meta-Selective olefination of fluoroarenes with alkynes using CO2 as a traceless directing group

Over the last few decades C-H olefination has received significant interest, due to the importance and usefulness of aryl olefins both as synthetic targets and intermediates. While a wide range of ortho-olefination protocols have been developed, only a small number of meta-olefinations are currently...

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Published in:Chemical science (Cambridge) Vol. 11; no. 16; pp. 4204 - 4208
Main Authors: Spencer, Andrew R. A., Korde, Rishi, Font, Marc, Larrosa, Igor
Format: Journal Article
Language:English
Published: CAMBRIDGE Royal Soc Chemistry 31.03.2020
Royal Society of Chemistry
The Royal Society of Chemistry
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ISSN:2041-6520, 2041-6539
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Abstract Over the last few decades C-H olefination has received significant interest, due to the importance and usefulness of aryl olefins both as synthetic targets and intermediates. While a wide range of ortho-olefination protocols have been developed, only a small number of meta-olefinations are currently available. Importantly, the most common approach to meta-olefination, using a large meta-directing template, is not suitable for substrates such as fluorobenzenes, which cannot be derivatised. We report that the meta-selective olefination of fluoroarenes can be achieved via the use of CO2 as a traceless directing group, which can be easily installed and removed in a one-pot process. Furthermore, this approach avoids the use of stoichiometric Ag(i)-salts, commonly used in C-H olefinations, and affords complete meta- over ortho/para-regioselectivity.
AbstractList Over the last few decades C–H olefination has received significant interest, due to the importance and usefulness of aryl olefins both as synthetic targets and intermediates. While a wide range of ortho-olefination protocols have been developed, only a small number of meta-olefinations are currently available. Importantly, the most common approach to meta-olefination, using a large meta-directing template, is not suitable for substrates such as fluorobenzenes, which cannot be derivatised. We report that the meta-selective olefination of fluoroarenes can be achieved via the use of CO2 as a traceless directing group, which can be easily installed and removed in a one-pot process. Furthermore, this approach avoids the use of stoichiometric Ag(i)-salts, commonly used in C–H olefinations, and affords complete meta- over ortho/para-regioselectivity. A transient directing group approach using CO2 facilitates the direct meta-olefination of fluorobenzenes with alkynes.
Over the last few decades C-H olefination has received significant interest, due to the importance and usefulness of aryl olefins both as synthetic targets and intermediates. While a wide range of ortho-olefination protocols have been developed, only a small number of meta-olefinations are currently available. Importantly, the most common approach to meta-olefination, using a large meta-directing template, is not suitable for substrates such as fluorobenzenes, which cannot be derivatised. We report that the meta-selective olefination of fluoroarenes can be achieved via the use of CO2 as a traceless directing group, which can be easily installed and removed in a one-pot process. Furthermore, this approach avoids the use of stoichiometric Ag(i)-salts, commonly used in C-H olefinations, and affords complete meta- over ortho/para-regioselectivity.Over the last few decades C-H olefination has received significant interest, due to the importance and usefulness of aryl olefins both as synthetic targets and intermediates. While a wide range of ortho-olefination protocols have been developed, only a small number of meta-olefinations are currently available. Importantly, the most common approach to meta-olefination, using a large meta-directing template, is not suitable for substrates such as fluorobenzenes, which cannot be derivatised. We report that the meta-selective olefination of fluoroarenes can be achieved via the use of CO2 as a traceless directing group, which can be easily installed and removed in a one-pot process. Furthermore, this approach avoids the use of stoichiometric Ag(i)-salts, commonly used in C-H olefinations, and affords complete meta- over ortho/para-regioselectivity.
Over the last few decades C–H olefination has received significant interest, due to the importance and usefulness of aryl olefins both as synthetic targets and intermediates. While a wide range of ortho-olefination protocols have been developed, only a small number of meta-olefinations are currently available. Importantly, the most common approach to meta-olefination, using a large meta-directing template, is not suitable for substrates such as fluorobenzenes, which cannot be derivatised. We report that the meta-selective olefination of fluoroarenes can be achieved via the use of CO2 as a traceless directing group, which can be easily installed and removed in a one-pot process. Furthermore, this approach avoids the use of stoichiometric Ag(i)-salts, commonly used in C–H olefinations, and affords complete meta- over ortho/para-regioselectivity.
Author Larrosa, Igor
Font, Marc
Spencer, Andrew R. A.
Korde, Rishi
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ContentType Journal Article
Copyright Copyright Royal Society of Chemistry 2020
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Issue 16
Keywords CARBOXYLATES
ORGANOMETALLIC CHEMISTRY
ARYLATION
ARENES
FLUORINE
BOND ACTIVATION
C-H FUNCTIONALIZATION
DERIVATIVES
HYDROARYLATION
ALKENYLATION
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Snippet Over the last few decades C-H olefination has received significant interest, due to the importance and usefulness of aryl olefins both as synthetic targets and...
Over the last few decades C–H olefination has received significant interest, due to the importance and usefulness of aryl olefins both as synthetic targets and...
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StartPage 4204
SubjectTerms Alkenes
Alkynes
Aromatic compounds
Carbon dioxide
Chemistry
Chemistry, Multidisciplinary
Physical Sciences
Regioselectivity
Science & Technology
Substrates
Title meta-Selective olefination of fluoroarenes with alkynes using CO2 as a traceless directing group
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https://pubmed.ncbi.nlm.nih.gov/PMC8152615
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