Formaldehyde → HCID 23356529, compound

Participants

Reaction Conditions

Reaction Steps

3 g (22.7 mmol) of 1-methylpyrrolo[1,2-a]pyrazine prepared in Preparation Example 2 was dissolved in water (15 ml)/concentrated hydrochloric acid (35 ml) mixture while cooling with ice-water. The resulting solution was heated to 70° C.; and 60 ml of formalin was added dropwise thereto over 40 minutes. The resulting solution was stirred at 75° C. for 30 minutes, cooled to 0° C. and then neutralized to pH8.0 with sodium hydroxide and sodium bicarbonate. The reaction mixture was extracted with ethyl acetate (100 ml×3), dried over MgSO4 and then concentrated. The residue was chromatographed over silica gel to obtain 1.8 g of title compound (yield: 48.9%).

Provenance & Evidence