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    Fluorinated diaminobutane derivatives
    1.
    发明授权
    Fluorinated diaminobutane derivatives 失效
    氟化二氨基丁烷衍生物

    公开(公告)号：US4435425A

    公开(公告)日：1984-03-06

    申请号：US373600

    申请日：1982-04-09

    申请人： Albert Sjoerdsma ,  Philippe Bey ,  Michel Jung ,  Fritz Gerhart ,  Daniel Schirlin

    发明人： Albert Sjoerdsma ,  Philippe Bey ,  Michel Jung ,  Fritz Gerhart ,  Daniel Schirlin

    IPC分类号： C07C57/52 ,  C07C57/76 ,  C07D209/48 ,  A61K31/13 ,  C07C87/22

    CPC分类号： C07D209/48 ,  C07C57/52 ,  C07C57/76 ,  Y10S514/811 ,  Y10S514/91 ,  Y10S514/916

    摘要： Fluorinated diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: ##STR1## wherein: R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl, or phenyl-(C.sub.1 -C.sub.4 alkyl);R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-(C.sub.1 -C.sub.4 alkyl), or R.sub.4, where R.sub.4 is as defined below;R.sub.3 represents hydrogen, or, except when R.sub.2 represents R.sub.4, R.sub.4, where R.sub.4 is as defined below;each R.sub.4, independently, represents C.sub.2 -C.sub.5 alkylcarbonyl, phenylcarbonyl, phenyl-(C.sub.1 -C.sub.4 alkyl) carbonyl, or an aminocarboxylic acid residue derived by removal of an hydroxy group from the carboxy moiety of an L-aminocarboxylic acid; andp represents 1 or 2,and pharmaceutically acceptable acid addition salts thereof.

    摘要翻译： PCT No.PCT / US81 / 01130 Sec。 371日期：1982年4月9日 102（e）日期1982年4月9日PCT PCT。1981年8月21日。体内氟化二氨基丁烷化合物是γ-氨基丁酸转氨酶的抑制剂，具有下式：其中：R1表示氢，C1-C6烷基 ，或苯基 - （C 1 -C 4烷基）; R 2表示氢，C 1 -C 6烷基，苯基 - （C 1 -C 4烷基）或R 4，其中R 4如下所定义; R 3表示氢，或者，当R 2表示R 4，R 4，其中R 4如下所定义; 每个R 4独立地表示C 2 -C 5烷基羰基，苯基羰基，苯基 - （C 1 -C 4烷基）羰基或通过从L-氨基羧酸的羧基部分除去羟基衍生的氨基羧酸残基; 和p代表1或2，及其药学上可接受的酸加成盐。

    Fluorinated amino-butyric acid and diaminobutane derivatives
    2.
    发明授权
    Fluorinated amino-butyric acid and diaminobutane derivatives 失效
    氟化氨基丁酸和二氨基丁烷衍生物

    公开(公告)号：US4418077A

    公开(公告)日：1983-11-29

    申请号：US295060

    申请日：1981-08-21

    申请人： Philippe Bey ,  Fritz Gerhart ,  Michel Jung ,  Daniel Schirlin

    发明人： Philippe Bey ,  Fritz Gerhart ,  Michel Jung ,  Daniel Schirlin

    IPC分类号： A61K31/13 ,  A61K31/135 ,  A61K31/16 ,  A61K31/165 ,  A61K31/195 ,  A61K31/22 ,  A61P25/00 ,  C07C211/15 ,  C07C229/20 ,  C07C233/36 ,  C07C233/47 ,  C07C237/06 ,  C07C271/22 ,  C07C273/10 ,  C07D209/48 ,  C07C87/22 ,  C07C87/28 ,  C07C101/24

    CPC分类号： C07D209/48 ,  C07C271/22

    摘要： Fluorinated aminobutyric acid and diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: ##STR1## wherein: Y represents hydrogen or fluorine;Z represents --CH.sub.2 NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2 are as defined below, or --COR.sub.3 where R.sub.3 is as defined below;R.sub.a represents hydrogen or R.sub.4, where R.sub.4 is as defined below;R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl-(C.sub.1 -C.sub.4 alkyl);R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-(C.sub.1 -C.sub.4 alkyl) or, when R.sub.a is hydrogen, R.sub.4, where R.sub.4 is as defined below;R.sub.3 represents hydroxy, or when R.sub.a is hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;each R.sub.4, independently, represents C.sub.2 -C.sub.5 alkylcarbonyl, phenylcarbonyl, phenyl-(C.sub.1 -C.sub.4 alkyl)-carbonyl, or an aminocarboxylic acid residue derived by removal of an hydroxy group from the carboxy moiety of an L-aminocarboxylic acid;R.sub.5 and R.sub.6, independently, represent hydrogen or C.sub.1 -C.sub.4 alkyl; andP represents 1 or 2.

    摘要翻译： 氟化氨基丁酸和二氨基丁烷化合物在体内是γ-氨基丁酸转氨酶的抑制剂，具有下式：其中：Y代表氢或氟; Z表示-CH2NR1R2，其中R1和R2如下所定义，或-COR 3，其中R3如下所定义; R a表示氢或R 4，其中R 4如下所定义; R1代表氢，C1-C6烷基或苯基 - （C1-C4烷基）; R 2表示氢，C 1 -C 6烷基，苯基 - （C 1 -C 4烷基）或当R a是氢时，R 4，其中R 4如下所定义; R3表示羟基，或当R a为氢时，C 1 -C 8烷氧基，-NR 5 R 6（其中R 5和R 6如下所定义）或通过从L-氨基羧酸的氨基部分除去氢原子得到的氨基羧酸残基; 每个R 4独立地表示C 2 -C 5烷基羰基，苯基羰基，苯基 - （C 1 -C 4烷基） - 羰基或通过从L-氨基羧酸的羧基部分除去羟基而衍生的氨基羧酸残基; R5和R6独立地表示氢或C1-C4烷基; P表示1或2。

    Fluorinated pentene diamine derivatives
    3.
    发明授权
    Fluorinated pentene diamine derivatives 失效
    氟化戊烯二胺衍生物

    公开(公告)号：US4439619A

    公开(公告)日：1984-03-27

    申请号：US295152

    申请日：1981-08-21

    申请人： Philippe Bey ,  Fritz Gerhart ,  Michel Jung

    发明人： Philippe Bey ,  Fritz Gerhart ,  Michel Jung

    IPC分类号： A61K31/57 ,  C07C43/17 ,  C07C233/00 ,  C07C233/34 ,  C07C271/20 ,  C07D209/48 ,  C07D487/18 ,  C07J5/00 ,  C07C101/24 ,  C07C87/26

    CPC分类号： C07D209/48 ,  C07C255/00 ,  C07C271/20 ,  C07C43/17

    摘要： Fluorinated alkenylene diamine compounds are inhibitors of ornithine decarboxylase enzyme in vivo and have the following formula: ##STR1## wherein: R.sub.a represents hydrogen or R.sub.2, where R.sub.2 is as defined below;R.sub.b represents hydrogen or, when R.sub.a is hydrogen, R.sub.2, where R.sub.2 is as defined below;R.sub.c represents hydrogen or --COR.sub.3, where R.sub.3 is as defined below;R.sub.1 represents hydrogen or C.sub.1 --C.sub.6 alkyl;each R.sub.2, independently, represents C.sub.2 -C.sub.5 alkylcarbonyl, phenylcarbonyl, phenyl-(C.sub.1 -C.sub.4 alkyl) carbonyl, or an aminocarboxylic acid residue derived by removal of an hydroxy group from a carboxy moiety of an L-aminocarboxylic acid;R.sub.3 represents hydroxy, or, when R.sub.a and R.sub.b are both hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.4 R.sub.5, where R.sub.4 and R.sub.5 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;R.sub.4 and R.sub.5, independently, represent hydrogen or C.sub.1 -C.sub.4 alkyl; andp represents 1 or 2.

    摘要翻译： 氟化亚烯基二胺化合物是体内鸟氨酸脱羧酶的抑制剂，具有下式：其中：R a表示氢或R 2，其中R 2如下所定义; Rb表示氢，或当R a为氢时，R 2，其中R 2如下所定义; R c表示氢或-COR 3，其中R 3如下所定义; R1代表氢或C1-C6烷基; 每个R 2独立地表示C 2 -C 5烷基羰基，苯基羰基，苯基 - （C 1 -C 4烷基）羰基或通过从L-氨基羧酸的羧基部分除去羟基衍生的氨基羧酸残基; R3表示羟基，或者当R a和R b均为氢时，C 1 -C 8烷氧基，-NR 4 R 5（其中R 4和R 5如下所定义）或通过从L的氨基部分除去氢原子得到的氨基羧酸残基 - 氨基羧酸; R 4和R 5独立地表示氢或C 1 -C 4烷基; p表示1或2。

    Preparation of fluorinated methyl aminoalkanoic acids and novel process intermediates
    4.
    发明授权
    Preparation of fluorinated methyl aminoalkanoic acids and novel process intermediates 失效
    氟化甲基氨基链烷酸的制备和新工艺中间体

    公开(公告)号：US4353828A

    公开(公告)日：1982-10-12

    申请号：US170395

    申请日：1980-07-21

    申请人： Philippe Bey ,  Fritz Gerhart ,  Viviane Van Dorsselaer

    发明人： Philippe Bey ,  Fritz Gerhart ,  Viviane Van Dorsselaer

    IPC分类号： C07F3/02 ,  C07C87/26 ,  C07D209/48

    CPC分类号： C07F3/02 ,  Y02P20/55

    摘要： Fluorinated alkenylamines of the Formula V ##STR1## wherein n represents 0, 1, 2 or 3; R.sub.1 represents hydrogen or C.sub.1 -C.sub.10 alkyl and Y represents (a), when n represents O, CH.sub.2 F, (b), when n represents 1, CH.sub.2 F or CHF.sub.2, or (c) when n represents 2 or 3, CH.sub.2 F, CHF.sub.2 or CF.sub.3 are novel process intermediates. They are obtained by hydrolysis and subsequent reduction of the corresponding alkenyl fluorinated methyl ketimine magnesium halides, which are novel compounds resulting from reaction of the corresponding alkenyl magnesium halides with the corresponding fluorinated acetonitriles. The fluorinated alkenylamines of Formula V are oxidized while the amino group is protected to provide, after removal of the amine protecting group, the corresponding fluorinated methyl aminoalkanoic acids which are useful pharmacological or anti-bacterial agents.

    摘要翻译： 式V的氟化烯基胺其中n表示0,1,2或3; R1表示氢或C1-C10烷基，Y表示（a），当n表示O，CH2F，（b）时，当n表示1时，CH2F或CHF2，或（c）当n表示2或3时，CH2F，CHF2或 CF3是新型工艺中间体。 它们通过水解和随后还原相应的烯基氟代甲基酮亚胺卤化镁得到，其是由相应的烯基卤化镁与相应的氟化乙腈反应得到的新化合物。 式V的氟化链烯基胺被氧化，同时保护氨基以除去胺保护基之后提供相应的氟化甲基氨基链烷酸，其是有用的药理学或抗菌剂。

    Continuous large-scale production of ethyl 2,2-difluoro-4-pentenoate and 2-fluorinated methyl aminoacetonitriles by use of a flow reactor
    10.
    发明授权
    Continuous large-scale production of ethyl 2,2-difluoro-4-pentenoate and 2-fluorinated methyl aminoacetonitriles by use of a flow reactor 失效
    通过使用流动反应器连续大规模生产2,2-二氟-4-戊烯酸乙酯和2-氟化甲基氨基乙腈

    公开(公告)号：US4847401A

    公开(公告)日：1989-07-11

    申请号：US145694

    申请日：1988-01-15

    申请人： Fritz Gerhart ,  Michael Kolb

    发明人： Fritz Gerhart ,  Michael Kolb

    IPC分类号： B01J19/00 ,  B01J19/18

    CPC分类号： B01J19/0013 ,  B01J19/18 ,  B01J2219/00058

    摘要： The large scale preparation of ethyl 2,2-difluoro-4- pentenoate and 2-fluorinated methyl aminoacetonitriles by reaction of 2-H-perfluoroethyl allyl ether and n-butyl lithium and fluoromethylacetonitrile and a Grignard reagent, respectively, is largly unsuccessful because of side reactions which convert intermediate products and reactants to undesired products. Applicants have overcome these problems by performing the reactions with cooling in a continuous manner in a flow reactor with short residence time.

    摘要翻译： 通过2-H-全氟乙基烯丙基醚和正丁基锂和氟甲基乙腈和格氏试剂的反应分别大规模制备2,2-二氟-4-戊烯酸乙酯和2-氟化甲基氨基乙腈，这是因为 将中间产物和反应物转化为不期望的产物的副反应。 申请人通过在具有短停留时间的流动反应器中连续冷却进行反应来克服这些问题。