Microwave (MW) assisted chemical reactions are currently gaining considerable importance in organic synthesis to contribute in green technology. Considering the importance of peptidomimetic steroid–amino acid conjugates – a novel class of hybrid compounds having diverse biological properties, we report here synthesis of these compounds of alanine and valine methyl esters with seco-steroids (A, B and D ring cleavage) in expedited way by MW promoted Ugi-four-component reaction (Ugi-4CR).