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10 条记录 (耗时 0.011 秒)

    Optically active 1,4-benzodiazepines and process for the preparation thereof
    3.
    发明授权
    Optically active 1,4-benzodiazepines and process for the preparation thereof 失效
    光学活性的1,4-苯并嗪及其制备方法

    公开(公告)号：US3998811A

    公开(公告)日：1976-12-21

    申请号：US493145

    申请日：1974-07-30

    申请人： Franjo Kajfez ,  Nikola Blazevic ,  Vitomir Sunjic

    发明人： Franjo Kajfez ,  Nikola Blazevic ,  Vitomir Sunjic

    IPC分类号： C07D243/24 ,  C07D243/28

    CPC分类号： C07D243/24 ,  C07D243/28

    摘要： Optically active compounds having the formula ##STR1## having an asymmetric carbon atom in position 3 having the S configuration and wherein R.sub.1 is selected from the class consisting of hydrogen, halogen, nitro, and trifluoromethyl groups, R.sub.2 is selected from the group consisting of hydrogen and C.sub.1-4 lower alkyl groups and R.sub.3 is selected from the group consisting of C.sub.1-4 lower alkyl, hydroxy C.sub.1-4 lower alkyl, phenyl, hydroxy phenyl, benzyl, hydroxy benzyl, and 3'-methyleneindolyl groups.They are obtained by reaction of a compound having the formula ##STR2## with a compound of the formula wherein A is a protective group.The compounds of formula I have sedative and tranquilizing properties.

    Piperazine derivatives
    4.
    发明授权
    Piperazine derivatives 失效
    哌嗪衍生物

    公开(公告)号：US3996222A

    公开(公告)日：1976-12-07

    申请号：US459682

    申请日：1974-04-10

    申请人： Franjo Kajfez ,  Vesna Sunjic ,  Vitomir Sunjic

    发明人： Franjo Kajfez ,  Vesna Sunjic ,  Vitomir Sunjic

    IPC分类号： C07D498/10

    CPC分类号： C07D498/10

    摘要： A process for the production of piperazine derivatives including the formation of compounds having the general formula ##STR1## wherein Y is a halogen atom, SO.sub.3 H.sup.-, SO.sub.4.sup.-.sup.- or another anion. The compounds exhibit cytostatic, cancer retardant and tranquilizing properties.

    摘要翻译： 一种制备哌嗪衍生物的方法，包括形成具有通式“IMAGE”的化合物，其中Y是卤素原子，SO 3 H - ，SO 4 - 或另一种阴离子。 这些化合物显示出细胞抑制，癌症阻滞和镇静作用。

    Optically active 1,4-benzodiazepines and process for use as a tranquilizer
    6.
    发明授权
    Optically active 1,4-benzodiazepines and process for use as a tranquilizer 失效
    光学活性1,4-苯并二氮杂和用作镇定剂的方法

    公开(公告)号：US4045569A

    公开(公告)日：1977-08-30

    申请号：US709858

    申请日：1976-07-29

    申请人： Franjo Kajfez ,  Nikola Blazevic ,  Vitomir Sunjic

    发明人： Franjo Kajfez ,  Nikola Blazevic ,  Vitomir Sunjic

    IPC分类号： C07D243/24 ,  C07K1/00 ,  A61K31/33 ,  A61K31/40

    CPC分类号： C07D243/24 ,  C07D243/28 ,  C07K1/006

    摘要： Compositions, useful as tranquilizers containing, as active ingredient, an optically active compound having the formula: ##STR1## having an asymmetric carbon atom in position 3 having the S configuration and wherein R.sub.1 is selected from the group consisting of hydrogen, halogen, nitro, and trifluoromethyl groups, R.sub.2 is selected from the group consisting of hydrogen and C.sub.1-4 lower alkyl groups and R.sub.3 is selected from the group consisting of C.sub.1-4 lower alkyl, hydroxy C.sub.1-4 lower alkyl, phenyl, hydroxyphenyl, benzyl, hydroxybenzyl, and 3'-methyleneindolyl groups, is described.They are obtained by reaction of a compound having the formula ##STR2## with a compound of the formula wherein A is a protective group.The compounds of formula I have sedative and tranquilizing properties.

    摘要翻译： 作为镇静剂的组合物，其作为活性成分含有具有下式的光学活性化合物：具有S构型的位置3中的不对称碳原子，其中R 1选自氢，卤素，硝基 和三氟甲基，R 2选自氢和C 1-4低级烷基，R 3选自C 1-4低级烷基，羟基C 1-4低级烷基，苯基，羟基苯基，苄基，羟基苄基 和3'-亚甲基吲哚基。

    Preparation of chiral 1,4-benzodiazepin-2-one-derivatives by reaction of (s)-.alpha.-amino acid chloride hydrochlorides etc.
    7.
    发明授权
    Preparation of chiral 1,4-benzodiazepin-2-one-derivatives by reaction of (s)-.alpha.-amino acid chloride hydrochlorides etc. 失效
    通过（s） - {60-氨基酰氯盐酸盐等的反应制备手性1,4-苯并二氮杂-2-酮衍生物

    公开(公告)号：US4010153A

    公开(公告)日：1977-03-01

    申请号：US492912

    申请日：1974-07-29

    申请人： Franjo Kajfez ,  Vitomir Sunjic

    发明人： Franjo Kajfez ,  Vitomir Sunjic

    IPC分类号： C07D243/14 ,  C07D243/16 ,  C07D243/18 ,  C07D243/24 ,  C07D243/28 ,  C07D403/06

    CPC分类号： C07D243/24 ,  C07D243/28 ,  Y02P20/55 ,  Y10S514/906

    摘要： A process is disclosed for preparing optically active 1,4-diazepine-2-ones by reacting an acid chloride-hydrochloride of an optically active .alpha.-amino acid with a substituted o-amino benzophenone, to form an intermediate product and subsequently cyclizing the intermediate product to form the desired 1,4-diazepine-2-one. The process is carried out in inert organic or aqueous-organic solvents. The process eliminates the need for using .alpha.-amino acids having bound to the amino group a protective group which must be removed before cyclization.

    摘要翻译： 公开了通过使光学活性α-氨基酸的酰氯盐酸盐与取代的邻氨基二苯甲酮反应制备光学活性1,4-二氮杂-2-酮的方法，以形成中间产物，随后环化中间体 产物形成所需的1,4-二氮杂-2-酮。 该方法在惰性有机溶剂或含水有机溶剂中进行。 该方法消除了使用与氨基结合的α-氨基酸需要在环化之前必须除去的保护基团。

    Optically active 1,4-benzodiazepines intermediates
    10.
    发明授权
    Optically active 1,4-benzodiazepines intermediates 失效
    光活性1,4-苯并二氮杂类中间体

    公开(公告)号：US4087614A

    公开(公告)日：1978-05-02

    申请号：US709859

    申请日：1976-07-29

    申请人： Franjo Kajfez ,  Nikola Blazevic ,  Vitomir Sunjic

    发明人： Franjo Kajfez ,  Nikola Blazevic ,  Vitomir Sunjic

    IPC分类号： C07D243/24 ,  C07K1/00 ,  C07C125/06 ,  C07D209/20

    CPC分类号： C07D243/24 ,  C07D243/28 ,  C07K1/006 ,  Y02P20/55

    摘要： Optically active intermediates of the formula: ##STR1## in the S optical configuration wherein R.sub.1 is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl, R.sub.2 is selected from the group consisting of hydrogen and C.sub.1-4 lower alkyl, and R.sub.3 is selected from the group consisting of C.sub.1-4 lower alkyl, hydroxy C.sub.1-4 lower alkyl, phenyl, hydroxyphenyl, benzyl, hydroxybenzyl, or 3'-methyleneindolyl, and A is a protective group, and their preparation is described. These compounds are useful in the preparation of corresponding optically active 1,4-benzodiazepines.

    摘要翻译： 下式的光学活性中间体：其中R 1选自氢，卤素，硝基和三氟甲基的S光学构型，R2选自氢和C 1-4低级烷基，和 R3选自C1-4低级烷基，羟基C1-4低级烷基，苯基，羟基苯基，苄基，羟基苄基或3'-亚甲基吲哚基，A为保护基，并描述其制备方法。 这些化合物可用于制备相应的光学活性1,4-苯并二氮杂。