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-chloro-phenyl)-acryloyl]-7-oxo-[1,4]diazepan-1-yl}-succinic acid 1-methyl ester (intermediate 8) with 1.1 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/MeOH 98:2-95:5), the titled compound in 76% yield as white foam. MS: 518.3 (MH+, 1Cl).

Provenance & Evidence