Overcoming the Necessity of γ-Substitution in δ-C(sp3)–H Arylation: Pd-Catalyzed Derivatization of α-Amino Acids

Despite the emergence of catalytic C(sp3 )−H arylation at the remote δ-position via challenging six-membered ring cyclometalation, the requirement of blocking the more reactive γ-position represents a restricting limitation. The use of the removable N-(2-pyridyl)sulfonyl directing group provides a v...

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Autores: Martínez-Mingo, Mario, García-Viada, Andrés, Alonso Montero, María Inés, Rodríguez Garrido, Nuria, Gómez Arrayas, Ramón Jesús, Carretero Gonzálvez, Juan Carlos
Tipo de recurso: artículo
Fecha de publicación:2021
País:España
Institución:Universidad Autónoma de Madrid
Repositorio:Biblos-e Archivo. Repositorio Institucional de la UAM
Idioma:inglés
OAI Identifier:oai:repositorio.uam.es:10486/695363
Acceso en línea:http://hdl.handle.net/10486/695363
https://dx.doi.org/10.1021/acscatal.1c00250
Access Level:acceso abierto
Palabra clave:Remote C(sp3 )−H arylation
Palladium-catalysis
α-amino acid
2-pyridylsulfonyl directing group
Late-stage functionalization
Peptide
Química
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spelling Overcoming the Necessity of γ-Substitution in δ-C(sp3)–H Arylation: Pd-Catalyzed Derivatization of α-Amino AcidsMartínez-Mingo, MarioGarcía-Viada, AndrésAlonso Montero, María InésRodríguez Garrido, NuriaGómez Arrayas, Ramón JesúsCarretero Gonzálvez, Juan CarlosRemote C(sp3 )−H arylationPalladium-catalysisα-amino acid2-pyridylsulfonyl directing groupLate-stage functionalizationPeptideQuímicaDespite the emergence of catalytic C(sp3 )−H arylation at the remote δ-position via challenging six-membered ring cyclometalation, the requirement of blocking the more reactive γ-position represents a restricting limitation. The use of the removable N-(2-pyridyl)sulfonyl directing group provides a viable solution to this challenge, expanding the scope of the Pd-catalyzed δ-C−H arylation of α-amino acid and amine derivatives with (hetero)aryl iodides. This method is compatible with complex, multifunctional structures at either reaction partner. Experimental and density functional theory studies provide insights about the underlying factors controlling site selectivityWe thank the Ministerio de Economía, Industria y Competitividad (MINECO) and Fondo Europeo de Desarrollo Regional (FEDER, UE) (Project CTQ2015-66954-P) and Ministerio de Ciencia e Innovación (MICINN)/FEDER, UE (Agencia Estatal de Investigación/Project PGC2018- 098660-B-I00) for the financial supportAmerican Chemical SocietyDepartamento de Química OrgánicaFacultad de Ciencias20212021-04-19research articlehttp://purl.org/coar/resource_type/c_2df8fbb1AMhttp://purl.org/coar/version/c_ab4af688f83e57aainfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10486/695363https://dx.doi.org/10.1021/acscatal.1c00250reponame:Biblos-e Archivo. Repositorio Institucional de la UAMinstname:Universidad Autónoma de MadridInglésengopen accesshttp://purl.org/coar/access_right/c_abf2info:eu-repo/semantics/openAccessoai:repositorio.uam.es:10486/6953632026-06-23T12:46:27Z
dc.title.none.fl_str_mv Overcoming the Necessity of γ-Substitution in δ-C(sp3)–H Arylation: Pd-Catalyzed Derivatization of α-Amino Acids
title Overcoming the Necessity of γ-Substitution in δ-C(sp3)–H Arylation: Pd-Catalyzed Derivatization of α-Amino Acids
spellingShingle Overcoming the Necessity of γ-Substitution in δ-C(sp3)–H Arylation: Pd-Catalyzed Derivatization of α-Amino Acids
Martínez-Mingo, Mario
Remote C(sp3 )−H arylation
Palladium-catalysis
α-amino acid
2-pyridylsulfonyl directing group
Late-stage functionalization
Peptide
Química
title_short Overcoming the Necessity of γ-Substitution in δ-C(sp3)–H Arylation: Pd-Catalyzed Derivatization of α-Amino Acids
title_full Overcoming the Necessity of γ-Substitution in δ-C(sp3)–H Arylation: Pd-Catalyzed Derivatization of α-Amino Acids
title_fullStr Overcoming the Necessity of γ-Substitution in δ-C(sp3)–H Arylation: Pd-Catalyzed Derivatization of α-Amino Acids
title_full_unstemmed Overcoming the Necessity of γ-Substitution in δ-C(sp3)–H Arylation: Pd-Catalyzed Derivatization of α-Amino Acids
title_sort Overcoming the Necessity of γ-Substitution in δ-C(sp3)–H Arylation: Pd-Catalyzed Derivatization of α-Amino Acids
dc.creator.none.fl_str_mv Martínez-Mingo, Mario
García-Viada, Andrés
Alonso Montero, María Inés
Rodríguez Garrido, Nuria
Gómez Arrayas, Ramón Jesús
Carretero Gonzálvez, Juan Carlos
author Martínez-Mingo, Mario
author_facet Martínez-Mingo, Mario
García-Viada, Andrés
Alonso Montero, María Inés
Rodríguez Garrido, Nuria
Gómez Arrayas, Ramón Jesús
Carretero Gonzálvez, Juan Carlos
author_role author
author2 García-Viada, Andrés
Alonso Montero, María Inés
Rodríguez Garrido, Nuria
Gómez Arrayas, Ramón Jesús
Carretero Gonzálvez, Juan Carlos
author2_role author
author
author
author
author
dc.contributor.none.fl_str_mv Departamento de Química Orgánica
Facultad de Ciencias
dc.subject.none.fl_str_mv Remote C(sp3 )−H arylation
Palladium-catalysis
α-amino acid
2-pyridylsulfonyl directing group
Late-stage functionalization
Peptide
Química
topic Remote C(sp3 )−H arylation
Palladium-catalysis
α-amino acid
2-pyridylsulfonyl directing group
Late-stage functionalization
Peptide
Química
description Despite the emergence of catalytic C(sp3 )−H arylation at the remote δ-position via challenging six-membered ring cyclometalation, the requirement of blocking the more reactive γ-position represents a restricting limitation. The use of the removable N-(2-pyridyl)sulfonyl directing group provides a viable solution to this challenge, expanding the scope of the Pd-catalyzed δ-C−H arylation of α-amino acid and amine derivatives with (hetero)aryl iodides. This method is compatible with complex, multifunctional structures at either reaction partner. Experimental and density functional theory studies provide insights about the underlying factors controlling site selectivity
publishDate 2021
dc.date.none.fl_str_mv 2021
2021-04-19
dc.type.none.fl_str_mv research article
http://purl.org/coar/resource_type/c_2df8fbb1
AM
http://purl.org/coar/version/c_ab4af688f83e57aa
dc.type.openaire.fl_str_mv info:eu-repo/semantics/article
format article
dc.identifier.none.fl_str_mv http://hdl.handle.net/10486/695363
https://dx.doi.org/10.1021/acscatal.1c00250
url http://hdl.handle.net/10486/695363
https://dx.doi.org/10.1021/acscatal.1c00250
dc.language.none.fl_str_mv Inglés
eng
language_invalid_str_mv Inglés
language eng
dc.rights.none.fl_str_mv open access
http://purl.org/coar/access_right/c_abf2
dc.rights.openaire.fl_str_mv info:eu-repo/semantics/openAccess
rights_invalid_str_mv open access
http://purl.org/coar/access_right/c_abf2
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv American Chemical Society
publisher.none.fl_str_mv American Chemical Society
dc.source.none.fl_str_mv reponame:Biblos-e Archivo. Repositorio Institucional de la UAM
instname:Universidad Autónoma de Madrid
instname_str Universidad Autónoma de Madrid
reponame_str Biblos-e Archivo. Repositorio Institucional de la UAM
collection Biblos-e Archivo. Repositorio Institucional de la UAM
repository.name.fl_str_mv
repository.mail.fl_str_mv
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