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CAS号607-68-1 2,4-二氯喹唑啉 | CAS号32315-10-9 三光气 | CAS号529-23-7 邻氨基苯甲醛 | CAS号204520-39-8 4-(α-methyl-α-h... | CAS号1336-21-6 氨水 | CAS号7471-58-1 3-(氯甲基)-6-(三氟甲基)吡啶 | CAS号86-96-4 2,4-喹唑啉二酮 | CAS号187336-10-3 2-chloro-4-(p-b... | CAS号43120-25-8 1-benzyl-1H-indazole | CAS号67-66-3 氯仿 | CAS号7471-58-1 3-(氯甲基)-6-(三氟甲基)吡啶 | CAS号36265-27-7 quinazolin-2-yl... | CAS号1687-51-0 2-氨基喹唑啉 | CAS号25855-20-3 2-phenylquinazoline | CAS号67092-26-6 2-piperidin-1-y... | CAS号6141-15-7 2-Methoxyquinazoline | CAS号62284-31-5 2-benzylquinazoline | CAS号51047-61-1 2-(哌嗪-1-基)喹唑啉📜2,4-喹唑啉二酮置于氨,二乙胺,Sodium Chloride,锌,三氯氧磷体系中,用 二氯甲烷,水 作为反应溶剂,化学反应 0.5H,反应生成 2-氯喹唑啉
参考文献:微波辅助合成喹啉,异喹啉,喹喔啉和喹唑啉衍生物作为cb2受体激动剂
标题:微波辅助合成喹啉,异喹啉,喹喔啉和喹唑啉衍生物作为cb2受体激动剂
摘要:使用微波辅助合成法合成喹啉,异喹啉,喹喔啉和喹唑啉衍生物,并使用[35 S]Gtpγs结合测定法测定其cb1 / Cb2受体活性.大部分制备的喹啉,异喹啉和喹喔啉基苯胺均显示出低效的部分cb2受体激动剂活性.最有效的cb2配体是4-吗啉基甲酮衍生物(化合物40E)(-Log Ec 50 = 7.8;e Max = 75%).异喹啉-1-基(3-三氟甲基-苯基)胺(化合物26C)是一种高效的cb2激动剂(-Log Ec 50 = 5.8; E Max = 128%).在这些研究中,没有发现明显的cb1受体激活或失活,除了40E表现出弱的cb1激动剂活性(cb1-Log Ec 50 = 5.0).这些配体用作开发选择性cb2受体激动剂的新型模板.
DOI:10.1016/j.Bmc.2010.11.059
专利信息
专利号:US-7825244-B2
优先权日:2005-06-10
标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis
发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG
权利人:JANSSEN PHARMACEUTICA NV
摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
专利号:US-6080860-A
优先权日:1992-08-31
标 题:Methods of making ureas and guanidines including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor
发明人:KARIMIAN KHASHAYAR; MURTHY KESHAVA; HALL DARREN
权利人:BRANTFORD CHEMICALSS INC
摘要:Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediates suitable for use in such methods of synthesis are taught.
专利号:US-5304647-A
优先权日:1988-02-09
标题:Method of preparation of halogenated diazines
发明人:STREKOWSKI LUCJAN; MOKROSZ MARIA; HARDEN DONALD B
权利人:UNIV GEORGIA STATE
摘要:A method of preparation of substituted halogenodiazines which are useful as intermediates in the synthesis of novel unfused heterobicyclic compounds, and the products thereof. The reaction consists of the addition of an organolithium reagent with subsequent dehydrogenation of the addition product. The reaction takes place in one reaction vessel, without isolation of the substituted halogenodihydrodiazine intermediate. The reactions proceed at moderate temperature and in a short amount of time, which decreases the probability of side reactions and increases yield. Furthermore, the workup step is conducted under two-phase conditions to prevent hydrolysis of the substituted halogenodiazine to a substituted hydroxydiazine. The method is easy, efficient and results in a high yield of product. The substituted halogenodiazines are used as intermediates in the synthesis of unfused heterobicyclic compounds containing an aromatic moiety, diazine, and another aromatic moiety, such as thiophene, benzene, or naphthalene, which have biological activity.
专利号:US-6930113-B2
优先权日:1996-11-01
标题 :Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use
发明人:GARVEY DAVID S; DE TEJADA INIGO SAENZ; EARL RICHARD A; KHANAPURE SUBHASH P
权利人:NITROMED INC
摘要:The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing diseases induced by the increased metabolism of cyclic guanosine 3′,5′-monophosphate (cGMP), such as hypertension, pulmonary hypertension, congestive heart failure, renal failure, myocardial infraction, stable, unstable and variant (Prinzmetal) angina, atherosclerosis, cardiac edema, renal insufficiency, nephrotic edema, hepatic edema, stroke, asthma, bronchitis, chronic obstructive pulmonary disease (COPD), cystic fibrosis, dementia, immunodeficiency, premature labor, dysmenorrhoea, benign prostatic hyperplasis (BPH), bladder outlet obstruction, incontinence, conditions of reduced blood vessel patency, e.g., postpercutaneous transluminal coronary angioplasty (post-PTCA), peripheral vascular disease, allergic rhinitis, glucoma, and diseases characterized by disorders of gut motility, e.g., irritable bowel syndrome (IBS).
专利号:WO-0168615-A1
优先权日:2000-03-13
标题 :Quinazoline synthesis
发明人:DENER JEFFREY MARK; LEASE TIMOTHY G; NOVACK AARON ROBERT
权利人:CHEMRX ADVANCED TECHNOLOGIES I; DENER JEFFREY MARK; LEASE TIMOTHY G; NOVACK AARON ROBERT
摘要:The present invention relates to a method for making a compound of Formulas I, II and III. The method of the present invention also enables parallel and simultaneous synthesis of a plurality of compounds represented by Formulas I, II and III.
专利号:WO-2015023170-A1
优先权日:2013-08-14
标题 :A method for preparation of erlotinib
发明人:KALVINS IVARS; PONOMARJOVS Jurijs; VARACEVA LARISA; CERNOBROVIJS ALEKSANDRS; LEBEDEVS ANTONS; CERNAKS DMITRIJS
权利人:LATVIAN INST ORGANIC SYNTHESIS
摘要:A method for the preparation N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)- quinazolin-4-amine (erlotinib) from 6,7-bis(2-methoxyethoxy)quinazolin-4(3H)-one and 3-aminophenylacetylene in the presence of titanium(IV) chloride and anisole is reported.