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PREPARATION METHODS FOR OSELTAMIVIR CARBOXYLIC ACID HYDROCHLORIDE AND ATOMIZED AGENT THEREOF

机译:奥司他米羧酸盐酸盐的制备方法及其原子化剂

摘要

A preparation method for oseltamivir carboxylic acid hydrochloride comprises the following steps: a, introducing protective groups A to amidos of oseltamivir phosphate 1, so as to obtain a compound 2; b, hydrolyzing ester groups on the compound 2 under the action of strong alkali, so as to obtain a compound 3; and c, taking off the protective groups A of the compound 3 by means of hydrogen chloride, so as to obtain oseltamivir carboxylic acid hydrochloride 4. A reaction route is shown in formula (I). By means of the directly synthesized oseltamivir carboxylic acid hydrochloride and an atomized agent thereof, direct stimulation effects of drugs on gastrointestinal tracts can be avoided, and possible adverse reactions can be reduced by using a low dosage.
机译:一种奥司他韦羧酸盐酸盐的制备方法,包括以下步骤:a,将保护基A引入磷酸奥司他韦1的酰胺基中,得到化合物2; b。在强碱作用下,水解化合物2上的酯基,得到化合物3; c,通过氯化氢脱除化合物3的保护基A,得到奥司他韦羧酸盐酸盐4。反应路线如式(I)所示。通过直接合成的奥司他韦羧酸盐酸盐及其雾化剂,可以避免药物对胃肠道的直接刺激作用,并且通过使用低剂量可以减少可能的不良反应。

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