PURPOSE: To obtain a benzoylacetylene derivative having a high activity as a specific inhibiting substance against a multiplication factor receptor, tyrosine kinase, and useful as a carcinostatic agent.
CONSTITUTION: A compound of formula I {R1, R5 are H, OR7 [R7 is H, a 1-6C alkyl capable of being substituted, COR8 (R8 is phenyl, a 1-5C alkyl capable of being substituted)], a halogen, a 1-5C alkyl capable of being substituted with a halogen, NR9R10 (R9, R10 are H, phenyl, a 1-5C alkyl capable of being substituted with phenyl, acetyl, etc.), CN, NO2, etc.; R6 is H, a 1-5C alkyl, group of formula VI (Y1-Y3 are H, phenyl, pyridyl, a 1-5C alkyl, a halogen), group of formula VII (Z1-Z3 are H, a 1-5C alkyl, a halogen), a 3-12C trialkylsilyl, COR12 (R12 is a 1-5C alkyl, phenyl, etc.), etc.} or its salt. This compound is obtained by reacting an acetylene derivative of formula III with an organic metal compound, a metal hydride, etc., reacting the obtained metal acetylide of formula IV with a benzaldehyde derivative of formula II, and subsequently oxidizing the obtained compound of formula V.
KITANO YASUNORI
INOKAWA HARUMOTO
SUZUKI TAKESHI
