Process for preparing 2-carbamoyloxyalkyl-1,4-dihydropyridine derivatives
    22.
    发明授权
    Process for preparing 2-carbamoyloxyalkyl-1,4-dihydropyridine derivatives 失效
    2-氨基甲酰氧基烷基-1,4-二氢吡啶衍生物的制备方法

    公开(公告)号:US4958024A

    公开(公告)日:1990-09-18

    申请号:US230418

    申请日:1988-08-10

    IPC分类号: C07D211/90 C07D295/205

    CPC分类号: C07D295/205 C07D211/90

    摘要: A process for preparing a 2-carbamoylocxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloxyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.

    Certain intermediate 3-carbamoyloxyalkyl propiolic acid derivatives
    23.
    发明授权
    Certain intermediate 3-carbamoyloxyalkyl propiolic acid derivatives 失效
    某些中间体3-氨基甲酰氧基烷基丙炔酸衍生物

    公开(公告)号:US4914227A

    公开(公告)日:1990-04-03

    申请号:US863984

    申请日:1986-05-16

    IPC分类号: C07D211/90 C07D295/205

    CPC分类号: C07D295/205 C07D211/90

    摘要: A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloxyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.

    Process for producing halogenated heteroaryl compounds
    25.
    发明授权
    Process for producing halogenated heteroaryl compounds 失效
    卤化杂芳基化合物的制备方法

    公开(公告)号:US6114524A

    公开(公告)日:2000-09-05

    申请号:US319642

    申请日:1999-06-08

    摘要: The present invention relates to a process for producing a compound represented by the formula (II): ##STR1## wherein X is a halogen atom, each of A.sup.1, A.sup.2 and A.sup.3 are the same or different and are selected from a carbon atom or a nitrogen atom, provided that at least A.sup.1, A.sup.2, or A.sup.3 is a nitrogen atom. Each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are selected from a hydrogen atom, a lower alkyl group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a halogen atom, and a nitro group. It is also provided that where R.sup.1 and R.sup.2 are adjacent to each other, R.sup.1 and R.sup.2 may be combined with each other to form a 5- or 6-membered ring which may carry on the ring thereof one substituent selected from the group consisting of a lower alkyl group, a nitrile group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a halogen atom, a nitro group, and an amino-(lower alkyl) group. The compound is prepared by reacting a compound represented by the formula (I): ##STR2## with a quaternary ammonium halide in the presence of phosphorus pentoxide.

    摘要翻译: PCT No.PCT / JP97 / 04508 Sec。 371 1999年6月8日第 102(e)日期1999年6月8日PCT 1997年12月9日PCT公布。 第WO98 / 25906号公报 日期:1998年6月18日本发明涉及式(II)表示的化合物的制造方法:其中,X为卤素原子,A1,A2和A3各自相同或不同,选自碳原子数 或氮原子,条件是至少A1,A2或A3为氮原子。 R 1,R 2,R 3和R 4各自相同或不同,选自氢原子,低级烷基,氰基,羧基,低级烷氧基羰基,卤素原子和硝基。 还提供其中R 1和R 2彼此相邻,R 1和R 2可以彼此组合以形成5-或6-元环,其可以在其环上带有一个选自以下的取代基: 低级烷基,腈基,羧基,低级烷氧基羰基,氨基甲酰基,卤素原子,硝基和氨基 - (低级烷基)基。 该化合物通过在五氧化二磷存在下使式(I)表示的化合物与季铵卤化物反应来制备。