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发明公开
CN105968016A 一种碳酸酯类光敏试剂及其制备方法、5`-光敏保护核苷的制备方法 无效 - 驳回

一种碳酸酯类光敏试剂及其制备方法、5`-光敏保护核苷的制备方法
摘要：
本发明涉及一种碳酸酯类光敏试剂及其制备方法、5'‑光敏保护核苷的制备方法。碳酸酯类光敏试剂，其结构式为：其中X为-OX’、咪唑基、取代咪唑基；5'-光敏保护核苷的制备方法步骤包括将2’-脱氧核苷与2-邻硝基苯-1-丙基碳酸酯类光敏试剂和三乙胺得5'-光敏保护核苷粗产物、粗产物提纯得到5'-光敏保护核苷。本发明5'-光敏保护核苷制备方法选择性平均提高了3.4倍，减化了提纯过程，提高了产率，大大降低了生产成本，同时避免了使用剧毒的双光气。
摘要（英）：

The invention relates to a carbonic ester type photosensitive reagent and a preparation method thereof as well as a preparation method of 5'-photolabile dN. The structural formula of the carbonic ester type photosensitive reagent is shown in the specification, wherein X is -OX', imidazolyl or substituted imidazolyl. The preparation method of 5'-photolabile dN comprises the following steps: preparing a crude product of 5'-photolabile dN from 2'-deoxynucleoside and 2-o-nitrobenzene-1-propyl carbonic ester type photosensitive reagent and triethylamine; and purifying the crude product to obtain the 5'-photolabile dN. According to the preparation method of 5'-photolabile dN, the selectivity is improved by 3.4 times on average, the purifying process is simplified, the yield is increased, the production cost is greatly reduced, and the use of virulent diphosgene is avoided.

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