Synthesis of tritium labelled diphenhydramine hydrochloride (benadryl )

Abstract
The synthesis and characterization of tritium‐labelled diphenhydramine hydrochloride is described. An attempt to label diphenhydramine directly with tritium by an exchange reaction (CH3COOH, 10 c 3H2O, Pt) resulted in a mixture of tritiated benzophenone, benzhydrol, diphenhydramine, and other products. A mixture of tritiated benzophenone and benzhydrol was isolated, reduced to benzhydrol‐3H, and then condensed with dimethylaminoethanol to yield diphenhydramine‐3H with the label in the benzhydryl group.

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