Budget Amount *help |
¥19,890,000 (Direct Cost: ¥15,300,000、Indirect Cost: ¥4,590,000)
Fiscal Year 2010: ¥3,250,000 (Direct Cost: ¥2,500,000、Indirect Cost: ¥750,000)
Fiscal Year 2009: ¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2008: ¥11,700,000 (Direct Cost: ¥9,000,000、Indirect Cost: ¥2,700,000)
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Research Abstract |
α-Imino esters behave as acceptors of nucleophiles at their nitrogen atoms in an "umpoled" manner, when appropriate nucleophiles are used. The tandem N-alkylation-C-allylation and N-alkylation-C-cyanation reaction of several α-imino esters with organoaluminums are carried out in good to excellent yields, where two nucleophiles attack across the C=N double bond. Moreover, three components coupling reaction of α-imino ester derived from ethyl glyoxylate, aluminum reagent, and various electrophiles proceeded to give the addition products in good yields. The alkoxycarbonyl iminium salt is easily prepared using the oxidation of amino ketene silyl acetal, and subsequent nucleophilic addition to this iminium species proceeds efficiently to afford the α-amino esters in good yields.
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