| 摘要 |
PURPOSE:To produce a condensed pyridine-based mevalonolactone intermediate exhibiting a reductase inhibitory effect and useful as an intermediate for synthesizing a medicine for improving hypercholesterolemia by reacting a specified condensed pyridine derivative with a base and subsequently condensing the resultant anion with a specified aldehyde compound. CONSTITUTION:A condensed pyridine derivative represented by formula I [X ring is a (substituted)phenyl or a 5- to 6-membered heteroaryl; R<1> and R<2> are each H, a 1 to 8C alkyl, a 3 to 7C cycloalkyl, a 1 to 3C alkoxy, etc.; R<3> is H, a 1 to 8C alkyl, a 2 to 6C alkenyl, etc.; Y is formula P<+>R<11>R<12>R<13>Hal<-> (R<11> to R<13> are each methyl, ethyl, phenyl, etc.; Hal is a halogen), etc.] is reacted with a base to produce its anion. The resultant anion is then condensed with an aldehyde compound expressed by formula II (R<9a> and R<9b> are each methoxymethyl, trimethysilyl, etc.; R<10> is methyl, ethyl, benzyl, etc.) or formula III, thus producing the objective condensed pyridine-based mevalonolactone intermediate represented by formula IV (Z is a group of formula V or VI) and useful as an intermediate for producing a medicine for improving hypercholesterolemia. |
