A mild and relatively simple way for preparation of 2-(3-hydroxy-1-adamantane)-2-oxoacetic acid (I) was reported. It was prepared from 1-adamantanecarboxylic acid (II) via sulfuric acid/nitric acid to get 3-hydroxy-1-adamantanecarboxylic acid (III); treated with the one-pot method through acylation, condensation, and decarboxylation to obtain 3-hydroxy-1-acetyladamantane (IV); and finally oxidized by potassium permanganate (KMnO4) to get the target compound (I). The overall yield was about 60%, which provides a new idea for commercial production of saxagliptin intermediate.

中文翻译：

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一种高效实用的沙格列汀中间体2-(3-羟基-1-金刚烷)-2-氧代乙酸的合成及其优化方法

报道了一种温和且相对简单的制备 2-(3-羟基-1-金刚烷)-2-氧代乙酸 (I) 的方法。由1-金刚烷甲酸(II)经硫酸/硝酸制得3-羟基-1-金刚烷甲酸(III)；用一锅法酰化、缩合、脱羧得到3-羟基-1-乙酰金刚烷(IV)；最后用高锰酸钾（KMnO4）氧化得到目标化合物（I）。总收率约为60%，为沙格列汀中间体的商业化生产提供了新思路。