通过氮杂环卡宾催化的曼尼希/内酰胺化多米诺反应实现苯并噻唑并嘧啶酮的区域和立体选择性合成。
Regio- and stereoselective synthesis of benzothiazolo-pyrimidinones via an NHC-catalyzed Mannich/lactamization domino reaction.
作者信息
Ni Qijian, Song Xiaoxiao, Xiong Jiawen, Raabe Gerhard, Enders Dieter
机构信息
Institute of Organic Chemistry, RWTH Aachen University, Landoltweg 1, 52074 Aachen, Germany.
出版信息
Chem Commun (Camb). 2015 Jan 25;51(7):1263-6. doi: 10.1039/c4cc08594a.
An NHC-catalyzed regio- and stereoselective Mannich/lactamization domino reaction of N-(benzothiazolyl)imines with α-chloroaldehydes has been developed. This new protocol provides a facile approach for the asymmetric synthesis of benzothiazolo-pyrimidinones and a pyrrolo[1,2-a]indolone in moderate to good yields (34-78%) and excellent stereoselectivities (87-99% ee, up to >20 : 1 d.r.).
已开发出一种由国家卫生健康委员会（NHC）催化的N-（苯并噻唑基）亚胺与α-氯代醛的区域和立体选择性曼尼希/内酰胺化多米诺反应。这一新方法为苯并噻唑并嘧啶酮和吡咯并[1,2-a]吲哚酮的不对称合成提供了一种简便途径，产率适中至良好（34-78%），立体选择性优异（对映体过量率为87-99%，非对映选择性高达>20:1）。
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