Design and synthesis of two Azetidin-haloperidol derivatives using some strategies

In this study is reported a straight forward route for synthesis of two azetidin-haloperidol derivatives using some strategies. The first stage was achieved by the synthesis of an azetidine derivative (3) by the reaction of a haloperidol derivative (1) with chloroacetyl chloride in presence oftriethylamine. The second stage was achieved by reaction of an estradiol derivative with 1 to forma haloperidol-estradiol derivative (5) using boric acid as catalyst. Finally, the third stage involves the synthesis of a second azetidine-derivative (6) by the reaction of 5 with chloroacetyl chloride usingtriethylamine as catalyst. The structure of the compounds obtained was confirmed by elemental analysis, spectroscopy and spectrometry data. The proposed method offers some advantages such as simple procedure, low cost, and ease of workup.