Process for the preparation of propargyl amines
    14.
    发明授权
    Process for the preparation of propargyl amines 失效
    炔丙胺的制备方法

    公开(公告)号:US4564706A

    公开(公告)日:1986-01-14

    申请号:US514149

    申请日:1983-07-14

    CPC分类号: C07C209/08

    摘要: The invention relates to a new process for the preparation of propargyl ammonium chlorides of the Formula I ##STR1## by alkaline decomposition of the d-tartarate of the 1-isomer of an amine of the Formula II ##STR2## and subsequent reaction of the amine of the Formula II with a halide of the Formula IIIX--CH.sub.2 --C.tbd.CH (III)in the presence of an organic solvent, alkali and waterin which in Formulae II and III respectively,n is 1 or 0 andX stands for halogenwhich comprises reacting the d-tartarate of the 1-isomer of an amine of the Formula II in aqueous suspension with an alkali, dissolving the base of the Formula II, thus set free without isolation in a water non-miscible organic solvent and reacting the same in the said phase with a halide of the Formula III, and thereafter--preferably after separating the aqueous layer--reacting the mixture which contains the amines of the Formulae II and IV ##STR3## in the organic phase in the presence of water with an organic acid or a solution which has a pH value of 1.5-6 and consists of an inorganic acid and water, thus dissolving in the two-phase mixture formed the salt of the amine of the Formula II in the aqueous layer and selectively separating the amine of the Formula II from the amine of the Formula IV, and thereafter adding after the separation of the phases hydrogen chloride to the amine of the Formula IV being in the organic phase and thus precipitating the salt of the Formula I.The compounds of Formula I are known pharmaceutical active ingredients. The advantage of the process of the present invention that it is highly economical and enables the recovery of the starting materials on large scale production too.

    摘要翻译: 本发明涉及通过碱式分解通式II(XIIX)的胺的1-异构体的d-酒石酸来制备式I的炔丙基氯化铵的新方法(I) 和随后的式II的胺与式III的X-CH 2 -C 3 CH 3(III)的卤化物在有机溶剂,碱和水的存在下分别反应,其中式II和III分别为n为1 或0和X表示卤素,其包括使式II的胺的1-异构体在水悬浮液中与碱反应,溶解式II的碱,因此在不分离的情况下在水中非游离 在所述相中与其反应,与式III的卤化物反应,然后优选在将含有式II和IV的胺的混合物(IV)的水层分离成 在有机酸存在下的有机相 或pH值为1.5-6且由无机酸和水组成的溶液,因此溶解在两相混合物中形成水性层中式II的胺的盐,并选择性地分离 式II的式II化合物,然后在将相氯化氢分离为式IV的胺之后加入有机相,由此沉淀式I的盐。式I的化合物是已知的 药用活性成分。 本发明方法的优点是高度经济且能够在大规模生产中回收原料。

    Combined compositions
    16.
    发明授权
    Combined compositions 失效
    组合成分

    公开(公告)号:US5424327A

    公开(公告)日:1995-06-13

    申请号:US303712

    申请日:1994-09-09

    CPC分类号: A01N53/00

    摘要: The invention relates to novel combined compositions for combatting plant, animal and sanitarian as well as forestry, horticultural and warehouse pests. These compositions contain a pyrethroid-type insecticide as an insecticidally active ingredient and at least one fungicide inhibiting the ergosterol biosynthesis as activity-strengthening agent as well as optionally piperonylbutoxide and other additives.The advantages of the compositions according to the invention consist therein that the activity-strengthening substances used are fungicidal agents widely used and have an advantageous toxicology. The activity-strengthening agent exerts a synergistic effect together with the pyrethroid-type insecticide.The combinations according to the invention bear an outstanding importance in the protection of stored crops.

    摘要翻译: 本发明涉及用于对抗植物,动物和卫生以及林业,园艺和仓库害虫的新型组合组合物。 这些组合物含有拟除虫菊酯型杀虫剂作为杀虫活性成分和至少一种抑制麦角甾醇生物合成作为活性增强剂以及任选的胡椒基丁醚和其它添加剂的杀真菌剂。 根据本发明的组合物的优点在于其中使用的活性增强物质是广泛使用的杀真菌剂并且具有有利的毒理学。 活性增强剂与拟除虫菊酯类杀虫剂一起发挥协同作用。 根据本发明的组合在保护作物方面具有突出的重要性。

    Chemical process for the preparation of pharmaceutically active compounds
    19.
    发明授权
    Chemical process for the preparation of pharmaceutically active compounds 失效
    用于制备药物活性化合物的化学方法

    公开(公告)号:US5023337A

    公开(公告)日:1991-06-11

    申请号:US469749

    申请日:1990-01-19

    IPC分类号: C07D235/32

    CPC分类号: C07D235/32

    摘要: The present invention is directed to the preparation of benzimidazole derivatives of the formula (I), ##STR1## wherein A=stands for S, SO or SO.sub.2,R.sup.1 =stands for C.sub.1-4 alkyl group,R.sup.2 =stands for C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl or C.sub.6-10 aryl or aralkyl,comprising reacting a sulphochloride of the formula (II) ##STR2## with an alkyl aluminum compound of the formula (III).R.sub.n.sup.2 AlClhd (3-n) (III)The reaction is performed in one step.

    摘要翻译: 本发明涉及制备式(I)的苯并咪唑衍生物,其中A = S,SO或SO 2,R 1 = C 1-4烷基,R 2代表C 1 1-4烷基,C 3-7环烷基或C 6-10芳基或芳烷基,其包括使式(II)的二氯化亚氨基与式(III)的烷基铝化合物反应。 Rn2AlClhd(3-n)(III)反应在一个步骤中进行。