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A suspension of 0.099 g (0.32 mmol) 4-(3-piperidin-1-yl-propyl)-[1,4]diazepan-5-one-dihydrochloride (intermediate 4B) and 0.077 g (0.38 mmol) of (E)-3-chloro-4-fluorocinnamic acid in 3 ml of CH2Cl2 was treated with 0.09 ml (0.64 mmol) of Et3N at RT, cooled (0° C.) and treated with a 0.085 g (0.41 mmol) of N,N′-dicyclohexylcarbodiimide. The reaction was warmed up over night to RT, then partitioned between EtOAc (×3)/saturated NaHCO3. The organic phases were washed with aqueous 10% NaCl, dried over Na2SO4 and evaporated to give after purification on catridges, Si-Amine, 70 ml, 20 g (EtOAc/n-heptane 9:1) 0.075 g (64%) of the title compound as a white solid. MS: 422.1 (MH+, Cl).

1. temperatureThe reaction was warmed up over night to RT
2. custompartitioned between EtOAc (×3)/saturated NaHCO3
3. washThe organic phases were washed with aqueous 10% NaCl
4. dry with materialdried over Na2SO4
5. customevaporated
6. customto give
7. customafter purification on catridges, Si-Amine, 70 ml, 20 g (EtOAc/n-heptane 9:1) 0.075 g (64%) of the title compound as a white solid