| Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2019: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2018: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2017: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| Outline of Final Research Achievements |
We suceeded in the highly enantioselective synthesis of bioactive N-C axally chiral quinazolin-4-one derivatives through the chiral Pd-catalyzed reductive asymmetric desymmetrization. The achiral MPLC of the optically active quinazolinone products led to the self-disproportionation of enantiomers (SDE) to give the optically pure quinazolinones. Furthermore, the SDE machanism was also revealed. The alpha-alkylation with the chiral enolate prepared from optically pure quinazolinones proceeded with high diastereoselectivity without the any decrease in the optically purity to afford pharmaceutically attractive compounds bearing a chiral center and a chiral axis. In the course of this work, unique N-C axally chiral quinazolin-4-one derivatives having ortho-fluorophenyl group at N3 position were also found.
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