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1. 发明授权

US4617377A Synergistine derivatives and their preparation 失效
标题翻译：协同主义衍生物及其制备
公开(公告)号：US4617377A
公开(公告)日：1986-10-14
申请号：US630256
申请日：1984-07-12
申请人： Jean-Pierre Corbet , Claude Cotrel , Daniel Farge , Jean-Marc Paris
发明人： Jean-Pierre Corbet , Claude Cotrel , Daniel Farge , Jean-Marc Paris
IPC分类号： C07D498/14 , A61K38/00 , C07K7/06 , C07K5/12
CPC分类号： C07K7/06 , A61K38/00 , Y10S930/19 , Y10S930/27
摘要： The invention provides new synergistine derivatives of the formula: ##STR1## in which Y=H or N(CH.sub.3).sub.2 and R represents: (a) H or OH,(b) a radical of the formula NR.sub.1 R.sub.2, in which R.sub.1 and R.sub.2 =H, phenyl or pyridyl (optionally substituted by dialkylamino (1 to 4 C), alkyl (1 to 10 C) [optionally substituted by OH, SH, COOH, anilino, or alkylamino or dialkylamino of which at least one of the alkyl parts is substituted by OH, SH, COOH or anilino 9 , alkenyl (3 or 4 C) or alkynyl (3 or 4 C), or alternatively R.sub.1 and R.sub.2 together form a heterocycle optionally containing another heteroatom such as O, S or N (optionally substituted by alkyl), or(c) a halogen atom, a trimethylsilyloxy or dialkylphosphoryloxy radical or a radical --OSO.sub.2 R.sub.3 or --OCOR.sub.4, R.sub.3 being alkyl, trifluoromethyl, trichloromethyl or optionally substituted phenyl and R.sub.4 being defined in the same way as R.sub.3 or being an acylalkyl, alkoxycarbonylalkyl or alkoxy radical, and also their salts and their preparation. These products are useful as intermediates in the synthesis of anti-bacterial synergistine derivatives.
摘要翻译：本发明提供下式的新的增效剂衍生物：其中Y = H或N（CH 3）2，R代表：（a）H或OH，（b）式NR1R2的基团，其中Y = H或N（CH3） R 1和R 2 = H，苯基或吡啶基（任选被二烷基氨基（1至4 C）取代），（1至10 C）烷基（任选被OH，SH，COOH，苯胺基或烷基氨基或二烷基氨基取代，烷基部分被OH，SH，COOH或苯胺基9，烯基（3或4 C）或炔基（3或4 C）取代，或者R 1和R 2一起形成任选地含有另外的杂原子如O，S或 N（任选被烷基取代），或（c）卤素原子，三甲基甲硅烷氧基或二烷基磷酰氧基或基团-OSO 2 R 3或-OCOR 4，R 3是烷基，三氟甲基，三氯甲基或任选取代的苯基，并且R 4的定义同 R3或为酰基烷基，烷氧基羰基烷基或烷氧基，以及它们的盐及其制备 ul作为抗菌增效剂衍生物合成中的中间体。

2. 发明授权

US4686309A 3-phenyl-2-propeneamine derivatives, their preparation and compositions containing them 失效
标题翻译： 3-苯基-2-丙烯胺衍生物，它们的制备方法和含有它们的组合物
公开(公告)号：US4686309A
公开(公告)日：1987-08-11
申请号：US702088
申请日：1985-02-15
申请人： Jean-Claude Barriere , Jean-Pierre Corbet , Claude Cotrel , Daniel Farge , Jean-Marc Paris
发明人： Jean-Claude Barriere , Jean-Pierre Corbet , Claude Cotrel , Daniel Farge , Jean-Marc Paris
IPC分类号： A61K31/135 , A61K31/10 , A61K31/137 , A61K31/21 , A61K31/22 , A61P25/24 , A61P25/26 , C07C67/00 , C07C213/00 , C07C213/02 , C07C215/28 , C07C215/30 , C07C215/42 , C07C219/22 , C07C219/32 , C07C239/00 , C07C271/20 , C07C313/00 , C07C317/28 , C07C317/36 , C07C319/20 , C07C323/27 , C07C323/32 , C07C323/65 , C07D207/08 , C07D213/38 , C07D213/70 , C07D295/084 , C07D295/092 , C07D307/32 , C07F9/40 , C07C91/16 , C07C67/02 , C07D211/70
CPC分类号： C07D207/08 , C07D213/38 , C07D213/70 , C07D295/092 , C07D307/32 , C07F9/4006
摘要： The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl, either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl, or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and (i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.7 =H or alkylcarbonyl, alkyloxycarbonyl, alkylaminocarbonyl or benzoyl, optionally substituted by one or two halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 groups, (ii) or Y and A together form a 1-hydroxycycloalkyl radical, the ring of which contains 5 or 6 C, optionally joined to a benzene ring, it being understood that the alkyl radicals and alkyl parts contain 1 to 4 C as a straight or branched chain, and that the invention relates to all the possible geometric and optical isomers as well as their mixtures.These compounds are useful as antidepressants.
摘要翻译：本发明提供下式的化合物：其中R = H，卤素，烷基，烷氧基，链烯基，NH 2，烷基氨基，二烷基氨基或CF 3，R 3 = H或烷基，R 4和R 5 = H，R 1和 R 2 = H或烷基，任选被烯基（2至4 C）取代，或者R 1和R 2一起形成含有4至7个环成员的饱和杂环，并任选地含有另外的杂原子，例如任选被烷基取代的O，S或N，或R4 = H，R1 = H或烷基，R2和R5一起形成亚烷基（3至4 C）基团，和（i）A =烷基或苯基，其未被取代或被一个或两个选自卤素，烷基，烷氧基，烷硫基，NH 2，烷基氨基，二烷基氨基，NO 2或CF 3，或者A =吡啶基，苄基或环烷基（3至6C），Y = S，SO或SO 2或基团：其中R 6 = H或烷基，R 7 = H或烷基羰基，烷氧基羰基，烷基氨基羰基或苯甲酰基，任选被一个或两个卤素，烷基，烷氧基，烷硫基，NH 2，烷基氨基，二烷基氨基，NO 2或CF 3基团，（ii）或Y和A一起形成1-羟基环烷基，其环含有5或6个C，任选地连接到苯环，应理解烷基和烷基部分含有1至4个C作为直链或支链，本发明涉及所有可能的几何和光学异构体及其混合物。这些化合物可用作抗抑郁药。

3. 发明授权

US4590004A Pristinamycin derivatives, their preparation and their use 失效
标题翻译：普瑞霉素衍生物，其制备及其应用
公开(公告)号：US4590004A
公开(公告)日：1986-05-20
申请号：US630284
申请日：1984-07-12
申请人： Jean-Pierre Corbet , Claude Cotrel , Daniel Farge , Jean-Marc Paris
发明人： Jean-Pierre Corbet , Claude Cotrel , Daniel Farge , Jean-Marc Paris
IPC分类号： C07D498/18 , A61K9/08 , A61K31/42 , A61K38/00 , A61P31/04 , C07D498/20 , C07K5/078 , C07K7/06 , C07K5/12
CPC分类号： C07K5/06182 , C07K7/06 , A61K38/00 , Y10S930/19 , Y10S930/27
摘要： The invention provides new pristinamycin II.sub.B derivatives of the formula: ##STR1## in which R represents alkylthio substituted by (i) alkylamino or dialkylamino of which the alkyl parts can form a pyrrolidin-1-yl, piperidino, azetidin-1-yl, azepin-1-yl, morpholino, thiomorpholino or piperazin-1-yl ring (optionally substituted by alkyl), or (ii) pyrrolidin-2-yl or pyrrolidin-3-yl, piperidin-2-yl, piperidin-3-yl or piperidin-4-yl, azetidin-2-yl or azetidin-3-yl or azepin-2-yl, azepin-3-yl or azepin-4-yl;a radical Het-S-, in which Het is pyrrolidin-3-yl, piperidin-3-yl or piperidin-4-yl, azetidin-3-yl or azepin-3-yl or azepin-4-yl optionally N-alkylsubstituted; ordialkylamino of which the alkyl parts can form a pyrrolidin-1-yl, piperidino, azetidin-1-yl, azepin-1-yl, morpholino, thiomorpholino or piperazin-1-yl ring (optionally substituted by alkyl), the said alkyls having 1 to 5 carbon atoms each in a linear or branched chain. The compounds of the formula (I) are useful as antimicrobial agents when used in association with known synergistines or synergistines of the formula: ##STR2##
摘要翻译：本发明提供了下式的新霉素霉素IIB衍生物：其中R表示被（i）烷基氨基或二烷基氨基取代的烷硫基，其烷基部分可以形成吡咯烷-1-基，哌啶子基，氮杂环丁烷-1-基，哌嗪-1-基，吗啉代，硫代吗啉代或哌嗪-1-基环（任选被烷基取代），或（ii）吡咯烷-2-基或吡咯烷-3-基，哌啶-2-基，哌啶-3-基 - 基或哌啶-4-基，氮杂环丁烷-2-基或氮杂环丁烷-3-基或氮杂-2-基，吖庚因-3-基或氮杂-4-基; 基团Het-S-，其中Het是吡咯烷-3-基，哌啶-3-基或哌啶-4-基，氮杂环丁烷-3-基或吖庚因-3-基或氮杂-4-基任选N-烷基取代 ; 或其二烷基氨基，其烷基部分可以形成吡咯烷-1-基，哌啶子基，氮杂环丁烷-1-基，吖庚因-1-基，吗啉代，硫代吗啉代或哌嗪-1-基环（任选被烷基取代），所述烷基具有1至5个碳原子，各自为直链或支链。当与已知的下式的增效剂或增效剂结合使用时，式（I）的化合物可用作抗微生物剂：（V）

4. 发明授权

US4755599A 3-phenyl-2-propeneamine derivatives, their preparation and composition containing them 失效
标题翻译： 3-苯基-2-丙烯胺衍生物，它们的制备方法和含有它们的组合物
公开(公告)号：US4755599A
公开(公告)日：1988-07-05
申请号：US10558
申请日：1987-02-03
申请人： Jean-Claude Barriere , Jean-Pierre Corbet , Claude Cotrel , Daniel Farge , Jean-Marc Paris
发明人： Jean-Claude Barriere , Jean-Pierre Corbet , Claude Cotrel , Daniel Farge , Jean-Marc Paris
IPC分类号： A61K31/135 , A61K31/10 , A61K31/137 , A61K31/21 , A61K31/22 , A61P25/24 , A61P25/26 , C07C67/00 , C07C213/00 , C07C213/02 , C07C215/28 , C07C215/30 , C07C215/42 , C07C219/22 , C07C219/32 , C07C239/00 , C07C271/20 , C07C313/00 , C07C317/28 , C07C317/36 , C07C319/20 , C07C323/27 , C07C323/32 , C07C323/65 , C07D207/08 , C07D213/38 , C07D213/70 , C07D295/084 , C07D295/092 , C07D307/32 , C07F9/40 , C07D279/04 , C07C149/24 , C07D205/04 , C07D223/04 , C07D275/02 , C07D277/04 , C07D401/06
CPC分类号： C07D207/08 , C07D213/38 , C07D213/70 , C07D295/092 , C07D307/32 , C07F9/4006
摘要： The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl,either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl,or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and(i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6 C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.7 =H or alkylcarbonyl, alkyloxycarbonyl, alkylaminocarbonyl or benzoyl, optionally substituted by one or two halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 groups,(ii) or Y and A together form a 1-hydroxycycloalkyl radical, the ring of which contains 5 or 6 C, optionally joined to a benzene ring,it being understood that the alkyl radicals and alkyl parts contains 1 to 4 C as a straight or branched chain, and that the invention relates to all the possible geometric and optical isomers as well as their mixtures.These compounds are useful as antidepressants.
摘要翻译：本发明提供下式的化合物：其中R = H，卤素，烷基，烷氧基，链烯基，NH 2，烷基氨基，二烷基氨基或CF 3，R 3 = H或烷基，R 4和R 5 = H，R 1和 R 2 = H或烷基，任选被烯基（2至4 C）取代，或者R 1和R 2一起形成含有4至7个环成员的饱和杂环，并任选地含有另外的杂原子，例如任选被烷基取代的O，S或N，或R4 = H，R1 = H或烷基，R2和R5一起形成亚烷基（3至4 C）基团，和（i）A =烷基或苯基，其未被取代或被一个或两个选自卤素，烷基，烷氧基，烷硫基，NH 2，烷基氨基，二烷基氨基，NO 2或CF 3，或者A =吡啶基，苄基或环烷基（3至6 C），Y = S，SO或SO 2或基团：其中R 6 = H或烷基，且R7 = H或烷基羰基，烷氧基羰基，烷基氨基羰基或苯甲酰基，任选被一个或两个卤素，烷基，烷氧基，烷硫基，NH 2，烷基氨基，二烷基氨基，NO 2或CF 3基团，（ii）或Y和A一起形成1-羟基环烷基，其环包含5或6个C，任选地连接到苯环，应理解烷基和烷基部分包含1至4 C作为直链或支链，本发明涉及所有可能的几何和光学异构体及其混合物。这些化合物可用作抗抑郁药。

5. 发明授权

US4618599A Synergistine derivatives having anti-bacterial activity and their use 失效
标题翻译：具有抗菌活性的协同主义衍生物及其用途
公开(公告)号：US4618599A
公开(公告)日：1986-10-21
申请号：US630288
申请日：1984-07-12
申请人： Jean-Pierre Corbet , Claude Cotrel , Daniel Farge , Jean-Marc Paris
发明人： Jean-Pierre Corbet , Claude Cotrel , Daniel Farge , Jean-Marc Paris
IPC分类号： C07D498/14 , A61K31/435 , A61K38/00 , A61P31/04 , C07D20060101 , C07D213/65 , C07D273/00 , C07D498/18 , C07K7/00 , C07K7/06 , A61K37/02 , C07K5/12
CPC分类号： C07K7/06 , A61K38/00 , Y10S930/19 , Y10S930/27
摘要： The invention provides new synergistine derivatives of the formula: ##STR1## in which Y=H or N(CH.sub.3).sub.2 and (a) R.sub.1 and R.sub.2 =H and R=pyrrolidin-3-ylthio or piperidin-3-ylthio or piperidin-4-ylthio (optionally substituted by alkyl), or altenatively R=alkylthio substituted by 1 or 2 SO.sub.3 H radicals or alkylamino or dialkylamino radicals (optionally substituted) or by 1 or 2 piperazino rings (optionally substituted) or morpholino, thiomorpholino, piperidino, pyrrolidin-1-yl, piperidin-2-yl, piperidin-3-yl or piperidin-4-yl or pyrrolidin-2-yl or pyrrolidin-3-yl rings (these last 5 rings being optionally substituted by alkyl), or(b) R.sub.1 and R.sub.2 form a bond and R=pyrrolidin-3-ylamino, piperidin-3-ylamino or piperidin-4-ylamino, pyrrolidin-3-yloxy, piperidin-3-yloxy or piperidin-4-yloxy, pyrrolidin-3-ylthio, piperidin-3-ylthio or piperidin-4-ylthio (optionally substituted by alkyl), or alternatively R=alkylamino, alkoxy or alkylthio substituted by 1 or 2 SO.sub.3 H radicals, alkylamino or dialkylamino radicals (optionally substituted) or trialkylammonio or imidazol-4-yl or imidazol-5-yl radicals or by 1 or 2 piperazino rings (optionally substituted by alkyl) or morpholino, thiomorpholino, piperidino, pyrrolidin-1-yl, piperidin-2-yl, piperidin-3-yl or piperidin-4-yl or pyrrolidin-2-yl or pyrrolidin-3-yl rings (these last two rings being optionally substituted by alkyl), and their salts, their preparation, and the pharmaceutical compositions in which they are present. These compounds are useful as anitbacterial agents.
摘要翻译：本发明提供下式的新增效剂衍生物：其中Y = H或N（CH 3）2和（a）R 1和R 2 = H，R =吡咯烷-3-基硫代或哌啶-3-基硫基或哌啶-4-基硫代（任选被烷基取代），或惰性地R =被1或2个SO 3 H基团取代的烷硫基或烷基氨基或二烷基氨基（任选取代的）或1或2个哌嗪子基环（任选取代的）或吗啉代，硫代吗啉代，哌啶子基，吡咯烷-1-基，哌啶-2-基，哌啶-3-基或哌啶-4-基或吡咯烷-2-基或吡咯烷-3-基环（这5个环任选被烷基取代）或（b）R 1和R 2形成键，R =吡咯烷-3-基氨基，哌啶-3-基氨基或哌啶-4-基氨基，吡咯烷-3-基氧基，哌啶-3-基氧基或哌啶-4-基氧基，吡咯烷 -3-烷硫基（任选被烷基取代），或者R =被1或2个SO 3 H基取代的烷基氨基，烷氧基或烷硫基，烷基氨基或二烷基氨基（任选取代的）或三烷基氨基或咪唑-4-基或咪唑-5-基或1或2个哌嗪子基环（任选被烷基取代）或吗啉代，硫代吗啉代，哌啶子基，吡咯烷-1-基，哌啶-2-基，哌啶-3-基或哌啶-4-基或吡咯烷-2-基或吡咯烷-3-基环（这些最后两个环任选被烷基取代），及其盐，它们的制备和药物组合物他们在场。这些化合物可用作厌氧细菌剂。

6. 发明授权

US4617290A Synergistine derivatives, their preparation and pharmaceutical compositions containing them 失效
标题翻译：协同三烯衍生物，它们的制备和含有它们的药物组合物
公开(公告)号：US4617290A
公开(公告)日：1986-10-14
申请号：US630245
申请日：1984-07-12
申请人： Jean-Pierre Corbet , Claude Cotrel , Daniel Farge , Jean-Marc Paris
发明人： Jean-Pierre Corbet , Claude Cotrel , Daniel Farge , Jean-Marc Paris
IPC分类号： C07D498/14 , A61K31/435 , A61K38/00 , A61P31/04 , C07K7/06 , A61K37/02 , C07K5/12
CPC分类号： C07K7/06 , A61K38/00
摘要： The invention provides novel synergistine derivatives of the formula: ##STR1## in which Y=H or N(CH.sub.3).sub.2 : and R.sub.1 =H and R.sub.2 =OH or alkyl optionally substituted by COOH, alkoxycarbonyl or OH or by alkylamino or dialkylamino the alkyl radicals of which can form a heterocycle, or R.sub.2 =cycloalkyl (of 3 to 7 carbons) or a heterocycle chosen from azetidine, pyrrolidine, piperidine or azepine (optionally substituted on the nitrogen by alkyl), or R.sub.1 =formyl or alkylcarbonyl and R.sub.2 =alkyl substituted by COOH or by alkylamino or dialkylamino the alkyl radicals of which can form a heterocycle, or R.sub.2 is a heterocycle as defined above, or R.sub.1 and R.sub.2, which are identical or different, represent alkyl optionally substituted by COOH, alkoxycarbonyl, OH, alkylamino, or dialkylamino of which the alkyl radicals can form a heterocycle, or R.sub.1 and R.sub.2 form an azetidine, pyrrolidine, piperidine, morpholine or piperazine ring (optionally substituted by alkyl), all the alkyls having 1 to 5 carbon atoms. These compounds are useful as antibacterial agents.
摘要翻译：本发明提供了下式的新型增效剂衍生物：其中Y = H或N（CH 3）2：和R 1 = H且R 2 = OH或任选被COOH，烷氧基羰基或OH取代的烷基或烷基氨基或二烷基氨基，其烷基可以形成杂环，或R2 =环烷基（3至7个碳）或选自氮杂环丁烷，吡咯烷，哌啶或吖庚因的杂环（任选在氮上被烷基取代），或R1 =甲酰基或烷基羰基并且R 2 =被COOH取代的烷基或被烷基氨基或二烷基氨基取代的烷基，其烷基可以形成杂环，或者R2是如上定义的杂环，或者相同或不同的R 1和R 2表示任选被COOH取代的烷基，烷氧基羰基，烷基氨基或二烷基氨基，其中烷基可形成杂环，或R 1和R 2形成氮杂环丁烷，吡咯烷，哌啶，吗啉或哌嗪环（任选被烷基取代），所有烷基具有1至5个碳原子。这些化合物可用作抗菌剂。

7. 发明授权

US5326782A Salts derived from 26-(dialkylaminoalkylsulphonyl)pristinamycin IIB 失效
标题翻译：衍生自26-（二烷基氨基烷基磺酰基）丙霉素IIB的盐
公开(公告)号：US5326782A
公开(公告)日：1994-07-05
申请号：US961925
申请日：1993-01-04
申请人： Jean-Claude Barriere , Jean-Pierre Corbet , Jean-Marc Paris , Xavier Radisson
发明人： Jean-Claude Barriere , Jean-Pierre Corbet , Jean-Marc Paris , Xavier Radisson
IPC分类号： A61K31/42 , A61K31/122 , A61K31/424 , A61K38/00 , A61P31/00 , A61P31/04 , C07D498/18 , C07K5/078 , C07D498/16
CPC分类号： C07K5/06182 , A61K38/00
摘要： Di-p-toluoyl tartrate, di-t-butylacetyl tartrate, di-butyryl tartrate and di-i-valeryl tartrate of (dialkylamino-2 alkyl)sulphonyl-26 pristinamycin II.sub.B having general formula (I) wherein Alk represents a straight or branched alkylene radical and R represents straight or branched alkyl radicals, said radicals having from 1 to 10 carbon atoms.
摘要翻译： PCT No.PCT / FR91 / 00582 Sec。 371日期：1993年1月4日 102（e）日期1993年1月4日PCT PCT 1991年7月15日PCT公布。出版物WO92 / 01694 （二烷基氨基-2-烷基）磺酰基-26嘌呤霉素IIB的具有通式（I）的酒石酸二 - 对甲苯酰酯，酒石酸二 - 叔丁基乙酯，酒石酸二丁酯和酒石酸二异戊酯，其中Alk表示直链或支链亚烷基，R表示直链或支链烷基，所述基团具有1至10个碳原子。

8. 发明授权

US4593101A Process for the preparation of 4-quinolinones 失效
标题翻译： 4-喹啉酮的制备方法
公开(公告)号：US4593101A
公开(公告)日：1986-06-03
申请号：US652527
申请日：1984-09-20
申请人： Michel Arnaud , Jean-Pierre Corbet
发明人： Michel Arnaud , Jean-Pierre Corbet
IPC分类号： C07D215/22 , C07D215/233 , C07D215/26 , C07D215/18
CPC分类号： C07D215/233
摘要： 1,2,3,4-Tetrahydro-4-quinolinone of formula: ##STR1## are prepared from a 3-anilinopropionic acid of formula: ##STR2## which is treated successively with phosgene, phosgene in the presence of dimethylformamide, a Lewis acid or a strong acid, and a base. In the formula (I) and (II), R denotes a hydrogen atom, a halogen atom or an alkyl (1 to 4 carbon atoms) or alkoxy (1 to 4 carbon atoms) radical, and R.sub.1 denotes a hydrogen atom or an alkyl radical (1 to 4 carbon atoms). The compounds of formula I are useful as intermediates in the production of known drugs.
摘要翻译：式（I）的1,2,3,4-四氢-4-喹啉酮由下式的3-苯胺基丙酸制备：（II），其依次用光气，光气存在下处理二甲基甲酰胺，路易斯酸或强酸和碱。在式（I）和（II）中，R表示氢原子，卤素原子或（1-4个碳原子的烷基）或烷氧基（1至4个碳原子）基团，R 1表示氢原子或烷基自由基（1至4个碳原子）。式I的化合物可用作生产已知药物的中间体。

9. 发明授权

US5187292A N-sulfomethylglycinate, use in the preparation of herbicides of the glyphosate type 失效
标题翻译： N-磺甲基甘氨酸盐，用于制备草甘膦类除草剂
公开(公告)号：US5187292A
公开(公告)日：1993-02-16
申请号：US844728
申请日：1992-03-02
申请人： Bernard Botannet , Jean-Louis Clavel , Jean-Pierre Corbet , Michel Mulhauser
发明人： Bernard Botannet , Jean-Louis Clavel , Jean-Pierre Corbet , Michel Mulhauser
IPC分类号： C07C309/14 , C07F9/38
CPC分类号： C07C309/14 , C07F9/3813
摘要： The invention relates to an N-sulfomethylglycinate of formula:HO.sub.3 S--CH.sub.2 --NH--CH.sub.2 --COOR.sub.1 (I)COOR.sub.1 being a hydrolysable carboxylic ester group.It also relates to a process for the preparation of the compound of formula (I) consisting in putting in contact sulfur dioxide, formaldehyde, and glycine in the presence of a R.sub.1 OH alcohol, or glycinate.It also relates to the use of the compound of formula (I) for the preparation of herbicides of the glyphosate type of reaction with a phosphite or a phosphonate of formula (R.sub.2 O).sub.2 P (O) H in which (R.sub.2 O).sub.2 P is a hydrolysable phosphonic ester group, then optionally by a subsequent hydrolysis reaction.
摘要翻译：本发明涉及下式的N-磺甲基甘氨酸盐：HO3S-CH2-NH-CH2-COOR1（I）COOR1是可水解羧酸酯基团。它还涉及制备在R1OH醇或甘氨酸盐存在下接触二氧化硫，甲醛和甘氨酸的式（I）化合物的方法。它还涉及式（I）化合物在制备草甘膦类型与式（R2O）2 P（O）H的亚磷酸酯或膦酸酯反应的除草剂中的用途，其中（R 2 O）2 P为可水解的膦酸酯基，然后任选地通过随后的水解反应。

10. 发明授权

US4755614A Preparation of herbicides containing a phosphonate group from intermediate benzoxazines 失效
标题翻译：从中间体苯并恶嗪制备含有膦酸酯基团的除草剂
公开(公告)号：US4755614A
公开(公告)日：1988-07-05
申请号：US841588
申请日：1986-03-20
申请人： Jean-Pierre Corbet
发明人： Jean-Pierre Corbet
IPC分类号： C07D265/16 , C07F9/38 , C07F9/40
CPC分类号： C07F9/4006 , C07D265/16 , C07F9/3813
摘要： Preparation of intermediates for herbicides of formula ##STR1## by the reaction of organic phosphites with benzoxazines of formulaBzx--CH.sub.2 --CO--Y (II)in whichBzx denotes the radical of formula: ##STR2## X is a usual substituent of phenols n is an integer from 0 to 4R.sup.1 and R.sup.2 are H or such that OR.sup.1 and OR.sup.2 are hydrolyzableY is --OM or --NR.sup.3 R.sup.4M is H or is such that COOM is a salt or an esterR.sup.3 and R.sup.4 are H or a hydrocarbon radical, and one of them can be R.sup.5 --SO.sub.2 --, andR.sup.5 is a hydrocarbon radical, substiuted if appropriate. Products obtained by the process and their use as herbicides.
摘要翻译：通过有机亚磷酸酯与式Bzx-CH2-CO-Y（Ⅱ）的苯并恶嗪的反应制备式（Ⅰ）的除草剂中间体，其中Bzx表示下式的基团：X是通常的取代基的酚n是0至4的整数R 1和R 2是H或使得OR 1和OR 2是可水解的，Y是-OM或-NR 3 R 4 M是H或使得COOM是盐或酯R3和R4是H或烃基，其中一个可以是R5-SO2-，R5是烃基，如果合适的话可以被取代。通过该方法获得的产品及其作为除草剂的用途。

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