31683-47-3Relevant academic research and scientific papers
Compound of dipyrrolopyridine structure Preparation method and medical application
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Paragraph 0099-0102, (2021/08/25)
The invention discloses a compound with a dipyrrolo-pyridine structure as well as a preparation method and medical application thereof. The compound provided by the invention has obvious inhibitory activity on JAK family proteins, is an effective JAK inhibitor, and has the prospect of being developed into drugs for inhibiting JAK and further treating diseases.
Pd-catalyzed sp-sp3cross-coupling of benzyl bromides using lithium acetylides
Buter, Jeffrey,Doze, Anna M.,Feringa, Ben L.,Mondal, Anirban,Visser, Paco
, p. 7529 - 7532 (2021/08/05)
Organolithium-based cross-coupling reactions have emerged as an indispensable method to construct C-C bonds. These transformations have proven particularly useful for the direct and fast coupling of various organolithium reagents (sp, sp2, and sp3) with aromatic (pseudo) halides (sp2). Here we present an efficient method for the cross-coupling of benzyl bromides (sp3) with lithium acetylides (sp). The reaction proceeds within 10 min at room temperature and can be performed in the presence of organolithium-sensitive functional groups such as esters, nitriles, amides and boronic esters. The potential application of the methodology is demonstrated in the preparation of key intermediates used in pharmaceuticals, chemical biology and natural products.
Pyrazolopyrimidine [3,4-d] compound as well as preparation method and application thereof
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Paragraph 0321; 0323; 0324; 0325, (2019/06/10)
The invention relates to a compound which is a Bruton tyrosine kinase inhibitor. In addition, the invention discloses a pharmaceutical ingredient and a preparation that comprise the compound, and an application of the kinase inhibitor. The compound can be used independently or combined with other compounds for treating kinase mediated or kinase-dependent symptoms.
Propargylsilanes as Reagents for Synergistic Gold(I)-Catalyzed Propargylation of Carbonyl Compounds: Isolation and Characterization of σ-Gold(I) Allenyl Intermediates
Fernández, Sergio,González, Jairo,Santamaría, Javier,Ballesteros, Alfredo
supporting information, p. 10703 - 10707 (2019/06/25)
Reported herein is the isolation and characterization, for the first time, of a σ-gold allenyl complex as an intermediate in gold catalysis. This intermediate was captured during the study of a novel gold(I)-catalyzed propargylation of carbonyl compounds with propargylsilanes. Notably, the gold-catalyzed propargylation reaction, which proceeds with aldehydes and ketones, can be driven to the formation of either homopropargyl silyl ethers or the in situ synthesis of corresponding 2-silyl-4,5-dihydrofurans.
Palladium-Catalyzed Coupling of Terminal Alkynes with Benzyl Ammonium Salts
Xu, Silin,Zhang, Zhenming,Han, Chunyu,Hu, Wenkai,Xiao, Tiwen,Yuan, Yanan,Zhao, Junfeng
, p. 12192 - 12197 (2019/10/11)
A highly efficient palladium-catalyzed Sonogashira coupling of benzylic ammonium salts with terminal alkynes is developed. This strategy provides a facile access to a series of internal alkyne derivatives in moderate to excellent yields via C-N bond cleavage and C(sp3)-C(sp) bond formation. The broad substrate scope and high functional group tolerance make this reaction attractive for organic synthesis.
Bifunctional Biphenyl-2-ylphosphine Ligand Enables Tandem Gold-Catalyzed Propargylation of Aldehyde and Unexpected Cycloisomerization
Li, Ting,Zhang, Liming
supporting information, p. 17439 - 17443 (2019/01/04)
Despite extensive studies in gold catalysis, σ-allenylgold species have not been invoked as catalytic intermediates and their reactivities not studied. This work reports for the first time they are generated in situ and undergo nucleophilic addition to activated aldehydes in a bifunctional phosphine ligand-enabled gold catalysis. This development reveals a broad range of opportunities to achieve propargylic C-H functionalization for the first time under catalytic and mild conditions. The homopropargylic alcohols generated undergo ligand-enabled cycloisomerizations involving an unexpected silyl migration.
Regio- and Stereospecific Copper-Catalyzed Substitution Reaction of Propargylic Ammonium Salts with Aryl Grignard Reagents
Guisán-Ceinos, Manuel,Martín-Heras, Victor,Tortosa, Mariola
, p. 8448 - 8451 (2017/07/06)
We have developed a copper-catalyzed substitution reaction of propargylic ammonium salts with aryl Grignard reagents. The reaction is stereospecific and α-regioselective and proceeds with exceptional functional group tolerance. Conveniently, a stable, inexpensive, and commercially available copper salt is used and no added ligand is required.
Direct Synthesis of α-Allenols from TMS-Protected Alkynes and Aldehydes Mediated by Tetrabutylammonium Fluoride
Huang, Xiaojun,Bugarin, Alejandro
supporting information, p. 12696 - 12700 (2016/08/30)
A unique chemoselective synthesis of α-allenic alcohols is presented. Tetrabutylammonium fluoride (TBAF) mediated this transformation under mild reaction conditions. A range of functional groups is well-tolerated in this reaction, while affording adducts
Regioselective Allylation of Carbon Electrophiles with Alkenyl-silanes under Dual Catalysis by Cationic Platinum(II) Species
Kinoshita, Hidenori,Kizu, Ryosuke,Horikoshi, Masahiro,Inoue, Gen,Fujimoto, Masayuki,Saito, Masanori,Ichikawa, Junji,Hosomi, Akira,Miura, Katsukiyo
supporting information, p. 520 - 534 (2016/02/16)
In the presence of catalytic amounts of platinum(II) chloride and silver(I) hexafluoroantimonate, (Z)-alkenylsilanes reacted with various carbon electrophiles (acetals, aminals, carboxylic anhydrides, alkyl chlorides, etc.) at the γ-position to give allylation products. A plausible mechanism for the platinum-catalyzed allylation involves alkene migration of alkenylsilanes to allylsilanes and subsequent allylation of carbon electrophiles, both of which are catalyzed by a cationic platinum(II) species.
Synthesis of Multinuclear Copper Complexes Bridged by Diquinolylamidinates and Their Application to Copper-Catalyzed Coupling of Terminal Alkynes and Aryl, Allyl, and Benzyl Halides
Nakane, Takayuki,Tanioka, Yuta,Tsukada, Naofumi
, p. 1191 - 1196 (2015/04/27)
A dinuclear copper complex containing N,N′-diquinolylformamidinate and a tetranuclear copper complex containing N,N′-diquinolylacetamidinate were synthesized. The structure of complexes was confirmed by X-ray analysis, showing that copper atoms were bridg
