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功能化四取代吡唑基杂环的合成——综述。

Synthesis of functionalized tetrasubstituted pyrazolyl heterocycles--a review.

机构信息

Medicinal Chemistry, Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St Lucie, FL 34987, USA.

出版信息

Eur J Med Chem. 2011 Nov;46(11):5258-75. doi: 10.1016/j.ejmech.2011.09.016. Epub 2011 Sep 19.

Abstract

Heterocyclic chemistry constitutes an essential branch of organic chemistry and heterocycles are widely known to display an array of biological properties. Pyrazoles represent key structural motifs in heterocyclic chemistry and are present in a large number of biologically active molecules relevant to the pharmaceutical and agrochemical industries. Compounds incorporating the pyrazolyl structural unit are being developed in a wide variety of therapeutic areas including CNS, metabolic diseases, and oncology. The current review summarizes recent advances in the synthesis of tetrasubstituted pyrazoles. The contents are discussed in five sections: (a) 1,3-dipolar cycloadditions, (b) related 1,3-dipolar cycloadditions, (c) condensations, (d) allenylphosphonates, and (e) synthesis of fused pyrazole containing heterocycles.

摘要

杂环化学是有机化学的一个重要分支,杂环广泛地显示出一系列的生物性质。吡唑是杂环化学中的关键结构基序,存在于大量与制药和农用化学品行业相关的具有生物活性的分子中。包含吡唑基结构单元的化合物正在广泛的治疗领域中得到开发,包括中枢神经系统、代谢疾病和肿瘤学。本综述总结了近年来四取代吡唑的合成进展。内容分为五个部分讨论:(a) 1,3-偶极环加成反应,(b) 相关的 1,3-偶极环加成反应,(c) 缩合反应,(d) 烯丙基膦酸酯,和 (e) 含稠合吡唑的杂环合成。

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