PROCESS FOR THE PREPARATION OF METHYL 6-(2,4-DICHLOROPHENYL)-5-4-(3S)-1-(3-FLUOROPROPYL)PYRROLIDIN-3-YLOXYPHENYL-8,9-DIHYDRO-7H-BENZO7ANNULENE-2-CARBOXYLATE

摘要

Herein is provided a novel process for the preparation of methyl 6-(2,4-dichlorophenyl)- 5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2- carboxylate by a Suzuki coupling of compound (3), wherein LG represents a leaving group, with an organoboron reagent: (3). Compound (3) is obtained by activation of compound (4) with a leaving group LG, and compound (4) is obtained by alpha-arylation of methyl 5-oxo-6,7,8,9-tetrahydro-5H- benzo[7]annulene-2-carboxylate with 1-LG'-2,4-dichlorobenzene, wherein LG' represents a leaving group: (4).