Acetic Acid → HCID 59134262, compound

Participants

Reaction Steps

0.3 ml (5.2 mmol) of acetic acid, 0.25 ml (3.33 mmol) of formaldehyde (37% in water) and 1.5 ml (1.5 mmol) of sodium cyanoborohydride (1M in THF) were added to a solution of 93 mg (0.142 mmol) of the amine from Example 40 in 7.5 ml of methanol. The reaction mixture was stirred at room temperature for 2 hours and concentrated in vacuo. The residue was diluted with 10 ml of DCM, basified with 7N—NH3 in methanol, filtered and concentrated. This residue was purified by preparative RP-HPLC. 50 mg of the desired compound were obtained. LC/MS (calculated, monoisotopic MW=669; measured value (M+H)=670)

Provenance & Evidence