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19 条记录 (耗时 0.036 秒)

    Process for the preparation of 2,6-dihalo-para-trifluoromethylaniline
    1.
    发明授权
    Process for the preparation of 2,6-dihalo-para-trifluoromethylaniline 有权
    2,6-二卤代对 - 三氟甲基苯胺的制备方法

    公开(公告)号：US07553993B2

    公开(公告)日：2009-06-30

    申请号：US10532160

    申请日：2003-10-24

    申请人： Bernard Buathier ,  Pierre Le Roy

    发明人： Bernard Buathier ,  Pierre Le Roy

    IPC分类号： C07C209/74 ,  C07C211/00

    CPC分类号： C07C209/74 ,  C07C211/52

    摘要： Process for the preparation of a compound of general formula (I): in which X represents a halogen atom, by reaction of para-trifluoromethylaniline of formula (II): with a dihalogen X2, the two compounds being introduced simultaneously into a polar aprotic solvent in a dihalogen/compound (II) molar ratio ranging from 1.9 to 2.5 and at a temperature ranging from 100 to 300° C.

    摘要翻译： 制备通式（I）化合物的方法：其中X表示卤素原子，通过式（II）的对三氟甲基苯胺与二卤素X2反应，将两种化合物同时引入极性非质子溶剂 二卤化物（II）摩尔比为1.9-2.5，温度为100-300℃。

    Cephalosporin derivatives
    3.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号：US4365062A

    公开(公告)日：1982-12-21

    申请号：US152153

    申请日：1980-05-21

    申请人： Daniel Farge ,  Claude Moutonnier ,  Pierre Le Roy ,  Jean-Francois Peyronel

    发明人： Daniel Farge ,  Claude Moutonnier ,  Pierre Le Roy ,  Jean-Francois Peyronel

    IPC分类号： C07D501/04 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D253/075 ,  C07D257/04 ,  C07D317/28 ,  C07D501/00 ,  C07D501/06 ,  C07D501/14 ,  C07D501/20 ,  C07D501/24 ,  C07D501/26 ,  C07D501/60

    CPC分类号： C07D253/075 ,  C07D257/04 ,  C07D317/28 ,  C07D501/00 ,  C07D501/24

    摘要： New cephalosporins of the formula: ##STR1## in which n=0 or 1, R.sub.1 is a radical of the formula: ##STR2## [in which R.sub.4 is a protective radical and R.sub.5 is hydrogen, alkyl, vinyl, cyanomethyl or a protective radical], or R.sub.1 is a protective radical and R.sub.2 is a protective radical or an enzymatically removable radical, or R.sub.1 is an acyl radical which may be substituted in various ways and R.sub.2 is a protective radical, in the 3-oxoethyl-bicyclooct-2-ene or -bicyclooct-3-ene or 3-oxoethylidene-bicyclooctane form if n=0, and in the 3-oxoethyl-bicyclooct-2-ene or 3-oxoethylidene-bicyclooctane form if n=1, are useful as intermediates for the preparation of 3-thiovinyl-cephalosporins useful as antibacterial agents.

    摘要翻译： 式（I）的新型头孢菌素，其中n = 0或1，R1是下式的基团：其中R 4是保护基，R 5是氢，烷基，乙烯基 ，氰基甲基或保护基]，或R 1是保护基，R 2是保护基或可酶还原的基团，或者R 1是可以以各种方式被取代的酰基，R 2是保护基， 如果n = 0，则为3-氧代乙基 - 双环辛-2-烯或双环辛-3-烯或3-氧亚乙基 - 双环辛烷，如果n = 1，则为3-氧代乙基 - 双环辛-2-烯或3-氧亚乙基 - 双环辛烷， 可用作制备用作抗菌剂的3-硫代乙烯基 - 头孢菌素的中间体。

    3-Vinyl-cephalosporin derivatives
    4.
    发明授权
    3-Vinyl-cephalosporin derivatives 失效
    3-乙烯基 - 头孢菌素衍生物

    公开(公告)号：US4307233A

    公开(公告)日：1981-12-22

    申请号：US152085

    申请日：1980-05-21

    申请人： Daniel Farge ,  Claude Moutonnier ,  Pierre Le Roy ,  Jean-Francois Peyronel

    发明人： Daniel Farge ,  Claude Moutonnier ,  Pierre Le Roy ,  Jean-Francois Peyronel

    IPC分类号： A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P3/02 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/14 ,  C07D501/18 ,  C07D501/20 ,  C07D501/24 ,  C07D501/38 ,  C07D501/46 ,  C07D501/58 ,  C07D501/60

    CPC分类号： C07D501/14

    摘要： Novel 3-vinyl-cephalosporin derivates of the general formula ##STR1## in the bicyclooct-2-ene or bicyclooct-3-ene form, in which R.sub.1 is a protective radical or is a radical of the general formula ##STR2## in which R.sub.5 is hydrogen, alkyl, vinyl or cyanomethyl, or a protective radical, and R.sub.6 is hydrogen or a protective radical, and R.sub.2 is a protective radical or an enzymatically removable radical, or R.sub.1 is an acyl radical, which may carry various substituents, and R.sub.2 represents a protective radical, and R.sub.3 and R.sub.4, which are identical or different, represent alkyl (optionally substituted by hydroxyl, alkoxy, amino, alkylamino or dialkylamino) or phenyl, or form, together with the nitrogen atom, a saturated 5-membered or 6-membered heterocyclic ring optionally containing another hetero-atom, their E- and Z-forms and their mixtures, are useful as intermediates for the preparation of 3-thiovinyl cephalosporins useful as antibacterial agents.

    摘要翻译： 双环-2-烯或双环-3-烯形式的新颖的3-乙烯基 - 头孢菌素衍生物，其中R 1是保护基或是通式为“IMAGE”的基团， （II），其中R 5是氢，烷基，乙烯基或氰基甲基或保护基，R 6是氢或保护基，R 2是保护基或可酶解的基，或者R 1是酰基， 并且R 2表示保护基，R 3和R 4相同或不同，代表烷基（任选被羟基，烷氧基，氨基，烷基氨基或二烷基氨基）或苯基取代，或与氮原子一起形成， 任选地含有另一个杂原子的饱和5元或6元杂环，它们的E-和Z-形式及其混合物可用作制备用作抗菌剂的3-硫代乙烯基头孢菌素的中间体。

    3-Thiovinyl-cephalosporins
    5.
    发明授权
    3-Thiovinyl-cephalosporins 失效
    3-硫代乙烯基头孢菌素

    公开(公告)号：US4307116A

    公开(公告)日：1981-12-22

    申请号：US152115

    申请日：1980-05-21

    申请人： Daniel Farge ,  Claude Moutonnier ,  Pierre Le Roy ,  Jean-Francois Peyronel

    发明人： Daniel Farge ,  Claude Moutonnier ,  Pierre Le Roy ,  Jean-Francois Peyronel

    IPC分类号： A61K20060101 ,  A61K31/545 ,  C07D20060101 ,  C07D277/38 ,  C07D417/12 ,  C07D501/00 ,  C07D501/24 ,  C07D501/36 ,  C07D501/46

    CPC分类号： C07D501/24

    摘要： Novel cephalosporins of the general formula (I); ##STR1## in which R is alkyl, L-2-amino-2-carboxy-ethyl, phenyl, pyridyl, pyridyl-N-oxide, pyrimidin-2-yl, substituted pyridazin-3-yl, 5,6-dioxo-1,4,5,6-tetrahydro-1,2,4-triazin-3-yl substituted in the 4-position, 1,3,4-triazol-5-yl or 2-alkoxycarbonyl-1,3,4-triazol-5-yl substituted in the 1-position, 1,4-dialkyl-5,6-dioxo-1,4,5,6-tetrahydro-1,2,4-triazin-3-yl, 1-alkyl-5,6-dioxo-1,4,5,6-tetrahydro-1,2,4-triazin-3-yl, 2-alkyl-5,6-dioxo-1,2,5,6-tetrahydro-1,2,4-triazin-3-yl, triazol-5-yl, 1,3,4-thiadiazol-5-yl which is substituted or unsubstituted, 1,2,4-thiadiazol-5-yl which is substituted, 1,3,4-oxadiazol-5-yl which is substituted or unsubstituted, oxazol-2-yl which is substituted or unsubstituted or tetrazol-5-yl which is substituted or unsubstituted in the 1-position, R' is a hydrogen atom or a radical of the general formula (II); ##STR2## and R.sup.o is hydrogen, alkyl, vinyl or cyanomethyl, as well as their salts, are useful as anti-bacterial agents.

    摘要翻译： 通式（I）的新型头孢菌素; （I）其中R是烷基，L-2-氨基-2-羧基 - 乙基，苯基，吡啶基，吡啶基-N-氧化物，嘧啶-2-基，取代的哒嗪-3-基，5,6 在4-位取代的1-二氧代-1,4,5,6-四氢-1,2,4-三嗪-3-基，1,3,4-三唑-5-基或2-烷氧基羰基-1,3 在1-位上取代的4-三唑-5-基，1,4-二烷基-5,6-二氧代-1,4,5,6-四氢-1,2,4-三嗪-3-基，1 - 烷基-5,6-二氧代-1,4,5,6-四氢-1,2,4-三嗪-3-基，2-烷基-5,6-二氧代-1,2,5,6-四氢 -1,2,4-三嗪-3-基，三唑-5-基，取代或未取代的1,3,4-噻二唑-5-基，被取代的1,2,4-噻二唑-5-基 被取代或未取代的取代或未取代的1,3,4-恶二唑-5-基，在1位被取代或未取代的四唑-5-基，R'是氢 原子或通式（II）的基团; （II）和Ro是氢，烷基，乙烯基或氰基甲基，以及它们的盐可用作抗细菌剂。

    Process for the preparation of ampicillin
    6.
    发明授权
    Process for the preparation of ampicillin 失效
    氨苄青霉素的制备方法

    公开(公告)号：US3978078A

    公开(公告)日：1976-08-31

    申请号：US557095

    申请日：1975-03-10

    申请人： Jean Bouchaudon ,  Pierre Le Roy ,  Mayer Naoum Messer

    发明人： Jean Bouchaudon ,  Pierre Le Roy ,  Mayer Naoum Messer

    IPC分类号： C07D499/68 ,  C07D499/80

    CPC分类号： C07D499/68 ,  C07D499/80

    摘要： Ampicillin is prepared by reacting an inorganic or organic base with a new penicillin G derivative of the formula: ##EQU1## (wherein R.sub.1 represents a group protecting the carboxy radical and R.sub.2 represents a strong electron-attracting group, e.g. a halogenoethyl group) to open the imidazolidine ring and give an intermediate product of the formula: ##EQU2## and removing by methods known per se the groups --R.sub.1 and R.sub.2 O--CS-- which protect the carboxy radical and amine functions respectively.

    摘要翻译： 氨苄青霉素通过使无机或有机碱与新的下式的青霉素G衍生物反应制备：OHS | ANGLE CH3 C6H5-CH2-C --- N ---- CH-CHC ANGLE |||| CH3 R2O-CS -NC = OO = CN --- CH-COOR1 ANGLE CH | C6H5（其中R1表示保护羧基的基团，R2表示强电子吸引基团，例如卤代乙基），以打开咪唑烷环，得到中间体 下式的产物：S ANGLE CH3 R2O-CS-NH-CH-CONH-CH-CHC ANGLE ||| CH3 C6H5O = CN --- CH-COOR1，通过本身已知的方法除去基团-R1和R2O -CS-分别保护羧基和胺官能团。

    .beta.-aminovinyl ketones, a preparation process and their use in the preparation of .beta.-diketones
    7.
    发明授权
    .beta.-aminovinyl ketones, a preparation process and their use in the preparation of .beta.-diketones 失效
    β-氨基乙烯基酮，其制备方法及其在制备β-二酮中的应用

    公开(公告)号：US5684206A

    公开(公告)日：1997-11-04

    申请号：US569266

    申请日：1996-03-20

    申请人： Michel Casado ,  Pierre Le Roy ,  Virginie Pevere

    发明人： Michel Casado ,  Pierre Le Roy ,  Virginie Pevere

    IPC分类号： B01J27/02 ,  B01J27/10 ,  C07B61/00 ,  C07C45/42 ,  C07C49/217 ,  C07C49/563 ,  C07C69/78 ,  C07C225/16 ,  C07C319/20 ,  C07C323/32 ,  C07C49/76

    CPC分类号： C07C323/32 ,  C07C319/20 ,  C07C2101/02

    摘要： Novel .beta.-aminovinyl ketones of the general formula ##STR1## wherein R.sup.1 is, in particular, an alkenyl, alkynyl, cycloalkyl or cycloalkenyl group; R.sup.2 is, in particular, an electron-attracting substituent such as nitro, acyl, ester, alkylthio, carbamoyl, thiocarbamoyl or haloalkyl; R.sup.3 is, in particular, an alkyl or alkoxy group or a halogen atom; n is 1 or 2 and m is 0, 1, 2 or 3. A method for preparing such compounds by carrying out a condensation reaction between ketone R.sup.1 --CO--CH.sub.3 and, in particular, benzonitrile substituted by (R.sup.2).sub.n and optionally (R.sup.3).sub.m, in the presence of a strong base, as well as a process employing said .beta.-aminovinyl ketones of general formula (VI) for preparing the corresponding .beta.-diketones, are also disclosed.

    摘要翻译： PCT No.PCT / FR94 / 00726 Sec。 371日期：1996年3月20日 102（e）1996年3月20日PCT 1994年6月16日PCT公布。 公开号WO95 / 00476 日期1995年1月5日通式（VI）的新型β-氨基乙烯基酮其中R 1特别是烯基，炔基，环烷基或环烯基; R2特别是吸电子取代基如硝基，酰基，酯，烷硫基，氨基甲酰基，硫代氨基甲酰基或卤代烷基; R3特别是烷基或烷氧基或卤素原子; n为1或2，m为0,1,2或3.通过进行酮R1-CO-CH3之间的缩合反应，特别是被（R 2）n取代的苄腈和任选（ R3）m，在存在强碱的情况下，以及采用通式（VI）的β-氨基乙烯基酮制备相应的β-二酮的方法也被公开。

    Novel process for the preparation of a synthetic intermediate for pesticides
    9.
    发明申请
    Novel process for the preparation of a synthetic intermediate for pesticides 有权
    制备农药合成中间体的新方法

    公开(公告)号：US20060142614A1

    公开(公告)日：2006-06-29

    申请号：US10532160

    申请日：2003-10-24

    申请人： Bernard Buathier ,  Pierre Le Roy

    发明人： Bernard Buathier ,  Pierre Le Roy

    IPC分类号： C07C211/45

    CPC分类号： C07C209/74 ,  C07C211/52

    摘要： Process for the preparation of a compound of general formula (I): in which X represents a halogen atom, by reaction of para-trifluoromethylaniline of formula (II): with a dihalogen X2, the two compounds being introduced simultaneously into a polar aprotic solvent in a dihalogen/compound (II) molar ratio ranging from 1.9 to 2.5 and at a temperature ranging from 100 to 300° C.

    摘要翻译： 制备通式（I）化合物的方法：其中X表示卤素原子，通过式（II）的对三氟甲基苯胺与二卤代X 2 H 2反应，将两种化合物 同时引入极性非质子溶剂中，二卤化物（II）摩尔比为1.9-2.5，温度为100-300℃。