专利号:US-5039814-A 优先权日:1990-05-02 标 题:Ortho-lithiation process for the synthesis of 2-substituted 1-(tetrazol-5-yl)benzenes 发明人:SHUMAN RICHARD F; KING ANTHONY O; ANDERSON ROBERT K 权利人:MERCK & CO INC 摘要:A process utilizes the tetrazole functional group to direct lithiation at the ortho position of a phenyltetrazole and generate a nucleophilic aryllithium species which then undergoes reaction with an electrophile to generate a 2-substituted 1-(tetrazol-5-yl)benzene. The process is useful in the production of intermediates in the synthesis of angiotensin II antagonists. This novel process is a more cost effective and versatile route for the large-scale preparation of these key intermediates.
专利号:WO-2023061999-A1 优先权日:2021-10-12 标 题 :Process for preparing a phenolic hydrocarbon 发明人:CORNELLA JOSEP; LE VAILLANT FRANCK 权利人:STUDIENGESELLSCHAFT KOHLE GGMBH 摘要:The present invention discloses a distinct mode of action of a nickel catalyst to forge C-0 bonds to unlock the mild utilization of N2O as O-atom transfer reagent in the synthesis of complex phenols from the corresponding aryl halides.
专利号:US-11299484-B2 优先权日:2018-10-10 标 题 :Inhibiting fatty acid synthase (FASN) 发明人:MARTIN MATTHEW W; ZABLOCKI MARY-MARGARET; MENTE SCOT; DINSMORE CHRISTOPHER; WANG ZHONGGUO; ZHENG XIAOZHANG 权利人:FORMA THERAPEUTICS INC 摘要:The present disclosure is directed to inhibitors of FASN. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of FASN. For instance, the disclosure is concerned with compounds and compositions for inhibition of FASN, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of FASN, and methods of synthesis of these compounds.
专利号:CA-2041620-C 优先权日:1990-05-02 标 题:An ortho-lithiation process for the synthesis of 2-substituted-1-(tetrazol-5-yl) benzenes
专利号:WO-2023283974-A1 优先权日:2021-07-12 标 题:Deuterated ammonia preparation method and deuteration reaction involving same as deuterium source 发明人:LANG JIANPING; GU HONGWEI; ZHU FENGYUAN; NIU ZHENG 权利人:UNIV SOOCHOW 摘要:A deuterated ammonia preparation method and a rapid deuterated reaction involving same as a deuterium source, which belong to the technical field of organic synthesis. The deuterated ammonia preparation method comprises the following steps: passing a nitrile compound through the action of a catalyst under a deuterium source atmosphere to obtain a deuterated amine. In the deuterated ammonia preparation method, a target product can be obtained in one step under mild conditions by means of a simple organic reaction, and the operation is simple; the produced deuterated ammonia can be directly used as a deuterium source, and undergoes a rapid hydrogen-deuterium exchange reaction with active hydrogen to synthesize a corresponding deuterated compound. An active hydrogen-containing compound comprises a hydroxyl compound, a thiol compound, an alkynyl compound, a phenolic compound, a silicon-hydrogen compound or an amino compound. The preparation method has mild reaction conditions and low operation costs and has good universality.
[参考文献]: Idriss Bennacef, Et Al. Dopamine D3 Receptor Antagonists: The Quest For A Potentially Selective Pet Ligand. Part 3: Radiosynthesis And In Vivo Studies. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5056-9.
合成参考文献
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