236406-37-4Relevant articles and documents
Copper(I)-catalyzed borylative exo -cyclization of alkenyl halides containing unactivated double bond
Kubota, Koji,Yamamoto, Eiji,Ito, Hajime
supporting information, p. 2635 - 2640 (2013/03/29)
A borylative exo-cyclization of alkenyl halides has been reported. The reaction includes the regioselective addition of a borylcopper(I) intermediate to unactivated terminal alkenes, followed by the intramolecular substitution of the resulting alkylcopper(I) moiety for the halide leaving groups. Experimental and theoretical investigations of the reaction mechanism have also been described. This reaction provides a new method for the synthesis of alkylboronates containing strained cycloalkyl structures from simple starting materials.
Synthesis and structure-activity relationship of a novel sulfone series of TNF-α converting enzyme inhibitors
Xue, Chu-Biao,Chen, Xiao-Tao,He, Xiaohua,Roderick, John,Corbett, Ronald L.,Ghavimi, Bahman,Liu, Rui-Qin,Covington, Maryanne B.,Qian, Mingxin,Ribadeneira, Maria D.,Vaddi, Krishna,Trzaskos, James,Newton, Robert C.,Duan, James J.-W.,Decicco, Carl P.
, p. 4453 - 4459 (2007/10/03)
Replacement of the amide functionality in IM491 (N-hydroxy-(5S,6S)-1- methyl-6-{[4-(2-methyl-4-quinolinylmethoxy)anilinyl]carbonyl} -5-piperidinecarboxamide) with a sulfonyl group led to a new series of α,β-cyclic and β,β-cyclic γ-sulfonyl hydroxamic acids, which were potent TNF-α converting enzyme (TACE) inhibitors. Among them, inhibitor 4b (N-hydroxy-(4S,5S)-1-methyl-5-{[4-(2-methyl-4- quinolinylmethoxy)phenyl]sulfonylmethyl}-4-pyrrolidinecarboxamide) exhibited IC50 values of 1 nM and 180 nM in porcine TACE (pTACE) and cell assays, respectively, with excellent selectivity over MMP-1, -2, -9 and -13 and was orally bioavailable with an F value of 46% in mice.
N-acyl cyclic amine derivatives
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, (2008/06/13)
The invention relates to compounds represented by the general formula [I][wherein Ar means an aryl group or a heteroaryl group which may have a substitutive group selected from a group consisting of a halogen atom, a lower alkyl group and a lower alkoxy group; R1 means a C3-C6 cycloalkyl group which is substitutable with a fluorine atom; R2 and R4 mean hydrogen atoms, groups represented by -(A1)m-NH-B or the like; R3 and R5 mean hydrogen atoms, C1-C6 aliphatic hydrocarbon groups or the like which are substitutable with a lower alkyl group(s); n means 0 or 1; and X means an oxygen atom or a sulfur atom]. Compounds according to the invention, since they not only have potent selective antagonistic activity against muscarinic M3 receptors but also exhibit excellent oral activity, durability of action and pharmacokinetics, are very useful as safe and effective remedies against respiratory, urinary and digestive diseases with little adverse side effects.