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15 条记录 (耗时 0.016 秒)

    Process for preparing 5-vinyl-2-pyrrolidinone and intermediates therefor
    1.
    发明授权
    Process for preparing 5-vinyl-2-pyrrolidinone and intermediates therefor 失效
    制备5-乙烯基-2-吡咯烷酮的方法及其中间体

    公开(公告)号：US4621145A

    公开(公告)日：1986-11-04

    申请号：US556204

    申请日：1983-11-29

    申请人： Wolfgang Frieben ,  Fritz Gerhart

    发明人： Wolfgang Frieben ,  Fritz Gerhart

    IPC分类号： B01J23/44 ,  B01J23/00 ,  B01J27/053 ,  C07B61/00 ,  C07D207/26 ,  C07D207/263 ,  C07D207/267 ,  C07D207/28 ,  C07D207/36

    CPC分类号： C07D207/267 ,  C07D207/26 ,  C07D207/28

    摘要： 4-Amino-5-hexenoic acid is prepared by:(a) reacting 5-oxo-2-pyrrolidine-acetonitrile with hydrogen and dimethylamine in the presence of a palladium catalyst to form N,N-dimethyl-2-[5'-oxo-2'-pyrrolidine]ethylamine;(b) oxidizing N,N-dimethyl-2-[5'-oxo-2'-pyrrolidine]-ethylamine to produce the corresponding N-oxide derivative;(c) pyrolysis of the N-oxide derivative to form 5-vinyl-2-pyrrolidinone;(d) optionally, separating N,N-dimethyl-2-[5'-oxo-2'-pyrrolidine]ethylamine by-product from the 5-vinyl-2-pyrrolidinone product; and(e) hydrolyzing 5-vinyl-2-pyrrolidinone to form 4-amino-5-hexenoic acid.

    摘要翻译： 4-氨基-5-己烯酸通过以下步骤制备：（a）在钯催化剂存在下，使5-氧代-2-吡咯烷 - 乙腈与氢气和二甲基胺反应，形成N，N-二甲基-2- [5'- 氧代-2'-吡咯烷]乙胺; （b）氧化N，N-二甲基-2- [5'-氧代-2'-吡咯烷] - 乙胺，得到相应的N-氧化物衍生物; （c）N-氧化物衍生物的热解以形成5-乙烯基-2-吡咯烷酮; （d）任选地，从5-乙烯基-2-吡咯烷酮产物中分离N，N-二甲基-2- [5'-氧代-2'-吡咯烷]乙胺副产物; 和（e）水解5-乙烯基-2-吡咯烷酮以形成4-氨基-5-己烯酸。

    Fluorinated amino-butyric acid and diaminobutane derivatives
    3.
    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。

    Continuous large-scale production of ethyl 2,2-difluoro-4-pentenoate and 2-fluorinated methyl aminoacetonitriles by use of a flow reactor
    7.
    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。