We investigated the effects of different drying methods (room temperature drying, heat pump drying, freeze drying, microwave vacuum drying [MVD], and combined microwave power vacuum drying) on the active ingredients of green coffee beans. We specifically focused on eleven phenolic acids, total phenolic content (TPC), total flavonoid content, antioxidant activity, polyphenol oxidase (PPO), the inhibition of linoleic acid peroxidation (LPO), and enzyme activity, and the bio‐accessibility in vitro and bioavailability of phenolics and antioxidant activities were also evaluated. MVD‐treated beans had the lowest PPO activity and the highest contents of 5‐caffeoylquinic acid (1.39 g/100 g DW), 3‐feruloylquinic acid (0.25 g/100 g DW), 4‐feruloylquinic acid (0.25 g/100 g DW), 5‐feruloylquinic acid (1.52 g/100 g DW), and TPC (5.98 g GAE/100 g DW), and the highest antioxidant activity. MVD was the least time‐consuming (0.63 hr/kg) and energy‐consuming (1.88 kwh/kg) method. Moreover, the strongest inhibition of LPO and α‐glucosidase was observed in MVD‐treated beans. Thus, MVD is suggested to be the most suitable drying technique for the preservation of phenolic compounds and bioactivities of green coffee beans.