Triethylamine → (4S)-6-Azaspiro[2.5]octan-4-ol hydrochloride

Participants

Reaction Steps

In analogy to the procedure described in example 6A, 2-{4-[(E)-3-(3,4-dichloro-phenyl)-acryloyl]-7-oxo-[1,4]diazepan-1-yl}-succinic acid 1-methyl ester (intermediate 7) with 1.5 eq. of Et3N (added before cooling) and 1.05 eq. of (S)-6-aza-spiro[2.5]octan-4-ol; hydrochloride (intermediate 2) gave, after purification on a SiO2-column (dichloromethane/Isopropanol 97.5:2.5-9:1 gradient), the titled compound in 33% yield as white foam. MS: 552.0 (MH+, 2Cl).

Provenance & Evidence