NOVEL BENZOYL GROUP-CONTAINING ACETYLENE COMPOUND AND ANTITUMOR AGENT CONTAINING THE SAME AS ACTIVE INGREDIENT

NOVEL BENZOYL GROUP-CONTAINING ACETYLENE COMPOUND AND ANTITUMOR AGENT CONTAINING THE SAME AS ACTIVE INGREDIENT

PURPOSE:To provide the novel compound excellent in antitumor activity and useful as an antitumor agent. CONSTITUTION:A compound of the formula I (R1 is 1-5C alkoxy; R2 is 1-5C alkoxy, OH, 1-5C acyloxy; R3 is H, 1-5C alkoxy; R5 is 1-8C nalkyl), e.g. 1-(3,4,5- trimethoxyphenyl)-2-octyne-1-one. The com...

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Bibliographische Detailangaben
Hauptverfasser: HORIUCHI FUMIKO, BANDOU KAZUNAMI, MORISHIGE HIDEAKI, KATO AKIHISA
Format: Patent
Sprache:eng
Schlagworte:
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
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
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Zusammenfassung:PURPOSE:To provide the novel compound excellent in antitumor activity and useful as an antitumor agent. CONSTITUTION:A compound of the formula I (R1 is 1-5C alkoxy; R2 is 1-5C alkoxy, OH, 1-5C acyloxy; R3 is H, 1-5C alkoxy; R5 is 1-8C nalkyl), e.g. 1-(3,4,5- trimethoxyphenyl)-2-octyne-1-one. The compound is obtained e.g. by dropping the THF solution of 1heptyne to the THF solution of n-butyl lithium, dropping the THF solution of 3,4,5-trimethoxybenzaldehyde of the formula II to the reaction solution to couple the benzaldehyde of the formula II with the 1- heptyne, and subsequently oxidizing the product with manganese dioxide in dichloromethane.