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West Chester, PA, United States

Thieu T.,Worldwide Discovery Research | Sclafani J.A.,Cephalon Inc. | Levy D.V.,Cephalon Inc. | McLean A.,Cephalon Inc. | And 4 more authors.
Organic Letters | Year: 2011

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-N bond and generates the pyrrolotriazine core through a stable bromoaldehyde intermediate followed by condensation with ammonium carbonate. © 2011 American Chemical Society. Source

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