13994-57-5Relevant academic research and scientific papers
Identification of a novel allosteric GLP-1R antagonist HTL26119 using structure- based drug design
O'Brien, Alistair,Andrews, Stephen P.,Baig, Asma H.,Bortolato, Andrea,Brown, Alastair J.H.,Brown, Giles A.,Brown, Sue H.,Christopher, John A.,Congreve, Miles,Cooke, Robert M.,De Graaf, Chris,Errey, James C.,Fieldhouse, Charlotte,Jazayeri, Ali,Marshall, Fiona H.,Mason, Jonathan S.,Mobarec, Juan Carlos,Okrasa, Krzysztof,Steele, Kelly N.,Southall, Stacey M.,Teobald, Iryna,Watson, Steve P.,Weir, Malcolm
, (2019)
A series of novel allosteric antagonists of the GLP-1 receptor (GLP-1R), exemplified by HTL26119, are described. SBDD approaches were employed to identify HTL26119, exploiting structural understanding of the allosteric binding site of the closely related Glucagon receptor (GCGR) (Jazayeri et al., 2016) and the homology relationships between GCGR and GLP-1R. The region around residue C3476.36b of the GLP-1R receptor represents a key difference from GCGR and was targeted for selectivity for GLP-1R.
α- and β-bis(1,1,1-trifluoro-5,5-dimethyl-5-methoxyacetylacetonato)copper(II): Transforming the dense polymorph into a versatile new microporous framework
Soldatov,Ripmeester,Shergina,Sokolov,Zanina,Gromilov,Dyadin
, p. 4179 - 4188 (1999)
Bis(1,1,1-trifluoro-5,5-dimethyl-5-methoxy-acetylacetonato)copper(II) was prepared in two polymorphic modifications. The orthorhombic α-form is stable and densely packed, with four trans and four cis square bischelate building blocks per unit cell. These are connected through additional coordination bonds to form a dense polymer network. For the trigonal β-form, the square bischelate complex units are present exclusively as the trans isomers. The distinctive assembly of these units results in a lattice with an open pore volume of about 17% that is accessible to a wide range of guests. The compound has a remarkably strong affinity for the porous β-form as evident from the efficient α-to-β conversion on contact not only with liquid guests but also with organic vapors at pressures well below the saturation pressure. Although the open β-form is metastable, it has a remarkable kinetic stability, most likely because of the trans-to-cis isomerization that must accompany the β-to-α transformation. Many sorbents play a dual role as stabilizing guest and as catalyst promoting the α-to-β or β-to-α conversion. Because of its versatile sorption properties and relative robustness, the β-form of the complex can be classified as a novel organic zeolite mimic.
Synthetic method of 3-methoxy-3-methylbutyne
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Paragraph 0021-0027, (2019/11/28)
The invention discloses a synthetic method of 3-methoxy-3-methylbutyne. The method comprises the following steps: using acetone and acetylene as starting raw materials, firstly synthesizing 3-methylbutyn-3-ol, and performing a reaction on the 3-methylbutyn-3-ol and dimethyl sulfate to obtain the 3-methoxy-3-methylbutyne. According to the synthetic method of the 3-methoxy-3-methylbutyne provided bythe invention, the raw materials used in the synthetic method have a low price and low costs and are easy to obtain, the synthetic method has a short synthetic route, a high yield, and high chemicalpurity of the obtained product, no special production equipment is needed in all reactions, and the obtained intermediate and the final product do not need to be treated by column chromatography and crystallization purification.
Palladium-Catalyzed [2+1] Cycloadditions Affording Vinylidenecyclopropanes as Precursors of 7-Membered Carbocycles
Lepronier, Aymeric,Achard, Thierry,Giordano, Laurent,Tenaglia, Alphonse,Buono, Gerard,Clavier, Herve
supporting information, p. 631 - 642 (2016/02/27)
Palladium(II) acetate in association with secondary phosphine oxides provides an efficient catalytic system for [2+1] cycloadditions starting from oxanorbornene derivatives and tertiary propargyl esters giving rise to vinylidenecyclopropanes. This reaction is specific to bidentate phosphinito-phosphinous acid ligands generated from secondary phosphine oxides. The [2+1] cycloaddition was found broad in scope with a high tolerance to various functional groups. Moreover, vinylidenecyclopropanes were straightforwardly converted into oxabicyclo[3.2.1]oct-2-ene derivatives through a palladium-catalyzed ring-expansion. Finally, the oxa bridge cleavage of oxatricyclic compounds yields functionalized 7-membered carbocycles.
Chemoenzymatic access to versatile epoxyquinol synthons
Pinkerton, David M.,Banwell, Martin G.,Willis, Anthony C.
supporting information; experimental part, p. 4290 - 4293 (2009/12/26)
The enantiomerically pure and readily available metabolites 10-12 have been converted over four simple steps Into the epoxyquinol derivatives 22-24, respectively. Compounds 23 and 24 or their Immediate precursors have been exploited In efficient total syn
The Stereochemistry of Organometallic Compounds. XXX. Hydrocyanation of Alkynol Ethers: a New Stereospecific Route to α-Alkylidene γ-Lactones
Jackson, W. Roy,Perlmutter, Patrick,Smallridge, Andrew J.
, p. 251 - 261 (2007/10/02)
The regioselectivity of hydrocyanation of a range of protected α- and β-hydroxyalkynes has been investigated and shown to by highly susceptible to steric effects.Some of the products from hydrocyanation of protected β-hydroxyalkynes have been converted into α-alkylidene γ-lactones.
Substituted 1-phenoxy-1-triazolyl-2-butanone compounds and their use as fungicides
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, (2008/06/13)
Substituted 1-phenoxy-1-triazolyl-2-butanone compounds which correspond to the formula STR1 wherein each X independently represents chloro, bromo, iodo, nitro, methyl, methoxy, or methylthio; n represents an integer of 0 to 3; and R represents methyl or e
