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A mixture 3-[7-(4-fluoro-phenyl)-4-oxo-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl]-thiobenzamide (Example 149) (78 mg, 0.2 mmol) and ethyl 4-chloro-3-oxo-butanoate (164 mg, 1.0 mmol) in ethanol (4 mL) was heated at reflux for 24 h. The solution was cooled to 0° C. and stirred for 0.5 h. The crystals were isolated by filtration and subsequently suspended in 2-amino-ethanol (4 mL). The mixture was stirred at 70° C. for 4 h, cooled to 23° C., and partitioned between ethyl acetate and H2O. The organic layer was dried over Na2SO4 and evaporated in vacuum and the residue was triturated with ethyl acetate to give the title compound as light yellow solid (37 mg).

1. temperatureat reflux for 24 h
2. customThe crystals were isolated by filtration
3. stirringThe mixture was stirred at 70° C. for 4 h
4. temperaturecooled to 23° C.
5. custompartitioned between ethyl acetate and H2O
6. dry with materialThe organic layer was dried over Na2SO4
7. customevaporated in vacuum
8. customthe residue was triturated with ethyl acetate