Nano-honeycomb electrode based QCM sensor and its application for PPI detection

An anodic aluminon oxide (AAO)-based nano honeycomb electrode was coated on a quartz crystal for use as a sensing device in a quartz crystal microbalance (QCM) to monitor the protein-protein interactions (PPIs). As examples, we detected PPIs of anti-Bcl-2 and Bcl-2, and Bcl-2 and Bax in real time. A sensor with a flat Au electrode showed a tiny frequency shift upon sample injection. However, our fabricated device could detect 10 μg/mL of Bcl-2 and Bax in sequence.2016年度関西大学研究拠点形成支援経

SYNTHESIS OF SUBSTITUTED t-BUTYL 3-ALKYLOXINDOLE-3-CARBOXYLATES FROM DI-t-BUTYL (2-NITROPHENYL)MALONATES

Using a novel tandem reduction-cyclization, we synthesized t-butyl 3-alkyloxindole-3-carboxylates from the di-t-butyl 2-alkyl-2-(2-nitrophenyl)malonate. Introduction of an α-substituent to the di-t-butyl 2-(2-nitrophenyl)-malonates and addition of acid promoted reactivity. This methodology was successfully applied to gram-scale-synthesis of the t-butyl 3-methyloxindole-3-carboxylate 1 and 3-hydroxymethyl-3-methyloxindole 2 without silica gel column chromatography.Part of this work was supported by the Kansai University Subsidy for Supporting Young Scholars, 2015 “Development of macrocyclization reaction via a photoaffinity reaction”, JSPS KAKENHI Grant Number 15K18903, Grant-in-Aid for Young Scientists (B) – Japan and MEXT – Supported Program for the Strategic Research Foundation at Private Universities (2013–2017) – Japan.2015年度関西大学若手研究者育成経

Process Development for the Synthesis of a Selective M₁ and M₄ Muscarinic Acetylcholine Receptors Agonist

A practical and chromatography-free synthetic process to selective M₁ and M₄ muscarinic acetylcholine receptors agonist was developed and demonstrated on a several hundred gram scale. The key feature of this route is <i>N,N</i>-dimethylcarbamoylation of the anilinic nitrogen on the spiro 7-azaindoline structure via intermolecular migration of the <i>N,N</i>-dimethylcarbamoyl group. The resulting compound <b>1</b> was prepared in 43% overall yield with a chemical purity >99% via six steps starting with (2-chloropyridin-3-yl)­acetonitrile

Cyclic Model for the Asymmetric Conjugate Addition of Organolithiums with Enoates

The chiral diether ligand controlled asymmetric conjugate addition of organolithiums to nona-2, 7-dienedioates preferentially proceeds via the s-cis conformation with coordination of the carbonyl oxygen atom to the lithium to give a lithium E-enolate intermediate. Subsequent intramolecular conjugate addition of the enolate also proceeds via a cyclic transition state involving the lithium and the s-cis-enoate, resulting in trans, trans-trisubstituted cyclohexanes with high enantiomeric excesses and yields

Asymmetric Synthesis of the Carbon-14-Labeled Selective Glucocorticoid Receptor Modulator using Cinchona Alkaloid Catalyzed Addition of 6-Bromoindole to Ethyl Trifluoropyruvate

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