反应详情

Prepare the corresponding ketone (2-methyl-9,10-dihydro-1-oxa-3-aza-benzo[f]azulen-4-one) as described by E. E. Galantay, et al, J. Med. Chem. (17) 1316-1327 (1974) and convert to the corresponding Z-isomer of the vinyl bromide using procedures essentially as described in Preparations 23 and 24. Then, following procedures essentially as described in Example 219, combine the ketone with 3-hydroxyphenyl boronic acid (207 mg, 1.5 mmmol). Purify the crude product using column chromatography (15% EtOAc/hexane to 30% EtOAc/hexane) to give 26 mg title compound, MS (ES) 304 (M+1). HPLC shows 93% purity at t=2.48 min.

1. customPurify the crude product