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2016 Fiscal Year Final Research Report

Efficient synthesis of compounds having various substitution patterns using ligand-controlled site-selective reactions

Research Project

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Project/Area Number 15K18833
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeMulti-year Fund
Research Field Chemical pharmacy
Research InstitutionUniversity of Shizuoka

Principal Investigator

Yamaguchi Miyuki  静岡県立大学, 薬学部, 助教 (70548932)

Project Period (FY) 2015-04-01 – 2017-03-31
Keywords触媒 / 位置選択性 / 配位子
Outline of Final Research Achievements

In this study, ligand-controlled site-selective reactions, which are powerful tools for effective synthesis of multisubstituted compounds, were developed. Dihydroxyterphenylphosphine (DHTP), which was previously developed by our group, was employed as a ligand, and various reactions were screened using a catalyst derived palladium and DHTP. As a result, arylation of nonsubstituted indole with chloroarenes proceeded C3-selectively using Pd-DHTP catalyst. On the other hand, other commercially available ligands used in cross coupling of chloroarenes afforded N-arylated product selectively. In addition, several DHTP analogs were designed as a new ligands and synthesized. These ligand showed different reactivity and site-selectivity from those of DHTP.

Free Research Field

有機化学

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Published: 2018-03-22  

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