共查询到19条相似文献,搜索用时 125 毫秒
1.
溴化铜对芳基烷基酮的选择性溴化反应研究 总被引:16,自引:2,他引:16
研究溴化铜对苯丙酮、间-氯苯丙酮、6-甲氧基-2-丙酰基萘、6-甲氧基-2-乙酰基萘、对-甲氧基苯乙酮和苯乙酮等芳基烷基酮的α-溴化反应,在乙醇或乙酸乙酯-氯仿混合溶剂中,溴化铜对芳基丙酮(苯丙酮、间-氯苯丙酮和6-甲氧基-2-丙酰基萘)溴化,高收率、高选择性地得到α-溴化产物。芳基乙酮(6-甲氧基-2-乙酰基萘、对-甲氧基苯乙酮和苯乙酮)的溴化铜溴化,在乙醇中反应,选择性得到α-溴化产物。 相似文献
2.
采用1,3-二溴-5,5-二甲基乙丙酰脲作催化剂,在丙酮溶剂中,以盐酸作催化剂,于室温快速(8min)、高收率(96%)地对2-甲氧基萘的萘环进行溴化,再经乙酰化、Bucherer-Berg环化和水解反应,制得萘普生中间体2-氨基-2-(5-溴-6-甲氧基-2-萘基)丙酸。并对环化反应的条件进行了优化,反应总收率68%。 相似文献
3.
2—甲氧基荼通过溴化、丙酰化和脱溴三步反应合成了6—甲氧基—2—萘丙酮。研究并优化了溴化反应中溶剂的用量和丙酰化的工艺条件。结果表明,经优化工艺能明显减少溴化反应的溶剂用量,6—甲氧基—2—萘丙酮的得率达到87.8%。 相似文献
4.
马英 《中国现代应用药学》1997,(Z1):66-67
以二氯乙烷和硝基甲烷代替硝基苯作为制备6-甲氧基-2-丙酰基萘(1)的溶剂,革除了毒性较大的硝基苯.改进后的工艺操作方便,产物收率高,质量也有明显提高.是一种适合工业生产的方法。 相似文献
5.
6.
7.
8.
dl—萘普生重排合成的工艺研究 总被引:9,自引:3,他引:6
以2-甲氧基萘为起始原料,通过丙酰化、溴化、缩酮化、重排及水解制成2-(5-溴-6-甲氧基-2-萘基)丙酸,再经催化转移氢解脱溴即得萘普生。工艺简便,反应条件温和,总收率达74%。 相似文献
9.
10.
研究1-[1-(6-甲氧基-2-萘基)乙基]-2-(4-硝基苄基)-6,7-二甲氧基-1,2,3,4-四氢异喹啉氢溴酸盐(编号P91024)遇光后颜色变暗的光降解产物。采用HPLC-MS及波谱分析鉴定光降解产物的化学结构,并经有机反应合成对照验证。P91024光降解的3个主要产物分别为溴化N-(4-硝基苄基)-6,7-二甲氧基-3,4-二氢异喹啉、1-[1-(6-甲氧基-2-萘基)乙基]-6,7-二甲氧基-1,2,3,4-四氢异喹啉和2-异丙基-6-甲氧基萘。 相似文献
11.
通过滴加溴化铜的甲醇溶液,6-甲氧在-2-丙酰萘在均相体系中回流,可高选择性地溴化,得到合成非甾体消炎镇痛药萘普生的关键中间体1-氧代-1-(6-甲基氧-2-萘基)-2溴丙烷,收率92.8%。 相似文献
12.
以2-甲氧基萘为起始原料,经二溴化、脱溴、偶联、缩酮化、重排、水解得dl-萘普生(1),以2-甲氧基萘计算,总收率为77%。 相似文献
13.
14.
15.
Karel Waisser Josef Matyk Jirí Kuneš Rafael Doležal Jarmila Kaustová Hans‐Martin Dahse 《Archiv der Pharmazie》2008,341(12):800-803
A series of 6‐chloro‐3‐(4‐alkylphenyl)‐4‐thioxo‐2H‐1,3‐benzoxazine‐2(3H)‐ones, 7‐chloro‐3‐(4‐alkylphenyl)‐4‐thioxo‐2H‐1,3‐benzoxazine‐2(3H)‐ones, 6‐bromo‐3‐(4‐alkylphenyl)‐4‐thioxo‐2H‐1,3‐benzoxazine‐2(3H)‐ones, 6,8‐dibromo‐3‐(4‐alkylphenyl)‐4‐thioxo‐2H‐1,3‐benzoxazine‐2(3H)‐ones, 6‐chloro‐3‐(4‐alkylphenyl)‐2H‐1,3‐benzoxazine‐2,4(3H)‐dithiones, 7‐chloro‐3‐(4‐alkylphenyl)‐2H‐1,3‐benzoxazine‐2,4(3H)‐dithiones, 6‐bromo‐3‐(4‐alkylphenyl)‐2H‐1,3‐benzoxazine‐2,4(3H)‐dithiones and 6,8‐dibromo‐3‐(4‐alkylphenyl)‐2H‐1,3‐benzoxazine‐2,4(3H)‐dithiones was synthesized. The compounds exhibited in‐vitro activity against Mycobacterium tuberculosis, M. kansasii (two strains), and M. avium. 6‐bromo‐3‐(4‐propylphenyl)‐4‐thioxo‐2H‐1,3‐benzoxazin‐2(3H)‐one and 6‐bromo‐3‐(4‐propylphenyl)‐2H‐1,3‐benzoxazin‐2,4(3H)‐dithione are the most active compounds against M. tuberculosis. The activity is similar to isoniazid (INH). The compounds under study have a broad spectrum of activity against potential pathogenic strains. The replacement of the oxo group by thioxo group of 3‐(4‐alkylphenyl)‐2H‐1,3‐benzoxazine‐2,4(3H)‐diones often led to an improvement in the antimycobacterial activity against M. tuberculosis. 相似文献
16.
Fengjiun Kuo Dean K. Clodfelter Tamara R. Priest 《Journal of labelled compounds & radiopharmaceuticals》2007,50(8):706-710
Carbon‐14‐labeled 6‐(4‐methanesulfonylphenyl)‐5‐[4‐(2‐piperidin‐1‐yl‐ethoxy)phenoxy]naphthalen‐2‐ol, a novel selective estrogen receptor modulator (SERM) was synthesized. The key component, 6‐methoxy‐1‐tetralone‐[carbonyl‐14C], was synthesized from 3‐(3‐methoxyphenyl)‐propionic acid via an intra‐molecular Friedel–Crafts acylation of 4‐(3‐methoxyphenyl)butanoic acid‐[carboxy‐14C]. A palladium catalyzed alpha‐keto arylation of 6‐methoxy‐1‐tetralone with 4‐methanesulfonyl‐phenyl bromide, followed by a sequence of bromination, DDQ dehydrogenation, aryl Ullmann reaction, and demethylation with BBr3 gave the desired product LY2066948‐[14C]. Copyright © 2007 John Wiley & Sons, Ltd. 相似文献
17.
ZJ0273 (propyl 4‐(2‐(4,6‐dimethoxypyrimidin‐2‐yloxy)benzylamino)benzoate), ZJ0702 (isopropyl 4‐(2‐(4,6‐dimethoxypyrimidin‐2‐yloxy)benzylamino)benzoate), ZJ0777 (2‐bromo‐N‐(2‐(4,6‐dimethoxypyrimidin‐2‐yloxy)benzyl)aniline), and SIOC0163 (5‐bromo‐N‐(2‐(4,6‐dimethoxypyrimidin‐2‐yloxy)benzyl)pyridin‐2‐amine) are active ingredients in oilseed rape herbicides. The middle aromatic ring‐deuterated form of ZJ0273 was synthesized from (2H6)phenol and have been successfully used as tracer in its metabolism and degradation study. The methoxyl‐deuterated forms of four ingredients were synthesized from (2H4)methanol, respectively, and they could be used as internal standards in quantitation of herbicide residue in rapeseed and its downstream foodstuff by using HPLC‐MS/MS. Copyright © 2010 John Wiley & Sons, Ltd. 相似文献
18.
2- ( 6-甲氧基 - 2 -萘基 )丙醛 ( 1 ) ,简称萘丙醛 ,系Darzens缩合法制备非甾体消炎镇痛药萘普生的关键中间体。可用酸性脱羧法合成[1,2 ] ,即以异丙醇为介质 ,在异丙醇钠催化下 ,用 6-甲氧基 - 2 -乙酰萘 ( 2 )与氯乙酸异丙酯反应得到缩水甘油酸酯 3,不经分离加入一定量的氢氧化钠溶液 ,水解得缩水甘油酸钠盐 4,回收异丙醇后 ,加入水及盐酸 ,脱羧后得到1。此法原料易得、操作简便 ,但在脱羧阶段需用大量盐酸中和水解时过量的氢氧化钠 ,这一过程放热剧烈 ,使温度难以控制在所要求的范围内 ,致使 1的质量不稳定 ,经常出现无法固化的现象 ,… 相似文献
19.
E Pogonowska 《Polish journal of pharmacology and pharmacy》1975,27(2):217-226
Distribution and elimination constants, half-times, plasma clearance and volume of distribution for 2-p-methoxy (AID) and 2-p-bromophenylindandione-1,3 (Br-PID) were estimated, basing on a two-compartment open pharmacokinetic models. Differences were found when similar processes of distribution and elimination of PID and its p- chloro, bromo and methoxy derivatives were compared. 相似文献