1200-15-3Relevant academic research and scientific papers
(Z)-Selective enol triflation of α-alkoxyacetoaldehydes: Application to synthesis of (Z)-allylic alcohols via cross-coupling reaction and [1,2]-wittig rearrangement
Kurosawa, Fumiya,Nakano, Takeo,Soeta, Takahiro,Endo, Kohei,Ukaji, Yutaka
, p. 5696 - 5703 (2015/06/16)
The stereoselective transformation of α-alkoxyacetoaldehydes to the corresponding (Z)-vinyl triflates was achieved by treatment with phenyl triflimide and DBU. The stereochemistry was explained by the "syn-effect," which was attributed primarily to an σ → π interaction. The β-alkoxy vinyl triflates obtained were applied to the stereoselective synthesis of structurally diverse (Z)-allylic alcohols via transition metal-catalyzed cross-coupling reaction and [1,2]-Wittig rearrangement.
Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists
Lainé, Dramane I.,McCleland, Brent,Thomas, Sonia,Neipp, Christopher,Underwood, Brian,Dufour, Jeremy,Widdowson, Katherine L.,Palovich, Michael R.,Blaney, Frank E.,Foley, James J.,Webb, Edward F.,Luttmann, Mark A.,Burman, Miriam,Belmonte, Kristen,Salmon, Michael
supporting information; experimental part, p. 2493 - 2505 (2010/03/04)
A novel 4-hydroxyl(diphenyl)methyl substituted quinuclidine series was discovered as a very promising class of muscarinic antagonists. The structure-activity relationships of the connectivity of the diphenyl moiety to the quinuclidine core and around the ring nitrogen side chain are described. Computational docking studies using an homology model of the M3 receptor readily explained the observed structure-activity relationship of the various compounds. Compound 14o was identified as a very potent, slowly reversible M3 antagonist with a very long in vivo duration of bronchoprotection.
Muscarinic acetylcholine receptor antagonists
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Page/Page column 20, (2008/06/13)
Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.
Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B
Collins, Ian,Caldwell, John,Fonseca, Tatiana,Donald, Alastair,Bavetsias, Vassilios,Hunter, Lisa-Jane K.,Garrett, Michelle D.,Rowlands, Martin G.,Aherne, G. Wynne,Davies, Thomas G.,Berdini, Valerio,Woodhead, Steven J.,Davis, Deborah,Seavers, Lisa C. A.,Wyatt, Paul G.,Workman, Paul,McDonald, Edward
, p. 1255 - 1273 (2007/10/03)
Structure-based drug design of novel isoquinoline-5-sulfonamide inhibitors of PKB as potential antitumour agents was investigated. Constrained pyrrolidine analogues that mimicked the bound conformation of linear prototypes were identified and investigated by co-crystal structure determinations with the related protein PKA. Detailed variation in the binding modes between inhibitors with similar overall conformations was observed. Potent PKB inhibitors from this series inhibited GSK3β phosphorylation in cellular assays, consistent with inhibition of PKB kinase activity in cells.
A efficient method for the reductive cleavage of aromatic acetals with ZrCl4-LiAlH4
Shaozu, Wu,Yulan, Zhang,Tianhui, Ren
, p. 445 - 447 (2007/10/02)
In our survey of the chemistry of ZrCl4-LiAlH4, we have found that acetals can be reduced to the corresponding ethers.We have explored the reductive condition and studied the reductive cleavage of different-membered cyclic acetals
REDUCTION OF ACETALS WITH CpTiCl3-LiAlH4
Shaozu, Wu,Yin, Chen,Yulan, Zhang
, p. 421 - 424 (2007/10/02)
The reduction of cyclic acetals and ketals derived from aromatic or aliphatic aldehydes and ketones with CpTiCl3-LiAlH4 system in diethyl ether at 30 deg C affords the corresponding hydroxyethyl ethers and the corresponding alkyl benzene or aliphatic hydrocarbons.
On the surface-anesthetic activity of some ether alcohols (author's transl)
Riemschneider,Rufer,Chik
, p. 2061 - 2063 (2007/10/05)
An account of the preparation and surface anesthetic potency of 12 ether alcohols of the type X-O-Y-OH is given in this paper. The anaesthetic intensity and effective duration of a chloronaphthalene derivative of this type lie within the range of action of cocain.
