Cesium carbonate → (S)-tert-butyl 3-(5-(4-(6-(1-tert-butoxy-2-ethoxy-2-oxoethyl)-7-(4-chlorophenyl)-5-methylbenzo[d]thiazol-2-yl)pyridin-2-yl)-1H-indazol-1-yl)azetidine-1-carboxylate

Participants

Reaction Conditions

Reaction Steps

To a solution of (S)-ethyl 2-(2-(2-(1H-indazol-5-yl)pyridin-4-yl)-7-(4-chlorophenyl)-5-methylbenzo[d]thiazol-6-yl)-2-tert-butoxyacetate (110 mg, 0.18 mmol) in DMF (3 mL) was added Cs2CO3 (117 mg, 0.36 mmol) and 1-Boc-3-iodoazetidine (76 mg, 0.27 mmol). The reaction mixture was heated at 60° C. overnight. The reaction mixture was washed by saturated NaHCO3, extracted by EtOAc, the organic phase was dried over MgSO4, filtered, concentrated down, purified by silica gel column, eluting by 0-60% EtOAc in hexanes to give the product. LCMS-ESI+: calc'd for C42H44ClN5O5S: 766.3 (M+H+); found: 766.3.

Provenance & Evidence