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A general approach toward the synthesis of 8-acylamidopyrazolo[1,5-a]-1,3,5-triazines

โœ Scribed by Pierre Raboisson; Dominique Schultz; Claire Lugnier; Romain Mathieu; Jean-Jacques Bourguignon


Publisher
Elsevier Science
Year
2003
Tongue
French
Weight
143 KB
Volume
44
Category
Article
ISSN
0040-4039

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โœฆ Synopsis


An expedient synthesis of 8-acylamidopyrazolo[1,5-a]-1,3,5-triazines was developed by treating 8-amino-4-[N-(4aminophenyl)-N-(methyl)amino]pyrazolo[1,5-a]-1,3,5-triazine with various acyl chlorides following by the displacement of the so-formed N-(methyl)-N-[4-(acylamido)phenyl]amino leaving group with various amines. Applications to high-throughput synthesis are suggested.


๐Ÿ“œ SIMILAR VOLUMES


Efficient synthesis of 8-substituted pyr
โœ Pierre Raboisson; Dominique Schultz; Claire Lugnier; Jean-Jacques Bourguignon ๐Ÿ“‚ Article ๐Ÿ“… 2002 ๐Ÿ› Elsevier Science ๐ŸŒ French โš– 91 KB

An efficient two-step synthesis of 8-acylated pyrazolo[1,5-a]-1,3,5-triazines has been accomplished. The key strategic elements of this novel synthetic approach involve the use of the N-methyl-N-phenylamino activating group, which was easily obtained in high yield by treatment of the pyrazolotriazin