| Budget Amount *help |
¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2017: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2016: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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| Outline of Final Research Achievements |
In this research, total synthesis of potent antibiotic cyclodepsipeptide piperidamycins was investigated. Originally developed Sc(OTf)3-catalyzed acylation of gamma-hydroxypiperazic acid derivative with piperazic chloride afforded the corresponding dipeptide, which was sequentially coupled with piperazic chlorides to provide desired tetrapiperazic acid derivative. After elongation to the hexapeptide by condensation with corresponding amino acids, removal of the protecting groups at N- and C-terminus afforded the cyclization precursor. Finally, macrolactonization using MNBA/DMAPO under high dilution conditions, followed by global deprotection of the protecting groups furnished plausible structure of piperidamycin F.
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