Multi-Gram Synthesis of Enantiopure 1,5-Disubstituted Tetrazoles Via Ugi-Azide 3-Component Reaction

被引：9

作者：

Capurro, Pietro ^{[1
]}

Moni, Lisa ^{[1
]}

Galatini, Andrea ^{[1
]}

Mang, Christian ^{[2
]}

Basso, Andrea ^{[1
]}

机构：

[1] Univ Genoa, Dipartimento Chim & Chim Ind, Via Dodecaneso 33, I-16146 Genoa, Italy

[2] AnalytiCon Discovery GmbH, Hermannswerder Haus 17, D-14473 Potsdam, Germany

来源：

MOLECULES | 2018年 / 23卷 / 11期

关键词：

multicomponent reactions; Ugi-azide; chiral imines; tetrazoles; diversity-oriented synthesis; CHIRAL CYCLIC IMINES;

D O I：

10.3390/molecules23112758

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Tetrazoles have been widely studied for their biological properties. An efficient route for large-scale synthesis of 1,5-disubstituted tetrazoles (1,5-DTs) is presented. The strategy exploits a reductive approach to synthetize a cyclic chiral imine substrate which is then converted into the target product through an Ugi-azide three-component reaction (UA-3CR). The final products are equipped with additional functionalities which can be further elaborated for the generation of combinatorial libraries of enantiopure heterocycles.

引用

页数：6

共 17 条

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