| Budget Amount *help |
¥18,850,000 (Direct Cost: ¥14,500,000、Indirect Cost: ¥4,350,000)
Fiscal Year 2014: ¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2013: ¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2012: ¥9,750,000 (Direct Cost: ¥7,500,000、Indirect Cost: ¥2,250,000)
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| Outline of Final Research Achievements |
In modern drug discovery, fluorine has served as one of the most important heteroatoms because the introduction of fluorine atom(s) into bioactive molecules often improves their properties such as biological activity, metabolic stability, bioavailability and lipophilicity. Therefore, the development of new synthetic methods for the regioselective introduction of fluorine atom(s) into bioactive molecules are highly desired to enhance the drug discovery.
In this project, two methods for nucleophilic deoxyfluorination of phenol and catechol derivatives have been developed. The deoxyfluorination along with the construction of bridged biaryl framework has also been devised. Validations of these methods are given in the synthesis of new fluorinated analogs of known anticancer allocolchicinoids as well as the convergent synthesis of the antipsychotic drug risperidone.
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