This study speaks about practical and efficient synthesis of 2-phenyl-4H-benzo[d][1,3]oxazine-4-one derivatives through copper catalyzed tandem reaction of 2-iodobenzoic acid with arylmethanamines under air. Compared to the literature methods toward the synthesis of 2-phenyl-4H-benzo[d][1,3]oxazine-4-one, the synthetic method reported in this paper has broad substrate scope, mild reaction condition and uses an inexpensive catalyst. In order to understand the interactions of biological molecules and for the designing of asymmetric catalytic systems particular significance must be given to chiral recognition. Among many chiral discrimination methods known, the method involves fluorescent chiral discrimination has advantages. Considering this we have designed and synthesized minor groove functionalized (S)-BINOL fluorescent probes starting from (S)-BINOL. The synthesized molecules introduce new opportunities in the field of chiral recognition.