Microwave-accelerated conjugate addition of 2-arylindoles to substituted β-nitrostyrenes in the presence of ammonium trifluoroacetate: an efficient approach for the synthesis of a novel class of CB1 cannabinoid receptor allosteric modulators
- J Heterocycl Chem. 2017 May;54(3):2079-2084. doi: 10.1002/jhet.2861.
- 1. Department of Pharmaceutical Sciences, School of Pharmacy, Bouvé College of Health Sciences, Northeastern University, Boston, MA 02115, USA.
2-Arylindoles, in general exhibit reduced reactivity towards the conjugate addition to substituted nitrostyrenes, when compared to indoles. We report here an efficient, expeditious and high-yielding conjugate addition of 2-arylindoles to substituted β-nitrostyrenes in the presence of ammonium trifluoroacetate under microwave irradiation. This method is mild with high and reproducible yields and is selective for addition of β-nitrostyrenes when compared to Other electrophiles. The results obtained from the optimized microwave method consistently provided improved yields in a shorter time compared to those of the conventional heating synthetic route.
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Cat. No.Product NameDescriptionTargetResearch Area
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target: Biochemical Assay ReagentsResearch Areas: Others