NOVEL 4H-1-BENZOPYRAN-4-ON DERIVATIVE

NEW MATERIAL: A compound of formula I (R1 is H, a 1-6C alkyl, a 3-6C cycloalkyl, etc.; R2 is H, a 1-6C alkyl, an aryl, etc.; R3 is H, a 1-4C alkyl, hydroxyl, etc.; R4 is H, hydroxyl, a 1-4C alkoxy, etc.; R5 is H, a 1-6C alkyl, a 3-6C cycloalkyl, etc.; (m) is 0-3; (n) is 0-2) and an acid-added salt t...

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Hauptverfasser: RAMUCHIYANDORA GANAPATEI NAIKU, RIHIARUTO HERUMUUTO RUTSUPU, HANSU HAARARUTO ZETORATSUEKU, BANSHI RARU, GEERUHARUTO DEIKUNAITE, IERUKU TSUETSUKU
Format: Patent
Sprache:eng
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Zusammenfassung:NEW MATERIAL: A compound of formula I (R1 is H, a 1-6C alkyl, a 3-6C cycloalkyl, etc.; R2 is H, a 1-6C alkyl, an aryl, etc.; R3 is H, a 1-4C alkyl, hydroxyl, etc.; R4 is H, hydroxyl, a 1-4C alkoxy, etc.; R5 is H, a 1-6C alkyl, a 3-6C cycloalkyl, etc.; (m) is 0-3; (n) is 0-2) and an acid-added salt thereof. EXAMPLE: (±)-cis-5,7-dihydroxy-2-(2-thienyl)-8-[4-(3-hydroxy-1-methyl)piperidinyl]-4 H-1-benzopyran-4-one. USE: Antitumor agent, inhibiting kinase or growth factor receptor tyrosine kinase for which oncogene codes. PREPARATION: A compound of formula II is reacted with an alkali metal and an alkyl ester to form the corresponding diketone of formula III, which, in turn, is cyclized by reaction with a mineral acid to obtain the objective compound of formula I.