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CAS号109-97-7 吡咯 | CAS号6147-66-6 二烯丙基胺盐酸盐 | CAS号77484-76-5 cis-3,4-dibromo... | CAS号7153-66-4 顺-4-氯-2-丁烯胺 盐酸盐 | CAS号111185-41-2 1H-Pyrrole, 2,5... | CAS号31970-04-4 3-吡咯烷-1-甲酸苄酯 | CAS号73286-70-1 N-B°C-3-吡咯啉 | CAS号109-96-6 3-吡咯啉吡咯置于盐酸,锌体系中,用 水 作为反应溶剂,化学反应 3.5H,以77%的收率获得产物2,5-二氢吡咯盐酸盐
参考文献:新型双环氮杂胺作为代谢型谷氨酸受体的负变构调节剂5的设计,合成和结构-活性关系
标题:新型双环氮杂胺作为代谢型谷氨酸受体的负变构调节剂5的设计,合成和结构-活性关系
摘要:通过合理设计确定了一系列新型的二芳基双环唑胺,它们是代谢型谷氨酸受体5(mglur5)的有效选择性负调节剂.合成了具有中等效力(ic 50 = 1.2μm)的初始命中化合物5A.对分子左侧结构活性关系(sar)的评估显示,偏爱直接连接至中央杂环的2-取代吡啶基.该分子的中央氮杂-氨基部分的变异显示出对[4,5-C]-恶唑并氮杂pine骨架的偏爱,而右侧变体则对邻位和间位偏爱-取代的苯环直接连接到饱和杂环的叔胺上.这些迭代导致了29B的合成,这是一种有效的(ic 50 = 16 Nm)和选择性的负调节剂,在腹膜内给药时,在大鼠中表现出非常好的脑穿透力,高的受体占有率以及大于1小时的作用持续时间.在大鼠和恒河猴中进行的正式pk研究表明,半衰期短是由于较高的首过清除率所致.
DOI:10.1021/jm100736H
专利信息
专利号:US-7687635-B2
优先权日:2002-01-22
标 题:Metal complexes useful in metathesis and other reactions
发明人:VERPOORT FRANCIS WALTER CORNELIUS; DE CLERCQ BOB
权利人:TELENE S A S
摘要:This invention provides metal complexes being useful as catalyst components in metathesis reactions and in reactions involving the transfer of an atom or group to an ethylenically or acetylenically unsaturated compound or another reactive substrate and, with respect to a sub-class thereof, for the polymerisation of α-olefins and optionally conjugated dienes, with high activity at moderate tempera-tures. It also provides methods for obtaining polymers with very narrow molecular weight distribution by means of a living reaction. It also provides methods for making said metal complexes and novel intermediates involved in such methods. It further provides derivatives of said metal complexes which are suitable for covalent bonding to a carrier, the product of such covalent bonding being useful as a supported catalyst for heterogeneous catalytic reactions. It also provides a direct one-step synthesis of pyrrole, furan and thiophene compounds from diallyl compounds.
专利号:US-2007185343-A1
优先权日:2004-02-26
标 题 :Metal complexes for use in olefin metathesis and atom group transfer reactions
发明人:VERPOORT FRANCIS WALTER C; DROZDZAK RENATA A; LEDOUX NELE; ALLAERT BART F
权利人:UNIV GENT
摘要:Improved catalysts useful in a number of organic synthesis reactions such as olefin metathesis and atom or group transfer reactions are made by bringing into contact a multi-coordinated metal complex comprising a multidentate Schiff base ligand, and one or more other ligands, with an acid under conditions such that said acid is able to at least partly cleave a bond between the metal and the multidentate Schiff base ligand of said metal complex, optionally through intermediate protonation of said Schiff base ligand.
专利号:EP-1577282-B1
优先权日:2004-02-26
标 题:Metal complexes for use in olefin metathesis and atom or group transfer reactions
发明人:VERPOORT FRANCIS WALTER CORNELIUS; DROZDZAK RENATA ANNA; LEDOUX NELE; ALLAERT BART FILIP
权利人:TELENE SAS
摘要:Improved catalysts useful in a number of organic synthesis reactions such as olefin metathesis and atom or group transfer reactions are made by bringing into contact a multi-coordinated metal complex comprising a multidentate Schiff base ligand, and one or more other ligands, with an acid under conditions such that said acid is able to at least partly cleave a bond between the metal and the multidentate Schiff base ligand of said metal complex, optionally through intermediate protonation of said Schiff base ligand.