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71. 发明授权

US4656290A Process for preparing thio, dithio or carbonyl compounds 失效
标题翻译：制备硫代，二硫代或羰基化合物的方法
公开(公告)号：US4656290A
公开(公告)日：1987-04-07
申请号：US691972
申请日：1985-01-16
申请人： Istvan Kaldor , Andras Szasz , Ilona Vegh nee Ba , Jozsef Heizer , Eva Behedek nee Haraszin
发明人： Istvan Kaldor , Andras Szasz , Ilona Vegh nee Ba , Jozsef Heizer , Eva Behedek nee Haraszin
IPC分类号： C07C49/00 , B01J27/00 , C07B31/00 , C07B35/02 , C07B35/06 , C07B45/06 , C07B61/00 , C07C45/00 , C07C45/65 , C07C67/00 , C07C313/00 , C07C319/14 , C07C319/24 , C07C321/00 , C07C321/14 , C07C321/28 , C07C321/30 , C07C323/00 , C07C323/12 , C07C323/16 , C07C323/17 , C07C323/21 , C07C323/25 , C07D235/32
CPC分类号： C07D235/32 , C07B45/06 , C07C201/12 , C07C319/14 , C07C319/24 , C07C321/14 , C07C321/28 , C07C45/65
摘要： A process is disclosed for the preparation of compounds of the Formula IR--X--R.sup.1 (I)wherein X is thio, dithio or carbonyl and R and R.sup.1 are defined hereinbelow which comprises reducing a compound of the Formula IIR--A (II)wherein A is chlorosulfonyl or a group of the Formula ##STR1## with a sulfur compound comprising sulfur which is of the (+)4 oxidation degree and is converted into the (+)6 oxidation degree during the process or with a sulfur compound which is decomposed in acidic medium to a compound of the latter oxidation degree in the presence of a catalytic amount but not more than 0.5 mole--related to 1 mole of the starting material of the Formula II--of elemental iodine or a compound capable of delivering hydrogen iodide in acidic medium or a compound which can be reduced to hydrogen iodide in acidic medium with the sulfur compound used.
摘要翻译：公开了制备式I的化合物RX-R1（Ⅰ）的方法，其中X是硫代，二硫代或羰基，R和R 1定义如下，其中包括将式Ⅱ的化合物RA（II）氯代磺酰基或一组式（IMAGE）与含硫（+）4氧化度的硫化合物反应，并在该过程中转化为（+）6氧化度，或与酸分解的硫化合物反应在相对于1摩尔元素碘的式II的原料或能够在酸性介质中输送碘化氢的化合物的催化量但不超过0.5摩尔存在下，将其培养至后一种氧化度的化合物或可以在酸性介质中用所用硫化合物还原成碘化氢的化合物。

72. 发明授权

US4638002A 2,3,4-trinor-1,5-inter-meta-phenylene-prostacyclin compounds useful in inhibiting thrombocyte aggregation 失效
公开(公告)号：US4638002A
公开(公告)日：1987-01-20
申请号：US576399
申请日：1983-12-30
申请人： Istvan Szekely , Sandor Botar , Krisztina Dolgos nee Kekesi , Bela Bertok , Antal Gajary , Tamas Szabolcsi , Gabor Kovacs , Marianna Lovasz nee Gaspar
发明人： Istvan Szekely , Sandor Botar , Krisztina Dolgos nee Kekesi , Bela Bertok , Antal Gajary , Tamas Szabolcsi , Gabor Kovacs , Marianna Lovasz nee Gaspar
IPC分类号： C07C69/76 , A61K31/343 , A61K31/5585 , A61P1/04 , A61P39/00 , C07C51/363 , C07C51/367 , C07C63/04 , C07C63/70 , C07C65/03 , C07C65/21 , C07C67/00 , C07C69/88 , C07C201/00 , C07C205/58 , C07C231/00 , C07C231/12 , C07C253/00 , C07C405/00 , C07D209/42 , C07D257/04 , C07D307/00 , C07D307/935 , C07D307/937 , C07D405/00 , C07D405/10 , C07F9/40 , C07F9/535 , C07F9/54 , A61K31/44
CPC分类号： C07D257/04 , C07C205/58 , C07C255/00 , C07C405/00 , C07C405/0041 , C07C405/0083 , C07C65/03 , C07C65/21 , C07D307/935 , C07D307/937 , C07D405/10 , C07F9/4015 , C07F9/5352 , C07F9/5456
摘要： The invention relates to new 2,3,4-trinor-1,5-inter-m-phenylene-PGI.sub.2 derivatives of the formula (I) ##STR1## wherein A stands for carboxy, cyano, tetrazolyl or --COOR.sup.3 or --CONR.sup.1 R.sup.2 ;R.sup.3 is C.sub.1-4 alkyl or an equivalent of a pharmacologically acceptable cation:R.sup.1 and R.sup.2 each stands for hydrogen, phenyl; C.sub.1-5 alkyl, optionally substituted by carboxy, hydroxy, phenyl or C.sub.2-5 alkoxycarbonyl; or C.sub.1-4 alkylsulfonyl; orR.sup.1 and R.sup.2 together form an .alpha.,.omega.-alkylene chain containing 3-6 carbon atoms;B stands for oxygen or methylene;Y is optionally bromo-substituted vinylene or a --C.tbd.C-- group:R.sup.4 stands for hydrogen or tetrahydro-pyran-2-yl;R.sup.5 represents an alkyl group containing 5-9 carbon atoms, which can be optionally interrupted by one or more oxygen atom(s) or --CH.dbd.CH-- or --C.tbd.C-- group(s) and/or optionally substituted by halogen; or a phenyoxymethyl group optionally substituted by halogen or trifluoromethyl; or an alkenoyloxymethyl group containing 3-5 carbon atoms;R.sup.6 is hydrogen or C.sub.1-4 alkyl;R.sup.7 stands for hydrogen, halogen, cyano, C.sub.1-4 alkyl or C.sub.1-4 alkoxy;R.sup.8 is hydrogen, halogen, cyano, nitro, hydroxy or C.sub.2-5 alkanoylamido;with the proviso that ifR.sup.5 stands for an alkyl group containing 5-9 carbon atoms which is unsubstituted or not interrupted by an oxygen atom or a --CH.dbd.CH-- or --C.tbd.C-- group; or a phenyoxymethyl group optionally substituted by halogen or trifluoromethyl, theneither R.sup.7 or R.sup.8 is other than hydrogen, or A is other than carboxy or --COOR.sup.3 and a process for the preparation thereof.The new compounds of the Formula I exhibit prolonged cytoprotecting and aggregation inhibiting and a low hypotensive effect and are superior to prostacycline in the prolonged duration of their activity.

73. 发明授权

US4599444A Process for the separation of isomeric cyclopropane-carboxylic acids 失效
标题翻译：异构环丙烷羧酸分离方法
公开(公告)号：US4599444A
公开(公告)日：1986-07-08
申请号：US581081
申请日：1984-02-17
申请人： Elemer Foggassy , Ferenc Faigl , Rudolf Soos , Jozsef Rakoczi
发明人： Elemer Foggassy , Ferenc Faigl , Rudolf Soos , Jozsef Rakoczi
IPC分类号： C07C61/37 , C07B31/00 , C07B53/00 , C07B57/00 , C07C51/00 , C07C51/487 , C07C61/40 , C07C67/00
CPC分类号： C07C51/487
摘要： The invention relates to a new process for separating the four stereoisomers of the cyclopropanecarboxylic acids of the formula ##STR1## wherein R stands for a methyl group or a halogen atom.The process comprisesreacting a salt formed with an alkali hydroxide or an alkali carbonate of dl-cis-trans-2,2-dimethyl-3-(2,2-disubstituted vinyl)-cyclopropanecarboxylic acids containing the isomers in any ratio or the pure dl-cis and dl-trans-2,2-dimethyl-3-(2,2-disubstituted vinyl)-cyclopropanecarboxylic acids prepared therefrom by the means of a selective dissolution with aromatic and aliphatic hydrocarbon solvents (suitably with benzene, extraction petroleum ether, n-hexane) with N-benzyl-2-aminobutanol enantiomers or with the hydrochlorides thereof in an aqueous medium or aqueous acetone medium, obtaining the crystalline diastereomeric salt from the solution by filtration, decomposing said salt by using a mineral acid, then separating the thus obtained optically active cyclopropanecarboxylic acidand obtaining the other isomer or other mixture of isomers from the filtrate of the said diastereomeric salt similarly after acidifying by a mineral acid, if desired, purifying the said optically active 2,2-di-methyl-3-(2,2-disubstituted vinyl)-cyclopropane-carboxylic acid isomers obtained by the above-mentioned procedure by a selective precipitation and recovering the resolving agent.
摘要翻译：本发明涉及用于分离式（I）的环丙烷羧酸的四种立体异构体的新方法，其中R代表甲基或卤素原子。该方法包括使含有任何比例的异构体的dl-顺 - 反-2,2-二甲基-3-（2,2-二取代的乙烯基） - 环丙烷羧酸的碱金属氢氧化物或碱金属碳酸盐形成的盐或纯的 dl-顺式和dl-反式-2,2-二甲基-3-（2,2-二取代的乙烯基） - 环丙烷羧酸，其通过选择性溶解与芳族和脂族烃溶剂（适合于苯，萃取石油醚正己烷）与N-苄基-2-氨基丁醇对映体或其盐酸盐在水性介质或丙酮水溶液中反应，通过过滤从溶液中获得结晶非对映体盐，通过使用无机酸分解所述盐，然后分离由此获得的光学活性环丙烷羧酸，并从所述非对映异构体盐的滤液中得到其它异构体或其它异构体混合物，同样地在无机酸酸化后，如果需要，通过选择性沉淀获得的通过上述方法获得的光学活性的2,2-二甲基-3-（2,2-二取代的乙烯基） - 环丙烷 - 羧酸异构体并回收拆分剂。

74. 发明授权

US4588526A Bronchodilatory azepino(1,2-A)pyrimidine derivatives and acid addition salts thereof and bronchodilating pharmaceutical compositions containing same 失效
标题翻译：支气管佐剂（1,2-A）嘧啶衍生物及其酸加成盐和含有其的支气管扩张药物组合物
公开(公告)号：US4588526A
公开(公告)日：1986-05-13
申请号：US550937
申请日：1983-11-10
申请人： Istvan Hermecz , Lelle Vasvari nee Debreczy , Agnes Horvath , Jozsef Kokosi , Sandor Virag , Tibor Breining
发明人： Istvan Hermecz , Lelle Vasvari nee Debreczy , Agnes Horvath , Jozsef Kokosi , Sandor Virag , Tibor Breining
IPC分类号： A61K31/519 , A61K31/55 , A61P11/08 , C07D487/04 , A61K31/505
CPC分类号： C07D487/04
摘要： The invention relates to new azepino[1,2-a]pyrimidine derivatives--of the general formula ##STR1## wherein p=1, 2 and acid addition salts thereof which can be prepared by(a) reacting a compound of the formula ##STR2## with a compound of the general formula ##STR3## wherein p is as defined above and R.sup.7 is alkoxycarbonyl containing 2 to 5 carbon atoms or carboxamido or(b) reacting a compound of the general formula ##STR4## wherein R.sup.8 is alkyl containing 1 to 4 carbon atoms with a compound of the general formula ##STR5## wherein R.sup.7 is as defined above and if desired converting a compound of the general formula I to acid addition salt thereof or setting it free from the salt thereof.The new compounds show bronchodilatory activity.
摘要翻译：本发明涉及通式为其中p = 1,2及其酸加成盐的通式为其中的氮杂[1,2-a]嘧啶衍生物及其酸加成盐，其可通过（a）使式图像II与具有通式III的化合物，其中p如上所定义，R 7是含有2至5个碳原子的烷氧基羰基或甲酰胺基，或（b）使通式为IV的化合物其中R8为含有1至4个碳原子的烷基与通式为其中R 7如上所定义的化合物反应，如果需要，将通式I的化合物转化为其酸加成盐或使其不含盐。新化合物显示支气管扩张活性。

75. 发明授权

US4529608A Honey powder preserving its natural aroma components 失效
标题翻译：蜂蜜粉保存其天然香气成分
公开(公告)号：US4529608A
公开(公告)日：1985-07-16
申请号：US549205
申请日：1983-11-04
申请人： Jozsef Szejtli , Marta Tardy nee Lengyel
发明人： Jozsef Szejtli , Marta Tardy nee Lengyel
IPC分类号： A23L1/00 , A23L1/08 , A23L1/22
CPC分类号： A23L27/77 , A23L21/25 , A23L27/70 , A23P10/43
摘要： A process for the preparation of honey powder preserving its natural aroma substances comprises(a) kneading 1 part by weight of honey, 0.8 part by weight of starch, pre-hydrolyzed starch or flour and 0.1-0.3 part by weight of cyclodextrin to yield a homogeneous mixture, subjecting the mixture thus obtained to thermal treatment at 100.degree. C. for 20 minutes, disintegrating the hot product obtained after thermal treatment, drying the product at a temperature of 50.degree.-55.degree. C., for 10-50 hours, adding 0.01-1.0% by weight of hydrophobic colloidal silicic acid or alkali earth stearate and grinding it to a powder; or(b) admixing 1 part by weight of honey with 6 parts by weight of a hot saturated aqueous cyclodextrin solution, freezing the homogeneous solution thus obtained, subjecting the product to lyphilization, adding 0.01-1.0% by weight of hydrophobic colloidal silicic acid or alkali earth stearate to the lyophilized product and grinding it to a powder.The advantage of the invention is that the aroma substances of honey are preserved and set free only during consumption.
摘要翻译：制备保存其天然芳香物质的蜂蜜粉的方法包括（a）捏合1重量份蜂蜜，0.8重量份淀粉，预水解淀粉或面粉和0.1-0.3重量份环糊精，得到均匀混合，将得到的混合物在100℃下热处理20分钟，将热处理后得到的热产物分解，在50-55℃的温度下干燥产物10-50小时，加入0.01-1.0重量％的疏水性胶体硅酸或碱土金属硬脂酸盐，并研磨成粉末; 或（b）将1重量份蜂蜜与6重量份热饱和水性环糊精溶液混合，冷却由此获得的均匀溶液，使产物进行裂解，加入0.01-1.0重量％的疏水胶体硅酸或碱土金属硬脂酸盐加入到冻干产品中并研磨成粉末。本发明的优点是蜂蜜的芳香物质被保存并且仅在消费期间释放。

76. 发明授权

US4528271A Process for the intensification of microbiological conversions of steroids using cyclodextrin additives 失效
标题翻译：使用环糊精添加剂加强类固醇微生物转化的过程
公开(公告)号：US4528271A
公开(公告)日：1985-07-09
申请号：US423084
申请日：1982-09-24
申请人： Eva Udvardy Nagy nee Cserey Pechany , Istvan Bartho , Gabor Hantos , Maria Trinn , Zsuzsa Vida , Jozsef Szejtli , Agnes Stadler nee Szoke , Ilona Habon , Marta Balazs nee Czurda
发明人： Eva Udvardy Nagy nee Cserey Pechany , Istvan Bartho , Gabor Hantos , Maria Trinn , Zsuzsa Vida , Jozsef Szejtli , Agnes Stadler nee Szoke , Ilona Habon , Marta Balazs nee Czurda
IPC分类号： C12P33/00 , C12P1/00 , C12P33/02 , C12P33/08 , C12P33/16 , C12P33/04 , C12P33/06 , C12P33/10 , C12P33/12 , C12P33/14 , C12P33/18 , C12P33/20
CPC分类号： C12P33/08 , C12P1/00 , C12P33/02
摘要： Microbiological conversions of cyclodextrins are intensified by adding to the reaction mixture 0.2 to 3 moles of .alpha.-, .beta.- or .gamma.-cyclodextrin or an optical mixture thereof pro mole of the steroid substrate, before, at the beginning or during the conversion. The cyclodextrin if desired, can be removed after the reaction. In this way the reaction velocity can be increased, the reaction time is reduced, the substrate concentration in the solution, i.e. its solubility is increased or the so called product inhibition may be avoided. In certain cases of more alternatives the desired reaction can be catalyzed and in this manner the selectivity is increased.
摘要翻译：在开始之前或转化期间，通过向反应混合物中加入0.2至3摩尔的α，β或γ-环糊精或其光学混合物来促进环糊精的微生物转化。如果需要，可以在反应后除去环糊精。以这种方式，可以增加反应速度，反应时间减少，溶液中的底物浓度，即其溶解度增加或者可以避免所谓的产品抑制。在更多选择的某些情况下，可以催化所需的反应，并且以这种方式增加了选择性。

77. 发明授权

US4508658A Pentahalophenyl ester of cyanoacetic acid derivatives 失效
标题翻译：氰乙酸衍生物的五氢苯基酯
公开(公告)号：US4508658A
公开(公告)日：1985-04-02
申请号：US113380
申请日：1980-01-18
申请人： Magda Huhn , Gabor Szabo , Peter Dvortsak , Marianna Karpati , Eva Somfai
发明人： Magda Huhn , Gabor Szabo , Peter Dvortsak , Marianna Karpati , Eva Somfai
IPC分类号： C07C255/41 , C07C67/00 , C07C253/00 , C07C253/30 , C07C255/19 , C07C255/32 , C07D213/26 , C07D213/57 , C07D307/38 , C07D333/12 , C07D333/24 , C07C121/46
CPC分类号： C07C255/00
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or C.sub.1 to C.sub.6 alkyl;R.sup.2 is hydrogen, phenyl, thienyl, furyl, pyridyl, C.sub.1 to C.sub.6 alkyl, furylalkyl where the alkyl is C.sub.1 to C.sub.6, or phenylalkyl where the alkyl is C.sub.1 to C.sub.6 ; orR.sup.1 and R.sup.2 together form C.sub.1 to C.sub.4 alkylene, furyl-C.sub.1 to C.sub.4 alkylene or phenyl-C.sub.1 to C.sub.4 alkylene; and X is halo; ora pharmaceutically acceptable salt thereof, are disclosed as well as a process for the preparation thereof. The new compounds are intermediates useful in the production of penicillins and cephalosporins with antibiotic activity.
摘要翻译：式IMA的化合物，其中R 1是氢或C 1 -C 6烷基; R2是氢，苯基，噻吩基，呋喃基，吡啶基，C1至C6烷基，其中烷基为C1至C6的呋喃基烷基，或烷基为C1至C6的苯基烷基; 或R 1和R 2一起形成C 1至C 4亚烷基，呋喃基-C 1至C 4亚烷基或苯基-C 1至C 4亚烷基; 且X为卤素; 或其药学上可接受的盐，以及其制备方法。新化合物是可用于生产具有抗生素活性的青霉素和头孢菌素的中间体。

78. 发明授权

US4486222A Herbicide composition and process for the preparation of the active ingredients herbicidal phenyl carbonates 失效
标题翻译：除草剂组合物和制备活性成分的方法除草苯基碳酸酯
公开(公告)号：US4486222A
公开(公告)日：1984-12-04
申请号：US469301
申请日：1983-02-24
申请人： Jozsef Schwartz , Marya Hornyak nee Hamori , Janos Sagi , Katalin Marmarosi nee Kellner , Erzsebet Radvanyi nee Hegedus , Zoltan Szigeti , Edit Cseh , Klara Bujtas nee Tolgyes
发明人： Jozsef Schwartz , Marya Hornyak nee Hamori , Janos Sagi , Katalin Marmarosi nee Kellner , Erzsebet Radvanyi nee Hegedus , Zoltan Szigeti , Edit Cseh , Klara Bujtas nee Tolgyes
IPC分类号： A01N37/34 , A01N47/06 , A01N47/22 , A01P13/00 , C07C255/53 , C07C329/00 , C07C121/75
CPC分类号： C07C255/00 , A01N47/06 , A01N47/22
摘要： New herbicidal compounds of the formula (I) ##STR1## wherein A is oxygen or sulfur;B is O-C.sub.1 to C.sub.4 alkyl, O-C.sub.2 to C.sub.6 alkenyl, O-C.sub.6 to C.sub.10 aryl, O-C.sub.1 to C.sub.4 -alkoxy-C.sub.1 to C.sub.4 alkyl, S-C.sub.1 to C.sub.4 alkyl or dimethylamino; andX is chloro, bromo or iodo, are disclosed, as well as herbicidal compositions containing said compounds.
摘要翻译：式（I）的新的除草化合物其中A是氧或硫; B为O-C1至C4烷基，O-C2至C6烯基，O-C6至C10芳基，O-C1至C4-烷氧基-C1至C4烷基，S-C1至C4烷基或二甲基氨基; 和X是氯，溴或碘，以及含有所述化合物的除草组合物。

79. 发明授权

US4419524A Process for the preparation of dihalovinylcyclopropanecarboxylic acids 失效
标题翻译：二卤乙烯基环丙烷羧酸的制备方法
公开(公告)号：US4419524A
公开(公告)日：1983-12-06
申请号：US350424
申请日：1982-02-19
申请人： Ferenc Lindwurm , Jozsef Muskovits , Sandor Zoltan , Rezso Kolta , Rudolf Soos , Tivadar Puskas , Eva Somfai , Gyorgy Hidasi
发明人： Ferenc Lindwurm , Jozsef Muskovits , Sandor Zoltan , Rezso Kolta , Rudolf Soos , Tivadar Puskas , Eva Somfai , Gyorgy Hidasi
IPC分类号： C07C61/40 , B01J31/02 , C07B61/00 , C07C27/02 , C07C51/00 , C07C51/09 , C07C67/00 , C07C69/743
CPC分类号： C07C51/09
摘要： The invention relates to a new process for the preparation of cyclopropanecarboxylic acids of the formula (I) ##STR1## wherein X and Y independently stand for halogen, by the alkaline hydrolysis of the corresponding alkyl esters having 1 to 6 carbon atoms in the alkyl moiety, in or without a water-miscible organic solvent, in the presence of a phase transfer catalyst. The hydrolysis is carried out with a 2 to 50% by weight aqueous alkali hydroxide solution. If desired, under suitable conditions the cis/trans ratio of the original ester can be altered in the end products. The cyclopropanecarboxylic acids of the formula (I) are obtained in a high purity and are useful intermediates of insecticidally active pyrethroids.
摘要翻译：本发明涉及一种制备式（I）的环丙烷羧酸的新方法，其中X和Y独立地代表卤素，通过碱性水解相应的具有1-6个碳原子的烷基酯在烷基部分，在或不与水混溶的有机溶剂中，在相转移催化剂的存在下。水解用2至50重量％的碱金属氢氧化物水溶液进行。如果需要，在合适的条件下，可以在最终产物中改变原始酯的顺式/反式比。式（I）的环丙烷羧酸以高纯度获得，是杀虫活性拟除虫菊酯的有用中间体。

80. 发明授权

US4395549A 6-Hydrazono-pyrido[2,1-b] quinazoline-11 ones 失效
标题翻译： 6-肼基 - 吡啶并[2,1-b]喹唑啉-11
公开(公告)号：US4395549A
公开(公告)日：1983-07-26
申请号：US308038
申请日：1981-10-02
申请人： Istvan Hermecz , Jozsef Kokosi , Agnes Horvath , Zoltan Meszaros , Gyorgy Szasz , Tibor Breining , Lelle Vasvari nee Debreczy
发明人： Istvan Hermecz , Jozsef Kokosi , Agnes Horvath , Zoltan Meszaros , Gyorgy Szasz , Tibor Breining , Lelle Vasvari nee Debreczy
IPC分类号： C07D487/04 , C07D487/14
CPC分类号： C07D487/04
摘要： Intermediates useful in the preparation of Rutecarpine and Rutecarpine derivatives are disclosed as well as a process for the preparation of said intermediates having the following formula: ##STR1## wherein R, R.sup.1 and R.sup.2 are the same or different and stand for hydrogen, halogen, nitro, carboxy, nitrile, alkoxy containing 1 to 4 carbon atoms, alkoxycarbonyl containing 1 to 4 carbon atoms in the alkoxy group, alkyl containing 1 to 4 carbon atoms, amino or hydroxy or R and R.sup.1 together stand for methylenedioxy, R.sup.2 stands for hydrogen, R.sup.3 represents hydrogen or alkyl containing 1 to 4 carbon atoms, R.sup.4 stands for phenyl, phenyl substituted by 1 to 3 same or different substituents selected from the group of halogen(s), alkyl, and alkoxy containing 1 to 4 carbon atoms, phenyloxy, hydroxy, nitro, amino, cyano, carboxy, alkoxycarbonyl having 1 to 4 carbon atoms, alkanoyl having 1 to 4 carbon atoms, methylenedioxy, trifluoromethyl, phenyl and dialkylamino having 1 to 4 carbon atoms in the alkyl part or naphthyl and the dotted line indicated an optional double bond. Also pharmaceutically acceptable acid addition and quaternary ammonium salts are disclosed.
摘要翻译：公开了用于制备罗非鱼和芦丁类衍生物的中间体以及制备具有下式的所述中间体的方法：其中R，R 1和R 2相同或不同并代表氢，卤素，硝基，羧基，腈，含有1至4个碳原子的烷氧基，烷氧基中含有1至4个碳原子的烷氧基羰基，含1至4个碳原子的烷基，氨基或羟基或R和R 1一起代表亚甲二氧基，对于氢，R 3表示氢或含有1至4个碳原子的烷基，R 4代表苯基，被1至3个相同或不同的取代基取代的苯基，所述取代基选自含1至4个碳原子的卤素，烷基和烷氧基，苯氧基，羟基，硝基，氨基，氰基，羧基，具有1至4个碳原子的烷氧基羰基，具有1至4个碳原子的烷酰基，亚甲二氧基，三氟甲基，苯基和在烷基中具有1至4个碳原子的二烷基氨基部分或萘基，虚线表示任选的双键。还公开了药学上可接受的酸加成盐和季铵盐。

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