ALPHA,BETA-DIARYLACRYLONITRILE DERIVATIVE AND ITS USE

• Main Authors: YAMADA AKIO, HASHIMOTO KOICHI, MORI SHIGEHIRO, HAMANO KOICHI, MORIUCHI NAOKO
• Format: Patent
• Language: English
• Published: 28.02.1995
• Edition: 6
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PURPOSE:To obtain a low toxic new compound having low side effects, strongly inhibiting 1,2-lipoxygenase activity in high selectivity, thus useful for preventing and treating circulatory diseases such as arteriosclerosis and for preventing metastasis of Lewis lung carcinoma, etc. CONSTITUTION:The objective compound of formula [R is H or OH; R and R are each H, cyano, however, being different from each other; Ar is formula II or III (X is O or S)], e.g. a compound of formula IV. The compound of formula I can be obtained, for example, by reaction of a 3,4-dihydroxybenzaldehyde or 3,4,5,-trihydroxybenzaldehyde of formula V (R is H or OH) with an aryl acetonitrile of the formula ArCH2CN such as thianaphthene-3-acetonitrile in ethanol in the presence of piperidine under heating and refluxing.