Synthesis 2012; 44(21): 3321-3326
DOI: 10.1055/s-0032-1317351
paper
© Georg Thieme Verlag Stuttgart · New York

A Paal–Knorr Approach to 3,4-Diaryl-Substituted Pyrroles: Facile Synthesis of Lamellarins O and Q

Armando Ramírez-Rodríguez
Departamento de Química Orgánica, Facultad de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, 04510 México, D.F., México   Fax: +52(55)56223722   eMail: joseavm@unam.mx
,
José M. Méndez
Departamento de Química Orgánica, Facultad de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, 04510 México, D.F., México   Fax: +52(55)56223722   eMail: joseavm@unam.mx
,
Cristina C. Jiménez
Departamento de Química Orgánica, Facultad de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, 04510 México, D.F., México   Fax: +52(55)56223722   eMail: joseavm@unam.mx
,
Fernando León
Departamento de Química Orgánica, Facultad de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, 04510 México, D.F., México   Fax: +52(55)56223722   eMail: joseavm@unam.mx
,
Alfredo Vazquez*
Departamento de Química Orgánica, Facultad de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, 04510 México, D.F., México   Fax: +52(55)56223722   eMail: joseavm@unam.mx
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Publikationsverlauf

Received: 11. Juni 2012

Accepted after revision: 14. September 2012

Publikationsdatum:
28. September 2012 (online)


Abstract

A very simple, yet efficient synthetic methodology, to obtain 3,4-diaryl-substituted pyrroles is described. The approach is based on the Knoevenagel condensation between arylacetonitriles and substituted aromatic aldehydes, followed by conjugate addition of cyanide to afford succinonitriles in excellent yields. The products thus obtained were subjected to DIBAL-H reduction, followed by cyclization under acidic conditions to produce the corresponding pyrroles in good overall yields. The utility of this protocol is exemplified by the synthesis of the marine alkaloids lamellarins O and Q.

Supporting Information

 
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