Highly Enantioselective Synthesis of 2,3-Dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-ones via Catalytic Asymmetric Intramolecular Cascade Imidization鈥揘ucleophilic Addition鈥揕actamizat

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• 作者：Yuwei He ; Chuyu Cheng ; Bin Chen ; Kun Duan ; Yue Zhuang ; Bo Yuan ; Meisan Zhang ; Yougui Zhou ; Zihong Zhou ; Yu-Jun Su ; Rihui Cao ; Liqin Qiu
• 刊名：Organic Letters
• 出版年：2014
• 出版时间：December 19, 2014
• 年：2014
• 卷：16
• 期：24
• 页码：6366-6369
• 全文大小：313K
• ISSN：1523-7052

文摘

Highly enantioselective catalytic asymmetric intramolecular cascade imidization鈥搉ucleophilic addition鈥搇actamization of N¹-alkylethane-1,2-diamine with methyl 2-formylbenzoate catalyzed by a chiral phosphoric acid represents the first efficient method for the preparation of medicinally interesting chiral 2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-ones with high yields and excellent enantioselectivities. This strategy has been shown to be quite general toward various methyl 2-formylbenzoates.