Innovative Molecular Transformations Based on Consecutive pai-Activation and Their Medicinal Applications

2016 Fiscal Year Final Research Report

• Project/Area Number: 24689001
• Research Category: Grant-in-Aid for Young Scientists (A)
• Allocation Type: Partial Multi-year Fund
• Research Field: Chemical pharmacy
• Research Institution: Kyoto University
• Principal Investigator: Hiroaki Ohno 京都大学, 薬学研究科(研究院), 教授 (30322192)
• Project Period (FY): 2012-04-01 – 2017-03-31
• Keywords: 多重結合 / 連続反応 / 全合成 / 化合物ライブラリー / アルカロイド / 薬らしさ / 天然物 / 金触媒

Outline of Final Research Achievements

As a fundamental study for discovery of lead compounds derived from natural products, development of cascade reactions for construction of drug-like heterocyclic scaffolds and total syntheses of bioactive natural products were carried out. The following remarkable results have been obtained: (1) several novel cascade reactions such as spiroindole synthesis, [4 + 2]-type indole synthesis, fused indolenine synthesis, and pyrrolocarbazole synthesis, have been developed; (2) asymmetric total synthesis of quinocarcin, asymmetric synthesis of a possible precursor of laurendecumallene B, asymmetric formal synthesis of strictamine have been achieved; and (3) potent CK2 inhibitors and isoform selective SphKs inhibitors have been identified.

Free Research Field

有機合成化学