| Budget Amount *help |
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2011: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2010: ¥2,600,000 (Direct Cost: ¥2,000,000、Indirect Cost: ¥600,000)
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| Research Abstract |
Whereasa range of related reactions of heteroatom-containing substrates (X = NR^2 or O) have been reported, the corresponding carbon analogue (X=CH2) had been overlooked until quite recently. We have disclosed that the benzylic C-H bond without an adjacent heteroatom could also participate in this type of transformation by selection of barbiturate as a electrophilic moiety, and the corresponding 3-aryltetraline derivatives were obtained in excellent chemical yield. Furthermore, we found thatt h I s reaction could be applied to an aliphatic substrates (without electronic assistance of adjacent heteroatom and arene).The asymmetric version of this type of reaction was also achieved by use of chiral phosphoric acid catalyst derived from BINOL. The synthetically useful tetrahydroquinoline derivatives were obtained with excellent enanioselectivities (over 90% ees).
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