Pyrrolidine → rac-(1-[(E)-3-(3,4-Dichloro-phenyl)-acryloyl]-4-[3-hydroxy-1-(pyrrolidine-1-carbonyl)-propyl]-[1,4]diazepan-5-one)

Participants

Reaction Steps

In analogy to the procedure described in example 3, treatment of (rac)-2-{4-[(E)-3-(3,4-dichloro-phenyl)-acryloyl]-7-oxo-[1,4]diazepan-1-yl}-4-hydroxy-butyric acid methyl ester (with 50% of the lactone, 1-[(E)-3-(3,4-dichloro-phenyl)-acryloyl]-4-(2-oxo-tetrahydro-furan-3-yl)-[1,4]diazepan-5-one) (intermediate 6) in EtOH with pyrrolidine over night at RT gave 88% of the titled compound as white foam. MS: 468.1 (MH+, 2Cl).

Provenance & Evidence