New One-Pot Synthesis of 1,3,5-Triazines: Three-Component Condensation, Dimroth Rearrangement, and Dehydrogenative Aromatization

A new, effective one-pot synthesis of the 6,N2-diaryl-1,3,5-triazine-2,4-diamines under microwave irradiation was developed. The method involved an initial three-component condensation of cyanoguanidine, aromatic aldehydes, and arylamines in the presence of hydrochloric acid. Without isolation, the r...

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Main Authors: Ahmad Junaid, Lim, Felicia Phei Lin, Tiekink, Edward R. T. *, Dolzhenko, Anton V
Format: Article
Published: American Chemical Society 2019
Subjects:
Online Access:http://eprints.sunway.edu.my/1072/
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author Ahmad Junaid,
Lim, Felicia Phei Lin
Tiekink, Edward R. T. *
Dolzhenko, Anton V
author_facet Ahmad Junaid,
Lim, Felicia Phei Lin
Tiekink, Edward R. T. *
Dolzhenko, Anton V
author_sort Ahmad Junaid,
building SU Institutional Repository
collection Online Access
description A new, effective one-pot synthesis of the 6,N2-diaryl-1,3,5-triazine-2,4-diamines under microwave irradiation was developed. The method involved an initial three-component condensation of cyanoguanidine, aromatic aldehydes, and arylamines in the presence of hydrochloric acid. Without isolation, the resulting 1,6-diaryl-1,6-dihydro-1,3,5-triazine-2,4diamines were treated with a base to initiate Dimroth rearrangement and spontaneous dehydrogenative aromatization, affording the desired compounds. The developed method was found to be sufficiently general in scope, tolerating various aromatic aldehydes and amines; by using their combinations in the first step, a representative library of 110 compounds was successfully prepared and screened for anticancer properties.
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publishDate 2019
publisher American Chemical Society
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spelling sunway-10722020-10-07T08:36:53Z http://eprints.sunway.edu.my/1072/ New One-Pot Synthesis of 1,3,5-Triazines: Three-Component Condensation, Dimroth Rearrangement, and Dehydrogenative Aromatization Ahmad Junaid, Lim, Felicia Phei Lin Tiekink, Edward R. T. * Dolzhenko, Anton V QD Chemistry A new, effective one-pot synthesis of the 6,N2-diaryl-1,3,5-triazine-2,4-diamines under microwave irradiation was developed. The method involved an initial three-component condensation of cyanoguanidine, aromatic aldehydes, and arylamines in the presence of hydrochloric acid. Without isolation, the resulting 1,6-diaryl-1,6-dihydro-1,3,5-triazine-2,4diamines were treated with a base to initiate Dimroth rearrangement and spontaneous dehydrogenative aromatization, affording the desired compounds. The developed method was found to be sufficiently general in scope, tolerating various aromatic aldehydes and amines; by using their combinations in the first step, a representative library of 110 compounds was successfully prepared and screened for anticancer properties. American Chemical Society 2019-06-10 Article PeerReviewed Ahmad Junaid, and Lim, Felicia Phei Lin and Tiekink, Edward R. T. * and Dolzhenko, Anton V (2019) New One-Pot Synthesis of 1,3,5-Triazines: Three-Component Condensation, Dimroth Rearrangement, and Dehydrogenative Aromatization. ACS Combinatorial Science, 21 (7). pp. 548-555. ISSN 2156 8952 https://pubs.acs.org/doi/full/10.1021/acscombsci.9b00079
spellingShingle QD Chemistry
Ahmad Junaid,
Lim, Felicia Phei Lin
Tiekink, Edward R. T. *
Dolzhenko, Anton V
New One-Pot Synthesis of 1,3,5-Triazines: Three-Component Condensation, Dimroth Rearrangement, and Dehydrogenative Aromatization
title New One-Pot Synthesis of 1,3,5-Triazines: Three-Component Condensation, Dimroth Rearrangement, and Dehydrogenative Aromatization
title_full New One-Pot Synthesis of 1,3,5-Triazines: Three-Component Condensation, Dimroth Rearrangement, and Dehydrogenative Aromatization
title_fullStr New One-Pot Synthesis of 1,3,5-Triazines: Three-Component Condensation, Dimroth Rearrangement, and Dehydrogenative Aromatization
title_full_unstemmed New One-Pot Synthesis of 1,3,5-Triazines: Three-Component Condensation, Dimroth Rearrangement, and Dehydrogenative Aromatization
title_short New One-Pot Synthesis of 1,3,5-Triazines: Three-Component Condensation, Dimroth Rearrangement, and Dehydrogenative Aromatization
title_sort new one-pot synthesis of 1,3,5-triazines: three-component condensation, dimroth rearrangement, and dehydrogenative aromatization
topic QD Chemistry
url http://eprints.sunway.edu.my/1072/
http://eprints.sunway.edu.my/1072/