Synthesis of 2‐Amino 3‐Substituted Quinazolin‐4(3H)‐one Derivatives via Iodine‐Mediated Guanidinylation of Pbf‐Activated Thiourea |
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| Authors: | Jizhen Li Yuhua Mi Jianghua He Xuyang Luo Erkang Fan |
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| Institution: | 1. College of Chemistry, Jilin University, , Changchun 130023, China;2. Biomolecular Structure Center, Department of Biochemistry, University of Washington, , Seattle, Washington 98195 |
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| Abstract: | 2‐Amino 3‐substituted‐quinazolin‐4(3H)‐one derivatives were synthesized from Pbf‐isothiocyanate and methyl anthranilate. The construction of the guanidine‐containing quinazolinone heterocyclic skeleton was achieved using Pbf‐activated thiourea treated with primary amines via iodine‐mediated guanidinylation. The desired compounds were obtained after Pbf cleavage by trifluoroacetic acid. |
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