Direct N‐Alkylation and Kemp Elimination Reactions of 1‐Sulfonyl‐1H‐Indazoles |
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Authors: | Prof Meng Tang Bingjie Chu Xiaowei Chang |
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Institution: | School of Pharmacy, Lanzhou University, Lanzhou, P.?R. China |
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Abstract: | The reactions of 1‐sulfonyl‐1H‐indazoles under basic conditions are discussed, and the direct N‐alkylation and Kemp elimination reactions of these compounds are reported. A series of 2‐(p‐tosylamino)benzonitriles and N‐alkyl indazoles were prepared in good yields. Moreover, the 2‐(p‐tosylamino)benzonitriles could be transformed into a diverse range of important derivatives in a one‐pot reaction. This method was successfully applied to the total syntheses of quindolinone and cryptolepinone; quindolinone was prepared in a one‐pot reaction from 1‐sulfonyl‐1H‐indazole. |
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Keywords: | alkylation elimination indazoles synthetic methods total synthesis |
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