36 research outputs found
ChemInform Abstract: Enantioselective Nitration of Chiral (E)-Crotylsilanes: A Concise Asymmetric Synthesis of (E)-Olefin Dipeptide Isosteres.
ChemInform Abstract: A Concise Enantioselective Synthesis of trans-Olefin Dipeptide Isosteres.
Dual antagonists of α5β1/αvβ1 integrin for airway hyperresponsiveness.
Inhibition of integrin α5β1 emerges as a novel therapeutic option to block transmission of contractile forces during asthma attack. We designed and synthesized novel inhibitors of integrin α5β1 by backbone replacement of known αvβ1 integrin inhibitors. These integrin α5β1 inhibitors also retain the nanomolar potency against αvβ1 integrin, which shows promise for developing dual integrin α5β1/αvβ1 inhibitor. Introduction of hydrophobic adamantane group significantly boosted the potency as well as selectivity over integrin αvβ3. We also demonstrated one of the inhibitors (11) reduced airway hyperresponsiveness in ex vivo mouse tracheal ring assay. Results from this study will help guide further development of integrin α5β1 inhibitors as potential novel asthma therapeutics
Optically Active γ-Hydroxy Sulfone Julia Reagents for the Synthesis of Peptidyl Olefin Peptidomimetics
Platinum catalysed hydrosilylation of propargylic alcohols
A facile and user-friendly protocol has been developed for the selective synthesis of E-vinyl silanes derived from propargylic alcohols using a PtCl2/XPhos catalyst system. The reaction is generally high yielding and provides a single regioisomer at the β-position with E-alkene geometry. The reaction is extremely tolerant of functionality and has a wide scope of reactivity both in terms of alkynes and silanes used. The catalyst loading has been investigated and it is found that good reactivity is observed at extremely low catalyst loadings. This methodology has also been extended to a one-pot hydrosilylation Denmark–Hiyama coupling
Enantiospecific Synthesis and Allylation of All-Carbon-Substituted α-Chiral Allylic Stannanes
Enantiospezifische Synthese und Allylierung ausschließlich Kohlenstoff-substituierter, α-chiraler Allylstannane
Domino Alkene-Isomerization–Claisen Rearrangement Strategy to Substituted Allylsilanes
A one-pot isomerization–Claisen protocol has been developed for the synthesis of highly substituted allylsilanes. Monosilylated divinyl ethers can be isomerized using a cationic iridium(I) catalyst followed by a thermal Claisen rearrangement to provide the allylsilanes in excellent yields and diastereoselectivities