Thermal Effects in the Organocatalytic Asymmetric Mannich Reaction

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.

有機(jī)催化不對(duì)稱Mannich反應(yīng)中的熱效應(yīng)

脯氨酸直接催化不對(duì)稱曼尼希反應(yīng)（Mannich Reaction）中的環(huán)己酮（cyclohexanone），甲醛（formaldehyde），和各種苯胺是熱加速。只需要0.5mol ％的催化劑，在微波輻射下,只要很短的時(shí)間內(nèi)完成反應(yīng)就能得到曼尼希（Mannich）產(chǎn)品達(dá)98 ％ ee。原位還原反應(yīng)中, 由酮造成的N -芳基氨基醇（N-aryl amino alcohols）多達(dá)86 ％的產(chǎn)量。
 

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