两个双醋瑞因单乙酰化杂质的合成

Synthesis of Two Monoacetyl Impurites of Diacerein

以双醋瑞因和大黄酸为原料,分别通过选择性水解及选择性乙酰化反应合成5-乙酰氧基-4-羟基-9,10-二氢-9,10-二氧代-2-蒽羧酸(1)和4-乙酰氧基-5-羟基-9,10-二氢-9,10-二氧代-2-蒽羧酸(2),其中1收率17.5%,纯度99.4%;2收率19.6%,纯度99.1%。结构均经~1H NMR、~13C NMR、红外光谱及质谱鉴定,HPLC行为与文献一致。

5-Acetoxy-4-hydroxy-9,10-dioxo-9,10-dihydroanthracene-2-carboxylic acid （1） was prepared via selective hydrolysis of diacerein with a yield of 17.5% and purity of 99.4%. 4-Acetoxy-5-hydroxy-9,10-dioxo-9,10- dihydroanthracene-2-carboxylic acid （2） was synthesized via selective acylation of rhein with a yield of 19.6 % and purity of 99.1%. Their chemical structures were confirmed via ^1H/^13C NMR, IR, MS and the HPLC information was consistent with the literature.