2011 Fiscal Year Final Research Report
Development of versatile 1, 2-Diamine synthetic methodology and its application for preparation of drug candidates.
Project/Area Number |
21590013
|
Research Category |
Grant-in-Aid for Scientific Research (C)
|
Allocation Type | Single-year Grants |
Section | 一般 |
Research Field |
Chemical pharmacy
|
Research Institution | Kumamoto University |
Principal Investigator |
ISHIZUKA Tadao 熊本大学, 大学院・生命科学研究部, 教授 (60176203)
|
Project Period (FY) |
2009 – 2011
|
Keywords | 有機化学 / ジアミン |
Research Abstract |
Synthetic strategy for chiral 1, 2-diamines, which are included in many kind of bioactive compounds, has been successfully developed. The versatile chiral synthon, 4, 5-dimethoxy-2-imidazolidinone, has been prepared by FeCl_3 catalized epoxidation-ring cleavage with H_2O or t-BuOH process followed by optical resolution. Diastereomeric methodology with camphor-derived chiral carboxylic acid has also successed with 93% de.
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