Process for preparing 2-amino-4-(4-fluorophenyl)-6-alkylpyrimidine-5-carboxylate

用式(I)表示的化合物的制备方法，式中R是氢或通式为-SO#-[2]R#+[1]的基团，R#+[1]是C#-[1-6]烷基；R#+[2]是氢或C#-[1-6]烷基；R#+[3]是C#-[1-6]烷基；R#+[4]是C#-[1-6]烷基。在该方法的第一步中，式II所示的化合物(式中R#+[3]和R#+[4]具有上述的定义)在路易斯酸的存在下与4-氟苄腈反应，产生式III所示的化合物(式中R#+[3]和R#+[4]具有上述的定义)；在第二步中，得到的式III所示的化合物与式IV所示的化合物(式中R和R#+[2]具有上述的定义)反应，产生式I表示的最终产物。∴ A process for the p...

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Bibliographic Details
Main Author U. VEITH
Format Patent
LanguageChinese
English
Published 01.09.2004
Edition7
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
APPARATUS THEREFOR
CHEMISTRY
GENERAL METHODS OF ORGANIC CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:用式(I)表示的化合物的制备方法，式中R是氢或通式为-SO#-[2]R#+[1]的基团，R#+[1]是C#-[1-6]烷基；R#+[2]是氢或C#-[1-6]烷基；R#+[3]是C#-[1-6]烷基；R#+[4]是C#-[1-6]烷基。在该方法的第一步中，式II所示的化合物(式中R#+[3]和R#+[4]具有上述的定义)在路易斯酸的存在下与4-氟苄腈反应，产生式III所示的化合物(式中R#+[3]和R#+[4]具有上述的定义)；在第二步中，得到的式III所示的化合物与式IV所示的化合物(式中R和R#+[2]具有上述的定义)反应，产生式I表示的最终产物。∴ A process for the preparation of a 4-(4-flourophenyl)-6-alkyl-2-N-alkansulfonyl-N-alkylamino)pyrimidine-5-carboxylic acid ester of formula (Ib), in which R1, R2, R3 and R4 are identical or different and are each a C1-6-alkyl. A 2-[-1-amino-1-(4-flourophenyl)methylene]-4-alkyl-3-oxo-alkanoic acid ester of formula (IIIb), in which R3 and R4 have the above-mentioned meanings, is reacted with an N-cyano-N-alkylalkanesulfonamide, optionally isolated or prepares in situ, of formula (IVb), in which R1 and R2 have the above-mentioned meanings, to give the final product of formula (Ib).
Bibliography:Application Number: CN20008011676