Abstract: The present invention belongs to the technical field of pharmaceutical chemistry, and particularly relates to a 1-aminobenzo[4,5]imidazo[1,2-a]pyrazine-3-formamide compound, and the preparation therefor and use thereof. The structure of the compound of the present invention is as shown in formula (I). The compound has a novel structure and is an adenosine receptor inhibitor, has good inhibitory activity on adenosine A2A receptors, has good subtype selectivity, and can be used as a targeted adenosine A2A receptor inhibitor for immunotherapy. By means of inhibiting the activity of the adenosine A2A receptor, the function of removing tumor cells by the immune system is released, so that the effect of treating tumors is achieved.