CAS: 170729-80-3; 5-(((2R,3S)-2-((R)-1-(3,5-Bis(Trifluoromethyl)Phenyl)Ethoxy)-3-(4-Fluorophenyl)Morpholino)Methyl)-1H-1,2,4-Triazol-3(2H)-One

上下游产品

CAS号252742-72-6 5-氯甲基-2,4 -二氢[ ... | CAS号171338-27-5 (2R,3S)-2-[(1R)... | CAS号368-63-8 3,5-二(三氟甲基)苯-1-醇 | CAS号1349902-81-3 tert-butyl 2-(1... | CAS号30071-93-3 3,5-双(三氟甲基)苯乙酮 | CAS号110843-90-8 4-苄基吗啉-2,3-二酮 | CAS号104-63-2 N-苄氨基乙醇 | CAS号287930-73-8 4-苄基-2-羟基-吗啉-3-酮

在 三乙基硅烷,三氟化硼乙醚体系中,用 乙腈 用作溶剂,化学反应 5.0H,以94%的收率获得阿瑞吡坦
参考文献:制备阿瑞匹坦的中间体及其制备方法与应用
标题:制备阿瑞匹坦的中间体及其制备方法与应用
摘要:本发明属于化合物及其合成技术领域,本发明提供了制备阿瑞匹坦的中间体及其制备方法与应用.本发明提供了式i和式ii所示的制备阿瑞匹坦的中间体,利用上述两种中间体通过缩合和还原反应制备阿瑞匹坦,相比现有制备阿瑞匹坦的方法,避免了在制备中间体过程中反应历程复杂,过渡态多,副产物多,质控复杂的缺点,使阿瑞匹坦的合成工艺过程更简单,工业生产的安全性和过程控制性得到增强,收率更高,且本发明的方法无污染,所用原料易得,工业化操作简单,能耗小,成本低,安全环保,适于工业化产业应用.

专利信息

专利号:US-6403793-B2
优先权日:2000-06-12
标 题 :Intramolecular glycosidation process for the synthesis of (2R, 2-alpha-R, 3a)-2-[1-(3,5- bis (trifluoromethyl) phenyl)ethoxy]-3-(4-fluorophenyl)-1,4-oxazine
发明人：PYE PHILIP J; ROSSEN KAI
权利人:MERCK & CO INC
摘要:The present invention is concerned with novel processes for the preparation of (2R-cis)-2-[[1-[3.5-bis(trifluoromethyl)phenyl]ethenyl]oxy]-3-(4-fluorophenyl)-4-(phenylmethyl) mopholine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.

专利号:US-2015239796-A1
优先权日:2014-02-19
标题:One pot synthesis of 18f labeledtrifluoromethylated compounds with difluoro(iodo)methane
发明人：RüHL THOMAS; RISS PATRICK; RAFIQUE WAQAS
权利人:UNIV OSLO
摘要:The present invention relates to compositions and methods for the synthesis of 18 F labeled compounds. In particular, the present invention relates to a copper (I) mediated one pot method for 18 F-trifluoromethylation of aromatic- or heteroaromatic halides with difluoro(iodo)methane (e.g., for use at PET imaging agents).

专利号:WO-2025102245-A1
优先权日:2023-11-14
标题:Synthesis method for dual endothelin receptor antagonist aprocitentan
发明人：XU XIANGUANG; WANG ZHEN; ZHU GUORONG; TU YONGJUN
权利人:ZHEJIANG TIANYU PHARMACEUTICAL CO LTD
摘要:Provided in the present invention is a synthesis method for aprocitentan, comprising the following steps: 1) a compound of formula X and a sulfonylation reagent compound of formula XI undergoing a sulfonylation reaction to prepare a compound of formula XII; and 2) removing an R protective group on the pyrimidine sulfonamide compound of formula XII obtained in the previous step, so as to obtain aprocitentan. The synthesis method of the present invention overcomes the problem in the prior art that preparing macitentan by means of condensation of chloropyrimidine and sulfonamide needs to use an excessive amount of a strong base and involves a relatively low conversion efficiency, relatively many side products and other defects. The synthesis method does not need using a fluorine reagent for fluorination, involves economical steps, is environmentally-friendly, and has a relatively low comprehensive production cost. Compared with existing methods for preparing aprocitentan, the method of the present invention has characteristics of easily available raw materials, being environmentally-friendly and economical, and the like, thereby facilitating the industrial production of aprocitentan.

专利号:US-9365532-B1
优先权日:2011-02-14
标题:Synthesis, composition and use of novel therapeutic and cosmetic Schiff base products formed by reaction of a carbonyl containing moeity with a transimination nucleophilic catalyst and the use of transimination nucleophilic catalysts to increase the rate at which carbonyl containing therapeutic and cosmetic actives form Schiff base products with biological amines
发明人：ISAACMAN STEVEN
权利人:ISAACMAN STEVEN; NANOMETICS LLC
摘要:The present invention relates to the synthesis, composition and use of novel moieties formed by reacting a transimination nucleophilic catalyst, molecular or polymeric, with carbonyl-containing therapeutic or cosmetic moieties. The resultant Schiff base product is highly reactive towards transimination with a biological amine. The catalyst and carbonyl-containing moiety can be molecular or polymeric, and the resultant chemical and physical properties of the Schiff base products can be engineered by appropriate selection of said catalyst. The present invention also relates to the synthesis, composition and use of novel moieties that are used as actives in sunless tanning preparations. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate at which a carbonyl-containing moiety reacts with a biological amine. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate and efficacy of commercial sunless tanning preparations. Improvements on stability and efficacy of said preparations are disclosed. While the invention has been described in terms of its preferred embodiments, those skilled in the art will recognize that the invention can be practiced with modification within the spirit and scope of the appended claims. Accordingly, the present invention should not be limited to the embodiments as described above, but should further include all modifications and equivalents thereof within the spirit and scope of the description provided herein.

专利号:US-2019031650-A1
优先权日:2016-01-29
标 题 :Dna alkylation and cross-linking agents as compounds and payloads for targeted therapies
发明人：HERZON SETH; HEALY ALAN; CRAWFORD JASON; VIZCAINO MARIA; NIKOLAYEVSKIY HERMAN
权利人:UNIV YALE
摘要:The present invention is directed to compounds related to precolibactin pharmaceutical compositions based upon these compounds and methods of synthesis which are employed to provide intermediates and final compounds, which are principally alkylating agents and anticancer compounds. The chemical synthetic approach disclosed facilitates the synthesis of numerous precolibactin analogs which can be used in the treatment of cancer.

专利号:US-2018140724-A1
优先权日:2015-05-27
标 题:Tumor Deliverable Iron and Protein Synthesis Inhibitors as a New Class of Drugs for the Diagnosis and Treatment of Cancer
发明人：DENG CHANGCHUN; LIPSTEIN MARK; O'CONNOR OWEN A
权利人:DENG CHANGCHUN; LIPSTEIN MARK; OCONNOR OWEN A; UNIV COLUMBIA
摘要:Tumor deliverable iron (TDI) drugs and pharmaceutical compositions and kits comprising them are provided and methods for delivering iron to tumors specifically, either intracellularly or extracellularly. As a result, TDI drugs are useful as a sensitizer for radiation therapy, radio-diagnosis, and chemotherapy, and are of interest. In other embodiments, tumor deliverable protein synthesis inhibitors (TDPSI) are provided and can be delivered to tumors, but not normal cells. These TDPSI drugs and pharmaceutical compositions and kits comprising them are useful for their treatment of cancer, either alone or in combination with other active anti-cancer drugs.