87708-16-5Relevant articles and documents
Histone deacetylase inhibitors and its preparation method and use thereof
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Paragraph 0064-0067, (2019/05/15)
The invention discloses a histone deacetylase inhibitor and its preparation method and use, the invention discloses a compound of the formula I as shown, or its crystalline form, or its pharmaceutically acceptable salt, or solvate thereof, or prodrug thereof, or its metabolic product. The invention of the formula I illustrated new compound, has shown good deacetylase inhibition activity, with the histone deacetylase for clinical treatment of diseases associated with abnormal activity of a new pharmaceutical may be.
FUSED-RING COMPOUNDS, PHARMACEUTICAL COMPOSITION AND USES THEREOF
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Paragraph 844; 845; 846, (2016/09/15)
This disclosure is related to a fused-ring compound of formula (I) and/or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the fused ring compound of formula (I) and/or a pharmaceutically acceptable salt thereof, preparation methods thereof, and use thereof in modulating activity of indoleamine 2, 3-dioxygenase (IDO) and/or tryptophan 2, 3-dioxygenase (TDO). This disclosure further provides methods of treating IDO and/or TDO-associated diseases, including cancer, viral infection and autoimmune diseases.
Copper-catalyzed oxidative amination and allylic amination of alkenes
Liwosz, Timothy W.,Chemler, Sherry R.
supporting information, p. 12771 - 12777 (2013/10/01)
Enamines and enamides are useful synthetic intermediates and common components of bioactive compounds. A new protocol for their direct synthesis by a net alkene C-H amination and allylic amination by using catalytic Cu II in the presence of MnO2 is reported. Reactions between N-aryl sulfonamides and vinyl arenes furnish enamides, allylic amines, indoles, benzothiazine dioxides, and dibenzazepines directly and efficiently. Control experiments further showed that MnO2 alone can promote the reaction in the absence of a copper salt, albeit with lower efficiency. Mechanistic probes support the involvement of nitrogen-radical intermediates. This method is ideal for the synthesis of enamides from 1,1-disubstituted vinyl arenes, which are uncommon substrates in existing oxidative amination protocols. A new protocol for the direct synthesis of enamides and allylic amines by oxidative N-H/C-H coupling of N-sulfonylanilines with vinylarenes is presented. The reaction works in both inter- and intramolecular modes and is catalyzed by copper salts by using MnO2 as the stoichiometric oxidant (see scheme). Nitrogen heterocycles including indoles, benzothiazine dioxides, and dibenzazepines can be formed. Copyright