3-氯-4-氟苯胺置于溴化亚铜 Sodium Nitrite体系中,用 水 作为反应溶剂,以187.2 G (89%)的收率获得产物3-氯-4-氟溴苯 参考文献:Process For The Preparation Of 标题:Process For The Preparation Of 摘要:本发明涉及一种制备公式i的化合物的方法,其中r1表示h,卤素,(c1-C4)烷基或(c1-C4)烷氧基,R2表示h,卤素,(c1-C4)烷基,(c1-C4)烷基硫代基,(c1-C4)烷氧基或二价基团3,4-0-Ch2-O.该方法包括在存在铜催化剂的情况下,将公式ii的化合物与公式iii的碱金属苯酚或碱土金属苯酚反应,其中x表示卤素,R2的含义与公式i中相同,M表示碱金属或碱土金属,R1的含义与公式i中相同.
专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:WO-03080621-A1 优先权日:2002-03-19 标题:Process and intermediates to substituted imidazopyrimidines 发明人:LI WENJIE; CAI DONGWEI; HOERRNER R SCOTT; JENSEN MARK S; LARSEN ROBERT D; PETASIS NICOS A 权利人:MERCK & CO INC; LI WENJIE; CAI DONGWEI; HOERRNER R SCOTT; JENSEN MARK S; LARSEN ROBERT D; PETASIS NICOS A 摘要:A novel process is provided for the preparation of imidazo[1,2-α]pyrimidines which are substituted at the 3-position with a substituted chlorophenyl group. Such compounds are useful in the synthesis of GABAA receptor ligands for the treatment of deleterious mental disorders. Also provided are intermediates obtained from the process useful in the synthesis of GABAA receptor ligands.
专利号:EP-4471014-A1 优先权日:2023-05-29 标 题 :Derivate of quinoxaline with thermally activated delayed fluorescence 发明人:SERDIUK ILLIA; MONKA MICHAL; GRZYWACZ DARIA 权利人:UNIV GDANSKI 摘要:The invention relates to the triarylamine derivatives of quinoxaline with thermally activated delayed fluorescence (TADF) bearing heavy atoms and methods of their synthesis. The emitters are characterized by spectral and photophysical properties with improved TADF parameters as compared to their analogues reported before. The disclosed emitters can convert triplet excitons into singlet ones faster and with higher efficiency. The emitters cover orange, red, and/or near infrared (NIR) spectral ranges. Furthermore, the mixtures of new emitters with fluorescent dopants exhibit narrowband NIR emission preserving fast triplet-singlet exciton conversion.The invention concerns functional organic materials which exhibit TADF and can be potentially used for the electroluminescence applications, e.g. in organic light emitting diodes (OLED), and/or applications of materials with long-lived excited states, e.g. photosensibilization, photocatalysis, and/or other fields where excited triplet states or excitons play important role.
专利号:CN-108997177-A 优先权日:2018-09-04 标题 :A kind of microwave-promoted method for the synthesis of N-benzenesulfonylnitroaniline compounds
专利号:US-2017369470-A1 优先权日:2014-12-16 标 题:Cyclic Compounds and Uses Thereof 发明人:BALOGLU ERKAN; SENAPEDIS WILLIAM; SHACHAM SHARON 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to substituted benzothiophenyl, substituted benzothiazolyl, substituted indolyl and substituted benzoimidazolyl compounds and, more particularly, to a compound represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of a disease or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, inflammatory diseases or an autoimmune system disease (e.g., a T-Cell mediated autoimmune disesase).
专利号:WO-2023057548-A1 优先权日:2021-10-07 标题:Ccr6 receptor modulators 发明人:AISSAOUI HAMED; ALLEMANN OLIVER; CAROFF EVA; MEYER EMMANUEL; RICHARD-BILDSTEIN SYLVIA 权利人:IDORSIA PHARMACEUTICALS LTD 摘要:The present invention relates to compounds of Formula (I), their synthesis and use as CCR6 receptor modulators for the prevention or treatment of e.g. inflammatory/autoimmune diseases/disorders and cancer.
参考文献:10.1055/s-0036-1588303 摘要:Rossi R, Bellina F, Lessi M, Manzini C, Marianetti G. Direct (Hetero)arylation Reactions of (Hetero)arenes as Tools for the Step- and Atom-Economical Synthesis of Biologically Active Unnatural Compounds Including Pharmaceutical Targets. Synthesis. 2016 Oct 11;48(22):3821–62. doi: 10.1055/s-0036-1588303.