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Iminosugars or azasugars,which exhibit effective inhibition against carbohydrate‐ processing enzymes,have attracted great interest for their potential clinical applications as anti‐HIV,anti‐diabetic,and anti‐cancer agents and immunomodulators in past decades.The bicyclic azasugars,including the naturally occurring and the synthetic compounds,have also been paid much attention due to their increased possibility leading to discovering new biologically active therapeutic agents.The promising activities and the potential applications in clinic trial of the azasugars inspired us to explore its innovative analogs to develop novel iminosugar‐based drugs.Recently,by using microwave‐ assisted one‐pot tandem Staudinger/aza‐Wittig/condensation reaction,we have conveniently synthesized a series of novel bi/tricyclic azasugars fused thiazolidin‐4‐one and thiazinan‐4‐one.The biological evaluation indicated that such bi/tricyclic azasugar hybrids exhibited good HIV reverse transcriptase(HIV‐RT)inhibitory activity in the preliminary HIV‐RT inhibition test.