An asymmetric addition of arylboronic acids to pyrazolinone ketimines is reported using palladium/chiral N,N′-disulfonyl bisimidazoline (Bim) catalytic system, producing 25 examples of enantioenriched 4-amino-5-pyrazolones bearing one quaternary carbon stereocenter with 60–91% yields and 81–98% ee. The reaction demonstrates remarkable compatibility regarding pyrazolinone ketimines and arylboronic acids, rendering an enantioselective access to chiral aza-heterocycles bearing α-tertiary amines.

中文翻译：

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Pd催化芳基硼酸不对称加成到吡唑啉酮酮亚胺

据报道，使用钯/手性N , N '-二磺酰基双咪唑啉 (Bim) 催化系统将芳基硼酸不对称加成到吡唑啉酮酮亚胺中，产生了 25 个对映体富集的 4-氨基-5-吡唑啉酮实例，带有一个季碳立体中心，占 60-91%产量和 81-98% ee。该反应证明了吡唑啉酮酮亚胺和芳基硼酸的显着相容性，使对映选择性获得带有α-叔胺的手性氮杂杂环。