Cesium carbonate → HCID 117683816, compound

Participants

Reaction Steps

Following the same procedure as in step 3 of Example 337 using 5-bromo-1,3-benzothiazole (74.9 mg, 0.35 mmol, 1.80 equiv), tert-butyl (3R)-3-[[5-iodo-6-methoxy-2-(morpholin-4-yl)pyrimidin-4-yl]amino]piperidine-1-carboxylate (100.0 mg, 0.19 mmol, 1.00 equiv), cesium carbonate (370 mg, 1.14 mmol, 6.00 equiv), Pd(PPh3)4 (40.4 mg, 0.035 mmol, 0.18 equiv), copper (I) iodide (6.7 mg, 0.035 mmol, 0.18 equiv) in DMF (5.0 mL). The crude product was purified by flash chromatography on silica gel, eluting with petroleum ether/ethyl acetate (10:1-5:1) to provide the title compound as a light yellow solid. MS m/z [M+H]+ (ESI): 605

Provenance & Evidence