Continuous-Flow Multistep Synthesis of Cinnarizine, Cyclizine, and a Buclizine Derivative from Bulk Alcohols
作者:Svetlana Borukhova、Timothy Noël、Volker Hessel
DOI:10.1002/cssc.201501367
日期:2016.1
Cinnarizine, cyclizine, buclizine, and meclizine belong to a family of antihistamines that resemble each other in terms of a 1‐diphenylmethylpiperazine moiety. We present the development of a four‐step continuous process to generate the final antihistamines frombulkalcohols as the starting compounds. HCl is used to synthesize the intermediate chlorides in a short reaction time and excellent yields
肉桂利嗪,环利嗪,丁克利嗪和甲氯嗪属于抗组胺药家族,它们在1-二苯基甲基哌嗪部分上彼此相似。我们提出了一个四步连续过程的开发过程,该过程从大量的醇类作为起始化合物生成最终的抗组胺药。HCl用于在短的反应时间内合成中间氯化物,并具有优异的收率。该方法学提供了合成用于药物合成的中间体的绝佳方法。在线分离允许在以下步骤中收集纯净的产品并立即消费它们。肉桂利嗪,环齐嗪和丁克利嗪衍生物的总分离产率分别为82%,94%和87%。这四个步骤的总停留时间为90分钟,生产率为2 mmol h -1。
Pyrimidine derivatives as IL-8 receptor antagonists
申请人:——
公开号:US20040087601A1
公开(公告)日:2004-05-06
Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula I
1
In these compounds, Q is preferably unsubstituted and substituted heterocyclyl; U is usually hydrogen or fluorine; and V is preferably hydrogen, halogen, alkyl, —O—alkyl or —S-alkyl. A representative example is:
2
Highly Efficient and Selective N-Alkylation of Amines with Alcohols Catalyzed by in Situ Rehydrated Titanium Hydroxide
作者:Feng Niu、Qiyan Wang、Zhen Yan、Bright T. Kusema、Andrei Y. Khodakov、Vitaly V. Ordomsky
DOI:10.1021/acscatal.9b05525
日期:2020.3.6
Catalytic N-alkylation of amines by alcohols to produce desired amines is an important catalytic reaction in industry. Various noble-metal-based homogeneous and heterogeneous catalysts have been reported for this process. The development of cheap non-noble-metal heterogeneous catalysts for the N-alkylation reaction would be highly desirable. Hereby, we propose the N-alkylation of amines by alcohols over
[EN] NOVEL NAPHTHOTHIOPHENE COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME<br/>[FR] NOUVEAU COMPOSÉ NAPHTOTHIOPHÈNE ET DISPOSITIF ÉLECTROLUMINESCENT ORGANIQUE LE CONTENANT
申请人:CANON KK
公开号:WO2011132623A1
公开(公告)日:2011-10-27
The present invention provides novel naphthothiophene compounds of general formula [1] wherein Ar and R are defined in the present claims, which have a high lowest excited triplet level (T1).
Method for the synthesis and purification of ethers
申请人:The United States of America, as represented by the Secretary of the Navy
公开号:US09862694B1
公开(公告)日:2018-01-09
Methods of synthesizing and purifying ethers are described. The synthesis and purification are achieved using an etherification technique followed by one or two fractional distillations. The etherification utilizes an element having low work function properties. Examples of low work function elements include, but are not limited to, metals or their hydrides, such as sodium, lithium or potassium or some combination thereof. This technique yields ethers of greater than 90% purity.