| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2015: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2014: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
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| Outline of Final Research Achievements |
Development of direct transformations of C-H bonds has attracted intense attention from chemical community. We particularly focus on C(sp3)-H bond oxidations and functionalizations of multiply substituted carboskeletons.
This time we have achieved the following three research results. 1) Enantioselective alkynylation of C(sp3)-H bonds adjacent to a nitrogen atom has been achieved using only chiral p-tolyl tert-butyldimethylsilylethynyl sulfoximine and benzophenone under photo-irradiation conditions. 2) Total synthesis of (+)-lactacystin, a potent inhibitor of the 20S proteasome has been achieved using the chemo- and stereoselective photoinduced intermolecular C(sp3)-H alkynylation and intramolecular C(sp3)-H acylation. 3) Total synthesis of (+)-zaragozic acid C, having inhibitory activity of mammalian squalene synthase, has been achieved using the chemo- and stereoselective photoinduced intramolecular C(sp3)-H acylation.
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