Abstract

Figueroa-Valverde Lauro¹*, Díaz-Cedillo Francisco², García-Cervera Elodia1, Pool-Gómez Eduardo¹, López-Ramos Maria¹, Rosas-Nexticapa Marcela³, Hau-Heredia Lenin¹, Sarabia-Alcocer Beatriz⁴

DOI : http://dx.doi.org/10.13005/ojc/300305

In this study is reporteda straightforward route for synthesis of two azetidin-haloperidol derivativesusing 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.

In this study ;Design and synthesis; estradiol derivative

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