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Hai-Na Yuan, Shuai Wang, Jing Nie, Wei Meng, Dr. Qingwei Yao and Prof. Jun-An Ma Hydrogen-Bond-Directed Enantioselective Decarboxylative Mannich Reaction of β-Ketoacids with Ketimines: Application to the Synthesis of Anti-HIV Drug DPC 083 Angewandte Chemie International Edition 52

Article first published online: 4 MAR 2013 | DOI: 10.1002/anie.201210361

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Key to success: The title reaction provides facile access to enantioenriched 3,4-dihydroquinazolin-2(1H)-ones containing a quaternary stereogenic center in high yields with excellent enantioselectivities. Subsequent transformations lead to the convenient preparation of the anti-HIV drug DPC 083 and N-fused polycyclic compounds without loss of enantiomeric excess.

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