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AN IMPROVED PROCESS FOR THE PREPARATION OF DROXIDOPA AND ITS INTERMEDIATE

机译:制备旱昔帕及其中间体的改进方法

摘要

The present invention provides an improved process for preparation of the L-threo-(2S,3R)-3-(3,4-dihydroxyphenyl)serine (I) or a salt thereof, which is known as Droxidopa; comprising (a) recovery of the by-product compound (V) (as described herein) from the crude compound (I), and (b) recycling and re-use it for the preparation of droxidopa. Accordingly, the present invention relates to an improved economical process for the preparation of L-threo-(2S,3R)-3-(3.4-dihydroxyphenyl)serine (I) or its pharmaceutically acceptable salts; wherein the process relates to recovery and recycling of the by-product compound (V) and also to re-use it for the preparation of droxidopa.
机译:本发明提供了制备L-三种 - (2S,3R)-3-(3,4-二羟基苯基)丝氨酸(I)或其盐的改进方法,其称为溴化吡普;包含(a)从粗化合物(I)中的副产物化合物(V)(如本文所述),并再循环并重新使用其用于制备溴化酞氧化酞甲醛。因此,本发明涉及制备L-Threo-(2S,3R)-3-(3.4-二羟基苯基)丝氨酸(I)或其药学上可接受的盐的改进的经济方法;其中,该方法涉及副产物化合物(V)的回收和再循环,也涉及重新使用它以制备溴化酞甲醛。

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