Triethylamine → HCID 23394046, compound

Participants

Reaction Conditions

Reaction Steps

To solution of compound A of Example 18 (63 mg, 0.16 mmol) in 1,4-dioxane (1.7 mL) at RT were added 4A sieves, triethylamine (0.91 mmol) and diphenylphosphoryl azide (0.41 mmol). The resulting mixture was warmed to 50° C. for 2 h, then to 80° C. and 2-(1-methylpyrrolidin-2-yl)-ethanol (0.82 mmol) was added. After 2 h, the mixture was cooled RT, filtered and water was added. The mixture was purified by reverse phase preparative HPLC. The appropriate fractions were collected and concentrated. The residue was further purified by silica gel column chromatography eluting with 1% NH4OH, 5% methanol in dichloromethane to afford the title compound (17 mg, 20%). LC/MS; (M+H)+=510.3

Provenance & Evidence