Phenoxide leaving group SNAr strategy for the facile preparation of 7-amino-3-aryl pyrazolo[1,5-a]pyrimidines from a 3-bromo-7-phenoxypyrazolo[1,5-a]pyrimidine intermediate

[Display omitted] We have discovered a 3-bromo-7-phenoxypyrazolo[1,5-a]pyrimidine intermediate that allows for the direct sequential funtionalization of the 3-position and 7-position of a pyrazolo[1,5-a]pyrimidine scaffold. The intermediate and general method described herein offer an improvement ov...

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Bibliographic Details
Published in:Tetrahedron letters 2015-10, Vol.56 (44), p.6077-6079
Main Authors: Catalano, John G., Gaitonde, Vishwanath, Beesu, Mallesh, Leivers, Anna L., Shotwell, J. Brad
Format: Article
Language:English
Subjects:
Heterocycle
Phenoxide
Pyrazolo[1,5-a]pyrimidine
SNAr
Suzuki
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Summary:[Display omitted] We have discovered a 3-bromo-7-phenoxypyrazolo[1,5-a]pyrimidine intermediate that allows for the direct sequential funtionalization of the 3-position and 7-position of a pyrazolo[1,5-a]pyrimidine scaffold. The intermediate and general method described herein offer an improvement over prior methods, particularly in cases where multiple unique 3-aryl substituents are to be incorporated in conjunction with multiple unique 7-amino substituents.
ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2015.09.068