反应详情

A mixture of (1R)-1′-{[1-(4-bromophenyl)cyclopropyl]carbonyl}-3H-spiro[2-benzofuran-1,3′-pyrrolidin]-3-one (68.0 mg, 0.000165 mol, example 238), pyrrolidine (42 μL, 0.00049 mol), molybdenum hexacarbonyl (44 mg, 0.00016 mol), trans-di(μ-acetato)bis[o-(di-o-tolylphosphino)benzyl]dipalladium (II) (16 mg, 0.000016 mol) and 1,8-diazabicyclo[5.4.0] undec-7-ene (76 μL, 0.00049 mol) (DBU) in anhydrous tetrahydrofuran (2.0 mL, 0.025 mol) in a microwave vial was irradiated with microwaves to 150° C. for 30 minutes. The reaction mixture was filtered. The filtrate was purified by prep-HPLC to afford the product as a solid (55.9 mg, 79% in yield). LC/MS (M+H+)=431.1.

1. customwas irradiated with microwaves to 150° C. for 30 minutes
2. filtrationThe reaction mixture was filtered
3. customThe filtrate was purified by prep-HPLC