Discovery and Process Synthesis of Novel 2,7-Pyrrolo[2,1-f][1,2,4]triazines

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• 作者：Tho Thieu ; Joseph A. Sclafani ; Daniel V. Levy ; Andrew McLean ; Henry J. Breslin ; Gregory R. Ott ; Roger P. Bakale ; Bruce D. Dorsey
• 刊名：Organic Letters
• 出版年：2011
• 出版时间：August 19, 2011
• 年：2011
• 卷：13
• 期：16
• 页码：4204-4207
• 全文大小：727K
• 年卷期：v.13,no.16(August 19, 2011)
• ISSN：1523-7052

文摘

The synthesis of a new kinase inhibitor template 2-anilino-7-aryl-pyrrolo[2,1-f][1,2,4]triazine is described which includes a late stage orthogonally reactive key intermediate amenable to rapid diversification as well an optimized in situ triflate displacement to install the C2-aniline. Furthermore, an efficient scalable process approach will be highlighted which begins with tert-butyl carbazate to provide the key N鈥揘 bond and generates the pyrrolotriazine core through a stable bromoaldehyde intermediate followed by condensation with ammonium carbonate.