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. 2019 Jan 24;8(1):114–125. doi: 10.1002/open.201800282

Scheme 1.

Scheme 1

Synthesis of AT2R ligands 40–51. a) ZnCl2, isobutylmagnesium chloride, Pd(t‐Bu3P)2, toluene, THF; b) 1. n‐BuLi (4.5 eq.), triisopropyl borate, THF; 2. methyliminodiacetic acid, DMSO, toluene; c) imidazole, DCM (to 16–17) ; d) 1. TEA, MsCl, DCM; 2. imidazole, DMF (to 18–19, 22–23, 25–27); e) 1. thionyl chloride, DCM; 2. imidazole DMF (to 20–21, 24); f) PdCl2(dppf), K2CO3, DME, H2O (to 28–33, 35–39); g) Pd(PPh3)4, K2CO3, EtOH, H2O, THF (to 34); h) 1. TFA; 2. butyl chloroformate, Na2CO3, DCM, H2O.