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    • 1. 发明专利
    • PRODUCTION OF PYRIDINE DERIVATIVE
    • JP2000044566A
    • 2000-02-15
    • JP21994398
    • 1998-08-04
    • KURARAY CO
    • KIKUYAMA SHIGEKIASANUMA GOROMATSUDA HIDEKISHIONO MANZO
    • C07D491/048C07D471/04C07D495/04
    • PROBLEM TO BE SOLVED: To obtain the subject compound useful as an intermediate for antiviral medicines, etc., in a good yield by reacting a specific pyridine derivative with a specified ester compound in the presence of a base and subjecting the reaction product to a hydrolysis reaction and a decarboxylation reaction. SOLUTION: This method for producing a compound of formula IV (R5 is a group of the formula: -CHR1R2) comprises reacting 1 mole of a pyridine ester derivative of formula I [X is a (substituted) alkoxyl group or the like; A is O, N or a divalent organic group] with 1-3 moles of an ester compound of formula II [R1 and R2 are each H or a (substituted) hydrocarbon; R3 is a (substituted) hydrocarbon] preferably in the presence of 1-3 moles of a base in a solvent preferably in an amount of 0.5-100 pts.wt. based on the compound of formula I preferably at 10-150 deg.C, and subsequently hydrolyzing and decarboxylating the obtained pyridine β-ketoester derivative of formula III [R4 is a (substituted) hydrocarbon]. Water is preferably used in the hydrolysis reaction in an amount of
    • 10. 发明专利
    • PRODUCTION OF 2-ARALKYLOXYPYRIDINE DERIVATIVE
    • JP2000034281A
    • 2000-02-02
    • JP35117498
    • 1998-12-10
    • KURARAY CO
    • KUWAYAMA TOMOYAASANUMA GORO
    • C07D213/64B01J23/04C07B61/00C07D213/71
    • PROBLEM TO BE SOLVED: To obtain a 2-aralkyloxypyridine derivative that can be derived to hydroxypyridine useful as a synthetic intermediate for medicines and agrochemicals by hydrogenolysis with industrial advantage by reacting a specific sulfonyl-pyridine derivative with an aralkyl alcohol in the presence of a base. SOLUTION: 2-Sulfonylpyridine derivative represented by formula I [R1 is H, a (substituted) alkyl or the like; R2 and R3 are each H, a halogen or the like; R4 is H, an alkoxy group; R5 is a (substituted) alkyl or the like] is reacted with an aralkyl alcohol, preferably in an amount of 1-10 moles per mole of the pyridine derivative (for example, benzyl alcohol) in the presence of a base (preferably an alkali metal hydroxide or the like), in a preferred embodiment, in a solvent (for example, pentane or the like) in an amount of >=10-fold weight of the base, preferably at a temp. of 80-120 deg.C to give the objective compound of formula II [R6 is a (substituted) aralkyl]. A phase transfer catalyst may be added to the reaction system in an amount of 0.01-10 wt.% based on the base.