Preparation of pyrazine derivatives

C - Chemistry – Metallurgy – 07 – D

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260/268, 260/266

C07D 241/24 (2006.01) C07D 241/12 (2006.01) C07D 403/06 (2006.01) C07D 413/06 (2006.01)

Patent

CA 1205075

ABSTRACT OF THE DISCLOSURE A process for the preparation of a pyrazine derivative of the formula: Image I wherein R1 represents hydroxy, C1-C6 alkoxy, or a group of the formula NR2R3 in which R2 and R3 are independently a hydrogen atom or C1-C6 alkyl or, together with the nitrogen atom to which they are linked, form a saturated ring having five or six atoms which may contain one or more additional heteroatoms; which process comprises reacting a compound of the formula: Image II wherein R represents a hydrogen atom, C1-C6 alkyl, or C1-C6 alkoxy, Y represents a hydrogen atom or a sodium, lithium, or potassium ion, and A is a nitrile group or a substituent of the formula COR1 where R1 is as defined above either with pyruvic aldehyde oxime of the formula: Image III abstract continued or with a pyruvic aldehyde oxime acetal derivative of the formula: IV Image wherein R4 and R5 are independently a hydrogen atom or C1-C6 alkyl or may be linked together so that the compound of formula IV is a cyclic acetal; and, when A is a nitrile group, hydrolyzing the reaction product.

422766

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