Formaldehyde → Trifluoroacetic acid

Participants

Reaction Steps

A methanolic solution of 2-{[(4-fluorobenzyl)amino]carbonyl}-3-hydroxy-10,10-dimethyl-4-oxo-4,6,7,8,9,10-hexahydropyrimido[1,2-a][1,4]diazepin-9-ium trifluoroacetate (prepared as described in Example 9, Step 1-2) was treated with formaldehyde (1.5 eq.) and sodium cyanoborohydride (1.2 eq.). The mixture was stirred at room temperature 3 hours and then directly purified by RP HPLC (C18, 5 μM, H2O/MeCN with 1% of TFA as eluant) to give the title product as TFA salt, after lyophilization of the appropriate fractions.

Provenance & Evidence