首页> 外国专利> METHOD OF PREPARING beta;-AZIDO CARBONYL COMPOUND FOR SYNTHESIS OF BETA;-AMINO ACIDS OR AMINO ALCOHOLS

METHOD OF PREPARING beta;-AZIDO CARBONYL COMPOUND FOR SYNTHESIS OF BETA;-AMINO ACIDS OR AMINO ALCOHOLS

机译:制备用于合成β-氨基氨基酸或氨基醇的β;-叠氮羰基化合物的方法

摘要

A method for preparing a beta-azido carbonyl compound is provided to obtain an intermediate useful for preparing beta-amino acids or aminoalcohols used in various medicines, particularly in beta-lactam antibiotics, HIV-protease inhibitor, etc., by a simple process with high efficiency. The method for preparing a beta-azido carbonyl compound represented by a formula 1 comprises a step of reacting an alpha, beta-unsaturated compound represented by a formula 2 with sodium azide in an organic solvent in the presence of hydrochloric acid and an organic catalyst. In the formulae 1 and 2, R1 is H or a C1-C6 alkyl; and R2 is H, a C1-C10 alkyl or hydroxy methyl substituted with benzyloxy, methyoxy or benzoyloxy, allyl group, or ester group.
机译:本发明提供了一种制备β-叠氮基羰基化合物的方法,该方法可通过简单的方法获得一种中间体,该中间体可用于制备用于各种药物,尤其是β-内酰胺抗生素,HIV-蛋白酶抑制剂等的各种药物中的β-氨基酸或氨基醇。高效率。制备由式1表示的β-叠氮基羰基化合物的方法包括以下步骤:在盐酸和有机催化剂存在下,在有机溶剂中使由式2表示的α,β-不饱和化合物与叠氮化钠反应。式1和式2中,R 1为H或C 1 -C 6烷基。 R 2为H,被苄氧基,甲氧基或苯甲酰氧基,烯丙基或酯基取代的C1-C10烷基或羟甲基。

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