Regioselective Functionalization of 4‑Methyl‑1H‑indole for Scalable Synthesis of 2‑Cyano-5-formyl-4-methyl‑1H‑indole

Regioselective Functionalization of 4‑Methyl‑1H‑indole for Scalable Synthesis of 2‑Cyano-5-formyl-4-methyl‑1H‑indole

We report a five-step synthesis of 2-cyano-5-formyl-4-methyl-1H-indole through sequential functionalization of readily available 4-methyl-1H-indole. Cyano and aldehyde functionalities are regioselectively installed at the 2 and 5 position, respectively. The sequence is concise and high-yielding, ame...

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Veröffentlicht in:Organic process research & development 2018-01, Vol.22 (1), p.97-102
Hauptverfasser: Zhang, Jun, Hu, Yun, Wang, Haiyu, Guo, Aixin, Kong, Jianshe, Ma, Rujian, Wu, Tao, Wang, Yi, Li, Lian-Sheng, Mai, Wanping, Ren, Pingda, Deng, Xiaohu
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Sprache:eng
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Zusammenfassung:We report a five-step synthesis of 2-cyano-5-formyl-4-methyl-1H-indole through sequential functionalization of readily available 4-methyl-1H-indole. Cyano and aldehyde functionalities are regioselectively installed at the 2 and 5 position, respectively. The sequence is concise and high-yielding, amenable for kilogram scale production.
ISSN:1083-6160
1520-586X
DOI:10.1021/acs.oprd.7b00370