DIBENZO[A, G]QUINOLIDINIUM DERIVATIVE HAVING CHOLESTEROL BIOSYNTHESIS INHIBITORY EFFECT

PROBLEM TO BE SOLVED: To obtain the subject new compound having almost no adverse effect and useful as a cholesterol biosynthesis inhibitory agent excellent in effectiveness. SOLUTION: This dibenzo[a, g]quinolidinium derivative is a compound of formula I [R1, R2 are each hydroxy, a 1-4C alkoxy or th...

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Hauptverfasser: TEI TAINO, KIM UI-DOK, KIN SHOGEN, KIN JUKO, BOKU JUNSHO, RI YUSEKI, HAKU YUKI
Format: Patent
Sprache:eng
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Zusammenfassung:PROBLEM TO BE SOLVED: To obtain the subject new compound having almost no adverse effect and useful as a cholesterol biosynthesis inhibitory agent excellent in effectiveness. SOLUTION: This dibenzo[a, g]quinolidinium derivative is a compound of formula I [R1, R2 are each hydroxy, a 1-4C alkoxy or the like; R3 is hydroxy or a 1-4C alkoxy; R4 is H, a 1-8C alkyl or the like; Z is a 5-12C alkyl, a 4-6C alkenyl, quinolinyl or a group of formula II (Z1 to Z5 are each H, a halogen, a 1-5C alkyl, trifluoromethyl, phenyl or the like; A, B are each C or N); X is an inorganic acid ion, an organic acid ion or a halide], for example, 5, 6- dihydro-2,-3-dimethoxybenzo[a]-9-dodecoxy-13-ethyl-10- methoxybenzo[g]quinolidinium chloride. The compound of the formula I is obtained by performing a de-blocking reaction of a compound of formula III to obtain a compound of formula IV, selectively O-alkylating to obtain a compound of formula V and reacting it with an alkyl-substituting compound of the formula: ZCH2-X.