Glyoxylic acid, monohydrate → HCID 118093096, compound

Participants

Reaction Conditions

Reaction Steps

37D (309 mg, 0.518 mmol), Intermediate 1 (205 mg, 0.570 mmol), glyoxylic acid monohydrate (47.7 mg, 0.518 mmol) were dissolved in CH3CN (3 ml) and DMF (0.5 ml). The mixture was stirred at 85° C. 20 h, then concentrated and purified by prep HPLC. The desired fractions were combined, concentrated. The residue was dissolved in THF (8 mL). 10% Pd/C was added and the mixture was hydrogenated at 40 psi for 3 h. The mixture was filtered, concentrated and purified by prep HPLC to give 37E (185 mg, 0.222 mmol, 42.8% yield). MS (ESI) m/z: 834.4 (M+H)+.

Provenance & Evidence