PURPOSE: To obtain the subject high-purity compounds useful as a synthetic intermediate for producing bisisoquinoline alkaloids in high yield by reacting an enamide in the presence of a radical former and tri-n-butylstannane in a solvent.
CONSTITUTION: For example, an enamide expressed by formula I (R1 and R2 are H, lower alkyl, halogen or alkoxy; R3 is H, alkyl or alkoxy; n is 1 or 2) is stirred in the presence of a radical former (preferably 2,2,- azobisisobutyronitrile) in an amount of 2-20mol% based on the compound expressed by formula I and tri-n-butylstannane in a molar amount of 1-4 times based on the compound expressed by formula I in a solvent (preferably toluene, etc.) in an inert atmosphere by heating at 80-140°C to afford the objective compounds expressed by formula II. Compounds expressed by formula IV are obtained from a compound expressed by formula III by carrying out similar reaction.
| JP6479913 | IRE-1α inhibitor |
| WO/2001/010835 | ANTIBACTERIAL AGENTS |
| WO/2022/253645 | MICROBIOCIDAL TETRAHYDROISOQUINOLINE DERIVATIVES |
SUZUKI MASATO
OGASAWARA KUNIRO
