Synthesis of 5-Arylpyrrole-2-carboxylic Acids as Key Intermediates for NBD Series HIV-1 Entry Inhibitors

被引：14

作者：

Belov, Dmitry S. ^{[1
]}

Ivanov, Vladimir N. ^{[1
]}

Curreli, Francesca ^{[2
]}

Kurkin, Alexander V. ^{[1
]}

Altieri, Andrea ^{[1
]}

Debnath, Asim K. ^{[2
]}

机构：

[1] Moscow MV Lomonosov State Univ, EDASA Sci, Sci Pk,Bld 75,77-101b, Moscow 119992, Russia

[2] New York Blood Ctr, Lindsey F Kimball Res Inst, Lab Mol Modeling & Drug Design, New York, NY 10065 USA

来源：

SYNTHESIS-STUTTGART | 2017年 / 49卷 / 16期

基金：

美国国家卫生研究院;

关键词：

HIV-1 entry inhibitors; pyrroles; carboxylic acids; arylation; trifluoroacetylation; SPECTRUM ANTI-HIV-1 ACTIVITY; DIRECT ARYLATION; FUNCTIONALIZATION; PYRROLE; DESIGN; COMPLEXES; CATALYST; BROMIDES; HALIDES; ANIONS;

D O I：

10.1055/s-0036-1588780

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

5-Arylpyrrole-2-carboxylic acids are important key intermediates in the synthesis of HIV-1 entry inhibitors (such as NBD-11021 and NBD-14010). Here we present a general method for the synthesis of some 5-arylpyrrole-2-carboxylic acids in three steps starting from pyrrole. By this method, the compounds could be prepared on gram scale and without chromatographic purification.

引用

页码：3692 / 3699

页数：8

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