治疗皮肤病和其他病况的一系列化合物

    公开(公告)号:CN113454054B

    公开(公告)日:2024-01-02

    申请号:CN201980082627.7

    申请日:2019-10-13

    Abstract: 途。本主题还包括治疗由寻常痤疮和相关炎症及公开了涉及预防和治疗疾病和病况的化合 炎症后色素沉着过度引起的皮肤病症。还公开了物和方法,其中一些疾病和病况是由黑素生成促 合成所预期的化合物的方法。(56)对比文件Yoshinao Tamar 等.Regio-andStereoselective Hydrosulfonylation ofConjugated Dienes via a (ir-Allyl)palladium Complexlab.J.Org.Chem.1983,4669-4681.CLINTON D. SNYDER 等.Synthesis ofmenaquinones.JOURNAL OF THE AMERICANCHEMICAL SOCIETY.1974,第96卷(第96期),8046-8054.QIANG-QIANG LI 等.Direct WittigOlefination of Alcohols.JOURNAL OFORGANIC CHEMISTRY..2017,第83卷(第83期),296-302.EMMA E. COYLE 等.Catalytic WittigReactions of Semi- and NonstabilizedYlides Enabled by Ylide Tuning.ANGEWANDTECHEMIE, INTERNATIONAL EDITION.2014,第53卷(第53期),12907-12911.DE OLIVEIRA FILHO 等.Structure-activity relationships of 110 candidatejuvenile hormone analogs.REVISTABRASILEIRA DE BIOLOGIA, SOCIEDADE DEBIOLOGIA DE BRASIL, RIO DE JANEIRO,BR.1981,第41卷197-203.WRIGHT 等.Juvenilizing activity ofcompounds related to the juvenile hormoneagainst pupae of the stable fly.JOURNALOF ECONOMIC ENTOMOLOGY.1972,第65卷1644-6747.MING-GUANG RONG 等.De Novo Synthesisof Phenols and Naphthols throughOxidative Cycloaromatization ofDienynes.ORGANIC LETTERS.2018,第20卷(第20期),6289-6293.KOTAKE 等.A general method for thepreparation of 2-substituted and 2,3-disubstituted furans. A new synthesis ofsesquirose furan.HETEROCYCLES.1978,第10卷105-109.GIORGI PASCAL D 等.BiomimeticCannabinoid Synthesis Revisited: Batchand Flow All-Catalytic Synthesis of (±)-ortho-Tetrahydrocannabinols and Analoguesfrom Natural Feedstocks.EUROPEAN JOURNALOF ORGANIC CHEMISTRY, WILEY-VCH, DE.2018,(第undefined期),1307-1311.ERIK W. WERNER 等.A Highly Selectiveand General PalladiumCatalyst for theOxidative Heck Reaction of ElectronicallyNonbiased Olefins.JOURNAL OF THE AMERICANCHEMICAL SOCIETY.2010,第132卷(第132期),13981-13983.SREBNIK M 等.BASE-CATALYZED DOUBLE-BOND ISOMERIZATIONS OF CANNABINOIDSSTRUCTURAL AND STEREOCHEMICALASPECTS.JOURNAL OF THE CHEMICAL SOCIETY,PERKIN TRANSACTIONS 1,ROYAL SOCIETY OFCHEMISTRY.GB.1984,(第undefined期),2881-2886.Yoshinao Tamar 等.Regio-andStereoselective Hydrosulfonylation ofConjugated Dienes via a (ir-Allyl)palladium Complexlab.J.Org.Chem.1983,4669-4681.CLINTON D. SNYDER 等.Synthesis ofmenaquinones.JOURNAL OF THE AMERICANCHEMICAL SOCIETY.1974,第96卷(第96期),8046-8054.QIANG-QIANG LI 等.Direct WittigOlefination of Alcohols.JOURNAL OFORGANIC CHEMISTRY..2017,第83卷(第83期),296-302.EMMA E. COYLE 等.Catalytic WittigReactions of Semi- and NonstabilizedYlides Enabled by Ylide Tuning.ANGEWANDTECHEMIE, INTERNATIONAL EDITION.2014,第53卷(第53期),12907-12911.DE OLIVEIRA FILHO 等.Structure-activity relationships of 110 candidatejuvenile hormone analogs.REVISTABRASILEIRA DE BIOLOGIA, SOCIEDADE DEBIOLOGIA DE BRASIL, RIO DE JANEIRO,BR.1981,第41卷197-203. (续)

    一种噁唑酰草胺中间体的合成方法

    公开(公告)号:CN113620830B

    公开(公告)日:2023-09-05

    申请号:CN202111128981.4

    申请日:2021-09-26

    Abstract: 本发明属于有机合成领域,尤其涉及一种噁唑酰草胺中间体的合成方法。该方法包括以下步骤:a)在催化剂存在条件下,2‑(4‑羟基苯氧基)丙酸和氯化试剂在有机溶剂中进行氯化反应,得到2‑(4‑羟基苯氧基)丙酰氯;b)在缚酸剂存在条件下,所述2‑(4‑羟基苯氧基)丙酰氯和N‑甲基‑2‑氟苯胺在有机溶剂中进行缩合反应,得到N‑(2‑氟苯基)‑2‑(4‑羟基苯氧基)‑N‑甲基丙酰胺。本发明提供的合成方法的反应收率高、产品纯度高,且所用原料价格相对低廉、易得,适用于工业化生产。实验结果表明:本发明提供的合成方法的反应收率>90%,产品纯度>95%。

    一种R-(+)-2-(4-羟基苯氧基)丙酸的制备方法

    公开(公告)号:CN110803987B

    公开(公告)日:2022-10-14

    申请号:CN201911080109.X

    申请日:2019-11-07

    Abstract: 本发明公开一种R‑(+)‑2‑(4‑羟基苯氧基)丙酸的制备方法,包括将苯酚和S‑2‑氯丙酸或其盐、水和第一催化剂在密闭环境中混合,并在惰性气体保护下,加热进行烷基化反应制备2‑苯氧基丙酸;将2‑苯氧基丙酸、第二催化剂、卤化试剂混合,在20‑30℃下反应制备2‑(4‑卤代苯氧基)丙酸;将2‑(4‑卤代苯氧基)丙酸,碱溶液,第三催化剂,在150‑160℃下密闭下微压反应,反应结束,经过滤、酸化处理制备R‑2‑(4‑羟基苯氧基)丙酸。本发明提供的方法,采用苯酚和有机酸或有机酸盐作为原料,纯化简单,纯度高。

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