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. Author manuscript; available in PMC: 2020 Mar 5.
Published in final edited form as: ChemMedChem. 2019 Feb 5;14(5):545–560. doi: 10.1002/cmdc.201800725

Scheme 1.

Scheme 1.

Reagents and conditions (a) TFA, dry CH2Cl2, 1 h, from 0 °C to 25 °C; (b). 9, i-PrOH, 80 °C, 18 h; (c) TFA, dry CH2Cl2, 1 h, from 0 °C to 25 °C, 66–86% (3 steps) (d) Suitable acids 5a,b and 6a,b and appropriate amines 10a or 10b, EDCI·HCl, HOBt·H2O, DIPEA, dry CH2Cl2, 15 h, rt, 39–78%.