Efficient synthesis of 1, 4-diaryl-5-methyl-1, 2, 3-triazole, a potential mGluR1 antagonist, and the risk assessment study of arylazides

…, S Kii, A Akao, K Sato, N Yasuda, T Mase

文献索引：Akao, Atsushi; Tsuritani, Takayuki; Kii, Satoshi; Sato, Kimihiko; Nonoyama, Nobuaki; Mase, Toshiaki; Yasuda, Nobuyoshi Synlett, 2007 , # 1 p. 31 - 36

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被引用次数: 19

摘要

A concise and practical synthesis of a 1, 4-diaryl-5-methyl-1, 2, 3-triazole is described. A mGluR1 antagonist 1 was prepared with one-pot operation by the Negishi coupling reaction between two building blocks, 5-bromophthalimidine (2) and 1-aryl-5-methyl-4-triazolylzinc (3- Zn). Bromide 2 was synthesized via N-selective cyclization of o-hydroxymethylbenzamide 8 easily prepared from phthalide 4. Zinc species 3-Zn was generated in situ by ...