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    • 5. 发明授权
    • Process for the preparation of pyrimidine compounds
    • 嘧啶化合物的制备方法
    • US08273878B2
    • 2012-09-25
    • US12404575
    • 2009-03-16
    • Lee NewtonMark Bailey
    • Lee NewtonMark Bailey
    • C07D239/02
    • C07D239/22C07C69/716C07D239/42C07D403/04
    • A process for the preparation of a compound of Formula (1) and intermediates useful therein are provided. The process comprises reacting a compound of formula R1—CO—CH2-E with a compound of formula R2—CHX1X2 in the presence of a compound of formula R3R4N—C(═NH)NH2 and a catalyst, thereby to form a dihydropyrimidine; and oxidizing the dihydropyrimidine to form the compound of Formula (I). R1 is H or an alkyl group; R2 is H, an alkyl or aryl group; R3 and R4 are each independently H, alkyl or aryl, or R3 and R4 are linked to form, together with the nitrogen to which they are attached to form a 5 to 7 membered heterocyclic ring; E is H, an unsubstituted alkyl group, an aryl group or an electron withdrawing group; and X1 and X2 are each independently leaving groups, or X1 and X2 together represent ═O.
    • 提供了制备式(1)化合物和其中有用的中间体的方法。 该方法包括在式R 3 R 4 N-C(= NH)NH 2)化合物和催化剂存在下使式R 1 -CO-CH 2 -E化合物与式R 2 -CHX 1 X 2化合物反应,从而形成二氢嘧啶; 并氧化二氢嘧啶以形成式(I)的化合物。 R1是H或烷基; R2是H,烷基或芳基; R 3和R 4各自独立地为H,烷基或芳基,或者R 3和R 4连接形成与它们所连接的氮一起形成5至7元杂环; E是H,未取代的烷基,芳基或吸电子基团; X1和X2各自独立地为离去基团,或者X1和X2一起表示= O。
    • 6. 发明申请
    • Process for the Preparation of Pyrimidine Compounds
    • 制备嘧啶化合物的方法
    • US20060052604A1
    • 2006-03-09
    • US10537723
    • 2003-12-09
    • Lee NewtonMark Bailey
    • Lee NewtonMark Bailey
    • C07D403/02C07D239/32
    • C07D239/22C07C69/716C07D239/42C07D403/04
    • A process for the preparation of a compound of Formula (I) and intermediates useful therein are provided. The process comprises reacting a compound of formula R1—CO—CH2-E with a compound of formula R2—CHX1X2 in the presence of a compound of formula R3R4N—C(═NH)NH2 and a catalyst, thereby to form a dihydropyrimidine; and oxidising the dihydropyrimidine to form the compound of Formula (1). R1 is H or an alkyl group; R2 is H, an alkyl or aryl group; R3 and R4 are each independently H, alkyl or aryl, or R3 and R4 are linked to form, together with the nitrogen to which they are attached to form a 5 to 7 membered heterocyclic ring; E is H, an unsubstituted alkyl group, and aryl group or an electron withdrawing group; and X1 and X2 are each independently leaving groups, or X1 and X2 together represent ═O.
    • 提供了制备式(I)化合物和其中有用的中间体的方法。 该方法包括使式R 1 -CO-CH 2 -E-E的化合物与式R 2的化合物反应, 1在式R 3的化合物的存在下,将N 2 O 2(NH)NH 2 和催化剂,从而形成二氢嘧啶; 并氧化二氢嘧啶以形成式(1)的化合物。 R 1是H或烷基; R 2是H,烷基或芳基; R 3和R 4各自独立地为H,烷基或芳基,或R 3和R 4连接 与它们所连接的氮一起形成5至7元杂环; E是H,未取代的烷基,芳基或吸电子基; 和X 1和X 2各自独立地为离去基团,或X 1和X 2一起代表 -
    • 7. 发明授权
    • Process for the preparation of pyrimidine compounds
    • 嘧啶化合物的制备方法
    • US07524955B2
    • 2009-04-28
    • US10537723
    • 2003-12-09
    • Lee NewtonMark Bailey
    • Lee NewtonMark Bailey
    • C07D239/02
    • C07D239/22C07C69/716C07D239/42C07D403/04
    • A process for the preparation of a compound of Formula (I) and intermediates useful therein are provided. The process comprises reacting a compound of formula R1—CO—CH2-E with a compound of formula R2—CHX1X2 in the presence of a compound of formula R3R4N—C(═NH)NH2 and a catalyst, thereby to form a dihydropyrimidine; and oxidising the dihydropyrimidine to form the compound of Formula (1). R1 is H or an alkyl group; R2 is H, an alkyl or aryl group; R3 and R4 are each independently H, alkyl or aryl, or R3 and R4 are linked to form, together with the nitrogen to which they are attached to form a 5 to 7 membered heterocyclic ring; E is H, an unsubstituted alkyl group, and aryl group or an electron withdrawing group; and X1 and X2 are each independently leaving groups, or X1 and X2 together represent ═O.
    • 提供了制备式(I)化合物和其中有用的中间体的方法。 该方法包括在式R3R4N-C(-NH)NH2化合物和催化剂存在下使式R 1 -CO-CH 2 -E化合物与式R 2 -CHX 1 X 2化合物反应,从而形成二氢嘧啶; 并氧化二氢嘧啶以形成式(1)的化合物。 R1是H或烷基; R2是H,烷基或芳基; R 3和R 4各自独立地为H,烷基或芳基,或者R 3和R 4连接形成与它们所连接的氮一起形成5至7元杂环; E是H,未取代的烷基,芳基或吸电子基; X1和X2各自独立地为离去基团,或者X1和X2一起表示-O。