activation/borylation reaction is described, which when followed by direct oxidation in a single or separate reaction vessel affords phenols without the need for any intermediate manipulations. More particularly, a process wherein Ir-catalyzed borylation of arenes using pinacolborane (HBPin) followed by oxidation of the intermediate arylboronic ester by OXONE is described.
专利号:US-2009275616-A1 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
专利号:US-2004030197-A1 优先权日:2002-07-19 标 题 :Process for the synthesis of phenols from arenes
专利号:US-7294732-B2 优先权日:2002-08-07 标 题:Silicon compound 发明人:OHNO KOHJI; TSUJII YOSHINOBU; FUKUDA TAKESHI 权利人:CHISSO CORP 摘要:A silicon compound represented by Formula (1). In Formula (1), R 1 is a group independently selected respectively from the group consisting of a hydrogen atom, alkyl, substituted or non-substituted aryl and substituted or non-substituted arylalkyl, and A 1 is an organic group substituted with a halogenated sulfonyl group and is preferably a group represented by Formula (2). In Formula (2), X is halogen; R 2 is alkyl; a is an integer of 0 to 2; and Z 1 is a single bond or alkylene having a carbon number of 1 to 10. n n n n n n n n n n The silicon compound provided by the present invention is a silsesquioxane derivative having an excellent living polymerizable radical polymerization initiating function. For example, it is possible to commence polymerization by allowing an acryl base monomer to coexist to form an acryl base polymer making use of one point of the structure of the silsesquioxane in the present invention as a starting point. Because a halogenated sulfonyl group has a strong electrophilicity, it is possible to synthesize various silsesquioxane derivatives by reacting the silicon compound provided by the present invention with various nucleophilic reagents, and it can actively be used as an intermediate useful for organic synthesis.
专利号:US-7691843-B2 优先权日:2002-07-11 标 题 :N-hydroxyamide derivatives possessing antibacterial activity 发明人:RAJU BORE G; O'DOWD HARDWIN; GAO HONGWU; PATEL DINESH V; TRIAS JAOQUIM 权利人:PFIZER 摘要:Novel N-hydroxyamide derivatives are disclosed. These N-hydroxyamide derivatives inhibit UPD-3-O—(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase, an enzyme present in gram negative bacteria and are therefore useful as antimicrobials and antibiotics. Methods of synthesis and of use of the compounds are also disclosed.