Iodoethane → HCID 10204220, compound

Participants

Reaction Steps

NaH (16 mg, 0.4 mmol) was added to a solution of (2R)-(2-methoxymethyl-pyrrolidin-1-yl)-[7-(2-methyl-1H-indol-5-yloxy)-thieno[3,2-b]pyridin-2-yl]-methanone (85 mg, 0.2 mmol) in DMF (5 mL), at 0° C. The reaction mixture was allowed to stir for 20 min, and EtI (57 mg, 0.40 mmol) was added dropwise. After 3 h the reaction was quenched with saturated aqueous KCN (10 mL). The aqueous layer was extracted with CH2Cl2 (3×15 mL). The combined organic extracts were dried (Na2SO4), and the solvent was removed. Purification by flash chromatography on silica gel (CH2Cl2/MeOH 94:6) afforded the title compound as a white solid (46 mg, 51%). MS: 450 (MH+); HPLC Rf: 6.83 min; HPLC purity: 95%.

Provenance & Evidence