MedChemComm
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– general procedure: to a solution of acid 5 (2.6 mmol) in
benzene (10 ml) thionyl chloride (2 ml of a 2.0 M CH2Cl2
solution; 4.0 mmol) was added. The reaction was stirred
under reux for 5 h and concentrated to give crude acid
chloride as a yellow solid. This yellow solid was dissolved
in dry CH2Cl2 (10 ml) and then added dropwise to the
corresponding anilines (2.6 mmol) in pyridine at 0 ꢁC.
Aer being stirred at room temperature for 4 h, the
reaction mixture was concentrated. The resulting mixture
was partitioned between ethyl acetate and water, the
organic layer was separated and washed with brine, dried
over sodium sulphate and ltered. The ltrate was
concentrated under reduced pressure. The residue was
puried by silica gel column chromatography using
EtOAc–hexane as eluent and characterized by NMR and
mass spectroscopy (details along with spectra are given in
the ESI).†
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broth dilution method against M. tuberculosis H37Rv (ATCC
27294; American Type Culture Collection, Manassas, VA,
Prodrugs
That
Covalently
Modify
the
Med. Chem. Commun.
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