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Process for the preparation of 2-(6-substituted-1,3-dioxane-4-yl)acetic acid derivatives

机译:制备2-(6-取代的1,3-二恶烷-4-基)乙酸衍生物的方法

摘要

The invention relates to the preparation of 2-(6-substituted-1,3-dioxane-4-yl)acetic acid derivatives of formula 1, where X stands for a leaving group, and R1, R2, and R3 each independently stand for an alkyl group with 1-3 carbon atoms from 4-hydroxy-6-X-substituted-methyl-tetrahydropyran-2-one compounds, where X is as defined above, with the aid of an acetalization agent, in the presence of an acid catalyst.;The invention also relates to the novel compounds of formula 1 as well as salts and acids to be prepared from these, with the OR3 group in formula 1 being replaced by an OY group, where X, R1 and R2 have the meanings defined above and where Y stands for an alkaline (earth) metal or a substituted or unsubstituted ammonium group or stands for hydrogen, and to the novel compounds of formula 2.;The products concerned are, after conversion into the t-butyl ester of 2-(6-hydroxymethyl-1,3-dioxane-4-yl)acetic acid, important as intermediary products in the preparation of statins.
机译:本发明涉及式1的2-(6-取代的-1,3-二恶烷-4-基)乙酸衍生物的制备,其中X代表离去基团,R 1 , R 2 和R 3 各自独立地代表4-羟基-6-X-取代的甲基-四氢吡喃-2-基中具有1-3个碳原子的烷基在酸催化剂的存在下,在缩醛化剂的帮助下,X为如上定义的一种化合物。本发明还涉及式1的新化合物以及由其制备的盐和酸,式1中的OR 3 组被OY组取代,其中X,R 1 和R 2 具有上面定义的含义,其中Y代表碱金属(地球)或取代或未取代的铵基团或代表氢,且与式2的新化合物相对应;所涉及的产物在转化为2-(6)的叔丁酯后-羟甲基-1,3-二恶烷-4-基)乙酸,进口蚂蚁为他汀类药物的制备中间体。

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