Formaldehyde → HCID 86595610, compound

Participants

Reaction Steps

To a solution of the compound obtained in Step 1 (100 mg) in dichloromethane (1.5 mL) was added formaline (35%, 87.6 μl). To this suspension was added 0.05 ml of MeOH. Then, sodium triacetoxyborohydride (433 mg) was added, and the mixture was stirred for 12 hrs. To the mixture were added water and 1N NaOH to adjust pH of aquaous phase (ca. pH 8–9). The mixture was extracted with dichloromethane. The organic layer was dried with MgSO4 and concentrated under redused pressure. Resulting oil was purified by silica gel column chromatograph (mixed solvent of CH2Cl2/MeOH 15/1 as an eluent) to give tert-butyl {4-[2-(2-(acetylamino)-5-{[[3-(N,N-dimethylamino)-3-oxopropyl](methyl)amino]methyl}-1,3-thiazol-4-yl)ethyl]phenyl}carbamate as pale yellow oil (90.4 mg).

Provenance & Evidence