3,4-二氟溴苯置于哌啶,吡啶,碘,Magnesium体系中,用 四氢呋喃 用作溶剂,化学反应 30.5H,反应生成3,4-二氟肉桂酸 参考文献:Synthesis And Mesomorphic Properties Of Tolane-Based Fluorinated Liquid Crystals With An Acrylate Linkage 标题:Synthesis And Mesomorphic Properties Of Tolane-Based Fluorinated Liquid Crystals With An Acrylate Linkage 摘要:Six Series Of Tolane-Based Fluorinated Liquid Crystals Containing An Acrylate Linker Were Synthesized And Their Mesomorphic Properties Were Characterized. The Compounds Generally Exhibit Sma And N Phases In Wide Temperature Ranges. The Introduction Of Acrylate Linkers Increases The Clearing Points By 20 Degrees C-30 Degrees C And Suppresses The Formation Of Higher Ordered Monotropic Smb Phases. Para-Fluorination Is Favorable For The Mesophase Stability,Whereas Meta-Fluorination Is Not. The Introduction Of A 2,3,5,6-Tetrafluorophenylene Group Decreases The Clearing Points And Also Suppresses The Formation Of The Monotropic Smb Phase. Doi:10.1080/15421406.2010.504638
专利号:EP-2644590-A1 优先权日:2012-03-30 标 题:Synthesis of 2-(3,4-difluorophenyl)cyclopropanamine derivatives and salts 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor.
专利号:US-2018148745-A1 优先权日:2015-05-26 标题:Hemoprotein catalysts for improved enantioselective enzymatic synthesis of ticagrelor 发明人:ARNOLD FRANCIS H; RENATA HANS; MCINTOSH JOHN A; LEWIS RUSSELL D; KAN SEK BIK JENNIFER; HERNANDEZ KARI; COELHO PEDRO; ROZZELL DAVID; ZHANG CHEN 权利人:CALIFORNIA INST OF TECHN; PROVIVI INC 摘要:The present invention provides methods by which trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine and related cyclopropane compounds are prepared using synthetic strategies that include a biocatalytic cyclopropanation step.
专利号:US-8183412-B2 优先权日:2000-06-02 标 题:Process for the preparation of cyclopropyl carboxylic acid esters and derivatives 发明人:CLARK ADRIAN; JONES ELFYN; LARSSON ULF; MINIDIS ANNA 权利人:CLARK ADRIAN; JONES ELFYN; LARSSON ULF; MINIDIS ANNA; ASTRAZENECA AB 摘要:The invention relates to a novel process for the preparation of certain cyclopropyl carboxylic acid esters and other cyclopropyl carboxylic acid derivatives; a novel process for the preparation of dimethylsulfoxonium methylide and dimethylsulfonium methylide; to the use of certain cyclopropyl carboxylic acid esters in a process for the preparation of intermediates that can be used in the synthesis of pharmaceutically active entities; and to certain intermediates provided by these processes.
专利号:US-9085605-B2 优先权日:2010-05-27 标 题:Chemical synthesis and anti-tumor and anti-metastatic effects of dual functional conjugate 发明人:LIU GANG; ZHAO NAN; MA YAO 权利人:LIU GANG; ZHAO NAN; MA YAO; SHENZHEN SALUBRIS PHARM CO LTD 摘要:The present invention discloses chemical synthesis, anti-tumor and anti-metastatic effects of a dual functional conjugate as shown by formula I. Specifically, paclitaxel or docetaxol is linked with muramyl dipeptide derivative to form a conjugate, thus dual anti-tumor and anti-metastatic effects are achieved by combination of chemotherapy and immunotherapy. The present invention also discloses that paclitaxel or docetaxol and muramyl dipeptide derivative conjugate is synthesized by combination of solid-phase and solution-phase synthesis, and said conjugate can be used in manufacture of anti-tumor medicaments as proved by reliable bioassays.
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:WO-0027817-A1 优先权日:1998-11-10 标 题:Oxazolidinones useful as alpha 1a adrenoceptor antagonists 发明人:NERENBERG JENNIE B; BOCK MARK G; PATANE MICHAEL A; SELNICK HAROLD G 权利人:MERCK & CO INC; NERENBERG JENNIE B; BOCK MARK G; PATANE MICHAEL A; SELNICK HAROLD G 摘要:Novel hydroxymethyl- and alkoxymethyl-oxazolidinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered uring flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
[参考文献]: Chi Wai Cheung, Et Al. Room Temperature Copper(Ii)-Catalyzed Oxidative Cyclization Of Enamides To 2,5-Disubstituted Oxazoles Via Vinylic C-H Functionalization. J Org Chem. 2012 Sep 7;77(17):7526-37.