Isopropanol → HCID 46852601, compound

Participants

Reaction Steps

4-Nitrophenyl 3-[(4-cyclobutyl-1,4-diazepan-1-yl)carbonyl]azetidine-1-carboxylate (50 mg, 0.12 mmol), 1,2,3,4-tetrahydroisoquinoline (25 μl, 0.19 mmol) and DIPEA (42 μl, 0.24 mmol) were stirred in 1,2-dichloroethane (2 ml) and isopropanol (1 ml) at 120° C. in a sealed tube for 16 hrs. The mixture was then cooled to RT, diluted with dichloromethane (30 ml) and washed with 1M aq. K2CO3 (2×15 ml), dried (MgSO4), filtered and concentrated at reduced pressure. The residue was purified by silica FCC (eluting with 99:1:1 to 92:8:1 gradient of DCM/MeOH/2M NH3 in MeOH) to give the title compound (9 mg, 19% yield) as colourless oil.

Provenance & Evidence