【药物名称】Doranidazole, PR-000350, PR-350, RP-343
化学结构式(Chemical Structure):
参考文献No.15500
标题:2-Nitroimidazole deriv., production thereof, and radiosensitizer containing the same as active ingredient
作者:Suzuki, T.; Sakaguchi, M.; Miyata, Y.; Suzuki, A.; Mori, T. (Pola Chemical Industries Inc.)
来源:EP 0513351; JP 1991223258; US 5270330; WO 9111440
合成路线图解说明:

The acetylation of meso-erythritol (I) with 3 equivalents of Ac2O in pyridine gives 1,3,4-triacetoxy-meso-erythritol (II) with some tetraacetoxy derivative that is separated by chromatography. The reaction of (II) with P2O5 and dimethoxyethane yields 1,3,4-triacetoxy-2-(methoxymethoxy)butane (III), which is treated with Ac2O and BF3/Et2O to afford 1,3,4-triacetoxy-2-(acetoxymethoxy)butane (IV). The condensation of (IV) with 2-nitroimidazole (V) by means of Ts-OH at 130 C or by means of hot N,N-bis(trimethylsilyl)acetamide (BSA) provides the precursor (VI), which is finally deacetylated by means of EtONa in ethanol or TEA in aqueous methanol to furnish the target trihydroxy derivative.

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