4-Fluoroaniline → N-(3-chloro-4-(2-iodothieno[3,2-b]pyridin-7-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

Participants

Reaction Steps

Prepared from 3-chloro-4-(2-iodothieno[3,2-b]pyridin-7-yloxy)benzenamine (0.300 g, 0.499 mmol) and 1-((4-fluorophenyl)carbamoyl)cyclopropanecarboxylic acid (0.167 g, 0.749 mmol; prepared from cyclopropane-1,1-dicarboxylic acid and 4-fluoroaniline using the methods described in WO 2005/030140 and by Shih and Rankin, Synth. Comm. 1996, 26(4), 833-836) according to the procedure for Example 72, Step B. The crude was purified by Biotage 40S (2:1EtOAc/Hexane). After concentration the product was a brown oil (160 mg, 26%). LRMS (ESI pos) m/e 608 (M+1).

Provenance & Evidence