METHOD OF MANUFACTURING 2-METHYLENE LACTAM

摘要

PROBLEM TO BE SOLVED: To obtain a nitrogen-containing heterocyclic compound useful as a synthetic intermediate for medicines and agricultural chemicals, and also an optically active heterocyclic compound important for revealing the pharmacological activity of medicines and agricultural chemicals. SOLUTION: In the manufacturing method, an alkynylamine (I) is reacted with an R3R4R5SnH (II) and CO to obtain 2-stannylmethylene lactam (III), then the lactam (III) is reacted with R7R8R9SiX (IV) to obtain 2-methylene lactam (V). In the formulae (I), (II), and (III), R1means a lower aliphatic hydrocarbon group or an aromatic hydrocarbon group; R2means a hydrogen atom, a lower aliphatic hydrocarbon group, or an aromatic hydrocarbon group; R3, R4, R5, R7, R8, and R9mean each a lower aliphatic hydrocarbon group or an aromatic hydrocarbon group; R6is a hydrogen atom, a lower aliphatic hydrocarbon group or an aromatic hydrocarbon group; n means 1, 2, or 3; and X means a halogen atom. The lower aliphatic hydrocarbon group or the aromatic hydrocarbon group may have a substitution group. COPYRIGHT: (C)2006,JPO&NCIPI