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    • 1. 发明授权
    • Process for the manufacture of dihydropyrimidines
    • 二氢嘧啶的制备方法
    • US5576432A
    • 1996-11-19
    • US363148
    • 1994-12-23
    • Roger LokAntony J. Williams
    • Roger LokAntony J. Williams
    • C07D498/04C07D513/04C07D517/04
    • C07D513/04
    • A process of preparing a dihydropyrimidine compound of the structure (I): ##STR1## wherein R.sup.1 and R.sup.2 are bonded together to form an aromatic or heterocyclic ring, which may be substituted or unsubstituted, or are individually selected from the group consisting of hydrogen, or a substituted or unsubstituted aliphatic, carbocyclic, or heterocyclic group;R.sup.3, R.sup.4 and R.sup.5 are individually selected from the group consisting of hydrogen or a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; andX represents the atoms necessary to form a 5 or 6 membered heterocyclic ring, and is selected from the group consisting of oxygen, sulfur, selenium, ##STR2## wherein R.sup.6, R.sup.7, and R.sup.8 are individually selected from the group consisting of a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; comprising combining a compound (A) of the structure: ##STR3## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are as previously defined, with a catalytic amount of a Group 11 or 12 metal cation catalyst at a temperature of less than about 50.degree. C. and in the presence of an organic solvent, to form compound (I).
    • 制备结构(I)的二氢嘧啶化合物的方法:其中R 1和R 2结合在一起以形成可被取代或未取代的芳族或杂环,或者分别选自氢, 或取代或未取代的脂族,碳环或杂环基团; R 3,R 4和R 5分别选自氢或取代或未取代的脂族,碳环或杂环基; X表示形成5或6元杂环所必需的原子,并且选自氧,硫,硒,其中R6,R7和R8分别选自取代的 或未取代的脂族,碳环或杂环基团; 包括将以下结构的化合物(A)与其中X,R 1,R 2,R 3,R 4,R 5,R 6,R 7和R 8如前所定义的化合物(A)与催化量的11或12族金属阳离子 催化剂在低于约50℃的温度下和在有机溶剂存在下反应形成化合物(I)。