40400-13-3Relevant academic research and scientific papers
Pd(II)-Catalyzed Synthesis of Benzocyclobutenes by β-Methylene-Selective C(sp3)-H Arylation with a Transient Directing Group
Chen, Xiangyang,Hoskin, John F.,Houk, K. N.,Provencher, Philip A.,Sorensen, Erik J.,Wong, Jonathan J.,Yu, Jin-Quan
, p. 20035 - 20041 (2021/12/09)
Methylene-selective C-H functionalization is a significant hurdle that remains to be addressed in the field of Pd(II) catalysis. We report a Pd(II)-catalyzed synthesis of benzocyclobutenes by methylene-selective C(sp3)-H arylation of ketones. The reaction utilizes glycine as a transient directing group and a 2-pyridone ligand, which may govern the methylene selectivity by making intimate molecular associations with the substrate during concerted metalation-deprotonation. This reaction is shown to be highly selective for intramolecular methylene C(sp3)-H arylation, thus enabling sequential C(sp3)-H functionalization.
INHIBITORS OF PURINE NUCLEOSIDE PHOSPHORYLASE - SYNTHESIS AND USE THEREOF FOR TREATMENT OF T-CELL ACUTE LYMPHOBLASTIC LEUKEMIA AND LYMPHOMA
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Page/Page column 56, (2021/05/07)
The present invention relates to new compounds of general formula I, their synthesis, their pharmaceutically acceptable salts, and their use in treatment of T-cell acute lymphoblastic leukemia and lymphoma.
CuSO4-Catalyzed Tandem C(sp3)-H Insertion Cyclization of Toluenes with Isonitriles to Form Indoles
Shan, Xiang-Huan,Wang, Mei-Mei,Tie, Lin,Qu, Jian-Ping,Kang, Yan-Biao
supporting information, p. 357 - 360 (2020/01/31)
A CuSO4-catalyzed tandem benzylic C-H insertion cyclization of toluene derivatives and isonitriles is described. The naturally abundant salt CuSO4 serves as a low-cost ligand-free redox catalyst. This reaction provides a practical mo
Nickel-Catalyzed Asymmetric Reductive 1,2-Carboamination of Unactivated Alkenes
He, Jun,Xue, Yuhang,Han, Bo,Zhang, Chunzhu,Wang, You,Zhu, Shaolin
, p. 2328 - 2332 (2020/01/08)
Starting from diverse alkene-tethered aryl iodides and O-benzoyl-hydroxylamines, the enantioselective reductive cross-electrophilic 1,2-carboamination of unactivated alkenes was achieved using a chiral pyrox/nickel complex as the catalyst. This mild, modular, and practical protocol provides rapid access to a variety of β-chiral amines with an enantioenriched aryl-substituted quaternary carbon center in good yields and with excellent enantioselectivities. This process reveals a complementary regioselectivity when compared to Pd and Cu catalysis.
Palladium-Catalyzed Synthesis of 6H-Dibenzo[c,h]chromenes and 5,6-Dihydrobenzo[c]phenanthridines: Application to the Synthesis of Dibenzo[c,h]chromene-6-ones, Benzo[c]phenanthridines, and Arnottin I
Pramanik, Subhendu,Jash, Moumita,Mondal, Debasmita,Chowdhury, Chinmay
supporting information, p. 5223 - 5238 (2019/11/11)
6H-Dibenzo[c,h]chromenes and 5,6-dihydrobenzo[c]phenanthridines have been synthesized via Palladium (II)-catalyzed domino reactions of acetylenic substrates involving intramolecular trans-oxo/amino palladation onto the triple bond followed by nucleophilic
Strategy for Overcoming Full Reversibility of Intermolecular Radical Addition to Aldehydes: Tandem C-H and C-O Bonds Cleaving Cyclization of (Phenoxymethyl)arenes with Carbonyls to Benzofurans
Zheng, Hong-Xing,Shan, Xiang-Huan,Qu, Jian-Ping,Kang, Yan-Biao
, p. 3310 - 3313 (2018/06/11)
An intermolecular addition of carbon radicals enabled by a cascade radical coupling strategy is developed. It includes an intermolecular alkyl radical addition to a carbonyl group followed by an intramolecular alkoxy radical addition to haloarenes and produces substituted benzofurans in high yields. The radical nature of this reaction is explored by radical trapping experiments and EPR analysis. The mechanism is investigated by KIE experiments and control experiments. This method could provide rapid and practical access to the key intermediate of TAM-16, a safe and potent antibacterial agent for treating tuberculosis, and, therefore, is of great importance for organic synthesis and the pharmaceutical industry.
Phenanthroline- tBuOK Promoted Intramolecular C-H Arylation of Indoles with ArI under Transition-Metal-Free Conditions
Shan, Xiang-Huan,Yang, Bo,Zheng, Hong-Xing,Qu, Jian-Ping,Kang, Yan-Biao
, p. 7898 - 7901 (2019/01/04)
The first example of phenanthroline-tBuOK promoted intramolecular radical C-H arylation of N-(2-iodobenzyl)indoles without involvement of transition metals has been developed. A variety of substituted 6H-isoindolo [2, 1-a] indoles were prepared by a simple and efficient intramolecular cyclization using 1,10-phenanthroline in the presence of potassium tert-butoxide and chlorobenzene. This strategy provides a fast and versatile access to isoindolo[2,1-a]indole derivatives for the synthesis of pharmaceuticals and organic electroluminescent (EL) materials.
PYRIDONE DERIVATIVES AND THEIR USE AS KINASE INHIBITORS
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Page/Page column 188; 189, (2017/05/10)
Disclosed in the present application is a compound of formula (I) as defined herein as well as a pharmaceutical composition comprising said compound. Further disclosed in the present application is the use of such pharmaceutical compositions for treating diseases, namely inter alia for use in the treatment of cancer, metabolic, inflammatory, autoimmune and viral diseases. The compounds disclosed herein are inhibitors of MNK1 and/or MNK2 kinases.
Silver-Catalyzed Decarboxylative Bromination of Aliphatic Carboxylic Acids
Tan, Xinqiang,Song, Tao,Wang, Zhentao,Chen, He,Cui, Lei,Li, Chaozhong
supporting information, p. 1634 - 1637 (2017/04/11)
The silver-catalyzed Hunsdiecker bromination of aliphatic carboxylic acids is described. With Ag(Phen)2OTf as the catalyst and dibromoisocyanuric acid as the brominating agent, various aliphatic carboxylic acids underwent decarboxylative bromination to provide the corresponding alkyl bromides under mild conditions. This method not only is efficient and general but also enjoys wide functional group compatibility. An oxidative radical mechanism involving Ag(II) intermediates is proposed.
C–C bond-forming reactions of ground-state aryl halides under reductive activation
Emery, Katie J.,Tuttle, Tell,Kennedy, Alan R.,Murphy, John A.
, p. 7875 - 7887 (2016/11/17)
Under basic conditions aryl halides can undergo SRN1 reactions, BHAS reactions and benzyne formations. Appropriate complex substrates afford an opportunity to study inherent selectivities. SRN1 reactions are usually favoured under ph
