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

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 compoun...

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Bibliographic Details
Published inSynthesis (Stuttgart) Vol. 49; no. 16; pp. 3692 - 3699
Main Authors Belov, Dmitry S., Ivanov, Vladimir N., Curreli, Francesca, Kurkin, Alexander V., Altieri, Andrea, Debnath, Asim K.
Format Journal Article
LanguageEnglish
Published STUTTGART Thieme Medical Publishers 16.08.2017
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
HALIDES
ANIONS
DESIGN
DIRECT ARYLATION
PYRROLE
COMPLEXES
HIV-1 entry inhibitors
CATALYST
pyrroles
BROMIDES
arylation
FUNCTIONALIZATION
carboxylic acids
SPECTRUM ANTI-HIV-1 ACTIVITY
trifluoroacetylation
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Summary: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.
ISSN:0039-7881
1437-210X
DOI:10.1055/s-0036-1588780