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.
有機催化不對稱(chēng)Mannich反應中的熱效應
脯氨酸直接催化不對稱(chēng)曼尼希反應(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)間內完成反應就能得到曼尼希(Mannich)產(chǎn)品達98 % ee。原位還原反應中, 由酮造成的N -芳基氨基醇(N-aryl amino alcohols)多達86 %的產(chǎn)量。
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