Abstract
Carboxylic acid additives have been shown to significantly improve the yield of the Pd-catalyzed intramolecular N-arylation of 2-aminopyrroles containing a 2-chlorophenylsulfonyl group at the 3-position to give a novel tricyclic ring system. Pivalic and phenylacetic acid provided the best yield enhancement, while acetic acid showed moderate enhancement. Other acids showed limited to no enhancement or even a detrimental effect on the reaction.
Original language | English (US) |
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Pages (from-to) | 6226-6229 |
Number of pages | 4 |
Journal | Tetrahedron Letters |
Volume | 54 |
Issue number | 46 |
DOIs | |
State | Published - Nov 13 2013 |
Keywords
- 2-Aminopyrrole
- Buchwald-Hartwig reaction
- Carboxylic acid additive
- Intramolecular
- N-arylation
- Pyrrolo[3,2-b]benzo[1,4]thiazine
ASJC Scopus subject areas
- Biochemistry
- Drug Discovery
- Organic Chemistry