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A Facile and Rapid Method for Synthesizing Indole–Chalcone Hybrids

Affiliation
Center for Drug Discovery, Faculty of Science, University of Buea, P.O. Box 63, Buea CM-00237, Cameroon;(S.A.T.);(D.B.E.)
Tanyi, Solange A.;
ORCID
0000-0002-4148-6372
Affiliation
Center for Drug Discovery, Faculty of Science, University of Buea, P.O. Box 63, Buea CM-00237, Cameroon;(S.A.T.);(D.B.E.)
Eni, Donatus B.;
ORCID
0000-0001-6559-2527
Affiliation
Department of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther-University of Halle-Wittenberg, 06120 Halle (Saale), Germany;(M.A.);(M.S.)
Abdelsalam, Mohamed;
ORCID
0000-0003-3876-2695
Affiliation
Department of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther-University of Halle-Wittenberg, 06120 Halle (Saale), Germany;(M.A.);(M.S.)
Schmidt, Matthias;
ORCID
0000-0002-5985-9261
Affiliation
Department of Medicinal Chemistry, Institute of Pharmacy, Martin-Luther-University of Halle-Wittenberg, 06120 Halle (Saale), Germany;(M.A.);(M.S.)
Sippl, Wolfgang;
ORCID
0000-0003-0795-394X
Affiliation
Center for Drug Discovery, Faculty of Science, University of Buea, P.O. Box 63, Buea CM-00237, Cameroon;(S.A.T.);(D.B.E.)
Ntie-Kang, Fidele

Indole–chalcone hybrids are a large group of compounds known for their excellent biological properties the help combat diverse pathogens. This study describes a rapid synthetic pathway for the synthesis of ten indole–chalcone hybrids, namely, 3 ( a – j ), from 1-Boc-3-formylindole ( 1 ) and acetophenone derivatives ( 2 ), in a one-pot approach. This synthesis involved an initial condensation reaction and subsequent deprotection of the Boc group. 1 H-NMR, 13 C-NMR, and MS were used to elucidate the structures of the final compounds. Contrary to previous methods for the synthesis of indole–chalcone hybrids, this novel synthetic method, which involves using a Boc-protected indole via microwave-assisted synthesis, is advantageous because it is a one-pot approach, making it facile and rapid.

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