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Noriyuki Hara, Prof. Shuichi Nakamura, Masahide Sano, Ryota Tamura, Prof. Yasuhiro Funahashi and Prof. Norio Shibata Enantioselective Synthesis of AG-041R by using N-Heteroarenesulfonyl Cinchona Alkaloid Amides as Organocatalysts Chemistry - A European Journal 18

Version of Record online: 26 JUN 2012 | DOI: 10.1002/chem.201200367

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Enantioselective catalysis: The organocatalytic enantioselective decarboxylative addition of malonic acid half thioesters to ketimines affords products with high enantioselectivities (see scheme; CPME=cyclopentyl methyl ether). The products can be converted into optically active AG-041R. Hydrogen bonding plays an important role in the enantioselectivity of the reaction.

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