Process for the preparation of intermediates useful in the synthesis of statin derivatives especially 7-amino 3 5-dihydroxy heptanoic acid derivatives, and intermediates thereof
申请人:——
公开号:US20040186313A1
公开(公告)日:2004-09-23
The invention relates to synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I wherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or N(CH
3
)OCH
3
, R
a
is a hydroxy-protecting group, and R
b
is a carboxy-protecting group, and, as well as to the compound of formula I, to further intermediates and methods for their preparation by Friedel-Crafts acylation.
1
本发明涉及制备他汀衍生物的合成方法,该方法通过式 I 的关键中间体进行,其中 X 为卤素、酰氧基、活化的烃氧基、活化的烃硫基或 N(CH
3
) OCH
3
, R
a
是羟基保护基团,而 R
b
是羧基保护基团,以及式 I 所示化合物的进一步中间体和通过 Friedel-Crafts 酯化反应制备它们的方法。
1