Metronidazole phosphate—A water??soluble prodrug for parenteral solutions of metronidazole

…, C Lewis, SM Machkovech, DJ Houser

Index: Cho; Kurtz; Lewis; Machkovech; Houser Journal of Pharmaceutical Sciences, 1982 , vol. 71, # 4 p. 410 - 414

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Citation Number: 45

Abstract

Abstract To develop a parenteral solution of relatively water-insoluble metronidazole (2- methyl-5-nitro-1H-imidazole-1-ethanol), its phosphate ester was synthesized via two routes. One route utilized 2-cyanoethyl phosphate and the other utilized pyrophosphoryl tetrachloride. The first method used dicyclohexylcarbodiimide as a coupling agent and the cy-anoethyl group was removed under mild alkaline conditions. The second method was ...