2016 Fiscal Year Final Research Report
Development of cascade cyclization reaction via the direct activation of propargylalcohols
| Project/Area Number |
26460009
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research (C)
|
| Allocation Type | Multi-year Fund |
|---|
| Section | 一般 |
|---|
| Research Field |
Chemical pharmacy
|
|---|
| Research Institution | Tokushima Bunri University (2015-2016)
The University of Tokushima (2014) |
|---|
Principal Investigator |
|
|---|
| Project Period (FY) |
2014-04-01 – 2017-03-31
|
| Keywords | プロパルギルアルコール / 活性化 / パラジウム / ルイス酸 / 求核剤 / 連続反応 |
|---|
| Outline of Final Research Achievements |
Propargylic compounds having an elimination group at the propargylic position are known as useful substrates in the palladium-catalyzed reactions. The reaction often employs activated propargylic alcohol derivatives such as propargylic esters, carbonates and halides, and no examples have been reported about the palladium-catalyzed reactions of underivatized propargylic alcohols with soft nucleophiles. The author developed palladium and boric acid-catalyzed cyclization of underivatized 1,3-diaryl propargylic alcohols with 1,3-cyclohexanediones. Boric acid plays a role for the efficient activation of the propargylic alcohols. Various substituted tetrahydrobenzofuranones were obtained in moderate to good yields. Reactions using 4-hydroxy-2-pyrones as the nucleophile also proceeded to afford the substituted dihydrofuropyranones.
|
| Free Research Field |
化学系薬学
|
