PURPOSE: A dihydro-oxazolobenzodiazepinone compound is provided to ensure selectivity to alpha5 subunits of GABA_A receptor and to treat or prevent psychological and nervous system. CONSTITUTION: A dihydro-oxazolobenzodiazepinone compound is denoted by chemical formula I. A method for preparing the compound of chemical formula I comprises: a step of cyclizing a compound of chemical formula II of a free form or salt form under the presence of 1,1'-carbonyldiimidazole to prepare a compound of chemical formula III; a step of reacting the compound of chemical formula III with reducing agent to prepare a compound of chemical formula IV; a step of acting a compound of chemical formula V with the compound of chemical formula IV to prepare a compound of chemical formula VI; a step of adding oxidizer to the compound of chemical formula VI to prepare a compound of chemical formula VII; and a step of reacting hydrazine with the compound of chemical formula VII.본 발명은 하기 화학식 (I)의 화합물 및 약제에 관한 것이다:상기 식에서, R1은 수소 원자 또는 알킬기를 나타내고;R2는 알킬기를 나타내며;R3는 아릴 또는 헤테로아릴기를 나타낸다.