Invention Application
US20030032842A1 Novel arylpropyl aldehyde derivatives, processes for producing the same, and methods of using the same 失效
新型芳基丙醛衍生物,其制备方法及其使用方法

Novel arylpropyl aldehyde derivatives, processes for producing the same, and methods of using the same
Abstract:
3-(3-Methyl-4-hydroxyphenyl)-3-methylbutyl aldehyde may be produced from 3-(3-methyl-4-hydroxyphenyl)-3-methylbutyric acid by converting the carboxyl group into a formyl group. N-nullN-null3-(3-methyl-4-hydroxyphenyl)-3-methylbutylnull-L-null-aspartylnull-L-phenylalanine 1-methyl ester, which is useful as a sweetener having a high potency of sweetness, can be easily and efficiently prepared on an industrial production from such an aldehyde derivative, via a reductive alkylation reaction with aspartame. Therefore, 3-(3-Methyl-4-hydroxyphenyl)-3-methylbutyl aldehyde is extremely excellent as an intermediate for the production of N-nullN-null3-(3-methyl-4-hydroxyphenyl)-3- methylbutylnull-L-null-aspartylnull-L-phenylalanine 1-methyl ester. The above butyric acid derivative is a novel compound, which can be easily produced by subjecting 3-(3-methyl-4-methoxyphenyl)-3-methylbutyric acid obtained by the reaction of 2-methoxytoluene with 3-methylcrotonic acid, to a reaction for converting a methoxy group into a hydroxyl group. The present invention further provides several novel compounds useful as a production intermediate, such as the above aldehyde derivative and the like.
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