NEW INTERMEDIATE FOR PRODUCING ENEYNE DERIVATIVE AND ITS PRODUCTION

PROBLEM TO BE SOLVED: To obtain a new compound useful as an intermediate for producing eneyne derivatives having strong inhibiting activities against the squalene epoxidases of fungi or mammalian and capable of being used as antifungal agents or anti-cholesterol agents. SOLUTION: A compound of formu...

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Hauptverfasser: AZEYANAGI SATORU, ASAI HIKARI, TANAKA YOSHIHARU, NAKAGAWA SUSUMU, ISHIHARA MAKOTO
Format: Patent
Sprache:eng
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Zusammenfassung:PROBLEM TO BE SOLVED: To obtain a new compound useful as an intermediate for producing eneyne derivatives having strong inhibiting activities against the squalene epoxidases of fungi or mammalian and capable of being used as antifungal agents or anti-cholesterol agents. SOLUTION: A compound of formula I [R14 is H or a lower alkyl; R25 is a group of formula II (R3 is H or a lower alkyl; R4 and R5 are each H, a halogen, hydroxyl group or the like) or the like; Wa is Cl or Br], for example, a compound of formula III. The compound of formula I is obtained, for example, by reacting a compound of formula IV (Z is a releasing group) with an amine compound of formula V, if necessary, in the presence of a base. The compound of formula I can be derived into an eneyne derivative by coupling the compound of formula I with a specific substituted acetylene derivative and subsequently N-alkylating the product.