Shin-ichi Ikeda

Catalytic enantioselective intermolecular [2 + 2 + 2] cycloaddition of an alkene and two alkynesElectronic supplementary information (ESI) available: experimental and spectroscopic data. See http://www.rsc.org/suppdata/cc/b2/b208313b/

A catalytic enantioselective intermolecular [2 + 2 + 2] cycloaddition of one molecule of alkene (enone) and two molecules of alkyne was developed in the presence of a nickel complex modified by chiral monodentate oxazoline ligands, which have not previously been used as chiral ligands for transition metals in asymmetric catalysts, and an aluminium phenoxide.

Nickel-catalyzed tandem coupling of allyl electrophiles, alkynes, and alkynyltins

Abstract The nickel-catalyzed intermolecular coupling of allyl acetate or allyl carbonate with alkynes and alkynyltins was carried out in the presence of LiCl to give 3,6-dien-1-yne regio- and stereoselectively. On the other hand, the intramolecular cyclization and coupling of ω-alkynyl electrophiles with alkynyltins gave five-membered cyclic products.

Nickel-catalyzed coupling of allyl chlorides and enynes

The Ni-catalyzed coupling of allyl chlorides and enynes has been developed; the cyclization of enynes was triggered by the addition of pi-allylnickel species to the alkyne part, followed by the incorporation of the alkene part.

Chemo- and regioselective cyclotrimerization of monoynes catalyzed by a nickel(0) and zinc(II) phenoxide system

A binary metal system of nickel(0) and zinc(II) phenoxide catalyzed the chemo- and regioselective cyclotrimerization of monoynes.

A small-molecule inhibitor of SOD1-Derlin-1 interaction ameliorates pathology in an ALS mouse model

Amyotrophic lateral sclerosis (ALS) is a devastating neurodegenerative disorder. Despite its severity, there are no effective treatments because of the complexity of its pathogenesis. As one of the underlying mechanisms of Cu, Zn superoxide dismutase (SOD1) gene mutation-induced ALS, SOD1 mutants (SOD1mut) commonly interact with an endoplasmic reticulum-resident membrane protein Derlin-1, triggering motoneuron death. However, the importance of SOD1-Derlin-1 interaction in in vitro human model and in vivo mouse model remains to be elucidated. Here, we identify small-molecular-weight compounds that inhibit the SOD1-Derlin-1 interaction by screening approximately 160,000 compounds. The inhibitor prevents 122 types of SOD1mut from interacting with Derlin-1, and significantly ameliorates the ALS pathology both in motoneurons derived from patient induced pluripotent stem cells and in model mice. Our data suggest that the SOD1-Derlin-1 interaction contributes to the pathogenesis of ALS and is a promising drug target for ALS treatment.Amyotrophic lateral sclerosis (ALS) is a neurological disease that leads to loss of voluntary muscle movement. Here, the authors screen for molecules that disrupt interaction between SOD1, a protein linked to ALS, and Derlin-1, and find an inhibitor that reduces pathology in an ALS mouse model.

Effects of monodentate oxazoline ligands in Ni/Al-catalyzed regioselective cyclotrimerization of enones and alkynes

A nickel and aluminium system including monodentate oxazoline ligands catalyzed the regioselective cyclotrimerization of enones and alkynes.