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Process for preparing intermediates and their use for making aliskiren and derivatives thereof

机译:中间体的制备方法及其在制备阿利吉仑及其衍生物中的用途

摘要

Disclosed herein is a process for the manufacture of a compound of formula III wherein said process comprises reacting a compound of formula I with a reagent able to transform hydroxy in formula I into X where X is a leaving group and is other than hydroxy or hydrogen, and wherein the reagent is selected from a hydrohalic acid, a thionyl halogenide, PX*3, POX*3, PX*5, POX*5 wherein X* is a halogenide, a combination of triphenylphosphine and halogen, or an active derivative of an organic sulfonic acid. Also disclosed are processes for the manufacture of useful intermediate compounds for making aliskiren.
机译:本文公开了一种制备式III化合物的方法,其中所述方法包括使式I化合物与能够将式I中的羟基转化为X的试剂反应,其中X是离去基团,并且不是羟基或氢,其中试剂选自氢卤酸,亚硫酰卤,PX * 3,POX * 3,PX * 5,POX * 5,其中X *为卤化物,三苯基膦和卤素的组合或有机磺酸。还公开了制备用于制备阿利吉仑的有用中间体化合物的方法。

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