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METHOD FOR SYNTHESIS OF METHYL 4-(3-BROMO-4-OXOBUTYL)BENZOATE

机译:合成4-(3-溴--4-氧杂丁基)苯甲酸甲酯的方法

摘要

The present invention relates to the field of medical chemistry, particularly to the process for preparation of 4-(3-bromo-4-oxobutyl)-benzoic acid. Pharmaceutically active compound disodium salt of N-[4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid could be prepared in multistep synthesis and one of intermediates is 4-(3-bromo-4-oxobutyl)-benzoic acid methyl ester (BROMOPRODUCT), commonly prepared by bromination of 4-(4-oxobutyl)-benzoic acid methyl ester (ALDEHYDE). This invention provides process for bromination of ALDEHYDE using in complex included bromine, particularly pyridinium bromide perbromide, characterised in that provides to obtain BROMOPRODUCT in simple process with high yield of end-product.
机译:本发明涉及医学化学领域,尤其涉及4-(3-溴-4-氧代丁基)-苯甲酸的制备方法。 N- [4- [2-(2-氨基-4,7-二氢-4-氧代-1H-吡咯并[2,3-d]嘧啶-5-基)乙基]苯甲酰基]-的药物活性化合物二钠盐可以通过多步合成法制备L-谷氨酸,中间体之一是4-(3-溴-4-氧代丁基)-苯甲酸甲酯(BROMOPRODUCT),通常通过溴化4-(4-氧代丁基)-苯甲酸制备甲酯(ALDEHYDE)。本发明提供了在包含溴的复合物中溴化乙醛的方法,所述溴特别是溴化吡啶鎓过溴化物,其特征在于提供了以简单的方法获得BROMOPRODUCT的最终产物的高收率。

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