专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US5521320A Process for the enantioselective synthesis of intermediates used in the preparation of physostigmine 失效
标题翻译：用于制备毒扁豆碱的中间体的对映选择性合成方法
公开(公告)号：US5521320A
公开(公告)日：1996-05-28
申请号：US67892
申请日：1993-05-27
申请人： Thomas B. K. Lee , George S. K. Wong
发明人： Thomas B. K. Lee , George S. K. Wong
IPC分类号： C07B57/00 , C07D209/10 , C07D209/34
CPC分类号： C07D209/34
摘要： This invention relates to a process of obtaining optically pure enantiomers of an alkylated oxindole selected from ##STR1## where R is methyl, ethyl or benzyl.
摘要翻译：本发明涉及一种获得烷基化羟吲哚的旋光纯对映异构体的方法，其中R是甲基，乙基或苄基。

2. 发明授权

US4118401A Preparation of 6,11-dihydro-11-oxodibenz[b,e]oxepin-2-acetic acid and precursors therefor 失效
标题翻译：制备6,11-二氢-11-氧代二苯并[b，e {9氧杂环庚烯-2-乙酸及其前体
公开(公告)号：US4118401A
公开(公告)日：1978-10-03
申请号：US843482
申请日：1977-10-19
申请人： Arthur R. McFadden , Richard C. Allen , Thomas B. K. Lee
发明人： Arthur R. McFadden , Richard C. Allen , Thomas B. K. Lee
IPC分类号： A61K31/335 , A61P25/04 , A61P29/00 , C07D295/185 , C07D313/12
CPC分类号： C07D295/185 , C07D313/12
摘要： A process, and intermediates for the preparation of 6,11-dihydro-11-oxodibenz[b,e]oxepin-2-acetic acid are described. The acid possesses antiinflammatory and analgesic activity.
摘要翻译：描述了制备6,11-二氢-11-氧代二苯并[b，e]氧杂七环素-2-乙酸的方法和中间体。酸具有抗炎和镇痛作用。

3. 发明授权

US5677457A Method of preparation of physostigmine carbamate derivatives from eseroline ethers 失效
标题翻译：从七叶皂甙醚制备毒扁豆烷氨基甲酸酯衍生物的方法
公开(公告)号：US5677457A
公开(公告)日：1997-10-14
申请号：US769409
申请日：1996-12-19
申请人： Thomas B. K. Lee , Zhongli Gao , Barbara S. Rauckman
发明人： Thomas B. K. Lee , Zhongli Gao , Barbara S. Rauckman
IPC分类号： C07D487/04 , C07D487/00
CPC分类号： C07D487/04
摘要： The present invention relates to a novel process for the preparation of physostigmine carbamate derivatives and to pharmaceutically acceptable salts thereof. The present invention further relates to a novel process for the preparation of eseroline derivatives and to pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及一种制备毒扁豆蛋白氨基甲酸酯衍生物及其药学上可接受的盐的新方法。本发明进一步涉及一种制备甲胎磷衍生物及其药学上可接受的盐的新方法。

4. 发明授权

US5498726A Preparation of physostigmine carbamate derivatives from physostigmine 失效
标题翻译：从毒扁豆碱制备毒扁豆碱氨基甲酸酯衍生物
公开(公告)号：US5498726A
公开(公告)日：1996-03-12
申请号：US216238
申请日：1994-03-22
申请人： George E. Lee , Thomas B. K. Lee , Donna M. Borek
发明人： George E. Lee , Thomas B. K. Lee , Donna M. Borek
IPC分类号： A61K31/40 , A61P25/04 , A61P25/28 , C07D20060101 , C07D487/04 , C07D487/00
CPC分类号： C07D487/04
摘要： This application relates to a new process for the preparation of a product of the formula ##STR1## wherein R, R.sup.1, R.sup.2, X and m are as defined within, which process comprises preparing treating a compound such as physostigmine to form eseroline which is then treated with an appropriate compound or its equivalent. Acetic acid is added to the reaction mixture after the formation of eseroline.
摘要翻译：本申请涉及制备式（I）的产物的新方法，其中R，R 1，R 2，X和m如上所定义，该方法包括制备治疗化合物如毒扁豆素以形成eseroline 然后用合适的化合物或其等同物处理。在形成eseroline后，将乙酸加入到反应混合物中。

5. 发明授权

US5302721A Method of preparation of physostigmine carbamate derivatives from eseretholes 失效
标题翻译：从eseretholes制备毒扁豆碱氨基甲酸酯衍生物的方法
公开(公告)号：US5302721A
公开(公告)日：1994-04-12
申请号：US918337
申请日：1992-07-21
申请人： George S. K. Wong , Thomas B. K. Lee , Franz J. Weiberth
发明人： George S. K. Wong , Thomas B. K. Lee , Franz J. Weiberth
IPC分类号： A61K31/40 , A61P25/04 , A61P25/28 , C07D209/02 , C07D487/04
CPC分类号： C07D487/04
摘要： This application relates to a new process for the preparation of a product of the formula ##STR1## wherein R is loweralkyl;R.sup.1 is hydrogen, loweralkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralkyl;R.sup.2 is loweralkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralkyl; orR.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached from a 3,4-dihydro-2H(1H)-isoquinoline group;X is loweralkyl, loweralkoxy, halogen or trifluoromethyl; andm is 0, 1 or 2;which process comprises(a) contacting a compound of formula II ##STR2## wherein R, X and m are as defined above and R.sup.3 is loweralkyl, with aluminum chloride followed by tartaric acidto afford a compound of formula III ##STR3## wherein R, X and m are as defined above; (b) contacting the reaction mixture containing the compound of Formula III either(1) with an isocyanate of the formula R.sup.1 NCO and obtaining a product of the formula I wherein R.sup.2 is hydrogen; or(2) with a compound of formula IV ##STR4## wherein R.sup.4 is hydrogen or loweralkyl in the presence of a carboxylic acid of the formulaR.sup.5 COOH wherein R.sup.5 is loweralkyl to afford a compound of formula V ##STR5## wherein R, R.sup.4, X and m are as above; contacting the reaction mixture containing the compound of Formula V with a compound of the formulaR.sup.1 R.sup.2 NH wherein R.sup.1 and R.sup.2 are as above; andisolating the product of Formula I.
摘要翻译：本申请涉及制备式（*化学结构*）（I）的产物的新方法，其中R是低级烷基; R 1是氢，低级烷基，低级环烷基，低级环烷基低级烷基，低级双环烷基，芳基或芳基低级烷基; R2是低级烷基，低级环烷基，低级环烷基低级烷基，低级双环烷基，芳基或芳基低级烷基; 或者R 1和R 2与它们所连接的氮原子一起与3,4-二氢-2H（1H） - 异喹啉基组合; X是低级烷基，低级烷氧基，卤素或三氟甲基; m为0,1或2; 该方法包括（a）使式II化合物（*化学结构*）（II）与其中R，X和m如上定义并且R3是低级烷基的化合物与氯化铝接触，然后与酒石酸接触，得到式III化合物（*化学结构*）（III）其中R，X和m如上所定义; （b）将含有式III化合物的反应混合物与式（1）的异氰酸酯与式R1NCO的异氰酸酯接触，得到其中R 2为氢的式I化合物; 或（2）式IV化合物（*化学结构*）（Ⅳ）其中R 4为氢或低级烷基，在式R 5 COOH的羧酸存在下，其中R 5为低级烷基，得到式Ⅴ化合物（* CHEMICAL 结构*）（V）其中R，R4，X和m如上所述; 将含有式V化合物的反应混合物与式R 1 R 2 NH的化合物接触，其中R 1和R 2如上所述; 并分离式I的产物。

6. 发明授权

US5053513A Method of reducing a carbonyl containing acridine 失效
标题翻译：减少含有亚油酸的方法
公开(公告)号：US5053513A
公开(公告)日：1991-10-01
申请号：US500967
申请日：1990-03-29
申请人： Thomas B. K. Lee , George E. Lee , George S. K. Wong , Donna M. Borek , Keith E. Goehring
发明人： Thomas B. K. Lee , George E. Lee , George S. K. Wong , Donna M. Borek , Keith E. Goehring
IPC分类号： B01J23/40 , C07B61/00 , C07D219/08 , C07D219/10 , C07D221/16
CPC分类号： C07D219/10
摘要： A method of reducing a carbonyl containing acridine of the formula ##STR1## where n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, trifluoromethyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl and R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl, is disclosed.

7. 发明授权

US4211877A Method of preparation of isopropyl 4,10-dihydro-10-oxothieno[3,2-c][1]benzoxepin-8-acetate 失效
标题翻译：制备4,10-二氢-10-氧代噻吩并[3,2-c] [1]苯并氧杂七环素-8-乙酸异丙酯的方法
公开(公告)号：US4211877A
公开(公告)日：1980-07-08
申请号：US11943
申请日：1979-02-13
申请人： Thomas B. K. Lee
发明人： Thomas B. K. Lee
IPC分类号： C07D495/04 , C07D495/02
CPC分类号： C07D495/04
摘要： Isopropyl 4,10-dihydro-10-oxothieno[3,2-c][1]benzoxepin-8-acetate is synthesized from 4-(2-carboxy-3-thienylmethoxy)phenylacetic acid by a process comprising acid halide formation, ring closure catalyzed by aluminum trihalide and esterification with isopropyl alcohol. The three reaction steps are carried out successively in the same reactor without any isolation or purification of intermediate products and a surprisingly high overall yield is obtained. Additionally, a valuable chemical, aluminum isopropoxide is obtained as a by-product of this process and significant advantages in terms of environmental pollution and waste water costs are achieved.
摘要翻译：由4-（2-羧基-3-噻吩基甲氧基）苯乙酸通过包含酰卤化合物的方法合成4,10-二氢-10-氧代噻吩并[3,2-c] [1]苯并氧杂七环素-8-乙酸异丙酯，封闭由三卤化铝催化并用异丙醇酯化。三个反应步骤在相同的反应器中连续进行，无需中间产物的任何分离或纯化，并且获得惊人的高总产率。此外，作为该方法的副产物，获得了有价值的化学物质异丙醇铝，并且在环境污染和废水成本方面实现了显着的优点。

8. 发明授权

US4153790A 4-Benzyloxy-3-(benzyloxy carbonyl)phenylthioacetmorpholide 失效
标题翻译： 4-苄氧基-3-（苄氧羰基）苯硫基乙酰吗啉
公开(公告)号：US4153790A
公开(公告)日：1979-05-08
申请号：US939177
申请日：1978-09-05
申请人： Arthur R. McFadden , Richard C. Allen , Thomas B. K. Lee
发明人： Arthur R. McFadden , Richard C. Allen , Thomas B. K. Lee
IPC分类号： A61K31/335 , A61P25/04 , A61P29/00 , C07D295/185 , C07D313/12 , C07D295/18
CPC分类号： C07D295/185 , C07D313/12
摘要： A process, and intermediates for the preparation of 6,11-dihydro-11-oxodibenz[b,e]oxepin-2-acetic acid are described. The acid possesses antiinflammatory and analgesic activity.
摘要翻译：描述了制备6,11-二氢-11-氧代二苯并[b，e]氧杂七环素-2-乙酸的方法和中间体。酸具有抗炎和镇痛作用。

9. 发明授权

US4709093A Method for the preparation of 4-phenyl-1,3-benzodiazepines and precursors thereof 失效
标题翻译： 4-苯基-1,3-苯并二氮杂的制备方法及其前体
公开(公告)号：US4709093A
公开(公告)日：1987-11-24
申请号：US757765
申请日：1985-07-23
申请人： Thomas B. K. Lee , George E. Lee
发明人： Thomas B. K. Lee , George E. Lee
IPC分类号： C07D243/04 , C07C103/44
CPC分类号： C07D243/04
摘要： A compound of the formula ##STR1## is prepared by reacting an N-acylated-o-toluidine of the formula ##STR2## with n-alkyllithium to form a dilithio intermediate of the formula ##STR3## which can then be quenched with N-benzylidenemethylamine to form compound II. Hydrolysis of compound(II)yields the free base ##STR4## or its salt, which can be cyclized to form 4,5-dihydro-2,3-dimethyl-4-phenyl-3H-1,3-benzodiazepine or its physiologically acceptable salts, which are useful as pharmacological agents.
摘要翻译：通过使式（III）的N-酰化的邻甲苯胺与正烷基锂反应以形成式（IV）的二元中间体制备式（II）化合物：然后用N-亚苄基甲基胺淬灭以形成化合物II。化合物（II）的水解产生游离碱（V）或其盐，其可以环化形成4,5-二氢-2,3-二甲基-4-苯基-3H-1,3-苯并二氮杂或其生理上可接受的盐，其可用作药理学试剂。

10. 发明授权

US4461728A Preparation of 4-phenyl-1,3-benzodiazepins 失效
标题翻译：制备4-苯基-1,3-苯并二氮杂
公开(公告)号：US4461728A
公开(公告)日：1984-07-24
申请号：US441128
申请日：1982-11-12
申请人： Thomas B. K. Lee , George E. Lee
发明人： Thomas B. K. Lee , George E. Lee
IPC分类号： C07C233/07 , C07D243/04 , C07C103/375
CPC分类号： C07C233/07 , C07D243/04
摘要： The invention relates to compounds of the formula ##STR1## where Y is --OH; halogen; ##STR2## where R.sub.1 is a straight chain or branched chain alkyl group having 1 to 5 carbon atoms, or aryl; and R.sub.2 is --C(CH.sub.3).sub.3 or --O--C(CH.sub.3).sub.3. Processes for preparing the compounds are provided. The compounds are useful as intermediates in the preparation of 4-phenyl-1,3-benzodiazepins, which exhibit activity as antidepressants, analgetics and anticonvulsants.
摘要翻译：本发明涉及式（I）的化合物，其中Y是-OH; 卤素; 其中R 1是具有1至5个碳原子的直链或支链烷基或芳基; 并且R 2是-C（CH 3）3或-O-C（CH 3）3。提供了制备化合物的方法。该化合物可用作制备4-苯基-1,3-苯并二氮杂的中间体，其表现出抗抑郁药，止痛药和抗惊厥药的作用。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式