Synlett 2015; 26(12): 1677-1682
DOI: 10.1055/s-0034-1380210
letter
© Georg Thieme Verlag Stuttgart · New York

Iodine-Mediated Domino Protocol for the Synthesis of Benz­amides from Ethylarenes via sp3 C–H Functionalization

Kamlesh S. Vadagaonkar
a   Department of Dyestuff Technology, Institute of Chemical Technology, Mumbai 400019, India
,
Hanuman P. Kalmode
a   Department of Dyestuff Technology, Institute of Chemical Technology, Mumbai 400019, India
,
Sattey Prakash
b   National Centre for Nanosciences and Nanotechnology, University of Mumbai, Mumbai 400098, India   eMail: achaskar25@gmail.com
,
Atul C. Chaskar*
a   Department of Dyestuff Technology, Institute of Chemical Technology, Mumbai 400019, India
b   National Centre for Nanosciences and Nanotechnology, University of Mumbai, Mumbai 400098, India   eMail: achaskar25@gmail.com
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Publikationsverlauf

Received: 18. März 2015

Accepted: 04. April 2015

Publikationsdatum:
21. Mai 2015 (online)


Dedicated to our mentor Prof. P. M. Bhate on the occasion of his 61st birthday

Abstract

An efficient, metal-free domino protocol for the synthesis of benzamides has been developed from ethylarenes using aqueous ammonia. The reaction proceeds through the formation of triiodomethyl ketone intermediate in the presence of iodine as the promoter and TBHP as an oxidant followed by nucleophilic substitution with aqueous ammonia, forming an amide. This operationally simple, functional-group-tolerant tandem approach provides an easy access to the broad range of biologically important benzamides.

Supporting Information

 
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  • 23 General Procedure for the Oxidative Amidation of Ethylarenes A sealed tube equipped with a magnetic stirring bar was charged with ethylarene (1, 1.0 mmol), aq NH3 (2, 25% aq solution, 10.0 mmol), I2 (1.1 mmol), and TBHP (6.0 mmol, 70% aq solution) at r.t. The resulting mixture was heated to 100 °C for 3.0 h. After completion of the reaction (monitored by TLC), sat. Na2S2O3 solution (10 mL) was added to the reaction mixture, and it was extracted with EtOAc (2 × 20 mL). The organic layer was washed with brine solution (20 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was purified by column chromatography on 100–200 mesh silica gel using EtOAc–n-hexane (1:2) as the eluent to obtain the corresponding benzamide 3.