| Budget Amount *help |
¥51,870,000 (Direct Cost: ¥39,900,000、Indirect Cost: ¥11,970,000)
Fiscal Year 2015: ¥11,050,000 (Direct Cost: ¥8,500,000、Indirect Cost: ¥2,550,000)
Fiscal Year 2014: ¥11,050,000 (Direct Cost: ¥8,500,000、Indirect Cost: ¥2,550,000)
Fiscal Year 2013: ¥11,700,000 (Direct Cost: ¥9,000,000、Indirect Cost: ¥2,700,000)
Fiscal Year 2012: ¥11,570,000 (Direct Cost: ¥8,900,000、Indirect Cost: ¥2,670,000)
Fiscal Year 2011: ¥6,500,000 (Direct Cost: ¥5,000,000、Indirect Cost: ¥1,500,000)
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| Outline of Final Research Achievements |
We attempted the chemoselective monoacylation of the insectidal and parasiticidal compound, avermectin B2a, which was discovered in our institute, using the organocatalyst developed by Kawabata’s group. Acetylation, using DMAP as a catalyst under Kawabata’s conditions, gave the monoacetate in 63% yields, without chemoselectivity. Application of the organocatalyst instead of DMAP increased 5-chemoselectivity. The reaction condition was effective for other acylation. Interestingly, trihaloacetylation under this condition provided poor chemoselectivity. After screening various organocatalysts, we found the ent-organocatalyst effectively catalyzed the 4”-regioselective monotrihaloacetylation. These results indicate the chemoselectivity of the acylation was controlled by the combination of organocatalyst with acid anhydride.
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