CAS: 134308-13-7; 3,4-Dihydroxy-4'-Methyl-5-Nitrobenzophenone

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CAS号134612-80-9 (4-羟基-3-甲氧基-5-硝...

De硝基托卡朋置于3-(Ethoxycarbonyl)-1-(5-Methyl-5-(Nitrosooxy)Hexyl)Pyridin-1-Ium Bis(Trifluoromethanesulfonyl)Imide体系中,化学反应 2.0H,以67%的收率获得托卡朋
参考文献:3-(乙氧羰基)-1-(5-甲基-5-(亚硝基氧基)己基)吡啶-1-鎓阳离子:亚硝酸叔丁酯的绿色替代品,用于在室温下合成含硝基的芳烃和药物
标题:3-(乙氧羰基)-1-(5-甲基-5-(亚硝基氧基)己基)吡啶-1-鎓阳离子:亚硝酸叔丁酯的绿色替代品,用于在室温下合成含硝基的芳烃和药物
摘要:由于其卓越的性能,特定任务的离子液体在绿色有机合成领域近几年来逐渐受到欢迎.在此,我们首次报道了一种新的特定任务的基于亚硝酸盐的离子液体,例如3-(乙氧基羰基)-1-(5-甲基-5-(亚硝基氧基)己基)吡啶-1-基双(三氟甲烷磺酰基)酰亚胺(ts-N-Il)源自可生物降解的烟酸乙酯,确实是一种高效且生态友好的试剂,用于合成高价值的硝基芳族化合物和药物,包括硝苯腈,托卡酮,尼古丁,氟他胺,尼洛沙胺和硝西epa.离子液体与亚硝酸盐基团的桥接不仅增加了直接c-N键形成反应的收率和速率,而且还使得产物易于分离和副产物的可回收性.非挥发性性质,易于合成,仅化学计量需要和温和性是ts-N-Il额外关注的部分,而与亚硝酸叔丁酯相比,后者是有机合成中广泛使用的出色且高度易燃的试剂.
Doi:10.1016/j.Tetlet.2019.151529

专利信息

专利号:US-11766432-B2
优先权日:2018-07-27
标题 :Cleavable conjugates of catechol compounds and water-soluble polymers and methods of treatment using the same
发明人：BENTLEY MICHAEL; FANG ZHIHAO; WEIMER REBECCA; VIEGAS TACEY; MOREADITH RANDALL
权利人:SERINA THERAPEUTICS INC
摘要:Described are conjugates comprising a water-soluble polymer linked to a compound comprising a catechol moiety via a cleavable linkage, wherein the cleavable linkage is formed between the water-soluble polymer and a first phenolic hydroxyl group of the catechol moiety and a second phenolic hydroxyl group of the catechol moiety is linked to a blocking group wherein the rate of hydrolytic release of the compound comprising the catechol moiety is controlled, at least in part, through structure or design of the blocking group on the second phenolic hydroxyl group of the catechol moiety. Therefore, the rate of hydrolytic release of the compound comprising the catechol moiety can be tuned through structural design of the group on the second phenolic hydroxyl group of the catechol moiety. Compounds used in the synthesis of the described conjugates and methods of using the described conjugate and other compounds in the treatment of dopamine-responsive disorders are also described.

专利号:US-2008125354-A1
优先权日:2005-11-21
标题 :Selective inhibition of matrix metalloproteinases
发明人：FIELDS GREGG B; HAMMER ROBERT
权利人:UNIV FLORIDA ATLANTIC; UNIV LOUISIANA STATE
摘要:Synthetic triple-helical peptides (THPs) are used for the design and synthesis of triple-helical transition state analog inhibitors. These inhibitors feature a phosphonate ester or phosphinic moiety in place of the scissle bond. These groups inhibit MMPs, and methods been developed for their convenient incorporation within a peptide sequence by solid-phase methods.

专利号:WO-2025128098-A1
优先权日:2023-12-13
标 题 :Solid oral dosage forms, kits, and methods of using the same
发明人：LI YING; LANGER ROBERT; TRAVERSO CARLO
权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

专利号:US-10377729-B2
优先权日:2015-06-15
标题 :Bis-furan derivatives as transthyretin (TTR) stabilizers and amyloid inhibitors for the treatment of familial amyloid polyneuropathy (FAP)
发明人：VIEIRA SIMÕES CARLOS JOSÉ; LOURENÇO DE ALMEIDA ZAIDA CATARINA; VASCONCELOS DIAS DE PINHO E MELO TERESA MARGARIDA; PONTES MEIRELES FERREIRA DE BRITO RUI MANUEL; SILVA COSTA DORA CRISTINA; CABRAL CARDOSO LOPES ANA LÚCIA
权利人:BSIM THERAPEUTICS S A
摘要:The design and synthesis of a novel bis-furan scaffold tailored for high efficiency at inhibiting transthyretin amyloid formation is reported. In vitro results show that the discovered compounds are more efficient inhibitors of amyloid formation than tafamidis, a drug currently used in the treatment of familial amyloid polyneuropathy (FAP), despite their lower molecular weight and lipophilicity. Moreover, ex vivo experiments with the strongest inhibitor in the series, conducted in human blood plasma from normal and FAP Val30Met-transthyretin carriers, disclose remarkable affinity and selectivity profiles. The promises and challenges facing further development of this compound are discussed under the light of increasing evidence implicating transthyretin stability as a key factor not only in transthyretin amyloidoses and several associated co-morbidities, but also in Alzheimer's disease.

专利号:US-12201669-B2
优先权日:2021-03-11
标 题:Small molecule suppressors of APOE gene expression and cerebral vascular amyloid pathology
发明人：TSAI LI-HUEI; BLANCHARD JOEL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present disclosure provides methods of inhibiting amyloid synthesis in a subject using small molecule inhibitors. The invention also includes methods of treating disease associated with amyloid synthesis, such as Alzheimer's disease. The small molecule inhibitors disclosed herein are compounds which are non-immunosuppressant cyclosporin including the pharmaceutically acceptable salts thereof.

专利号:US-2018370958-A1
优先权日:2017-06-27
标题:Route Of Synthesis For Opicapone
发明人：NABOLD CHRISTIAN FRECH; AEBERSOLD CHRISTINE; GRIECO PASQUALE GABRIELE; AESCHBACHER ROMAN GERBER
权利人:AZAD PHARMACEUTICAL INGREDIENTS AG
摘要:The present invention relates to a new route of synthesis for obtaining Opicapone ((4Z)-4-[3-(2,5-dichloro-4,6-dimethyl-1-oxidopyridin-1-ium-3-yl)-2H-1,2,4-oxadia-zol-5-ylidene]-2-hydroxy-6-nitrocyclohexa-2,5-dien-1-one), new intermediates in the reaction path and the new substance 2,5-dichloro-N-hydroxy-4,6-dimethylpyridine-3-carboximidoyl chloride.