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1.
溴化铜存在下,对异丁基苯丙酮(2)、乙二醇和过溴型三甲基苄铵树脂一锅反应转化成2-(1-溴乙基)-2-(4-异丁基苯基)-1,3-二氧戊环(3),再经重排、水解即得布洛芬(1),以异丁基苯丙酮计算,总收率88.7%。探讨了反应温度,溴化铜的用量对(3)收率的影响。还考察了添加不同Lewis酸对无水乙酸锌催化(3)重排时间的影响。  相似文献   

2.
溴化铜存在下,对异丁基苯丙酮(2)、乙二醇和过溴型三甲基苄铵树脂一锅反应转化成2-(1-溴乙基)-2-(4-异丁基苯基)-1,3-二氧戊环(3),再经重排、水解即得布洛芬(1),以异丁基苯丙酮计算,总收率88.7%。探讨了反应温度,溴化铜的用量对(3)收率的影响。还考察了添加不同Lewis酸对无水乙酸锌催化(3)重排时间的影响。  相似文献   

3.
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   

4.
ND-57依曲康唑(Itraconazole)顺-4-[4-[4-[4--[[2-(2,4-二氯苯基)-2-2(1H-1,2,4-三唑-1-基甲基)-1,3-二氧戊环-4-基]甲氧基]苯基]-1-哌嗪基]苯基]-2,4-二氢-2-(1-甲基丙基)-3...  相似文献   

5.
ND-58沙柏康唑(Saperconazole,R66905)顺-4-[4-[4-[4-[[2-(2,4-二氟苯基)2-(1H-1,2,4-三唑-1-基甲基)-1,3-二氧戊环-4-基]甲氧基]苯基]哌嗪基]苯基]-2,4-二氢-2-(1-甲基丙基)...  相似文献   

6.
以3-溴苯丙酮(2)为起始原料,经1,2-芳基重排,水解制得2-(3-溴苯基)丙酸(3)。再经羧基保护,格氏反应,水解,氧化即得酮基布洛芬(I),总收率43.7%。  相似文献   

7.
4-溴-3,5-二甲氧基苯甲酸的合成   总被引:2,自引:0,他引:2  
苄基嘧啶衍生物的重要中间体──4-溴-3,5-二甲氧基苯甲酸(1)可以对氨基苯甲酸(4)为起始原料,经溴化、甲氧基化、Sandmeyer反应制得,总收率达57%以上。  相似文献   

8.
1-(2,6-二甲基苯氧基)-2-(3,4-二甲氧基苯乙氨基)丙烷盐酸盐对兔血小板胞浆游离钙浓度的影响夏敬生,罗湘,曾繁典(同济医科大学临床药理研究室,武汉430030)1-(2,6-二甲基苯氧基)-2-(3,4-二甲氧基苯乙氨基)丙烷盐酸盐[1-(...  相似文献   

9.
合成了2-甲基-3-苯基-4-(2羟基-4-甲氧基)苯丁烯醇-2,并对其进行了GC-MS分析,结果在EI-MS(70eV)条件下具有284(5%)分子离子峰;进行了GC-MS分析时,当选择起始温度T=100℃,升温速度为30℃/min条件时,于6.3min分离出产物,并显示有266(10%)的分子离子峰,表明GC过程中发生了脱水。  相似文献   

10.
研究白细胞介素-1β(IL-1β)对牛脑微血管平滑肌细胞(BCSMC)增殖的影响。浓度为5~100ng·L-1的IL-1β与BCSMC共同孵育24h,即可明显诱导BCSMC的增殖,IL-1β浓度为50ng·L-1时,增殖率为17%。欧芹素乙,异欧芹素乙,6-(α,α-二苯基乙酰哌嗪基苯基-4,5-二氢-5-甲基-3(2H)-哒嗪酮(简称DMDP),6-(α-本基乙酰哌嗪基苯基)-4,5-二氢-5-甲基-3(2H)-哒嗪酮(简称PMDP)分别在不同浓度可显著抑制IL-1β所诱导的BCSMC增殖。  相似文献   

11.
合成了 2个二芳基碘离子氟硼酸盐衍生物 :双 (3 异丙基 4 甲氧基苯基 )碘离子氟硼酸盐 (Ⅰ )和双 (4 甲氧基苯基 )碘离子氟硼酸盐 (Ⅱ ) ,并进行了1H NMR测试 ,收率和纯度高于文献水平 .  相似文献   

12.
A series of 3,5‐disubstituted‐1,2,4‐oxadiazoles has been prepared and evaluated for phosphodiesterase inhibition (PDE4B2). Among the prepared 3,5‐disubstituted‐1,2,4‐oxadiazoles, compound 9a is the most potent inhibitor (PDE4B2 IC50 = 5.28 μm ). Structure–activity relationship studies of 3,5‐disubstituted‐1,2,4‐oxadiazoles revealed that substituents 3‐cyclopentyloxy‐4‐methoxyphenyl group at 3‐position and cyclic ring bearing heteroatoms at 5‐position are important for activity. Molecular modeling study of the 3,5‐disubstituted‐1,2,4‐oxadiazoles with PDE4B has shown similar interactions of 3‐cyclopentyloxy‐4‐methoxyphenyl group; however, heteroatom ring is slightly deviating when compared to Piclamilast. 3‐(3‐Cyclopentyloxy‐4‐methoxyphenyl)‐5‐(piperidin‐4‐yl)‐1,2,4‐oxadiazole ( 9a ) exhibited good analgesic and antiinflammatory activities in formalin‐induced pain in mice and carrageenan‐induced paw edema model in rat.  相似文献   

13.
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   

14.
目的建立利用仪器测定对氯苯氧异丁酸甲氧基苯丙烯酸酯(AZ)化学结构的方法。方法通过元素分析仪分析AZ的元素组成,并利用核磁共振谱(NMR)、质谱(MS)、红外光谱(IR)、紫外光谱(uV)进行结构分析。结果AZ的结构为E-4-(2-(4-氯苯氧基)-2-甲基-苯酰氧基-3-甲氧基-苯丙烯酸,元素组成为C20H19CIO6,相对分子质量为390.814。结论该方法准确可行,可为以后AZ的结构鉴定提供依据。  相似文献   

15.
The knowledge of pharmacokinetic (PK) properties of synthetic cannabinoids (SCs) is important for interpretation of analytical results found for example in intoxicated individuals. In the absence of human data from controlled studies, animal models elucidating SC PK have to be established. Pigs providing large biofluid sample volumes were tested for prediction of human PK data. In this context, the metabolic fate of two model SCs, namely 4‐ethylnaphthalen‐1‐yl‐(1‐pentylindol‐3‐yl)methanone (JWH‐210) and 2‐(4‐methoxyphenyl)‐1‐(1‐pentyl‐indol‐3‐yl)methanone (RCS‐4), was elucidated in addition to Δ9‐tetrahydrocannabinol (THC). After intravenous administration of the compounds, hourly collected pig urine was analyzed by liquid chromatography‐high resolution mass spectrometry. The following pathways were observed: for JWH‐210, hydroxylation at the ethyl side chain or pentyl chain and combinations of them followed by glucuronidation; for RCS‐4, hydroxylation at the methoxyphenyl moiety or pentyl chain followed by glucuronidation as well as O ‐demethylation followed by glucuronidation or sulfation; for THC, THC glucuronidation, 11‐hydroxylation, followed by carboxylation and glucuronidation. For both SCs, parent compounds could not be detected in urine in contrast to THC. These results were consistent with those obtained from human hepatocyte and/or human case studies. Urinary markers for the consumption of JWH‐210 were the glucuronide of the N ‐hydroxypentyl metabolite (detectable for 3–4 h) and of RCS‐4 the glucuronides of the N ‐hydroxypentyl, hydroxy‐methoxyphenyl (detectable for at least 6 h), and the O ‐demethyl‐hydroxy metabolites (detectable for 4 h). Copyright © 2016 John Wiley & Sons, Ltd.  相似文献   

16.
The feasibility of nucleophilic displacement of bromide in the 4‐bromopyrazole ring with [18F]fluoride has been demonstrated by the synthesis of two radiolabeled compounds: N‐(piperidin‐1‐yl)‐5‐(4‐methoxyphenyl)‐1‐(2‐chlorophenyl)‐4‐[18F]fluoro‐1H‐pyrazole‐3‐carboxamide, ([18F] NIDA‐42033) 1b and 1‐(2‐chlorophenyl)‐4‐[18F]fluoro‐5‐(4‐methoxyphenyl)‐1H‐pyrazole‐3‐carboxylic acid, ethyl ester 4 . The radiochemical yields were in the range of 1–6%. [18F]NIDA‐42033, a potential radiotracer for the study of CB1 cannabinoid receptors in the animal brain by positron emission tomography, has been synthesized in sufficient quantities with specific radioactivity greater than 2500 mCi/μmol and radiochemical purity >95%. Copyright © 2002 John Wiley & Sons, Ltd.  相似文献   

17.
羊红膻根中羊红膻素A及羊红膻素B的分离和鉴定   总被引:3,自引:0,他引:3  
从草药羊红膻(Pimpinela thelungiana Wolf)根中分得2个化合物,经光谱解析(UV,IR,MS,1HNMR,1H 1HCOSY,13CNMR,13C-1HCOSY和DEPT),鉴定为2-(1-ethoxy-2-hydroxy)propyl-4-methoxyphenol(I)和2-(1-ethoxy-2-hydroxy)propyl-4-methoxyphenyl-2-methyl-butyrate(II),分别命名为羊红膻素A及羊红膻素B,为2个新的天然产物,药理实验表明这2个新化合物均有较明显的降压活性。  相似文献   

18.
本实验探讨了内源性速激肽是否参与白三烯C4(LTC4)的气道效应.LTC4(0.5μgkg-1,iv)可增高豚鼠肺内压(IPP)和气道内依文思蓝渗出。速激肽NK-1受体拮抗剂CP-96345{(2S,3S)-顺式-2-(二苯甲基)-N-[(2-甲氧苯)-甲基]-1-杂氮双环[2.2.2]辛烷-3-胺}1mgkg-1,iv,可减弱LTC4诱导的依文思蓝渗出;NK-2受体拮抗剂SR-48968{(S)-N-甲基-N-[4-(4-乙酰氨基-4-苯基哌啶)-2-(3,4-二氯苯基)丁基]苯甲酰胺},1mgkg-1,iv,可抑制IPP的增高.白三烯拮抗剂ONO-1078(0.03mgkg-1,iv)可阻断这两种反应.结果说明内源性速激肽增强LTC4的气道作用,其中NK-1受体介导微血管渗漏,NK-2受体介导支气管收缩.  相似文献   

19.
Exposure of 4-methoxy-2-(3-phenyl-2-propynyl)phenol (CO/1828) to air and light (accelerated by temperature) yields 1-(2-hydroxy-5- methoxyphenyl)-3-phenylpropynone as the major degradation product. With extraction, this product rapidly degrades to 5-methoxyaurone and 6-methoxyflavone. In addition, a mixture of dimeric and heterodimeric compounds that are not fully identified was observed. These results indicate the formation of a reactive ortho-quinone methide as an unstable intermediate. This hypothesis is supported by evidence that the aurone slowly isomerizes into the flavone in control samples. Identification of compounds was accomplished with mass spectrometry, nuclear magnetic resonance spectrometry, UV-high-performance liquid chromatography, and comparison with authentic samples.  相似文献   

20.
Sixteen 3‐aryl‐5‐(4‐fluorophenyl)‐N‐substituted‐4,5‐dihydro‐1H‐pyrazole‐1‐carbothioamide derivatives were synthesized and their structure were identified by UV, IR, 1H NMR, mass spectra, and microanalyses. The compounds were evaluated in vitro for their human monoamine oxidase (hMAO) inhibitory activities and their MAO‐A and ‐B selectivity. All the compounds were found to potently inhibit MAO‐A isoforms. 5‐(4‐Fluorophenyl)‐3‐(4‐methoxyphenyl)‐N‐methyl‐4,5‐dihydro‐1H‐pyrazole‐1‐carbothioamide (1.0 × 10?3 µM) was found to inhibit hMAO‐A most selectively and potently. The binding mode of 5‐(4‐fluorophenyl)‐3‐(4‐methoxyphenyl)‐N‐methyl‐4,5‐dihydro‐1H‐pyrazole‐1‐carbothioamide to hMAO‐A was also predicted using docking studies.  相似文献   

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