邻碘溴苯置于乙醇,间氯过氧苯甲酸,Potassium Hydroxide体系中,用 二氯甲烷,2,2,2-三氟乙醇,水 作为反应溶剂,化学反应 24.0H,反应生成 2-溴硫代苯酚 参考文献:二芳基碘盐与烷基黄原酸钾的反应作为获取有机硫化合物的切入点 标题:二芳基碘盐与烷基黄原酸钾的反应作为获取有机硫化合物的切入点 摘要:通过过渡金属催化或 S N Ar 反应制备s-芳基黄原酸酯因其在所用条件下的进一步转化而变得复杂.相比之下,O-烷基黄原酸钾与二芳基碘盐的 S-芳基化反应在温和条件下进行,从而能够获得取代的s-芳基黄原酸.该方法表现出非常好的官能团耐受性,可应用于药物分子的后期c-H功能化.由此产生的s-芳基黄原酸酯的不同转化提供了快速获得一系列与药物化学相关的有机硫化合物的途径. DOI:10.1021/acs.Orglett.2C04143
专利信息
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-6090810-A 优先权日:1995-09-01 标题:Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities 发明人:KLEIN ELLIOTT S; JOHNSON ALAN T; STANDEVEN ANDREW M; BEARD RICHARD L; GILLETT SAMUEL J; DUONG TIEN T; NAGPAL SUNIL; VULIGONDA VIDYASAGAR; TENG MIN; CHANDRARATNA ROSHANTHA A 权利人:ALLERGAN SALES INC 摘要:Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.
专利号:US-5877207-A 优先权日:1996-03-11 标 题:Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities 发明人:KLEIN ELLIOTT S; JOHNSON ALAN T; STANDEVEN ANDREW M; BEARD RICHARD L; GILLETT SAMUEL J; DUONG TIEN T; NAGPAL SUNIL; VULIGONDA VIDYASAGAR; TENG MIN; CHANDRARATNA ROSHANTHA A 权利人:ALLERGAN SALES INC 摘要:Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.
专利号:US-9481645-B2 优先权日:2014-02-21 标 题:Composition, synthesis, and use of a new class of isonitriles 发明人:FLEMING FRASER FERGUSSON; LUJAN-MONTELONGO JESUS ARMANDO 权利人:DUQUESNE UNIV OF THE HOLY GHOST 摘要:This invention relates to novel isonitriles, including arylthio isonitriles, and methods for their preparation. The isonitriles include a conjugated ring system. The structure is designed with the flexibility to have multiple substitution patterns. The isonitriles may be used in applications including, but not limited to, pharmaceutical compositions.
专利号:WO-2024041503-A1 优先权日:2022-08-22 标 题:Compounds targeting y220c mutant of p53 发明人:LI SUJING; LI AMIN; ZHENG QIAN; Dang Chaojie; FAN XINRUI; LONG WEI; WANG YANPING 权利人:JACOBIO PHARMACEUTICALS CO LTD 摘要:The present invention discloses compounds of formula (I) which can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. Also provided are processes for the synthesis and use of the compounds of formula (I).
专利号:US-5218109-A 优先权日:1988-07-05 标 题:Steroid compounds 发明人:TSUJI JIRO; TAKAHASHI TAKASHI; TSUJI MASAO; NAKAGAWA NAOSHI; TAKIGAWA TETSUO 权利人:KURARAY CO 摘要:Steroid compounds of the following general formulas (I), (II) and (III) are provided: ##STR1## In the above formulas, R 1 and R 2 each is a hydrogen atom or a hydroxyl-protecting group, R is a group of the formula --CH 2 --X (in which X is a substituent such as a hydroxyl group), a carboxyl group or a protected carboxyl group, A 1 is an aryl group, a lower alkyl group or an aralkyl group, and Z 1 , Z 2 , Z 3 and Z 4 each is a hydrogen atom, a hydroxyl group or a protected hydroxyl group. n The above steroid compounds are useful as intermediates for the synthesis of vitamin D 3 derivatives having a hydroxyl group at the 1α-position.