103935-47-3Relevant academic research and scientific papers
Vinyl Thianthrenium Tetrafluoroborate: A Practical and Versatile Vinylating Reagent Made from Ethylene
Juliá, Fabio,Yan, Jiyao,Paulus, Fritz,Ritter, Tobias
supporting information, p. 12992 - 12998 (2021/09/03)
The use of vinyl electrophiles in synthesis has been hampered by the lack of access to a suitable reagent that is practical and of appropriate reactivity. In this work we introduce a vinyl thianthrenium salt as an effective vinylating reagent. The bench-stable, crystalline reagent can be readily prepared from ethylene gas at atmospheric pressure in one step and is broadly useful in the annulation chemistry of (hetero)cycles, N-vinylation of heterocyclic compounds, and palladium-catalyzed cross-coupling reactions. The structural features of the thianthrene core enable a distinct synthesis and reactivity profile, unprecedented for other vinyl sulfonium derivatives.
Pd/Cu-Catalyzed Vinylation of Terminal Alkynes with (2-Bromoethyl)diphenylsulfonium Triflate
Ming, Xiao-Xia,Wu, Shuai,Tian, Ze-Yu,Song, Jia-Wei,Zhang, Cheng-Pan
supporting information, p. 6795 - 6800 (2021/09/08)
The potential of (2-bromoethyl)diphenylsulfonium triflate to be a powerful vinylation reagent was determined by the Sonogashira cross-coupling reactions with terminal alkynes. The vinylation proceeded smoothly at 25 °C under Pd/Cu catalysis to afford a variety of 1- and 2-unsubstituted 1,3-enynes in moderate to excellent yields. This protocol represents the first application of (2-haloethyl)diphenylsulfonium triflate as a CH═CH2 transfer source in organic synthesis.
SPIRO-SULFONIMIDAMIDE DERIVATIVES AS INHIBITORS OF MYELOID CELL LEUKEMIA-1 (MCL-1) PROTEIN
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Paragraph 00437; 00439, (2021/10/22)
The disclosure is directed to compounds of Formula (I). Pharmaceutical compositions comprising compounds of Formula (I) as well as methods of their use and preparation, are also described.
ALPHA-HYDROXY PHENYLACETIC ACID PHARMACOPHORE OR BIOISOSTERE MCL-1 PROTEIN ANTAGONISTS
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Page/Page column 300, (2019/10/01)
Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
TRIOXACARCIN-ANTIBODY CONJUGATES AND USES THEREOF
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Paragraph 00474; 00477, (2019/02/25)
Provided herein are trioxacarcin-antibody drug conjugates of Formula (I): and pharmaceutically acceptable salts thereof, wherein R7 is -L-B, wherein L is a linking group, and B is an antibody or antibody fragment. Also provided are methods of preparing the antibody-drug conjugates, pharmaceutically acceptable compositions thereof, and methods of their use and treatment. Further provided are precursors to the trioxacarcin- antibody drug conjugates (e.g., compounds of Formula (II), novel trioxacarcins without an antibody conjugated thereto), pharmaceutical compositions thereof, and methods of their use and treatment.
Salts and crystals of EGFR (epidermal growth factor receptor) inhibitor and their preparation methods
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Paragraph 0098; 0099; 0100, (2018/05/16)
The invention discloses salts and crystals of an EGFR (epidermal growth factor receptor) inhibitor and their preparation methods, as well as application of the salts and crystals in preparation of drugs to treat non-small cell lung cancer.
Annulation of β-naphthols and 4-hydroxycoumarins with vinylsulfonium salts: Synthesis of dihydrofuran derivatives
Chen, Zi-Cong,Tong, Lang,Du, Zhi-Bo,Mao, Zhi-Feng,Zhang, Xue-Jing,Zou, Yong,Yan, Ming
supporting information, p. 2634 - 2638 (2018/04/26)
A new synthetic approach to dihydrofuran derivatives via the annulation reaction of β-naphthols and 4-hydroxycoumarins with vinylsulfonium salts has been developed. A variety of dihydrofuran derivatives were prepared in moderate to good yields under mild conditions. The products could be readily transformed to the corresponding furans via the dehydrogenation with DDQ.
FUSED-RING OR TRICYCLIC ARYL PYRIMIDINE COMPOUND USED AS KINASE INHIBITOR
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Paragraph 0286; 0287; 0288, (2018/03/25)
Disclosed is a fused-ring or tricyclic aryl pyrimidine compound used as a mutation selectivity EGFR inhibitor. Specifically, disclosed is a compound represented by formula (I) and used as an EGFR inhibitor or a pharmaceutically acceptable salt thereof.
COMPOUNDS THAT INHIBIT MCL-1 PROTEIN
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Page/Page column 180, (2017/09/15)
Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
COMPOUNDS AND METHODS FOR INHIBITING PRODUCTION OF TRIMETHYLAMINE
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Paragraph 0107; 0108; 0126; 0127, (2017/07/01)
The invention provides a method of inhibiting the conversion of choline or carnitine to trimethylamine (TMA) and lowering TMAO in an individual comprising administering to the individual a composition comprising a compound set forth in FORMULA (I): The in
