Potassium Carbonate → 9-tert-butyl-2,13-di-(pyridin3-yl)-3-methoxy-5,6,9,10,11,12-hexahydro-8H-azepino[4',3':4,5]pyrrolo[2,1-a]isoquinolin-8-one

Participants

Reaction Conditions

Reaction Steps

A mixture of 45 mg of 13d, 20 mg of pyridine-3-boronic acid, 30 mg of K2CO3 and 10 mg of Pd(PPh3)4 in 2 ml of degassed dimethoxyethane was heated at 90° C., for 16 hr. The reaction mixture was cooled, diluted with water and the product was extracted with ethyl acetate. The extract was washed once with 2N KOH and once with water, dried and concentrated. The residue was purified by chromatography over silica gel, using a gradient of toluene/acetone as eluent. The isolated product was triturated with diethyl ether, to provide 31 mg of 13e as white, crystalline material; Mp 310-312° C.

Provenance & Evidence