Formaldehyde → HCID 131730999, compound

Participants

Reaction Steps

37.9 mg of 6-[(4-morpholinophenyl)amino]-4-[(pyrrolidin-2-ylmethyl)amino]pyridine-3-carboxyamide (the compound of Example 358) was dissolved in 2 mL of methylene chloride, to which, under ice cooling, 19.4 mg of 37% formaldehyde in water, 40.5 mg of sodium triacetoxyborohydride and acetic acid were sequentially added, and stirred at room temperature for 2 hours. To the reaction mixture, saturated sodium bicarbonate in water was added, extracted with chloroform:methanol=10:1, the extract washed with saturated saline, and dried on anhydrous sodium sulfate. The solvent was evaporated, and the residue was recrystallized from chloroform-ether to obtain 27.5 mg (70%) of the title compound as a light yellow crystalline powder.

Provenance & Evidence