One may synthesize cocaine transition state analogs based on the A-oxide group with general structure: ##STR59## wherein each of R1, R2, R3, or R4 is independently hydrogen, or a lower alkyl; or wherein one but only one of R1, R2, or R3 is a lower alkyl azide group, a lower alkyl amine, a group comprising a lower alkyl group linked to a lower alkyl carboxylic acid or derivative, with each of the r