Inorganic base-catalyzed formation of antivirally active N-substituted benzamides from α-amido sulfones and N-nucleophile

Table 1 Effect of different solvents and bases for the synthesis of 5a^a

Entry	Solvent	Base	Equiv	Yield (%) ^c
1	Toluene	KOH	1.2	30
2	THF	KOH	1.2	58
3	CH₃CN	KOH	1.2	63
4	CH₂Cl₂	KOH	1.2	70
5 ^b	CH₂Cl₂	KOH	1.0	64
6	CH₂Cl₂	Na₂CO₃	1.2	52
7	CH₂Cl₂	NaOH	1.2	65

^a Unless otherwise noted, reactions were carried out with 0.5 mmol (1.0 equiv) of 4a, 0.6 mmol (1.2 equiv) of 3a in 5.0 mL solvent and 1 mL H₂O using 0.6 mmol (1.2 equiv) of basic catalyst at room temperature for 24 h. ^b Reaction was carried out with 0.5 mmol (1.0 equiv) of KOH at room temperature for 24 h. ^c Isolated yield after chromatographic purification.

ISSN: 2661-801X