4-氟-2-甲氧基苯乙酮置于4,4'-硫联二(6-叔丁基-2-甲基苯酚),间氯过氧苯甲酸,Sodium Hydroxide体系中,用 二氯甲烷,乙醇 作为反应溶剂,化学反应 2.0H,以71%的收率获得产物4-氟-2-甲氧基苯酚 参考文献:Studies Toward The Discovery Of The Next Generation Of Antidepressants. 3. Dual 5-Ht1A And Serotonin Transporter Affinity Within A Class Of N-Aryloxyethylindolylalkylamines 标题:Studies Toward The Discovery Of The Next Generation Of Antidepressants. 3. Dual 5-Ht1A And Serotonin Transporter Affinity Within A Class Of N-Aryloxyethylindolylalkylamines 摘要:N-Aryloxylethylindolealkylamines (5) Having Dual 5-Ht Transporter And 5-Ht1A Affinity Are Described. These Compounds Represent Truncated Analogues Of Our Previously Reported Piperidinyl Derivatives (3). Compounds In This Investigation Were Found To Have More Similar Affinities And Functional Activities For The 5-Ht1A Receptor And 5-Ht Transporter. Though 5-Ht1A Antagonism Is Not Consistently Observed Throughout Series 5,Several Molecular Features Were Found To Be Essential To Obtain High And Balanced Activities. The Proper Placement Of A Heteroatom In The Aryl Ring And The Length Of The Linkage Used To Tether The Indole Moiety Had Significant Influence On 5-Ht1A And 5-Ht Transporter Affinities. Introduction Of A Halogen Into The Aryl Ring Usually Lowered Intrinsic Activity And In Some Cases Led To Full 5-Ht1A Antagonists. Compounds 33 And 34 Were Observed To Be Full 5-Ht1A Antagonists With K-I Values Of Approximately 30 Nm For The 5-Ht1A Receptor And K-I Values Of 5 And 0.5 Nm For The 5-Ht Transporter,Respectively. Unfortunately,Similar To Our Previous Series (3),Compounds In This Report Also Had High Affinity For The Alpha(1) Receptor. DOI:10.1021/jm0304010
专利号:WO-2009081259-A1 优先权日:2007-12-21 标题 :Phenoxy-pyridyl derivatives 发明人:BARTA NANCY SUE; CAMPBELL BRIAN MICHAEL; DOUNAY AMY BETH; GRAY DAVID LAWRENCE FIRMAN; ZORN STEVIN HOWARD 权利人:PFIZER; BARTA NANCY SUE; CAMPBELL BRIAN MICHAEL; DOUNAY AMY BETH; GRAY DAVID LAWRENCE FIRMAN; ZORN STEVIN HOWARD 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-9745253-B2 优先权日:2015-03-13 标 题 :Alpha-cinnamide compounds and compositions as HDAC8 inhibitors 发明人:BAIR KENNETH W; Barczak Nicholas; HAN BINGSONG; LANCIA JR DAVID R; LIU CUIXIAN; MARTIN MATTHEW W; NG PUI YEE; Rudnitskaya Aleksandra; THOMASON JENNIFER R; ZABLOCKI MARY MARGARET; ZHENG XIAOZHANG 权利人:FORMA THERAPEUTICS INC 摘要:The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.
专利号:US-10730849-B2 优先权日:2016-10-04 标 题:Benzo[b]thiophene compounds as STING agonists 发明人:ALTMAN MICHAEL D; CASH BRANDON D; CHANG WONSUK; CUMMING JARED N; HAIDLE ANDREW M; HENDERSON TIMOTHY J; JEWELL JAMES P; LARSEN MATTHEW A; LIANG RUI; LIM JONGWON; LU MIN; OTTE RYAN D; SIU TONY; TROTTER BENJAMIN WESLEY; TYAGARAJAN SRIRAM 权利人:MERCK SHARP & DOHME 摘要:Compounds of general formula (Ia), compounds of general formula (Ia′), compounds of general formula (Ib), compounds of general formula (Ib′), compounds of general formula (I), compounds of general formula (I′), and their pharmaceutically acceptable salts, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 8 , R 9 , X 1 , X 2 , and X 3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds of the disclosure.
专利号:CN-119161252-A 优先权日:2024-09-10 标 题 :Continuous flow synthesis method of 4-fluoro-2-methoxy-5-nitrophenol
[参考文献]: P K Chakraborty, Et Al. Oxidation Of Substituted 4-Fluorobenzaldehydes: Application To The No-Carrier-Added Syntheses Of 4-[18F]Fluoroguaiacol And 4-[18F]Fluorocatechol. Int J Rad Appl Instrum A. 1991;42(7):673-81.
合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).