The proline-catalyzed direct asymmetric Mannich reaction between cyclohexanone, formaldehyde, and various anilines is thermally accelerated. With only 0.5 mol % of catalyst, Mannich products with up to 98% ee have been obtained after a short period of time in reactions performed under microwave irradiation. In situ reduction of the resulting ketones affords N-aryl amino alcohols in up to 86% yield.
有机催化不对称Mannich反应中的热效应
脯氨酸直接催化不对称曼尼希反应(Mannich Reaction)中的环己酮(cyclohexanone),甲醛(formaldehyde),和各种苯胺是热加速。只需要0.5mol %的催化剂,在微波辐射下,只要很短的时间内完成反应就能得到曼尼希(Mannich)产品达98 % ee。原位还原反应中, 由酮造成的N -芳基氨基醇(N-aryl amino alcohols)多达86 %的产量。
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