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11. 发明授权

US5319140A Intermediates for cephalosporins with sulfur containing oxyimino side chain 失效
标题翻译：含硫氧基亚氨基侧链的头孢菌素中间体
公开(公告)号：US5319140A
公开(公告)日：1994-06-07
申请号：US885581
申请日：1992-05-19
申请人： Erwin Gotschi
发明人： Erwin Gotschi
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07C67/00 , C07C313/00 , C07C317/22 , C07C317/24 , C07C317/46 , C07C323/22 , C07C323/34 , C07C323/35 , C07C323/52 , C07C323/60 , C07C323/61 , C07C323/62 , C07C323/65 , C07C323/66 , C07D277/40 , C07D501/20 , C07D501/22 , C07D501/34 , C07D501/36 , C07D501/46 , C07D501/56 , C07C321/24
CPC分类号： C07D501/20 , C07D277/40
摘要： Antibacterial compounds of the formula ##STR1## wherein R is a mononuclear carbocyclic aromatic group, a 5-membered aromatic heterocyclic group which contains as the hereto (non-carbon) ring member(s) an oxygen or sulphur atom or an imino or lower alkylimino group and, optionally, one or two nitrogen atoms, or a 6-membered aromatic heterocyclic group which contains one to three nitrogen atoms as the hereto ring member(s); R.sup.1 is hydrogen or a 3-substituent which is usable in cephalosporin chemistry; A is lower alkylene or C.sub.3-7 -cycloalkylene which is optionally substituted with carboxy, carbamoyl, lower alkylcarbamoyl or di(lower alkyl)carbamoyl; Q is lower alkylene or C.sub.3-7 -cycloalkylene which is optionally substituted with carboxy, carbamoyl, lower alkylcarbamoyl or di(lower alkyl)carbamoyl or the group --NR.sup.2 -- or --NR.sup.2 NR.sup.3 --; R.sup.2 and R.sup.3 are independently hydrogen or lower alkyl; p and m are the zero or 1, n is zero, 1 or 2; R.sup.4 is hydrogen, lower alkanoyl or tri(lower alkyl)silyl; two R.sup.4 groups together represent diphenylmethylene; R.sup.5 is hydrogen, lower alkyl, hydroxy, lower alkoxy, halogen, nitro, --OCOR.sup.7, --OCOOR.sup.71, --N(R.sup.7).sub.2, --NHCOR.sup.7, --NHCOOR.sup.71, --COR.sup.7, --SR.sup.7, --SOR.sup.7, --SO.sub.2 R.sup.7, --SO.sub.3 H, --COOR.sup.7 or --CON(R.sup.7).sub.2 ; R.sup.6 is hydrogen, lower alkyl or halogen, R.sup.7 is hydrogen or lower alkyl; R.sup.71 is lower alkyl, and the two --OR.sup.4 groups are attached to the phenyl ring via adjacent carbon atoms, as well as readily hydrolyzable esters and pharmaceutically acceptable salts of these compounds and hydrates of compounds of formula I and of their esters and salts.
摘要翻译：其中R是单核碳环芳族基团的5元芳族杂环基团，其中含有氧原子或硫原子或亚氨基或低级亚烷基的非芳族杂环基团烷基亚氨基和任选的一个或两个氮原子，或含有一至三个氮原子的6-元芳族杂环基作为本文的环成员; R1是氢或可用于头孢菌素化学的3-取代基; A是低级亚烷基或任选被羧基，氨基甲酰基，低级烷基氨基甲酰基或二（低级烷基）氨基甲酰基取代的C 3-7 - 亚环烷基; Q是低级亚烷基或任选被羧基，氨基甲酰基，低级烷基氨基甲酰基或二（低级烷基）氨基甲酰基或-NR 2 - 或-NR 2 NR 3 - 基团取代的C 3-7 - 亚环烷基; R2和R3独立地是氢或低级烷基; p和m为零或1，n为零，1或2; R4是氢，低级烷酰基或三（低级烷基）甲硅烷基; 两个R 4基团一起表示二苯基亚甲基; R5是氢，低级烷基，羟基，低级烷氧基，卤素，硝基，-OCOR7，-OCOOR71，-N（R7）2，-NHCOR7，-NHCOOR71，-COR7，-SR7，-SOR7，-SO2R7，-SO3H， -COOR7或-CON（R7）2; R6是氢，低级烷基或卤素，R7是氢或低级烷基; R71是低级烷基，并且两个-OR4基团通过相邻的碳原子连接到苯环上，以及这些化合物的易水解的酯和药学上可接受的盐以及式I化合物及其酯和盐的水合物。

12. 发明授权

US5298513A Substituted basic 2-aminotetralin in pharmaceuticals 失效
标题翻译：药物中取代的碱性2-氨基四氢萘酮
公开(公告)号：US5298513A
公开(公告)日：1994-03-29
申请号：US891485
申请日：1992-05-29
申请人： Rudolf Schohe , Thomas Glaser , Jorg Traber , George S. Allen
发明人： Rudolf Schohe , Thomas Glaser , Jorg Traber , George S. Allen
IPC分类号： C07C253/00 , A61K31/135 , A61K31/18 , A61K31/40 , A61K31/435 , A61K31/445 , A61K31/495 , C07C67/00 , C07C227/00 , C07C227/02 , C07C231/00 , C07C233/00 , C07C233/62 , C07C255/58 , C07C271/06 , C07C271/08 , C07C311/00 , C07C311/02 , C07C311/37 , C07C313/00 , C07C317/00 , C07C317/04 , C07C317/14 , C07D209/14 , C07D209/16 , C07D209/44 , C07D209/48 , C07D209/50 , C07D211/26 , C07D211/58 , C07D211/88 , C07D213/82 , C07D275/02 , C07D275/06 , C07D279/02 , C07D285/14 , C07D295/096 , C07D295/10 , C07D453/02 , C07D471/10 , C07D521/00
CPC分类号： C07D209/48 , C07C233/62 , C07C255/00 , C07D209/14 , C07D209/16 , C07D209/44 , C07D211/26 , C07D211/58 , C07D211/88 , C07D213/82 , C07D275/02 , C07D275/06 , C07D279/02 , C07D285/14 , C07D295/096 , C07D453/02 , C07D471/10 , C07C2103/74
摘要： For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine ora group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andX denotes oxygen, sulphur or NR.sup.5,and their salts.
摘要翻译：为了治疗中枢神经系统，心血管系统或肠道疾病，新的取代的碱式2-氨基四氢萘酚（其中R 1表示氢或烷基，R 2表示氢，烷基或酰基），式（* CHEMICAL STRUCTURE *）并且R 3表示奎宁环或式 - （CH 2）a -R 4，-CH 2 -CH = CH-（CH 2）b -R 4，-CH 2 -C（三键）C-（CH 2）b -R 4，（ *化学结构*）其中a表示1至10的数字，b表示数字0,1,2,3或4，c表示数字0,1或2，d表示数字2或3，X表示氧，硫或NR5及其盐。

13. 发明授权

US5264613A Process for preparing ester of hydroxymethylbenzocyclobutenes 失效
标题翻译：制备羟甲基苯并环丁烯酯的方法
公开(公告)号：US5264613A
公开(公告)日：1993-11-23
申请号：US861700
申请日：1992-04-10
申请人： P. J. Thomas , R. Garth Pews
发明人： P. J. Thomas , R. Garth Pews
IPC分类号： C07C69/007 , C07C69/44 , C07C69/80 , C07C69/82 , C07C69/96 , C07C69/76 , C07C69/34 , C07C313/00
CPC分类号： C07C69/007 , C07C69/44 , C07C69/80 , C07C69/82 , C07C69/96
摘要： A process for preparing carboxylic acid esters of of the formulaX--(COOCH.sub.2 A).sub.nwherein A is the residue of a substituted or unsubstituted 3- or 4-benzocyclobutene compound, X is an n-valent organic bridging group, and n is 2,3, or 4, comprises reacting a substituted or unsubstituted 3- or 4-hydroxymethylbenzocyclobutene compound with a compound of the formula X--(COY).sub.n, wherein X is an n-valent organic bridging group and Y is Cl or Br. Esters of inorganic acids of the formulaX'(OCH.sub.2 A).sub.nwherein X' is a residue of an inorganic acid halide, n is 2 or 3, and A is the residue of a substituted or unsubstituted 3- or 4-benzocyclobutene compound, are prepared by reacting an inorganic halide of the formula X'Y.sub.n, wherein Y is Br or Cl, with a substituted or unsubstituted 3- or 4-hydroxymethylbenzocyclobutene compound. Biscarbonates of the formula X"[OC(.dbd.O)CH.sub.2 A].sub.2 wherein X" is the residue of a diphenol are prepared by reaction between a bis(halocarbonyl) compound of the formula X"[OC(.dbd.O)Y].sub.2, wherein Y is Cl or Br, and a substituted or unsubstituted 3- or 4-hydroxymethylbenzocyclobutene compound. The resulting esters are useful for making resins.
摘要翻译：一种制备式X-（COOCH 2 A）n的羧酸酯的方法，其中A是取代或未取代的3-或4-苯并环丁烯化合物的残基，X是n价有机桥基，n是2， 3或4包括使取代或未取代的3-或4-羟甲基苯并环丁烯化合物与式X-（COY）n的化合物反应，其中X为n价有机桥基，Y为Cl或Br。式X'（OCH 2 A）n的无机酸的酯，其中X'为无机酰卤的残基，n为2或3，A为取代或未取代的3-或4-苯并环丁烯化合物的残基，为通过使式X'Yn的无机卤化物（其中Y是Br或Cl）与取代或未取代的3-或4-羟甲基苯并环丁烯化合物反应制备。式X“[OC（= O）CH 2 A] 2的双碳酸酯，其中X”是二酚的残基，通过式X“[OC（= O）Y ] 2，其中Y是Cl或Br，以及取代或未取代的3-或4-羟甲基苯并环丁烯化合物。所得的酯可用于制备树脂。

15. 发明授权

US5158981A Antiandrogenic compounds and methods 失效
标题翻译：抗原化合物和方法
公开(公告)号：US5158981A
公开(公告)日：1992-10-27
申请号：US502922
申请日：1990-03-30
申请人： Marie-Madeleine Bouton , Jean Jacques , Andre Pierdet
发明人： Marie-Madeleine Bouton , Jean Jacques , Andre Pierdet
IPC分类号： C07C69/013 , A61K8/00 , A61K8/11 , A61K8/35 , A61K8/37 , A61K8/49 , A61K31/045 , A61K31/12 , A61K31/215 , A61K31/22 , A61K31/44 , A61K31/4406 , A61K31/455 , A61P17/00 , A61P43/00 , A61Q5/00 , C07C45/00 , C07C45/61 , C07C45/67 , C07C49/513 , C07C49/517 , C07C49/737 , C07C49/753 , C07C67/00 , C07C69/03 , C07C69/08 , C07C313/00 , C07C323/13 , C07D213/79 , C07D213/80 , C07D317/70 , C07D317/72
CPC分类号： C07D213/80 , C07C49/513 , C07D317/70 , C07D317/72 , C07C2103/16
摘要： A antiandrogenic compositions comprising an anti-androgenically effective amount of at least one compound of the formula ##STR1## wherein R is alkyl of 1 to 4 carbon atoms, R.sub.1 is alkyl of 1 to 2 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms optionally interrupted with a heteroatom, alkenyl and alkynyl of 2 to 8 carbon atoms optionally interrupted with a heteroatom, formyl and acyl of an organic carboxylic acid of 2 to 18 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, the dotted lines indicate optional presence of a double bond between the 4(5) and 5a(6) carbons and the wavy line indicates that R.sub.4 may be in the .alpha.- or .beta.-position and a non-toxic, pharmaceutical carrier or excipient and a method of treating hyperandrogenic conditions in warm-blooded animals.

16. 发明授权

US5157142A Thiocarbamates and their derivatives 失效
标题翻译：甲硫氨酸及其衍生物
公开(公告)号：US5157142A
公开(公告)日：1992-10-20
申请号：US875158
申请日：1986-06-17
申请人： Kenneth G. Davenport
发明人： Kenneth G. Davenport
IPC分类号： B01J27/06 , B01J27/00 , C07B61/00 , C07C67/00 , C07C313/00 , C07C319/02 , C07C323/34 , C07C325/00 , C07C333/02 , C07C333/04
CPC分类号： C07C333/02
摘要： A process is provided for preparing N-acyl-aminothiophenols, e.g., N-acetyl-para-aminothiophenol, or aminothiophenols, e.g., para-aminothiophenol, by reacting a hydroxy aromatic ketone, e.g., 4-hydroxyacetophenone (4-HAP), with hydroxylamine or a hydroxylamine salt, to form the oxime of the ketone, subjecting the oxime to a Beckmann rearrangement in the presence of a catalyst to form the N-acyl-hydroxy aromatic amine, e.g., N-acetyl-para-aminophenol (APAP), reacting the N-acyl-hydroxy aromatic amine with an N,N-di (organo) thiocarbamoyl halide, e.g., N,N-dimethylthiocarbamoyl chloride, to form an O-(N-acyl-aminoaryl)-N,N-di (organo) thiocarbamate, e.g., O-(N-acetyl-para-aminophenyl)-N,N-dimethylthiocarbamate, pyrolytically rearranging the O-(N-acyl-aminoaryl)-N,N-di (organo) thiocarbamate to form an S-(N-acyl-aminoaryl)-N,N-di (organo) thiocarbamate, e.g., S-(N-acetyl-para-aminophenyl)-N,N-dimethylthiocarbamate, and hydrolyzing the latter compound to obtain the N-acyl aminothiophenol or aminothiophenol. The N-acyl aminothiophenol may be reacted with an acylating agent to form the N,S-diacyl-aminothiophenol, e.g., N,S-diacetyl-p-aminothiophenol, or may be further hydrolyzed to the aminothiophenol, e.g., p-aminothiophenol.
摘要翻译：提供了通过使羟基芳族酮例如4-羟基苯乙酮（4-HAP）与N-羟基芳基酮（4-HAP）反应来制备N-酰基 - 氨基噻吩酚的方法，例如N-乙酰基对氨基苯硫酚或氨基硫酚，例如对氨基苯硫酚羟胺或羟胺盐，以形成酮的肟，在催化剂存在下使肟进行贝克曼重排以形成N-酰基 - 羟基芳族胺，例如N-乙酰基对氨基苯酚（APAP），使N-酰基 - 羟基芳族胺与N，N-二（有机）硫代氨基甲酰基卤化物例如N，N-二甲基硫代氨基甲酰氯反应，形成O-（N-酰基 - 氨基芳基）-N，N-二（有机）硫代氨基甲酸酯，例如O-（N-乙酰基 - 对 - 氨基苯基）-N，N-二甲基硫代氨基甲酸酯，热解重新排列O-（N-酰基 - 氨基芳基）-N，N-二（有机））硫代氨基甲酸酯，形成 S-（N-酰基 - 氨基芳基）-N，N-二（有机）硫代氨基甲酸酯，例如S-（N-乙酰基 - 对氨基苯基）-N，N-二甲基硫代氨基甲酸酯，并水解后一种化合物，得到N- 酰基氨基苯硫酚氨基苯硫酚 N-酰基氨基苯硫酚可以与酰化剂反应形成N，S-二酰基 - 氨基苯硫酚，例如N，S-二乙酰基对氨基苯硫酚，或者可以进一步水解成氨基苯硫酚，例如对氨基苯硫酚。

17. 发明授权

US5145954A Derivatives of alphaphenylacrylic acid and their use in agriculture 失效
标题翻译：碱性丙烯酸的衍生物及其在农业中的应用
公开(公告)号：US5145954A
公开(公告)日：1992-09-08
申请号：US39458
申请日：1989-04-17
申请人： Vivienne M. Anthony , John M. Clough , Paul DeFraine , Christopher R. A. Godfrey , Thomas E. Wiggins , David J. Tapolczay
发明人： Vivienne M. Anthony , John M. Clough , Paul DeFraine , Christopher R. A. Godfrey , Thomas E. Wiggins , David J. Tapolczay
IPC分类号： C07D319/24 , A01N37/34 , A01N37/36 , A01N37/38 , A01N37/42 , A01N37/44 , A01N37/46 , A01N37/48 , A01N37/50 , A01N41/10 , A01N43/04 , A01N43/08 , A01N43/24 , A01N43/40 , A01N43/48 , A01N45/00 , A01N47/02 , C07C67/00 , C07C69/00 , C07C313/00 , C07C317/00 , C07C317/14 , C07C319/14 , C07C319/20 , C07C323/56 , C07C323/58 , C07C323/65 , C07D213/55 , C07D213/64 , C07D307/54 , C07D307/68 , C07D307/91 , C07D333/18 , C07D333/24 , C07D339/08 , C07D521/00
CPC分类号： C07D307/54 , A01N37/36 , A01N43/08 , C07C323/56 , C07C323/58 , C07C323/62 , C07C323/65 , C07C2103/26
摘要： Compounds of formula: ##STR1## and stereoisomers thereof, wherein R.sup.1 and R.sup.2, which are the same or different, are optionally substituted alkyl; W, X, Y and Z, which are the same or different, are hydrogen, halogen, hydroxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted aryloxyalkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted alkynyl, optionally substituted amino, optionally substituted arylazo, optionally substituted heteroarylalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted acylamino, nitro, cyano, --OR.sup.3, --SR.sup.3, --CO.sub.2 R.sup.4, --CONR.sup.5 R.sup.6, --COR.sup.7, --CR.sup.8 .dbd.NR.sup.9, --N.dbd.CR.sup.10 R.sup.11, --SOR.sup.12 or --SO.sub.2 R.sup.13, or any two of W, X, Y, and Z, in adjacent positions on the phenyl ring, optionally join to form an optionally substituted fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; R.sup.3 is optionally substituted alkyl, or cycloalkyl optionally containing a hetero atom in the cycloalkyl ring, optionally substituted alkenyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted acyl, or optionally substituted heteroaryl; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.10 and R.sup.11, which are the same or different, are hydrogen or optionally substituted alkyl, optionally substituted cycloalkyl, cycloalkylalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted aralkyl; and R.sup.9, R.sup.12 and R.sup.13 are optionally substituted aryl or optionally substituted heteroaryl. The compounds are useful in agriculture as fungicides, plant growth regulators and insecticides.

18. 发明授权

US5124353A Fungicidal alpha-substituted acrylates 失效
标题翻译：杀真菌α-取代丙烯酸酯
公开(公告)号：US5124353A
公开(公告)日：1992-06-23
申请号：US416609
申请日：1989-10-03
申请人： John M. Clough , Christopher R. A. Godfrey
发明人： John M. Clough , Christopher R. A. Godfrey
IPC分类号： C07C253/00 , A01N37/34 , A01N37/36 , A01N37/38 , A01N37/42 , A01N37/44 , A01N37/46 , A01N37/48 , A01N39/00 , A01N39/02 , A01N43/40 , C07C67/00 , C07C69/618 , C07C69/734 , C07C229/30 , C07C229/44 , C07C233/15 , C07C233/25 , C07C233/43 , C07C233/54 , C07C235/42 , C07C237/30 , C07C255/54 , C07C255/57 , C07C313/00 , C07C323/54 , C07C323/62 , C07C323/63 , C07C325/00 , C07D207/323 , C07D213/30 , C07D213/64 , C07D307/38 , C07D307/54 , C07D333/14 , C07D333/24 , C07D333/54
CPC分类号： C07C321/00 , A01N37/36 , A01N37/44 , A01N39/00 , A01N39/02 , A01N43/40 , C07C323/00
摘要： Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein V is an oxygen or a sulphur atom; X and Y, which may be the same or different, are hydrogen or halogen atoms, or optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkynyl, haloalkyl, alkoxy, haloalkoxy, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, nitrile, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6 groups; or the groups X and Y, when they are in adjacent positions on the phenyl ring, may join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; and Z is optionally substituted methylene, optionally substituted amino, oxygen or sulphur and when Z is a substituted methylene group, the substituent may join the 2-position of the phenyl ring to form a non-aromatic fused ring; R.sup.1 and R.sup.2 are alkyl groups containing from one to four carbon atoms, optionally substituted with one or more halogen atoms; and R.sup.3, R.sup.4, R.sup.5, and R.sup.6, which may be the same or different, are hydrogen atoms or optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, optionally substituted aryl, optionally substituted aralkyl, or cycloalkylalkyl groups: and metal complexes thereof.
摘要翻译：式（I）化合物：其中V是氧或硫原子; X和Y可以相同或不同，是氢或卤素原子，或任选取代的烷基，任选取代的烯基，任选取代的芳基，任选取代的杂芳基，任选取代的炔基，卤代烷基，烷氧基，卤代烷氧基，任选取代的芳氧基，取代的芳基烷氧基，任选取代的酰氧基，任选取代的氨基，酰氨基，硝基，腈，-CO 2 R 3，-CONR 4 R 5或-COR 6基团; 或基团X和Y当它们在苯环上的相邻位置时，可以连接形成任选含有一个或多个杂原子的芳族或脂族稠合的稠环; Z是任选取代的亚甲基，任选取代的氨基，氧或硫，当Z是取代的亚甲基时，取代基可以连接苯环的2-位，形成非芳香稠环; R1和R2是含有1-4个碳原子的烷基，任选地被一个或多个卤素原子取代; 和可以相同或不同的R 3，R 4，R 5和R 6是氢原子或任选取代的烷基，环烷基，烯基，炔基，任选取代的芳基，任选取代的芳烷基或环烷基烷基：及其金属络合物。

19. 发明授权

US5118856A Preparation of cyclohexane-dione derivatives 失效
标题翻译：环己酮衍生物的制备
公开(公告)号：US5118856A
公开(公告)日：1992-06-02
申请号：US562445
申请日：1990-08-02
申请人： Gernot Reissenweber , Winfried Richarz
发明人： Gernot Reissenweber , Winfried Richarz
IPC分类号： C07B37/10 , C07B41/06 , C07C45/00 , C07C45/45 , C07C45/48 , C07C45/65 , C07C45/67 , C07C45/68 , C07C49/403 , C07C49/613 , C07C49/647 , C07C49/703 , C07C49/713 , C07C49/723 , C07C49/743 , C07C49/747 , C07C67/00 , C07C67/347 , C07C69/757 , C07C313/00 , C07C323/22 , C07C401/00 , C07C403/16 , C07D213/46 , C07D213/50 , C07D309/06 , C07D309/22 , C07D335/02
CPC分类号： C07C45/676 , C07C319/20 , C07D213/50 , C07D309/06 , C07D309/22 , C07D335/02 , C07C2101/14 , C07C2101/16 , C07C2101/20 , C07C2102/42
摘要： A process for the preparation of cyclohexanedione derivatives of the general formula I ##STR1## where R.sup.1 is C.sub.2 -C.sub.8 -alkyl, C.sub.2 -C.sub.8 -alkenyl, C.sub.3 -C.sub.12 -cycloalkyl, C.sub.5 -C.sub.12 -cycloalkyl with 0-4 olefinically unsaturated bonds, C.sub.2 -C.sub.8 -alkylthioalkyl, C.sub.6 -C.sub.12 -bicycloalkyl with 0-3 olefinically unsaturated bonds, unsubstituted or substituted aryl or hetaryl, or a heterocyclic radical of 4 to 7 atoms of which not more than 3 may be hetero-atoms chosen from O, S and N, the radical being saturated or olefinically unsaturated, by reacting an .alpha.,.beta.-unsaturated ketone (II) with a dialkyl malonate in the presence of a base to give the alkoxycarbonylcyclohexenolone or its salt (III) ##STR2## and acylation, hydrolysis and decarboxylation of (III), wherein the .alpha.,.beta.-unsaturated ketone (II) is reacted, in the presence of a base, with the dialkyl malonate in a solvent from which the alcohol liberated from the malonate can be distilled off, the alcohol is distilled off, where appropriate as an azeotrope, the salt of the alkoxycarbonylcyclohexenolone is reacted with a carboxylic acid halide and the product, where appropriate after removal of excess acyl halide, is treated with an acylation catalyst, hydrolyzed and decarboxylated.
摘要翻译：制备通式I（I）的环己二酮衍生物的方法，其中R 1是C 2 -C 8 - 烷基，C 2 -C 8 - 烯基，C 3 -C 12 - 环烷基，具有0-4烯属的C 5 -C 12 - 环烷基不饱和键，C 2 -C 8烷硫基烷基，具有0-3烯属不饱和键的C 6 -C 12 - 双环烷基，未取代或取代的芳基或杂芳基，或其中不超过3的4至7个原子的杂环基可以是选择的杂原子通过在碱存在下使α，β-不饱和酮（II）与丙二酸二烷基酯反应得到烷氧基羰基环己烯醇或其盐，从O，S和N中选择饱和或烯属不饱和基团（III）和（III）的酰化，水解和脱羧反应，其中α，β-不饱和酮（II）在碱的存在下与丙二酸二烷基酯在可从其中释放出来的丙二酸酯释放的醇的溶剂中反应关闭，酒精被蒸馏掉，在适当的地方作为azeo 将烷氧基羰基环己烯醇的盐与羧酸卤化物反应，并且在除去过量酰基卤后适当的产物用酰化催化剂处理，水解和脱羧。

20. 发明授权

US5101069A Process for the preparation of hydroxyethylsulfonylnitro- and hydroxyethylsulfonylamino-benzoic acids 失效
标题翻译：羟基乙烯基硝基和羟基乙烯基亚氨基苯甲酸的制备方法
公开(公告)号：US5101069A
公开(公告)日：1992-03-31
申请号：US550179
申请日：1990-08-03
申请人： Theodor Papenfuhs
发明人： Theodor Papenfuhs
IPC分类号： C07C313/00 , C07C67/00 , C07C315/02 , C07C317/44 , C07C317/48
CPC分类号： C07C317/44
摘要： A process for the preparation of compounds of the formula (5) ##STR1## in which R denotes a hydrogen or oxygen atom and the --N(R).sub.2 group and the hydroxyethylsulfonyl group are in the ortho- or para-position relative to one another by converting 1 mol of a halonitrobenzoic acid of the formula (2) ##STR2## in which X denotes a fluorine, chlorine, bromine or iodine atom and the nitro group and the halogen atom are in the ortho- or para-position relative to one another, with at least 1 mol of mercaptoethanol in an aqueous solution or suspension or in an organic solvent in the presence of an acid-binding agent at temperatures from about 20.degree. to about 100.degree. C., to the corresponding hydroxyethylmercaptonitrobenzoic acid of the formula (3) ##STR3## oxidizing these acids in a manner known per se to the corresponding hydroxyethylsulfonylnitrobenzoic acids of the formula (5) (R=0) mentioned and reducing the latter, if necessary, in a manner known per se to the corresponding hydroxyethylsulfonylaminobenzoic acids of the general formula (4) ##STR4## in which the amino and hydroxyethylsulfonyl group are in the ortho- or para-position relative to one another.

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