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Synthesis of the ‘853 derivatives with a modified spacer, reagents and conditions: (a) 1. EDC × HCl, HOAt, DMF, rt, 10 min, 2. 6-fluoro-1H-indazole-3-amine (13), rt, 10a and 10b: 3 h, 10c: 2 h, 10d: 1 h, 10e: 1.5 h (10a: 27%, 10b: 45%, 10c: 43%, 10d: 30%, 10e: 42%).
