专利号:US-2025026768-A1 优先权日:2023-06-30 标题:Method for the synthesis of axially chiral organoboron compounds 发明人:PING YIFAN; CHE CHI-MING 权利人:LABORATORY FOR SYNTHETIC CHEMISTRY AND CHEMICAL BIOLOGY LTD 摘要:A highly efficient and atroposelective Rh-catalyzed [2+2+2] cycloaddition for the synthesis of axially chiral aryboron compounds is developed. The reactions of diynes and alkynylborons smoothly occur in an atom-economical manner, affording a variety of C—B atropisomers in excellent yields and enantioselectivities. The protocol features mild conditions, broad substrate scope, and good functional tolerance. The obtained C—B atropisomers show powerful synthetic applications in terms of producing novel chiral phosphine ligands.
专利号:WO-2024174285-A1 优先权日:2023-02-21 标题:Method for preparing halogenated compound from metal halide salt on basis of mobile phase 发明人:SU REN; Ye Jiani 权利人:UNIV SOOCHOW 摘要:Disclosed is a method for preparing a halogenated compound from a metal halide salt on the basis of a mobile phase. The method comprises: converting an aromatic hydrocarbon, alkane or nitrile compound into a halogenated compound by means of a cheap metal halide salt and a photocatalyst under illumination. The method uses a cheap and safe halide salt as a halogen source, does not introduce additional elemental halogen or an additional oxidant, can implement a reaction at normal temperature and normal pressure, is high in terms of selectivity and friendly to environment, and can be used for replacing an existing synthesis reaction system for halogenated compounds. A mobile phase device is used to replace a tank reactor, such that operation is easy and convenient, the price is low, the substrate adaptability is high, the continuous synthesis of halogenated compounds can be achieved, and the method is suitable for industrial large-scale production.
专利号:WO-9943409-A1 优先权日:1998-02-27 标 题:Hplc fractionation of complex chemical mixtures 发明人:COOK PHILLIP DAN; CUMMINS LENDELL L; GRIFFEY RICHARD H; KAWASAKI ANDREW M; GAUS HANS; AN HAOYUN 权利人:ISIS PHARMACEUTICALS INC; COOK PHILLIP DAN; CUMMINS LENDELL L; GRIFFEY RICHARD H; KAWASAKI ANDREW M; GAUS HANS; AN HAOYUN 摘要:The rapid deconvolution of complex chemical mixtures, such as combinatorial libraries prepared via solution-phase simultaneous addition of functionalities is demonstrated using HPLC. Libraries containing 25-216 members were screened for biological activity and active libraries are fractionated into discreet pools using preferred reversed-phase HPLC. The entire process can be completed from a single synthesis of 15-50 mg, without the need for fixed positions, serial synthesis, or tagging.
专利号:US-6150129-A 优先权日:1996-08-01 标 题 :Antimicrobial determination of N-(aminoalkyl) and/or N-(Amidoalkyl) dinitrogen heterocyclic compositions 发明人:COOK PHILLIP DAN; KAWASAKI ANDREW M; KUNG PEI PEI 权利人:ISIS PHARMACEUTICALS INC 摘要:Compositions are provided comprising novel di-nitrogen heterocycle compounds containing N-(aminoalkyl) and/or N-(amidoalkyl) groups. An additional situs of functionality is also provided. The compounds and compositions of the invention are useful as antibacterial and other pharmaceutical agents and as intermediates for preparation of other pharmaceutical agents. In addition, compounds of the present invention are useful as research reagents including employment as species for effecting combinatorial synthesis.
专利号:US-2023192718-A1 优先权日:2018-03-30 标 题 :Bicyclic enone carboxylates as modulators of transporters and uses thereof 发明人:SANDANAYAKA VINCENT 权利人:NIROGY THERAPEUTICS INC 摘要:The invention generally relates to the field of monocarboxylate transporter inhibitors, and more particularly to new bicyclic enone carboxylate enone compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with monocarboxylate transporter activity such as in treating cancer and other neoplastic disorders, tissue and organ transplant rejection.
专利号:US-8952042-B2 优先权日:2009-08-19 标 题 :FXR (NR1H4) binding and activity modulating compounds 发明人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF 权利人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF; PHENEX PHARMACEUTICALS AG 摘要:The present invention relates to compounds of formula (1): n nwhere R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
参考标题:Synthesis Of Phenanthridines Through Palladium-Catalyzed Cascade Reaction Of 2-Halo-N-Ms-Arylamines With Benzyl Halides/sulfonates 作者:Si-Yi Yang,Wen-Yong Han,Ding-Lei Zhang,Xiao-Jian Zhou,Mei Bai,Bao-Dong Cui,Nan-Wei Wan,Wei-Cheng Yuan,Yong-Zheng Chen |发布日期:2017.2.3 摘要:An Efficient Palladium-Catalyzed Nucleophilic Substitution/c-H Activation/aromatization Cascade Reaction Between Readily Available 2-Halo-N-Ms-Arylamines (Ms = Methanesulfonyl) And Benzyl Halides/sulfonates Has Been Described. A Wide Variety Of Phenanthridines Were Synthesized In A One-Pot Fashion In Moderate To High Yields (37-86 %). Notably, This Method Provides A Straightforward, Facile Approach
合成参考文献
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