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. 2016 Apr 30;21(5):578. doi: 10.3390/molecules21050578

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© 2016 by the authors.

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).

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Scheme 2 — Multistep synthesis of the key benzothiazole 1. Reagents and conditions: (a) Boc₂O (2.3 equiv), DMAP (1.0 equiv), Et₃N (1.0 equiv), THF, r.t., 5 h; (b) HCO₂NH₄ (5.0 equiv), Pd/C (10%), EtOH, 78 °C (μw), 15 min; (c) NBS (1.0 equiv), DMF, −10 °C, 3 h; (d) Appel salt (1.2 equiv), Py. (2.3 equiv), CH₂Cl₂, r.t., 3 h; (e) TFA, CH₂Cl₂, r.t., 2 h; (f) CuI (1.0 equiv), Py., 115 °C (μw), 30 min.