Abstract: New benzodiazepine compounds, and a preparation method therefor and the use thereof are provided. Short-acting benzodiazepine derivatives have the characteristics of a fast onset, short acting time, deep strength, being quickly metabolized, fast wake-up, etc. In anesthesia experiments on mice and rats, short-acting benzodiazepine derivatives have a comparable onset time to remazolam, but have a significantly shortened acting time and wake-up time. Moreover, some of the compounds have a significantly enhanced depth of action. Thus, the compounds have the characteristics of a faster onset, shorter acting time, greater strength of action, being metabolized faster, faster wake-up, etc. In long-term infusion anesthesia experiments on rats, compared with remazolam, the short-acting benzodiazepine derivatives have a significantly shortened wake-up time and recovery time, and have the characteristics of faster wake-up, a faster recovery, etc.