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. 2019 Dec 2;11:173. doi: 10.1186/s13148-019-0763-5

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© The Author(s). 2019

Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.

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Scheme 1 — Reagents and conditions: (a) glacial acetic acid, sealed tube, 100 °C, 1.5 h (35-80%); (b) Pd(OAc)₂, PH(tBu)₃BF₃, potassium tert-butoxide, dry toluene, sealed tube, N₂, 80 °C, 4 h (76-80%); (c) trichloroacetyl chloride, dry 1,2-dichloroethane, sealed tube, 0 °C to 70 °C, 1 h; (d) I. 2 N KOH (aq), EtOH, r.t. to 60 °C; II. 2 N HCl (aq) (54-73 %); (e) triethylamine, TBTU, dry DMF, N₂, r. t., 4 h (52-75%)