| Budget Amount *help |
¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2014: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2013: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Outline of Final Research Achievements |
Synthetic studies of piperidamycin F and JBIR-39 were investigated. Acylation of gamma-hydroxypiperazic acid with acid chloride was efficiently performed in the presence of Sc(OTf)3 to afford the corresponding dipeptide in good yield. Synthesis of oligopiperazic acid structure, followed by removal of the protecting groups furnished the natural product JBIR-39. The structure of JBIR-39 was unequivocally determined, and its absolute configurations were established to be 2S, 6S, 8S, 11R, 16S, 21R, 26S, 27S. Based on the above results, synthesis of pipericamycin F was also investigated and preparation of its macrocyclic structure was carried out by macrolatonization using 2-methyl-6-nitrobenzoic anhydride (MNBA).
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