CAS: 623-08-5; N,4-Dimethylaniline

上下游产品

diazomethane p-toluidinep-toluidine methyl magnesium iodide diethyl etherN-methyl-p-toluidino)-pentamethinium ; bromide1,5-bis-(N-methyl-p-toluidino)-pentamethinium ; bromide 1,4,6-trimethylquinolin-2(1H)-one N-methyl-N-(4-methylphenyl)carbamoyl chloride N-methyl-N-(p-tolyl)benzo[d]thiazol-2-amine

4-甲基乙酰苯胺置于盐酸,Sodium Hydride体系中,用 四氢呋喃,水,乙二醇 作为反应溶剂,化学反应 7.0H,反应生成 N-甲基-对甲基苯胺
参考文献:具有双重雌激素受体α降解和组蛋白脱乙酰酶抑制活性的新型混合偶联物用于乳腺癌治疗
标题:具有双重雌激素受体α降解和组蛋白脱乙酰酶抑制活性的新型混合偶联物用于乳腺癌治疗
摘要:以雌激素受体为靶点的激素疗法在临床上广泛用于治疗乳腺癌,如他莫昔芬,但多为部分激动剂,长期使用会引起严重的副作用.选择性雌激素受体下调剂 (Serd) 的使用可能是乳腺癌治疗的有效替代方案,通过直接降解 Erα 蛋白来关闭 Erα 信号传导.然而,临床上单独使用的serd氟维司群,口服生物利用度低,需要静脉注射,严重限制了其临床应用.另一方面,双靶点或多靶点偶联物能够通过不同途径协同抗肿瘤活性,因此与单一靶向治疗相比可以提高治疗效果.在这项研究中,我们通过将特权 Serd 骨架 7-氧杂双环 [2.2.1] 庚烷磺酰胺 (Obhsa) 与组蛋白脱乙酰酶抑制剂侧链相结合,设计并合成了一系列针对 Erα 降解和组蛋白脱乙酰酶抑制的新型双功能偶联物.我们发现obhsa单元的磺酰胺氮和苯基上的取代基对生物活性有显着影响.其中,共轭具有n-甲基和萘基的16I对 Mcf-7 细胞表现出有效的抗增殖活性,以及优异的
DOI:10.1016/j.Bmc.2021.116185

专利信息

专利号:US-9932280-B2
优先权日:2013-05-13
标 题:Synthesis of olefins from oxygen-free direct conversion of methane and catalysts thereof
发明人：BAO XINHE; GUO XIAOGUANG; FANG GUANGZONG; DENG DEHUI; MA HAO; TAN DALI
权利人:DALIAN INST CHEM & PHYSICS CAS
摘要:Provided is a method for the preparation of a metal lattice-doping catalyst in an amorphous molten state, and the process of catalyzing methane to make olefins, aromatics, and hydrogen using the catalyst under oxygen-free, continuous flowing conditions. Such a process has little coke deposition and realizes atom-economic conversion. Under the conditions encountered in a fixed bed reactor (i.e. reaction temperature: 750Ëœ1200° C.; reaction pressure: atmospheric pressure; the weight hourly space velocity of feed gas: 1000Ëœ30000 ml/g/h; and fixed bed), conversion of methane is 8-50%. The selectivity of olefins is 30Ëœ90%. And selectivity of aromatics is 10Ëœ70%. There is no coking. The reaction process has many advantages, including a long catalyst life (>100 hrs), high stability of redox and hydrothermal properties under high temperature, high selectivity towards target products, zero coke deposition, easy separation of products, good reproducibility, safe and reliable operation, etc., all of which are very desirable for industrial application.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人：MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:US-4092329-A
优先权日:1972-12-01
标 题:Process for the synthesis of certain 2-amino-5-cyanothiophenes
发明人：JOTTERAND ARMAND
权利人:SANDOZ LTD
摘要:The invention relates to a process which comprises reacting a compound of formula I, ##STR1## in which A 1 is a radical which does not compete with the activity of the ##STR2## OR A TAUTOMER THEREOF, WITH A COMPOUND OF FORMULA II, n n a.sub.2 -- ch.sub.2 -- cn ii n n in which A 2 is a radical which does not compete with the activity of the --CH 2 CN group of the compound of formula II but provides the vicinal methylene group with sufficient acidity to react with the â•?NH group of the compound of formula I, n and with sulphur, n To obtain a compound of formula III, ##STR3## in which A 1 and A 2 are as defined above, which compounds of formula III are useful as intermediates for the production of dyestuffs.

专利号:WO-2015058868-A1
优先权日:2013-10-25
标题 :Compositions and methods for the treatment of cancer
发明人：JIMENO DOÑAQUE JOSÉ Mª
权利人:PANGAEA BIOTECH S L
摘要:The invention relates to anti-tumor compounds which have been designed to functionally disrupt the cross-talk between AEG-1 and the p65 subunit of NF-κB. Therefore, the invention relates to methods and compositions for the treatment of cancer using the compounds identified in the present invention, as well as compositions adequate for sustained release of the compounds of the invention to be administered to the surgical site after resection of the tumor. The invention also provides methods for the synthesis of the compounds of the invention.

专利号:US-9040480-B2
优先权日:2006-02-08
标题:Synthesis of glucagon-like peptide
发明人：WERBITZKY OLEG; VARRAY STÉPHANE; GIRAUD MATTHIEU; MEININGHAUS CARSTEN
权利人:LONZA AG
摘要:A new method of synthesizing GLP-1 peptide is devised.

专利号:US-8933227-B2
优先权日:2009-08-14
标题 :Selective synthesis of functionalized pyrimidines
发明人：LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN
权利人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN; BOEHRINGER INGELHEIM INT
摘要:The present invention relates to a process for making 2,4-differentiated 5-trifluoromethyl pyrimidines and 2-amino-5-trifluoromethyl-pyrimidine derivatives, which compounds are useful in the preparation of pharmacologically active compounds.