Polycyclic compound and preparation method and application thereof
The invention discloses a polycyclic compound and a preparation method and application thereof. The invention provides a polycyclic compound shown as a formula I or a pharmaceutically acceptable saltthereof. The compound has a relatively good inhibition effect on CDK7.
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Paragraph 0267-0268; 0272-0275
(2020/07/15)
P -Toluenesulfonic Acid Induced Conversion of Fluorinated Trimethylsilylethynylanilines into Aminoacetophenones: Versatile Precursors for the Synthesis of Benzoazaheterocycles
A simple and efficient approach to the synthesis of fluorinated amino-substituted acetophenones in good to excellent yields is reported. The heart of the proposed method consists of conversion of a Me 3 Si-C≡C- moiety into a MeC(=O)- group in the presence of p -tolu ene sulfonic acid (p -TSA) passing a stage of ethynylaniline formation. The reaction is metal-free, proceeds under mild conditions, and uses readily available starting compounds (trimethylsilylarylacetylene derivatives). The reaction provides access to amino-substituted acetophenones, which may serve as precursors for the synthesis of polyfluorinated azaheterocycles, having potential anticarcinogenic activity.
Politanskaya, Larisa,Tretyakov, Evgeny
p. 555 - 564
(2017/11/03)
CuI-Catalyzed intramolecular aminocyanation of terminal alkynes in N-(2-ethynylphenyl)-N-sulfonylcyanamides via Cu-vinylidene intermediates
CuI-Catalyzed intramolecular aminocyanation of terminal alkynes in N-(2-ethynylphenyl)-N-sulfonylcyanamides was initiated by the formation of Cu-acetylide to trigger N-CN bond cleavage of the N-sulfonylcyanamide moiety followed by CN migration to form a β-cyano Cu-vinylidene intermediate. Subsequently, the indole ring closure furnished the corresponding 1-sulfonyl-3-cyanoindoles.
Liao, Zhen-Yuan,Liao, Pen-Yuan,Chien, Tun-Cheng
supporting information
p. 14404 - 14407
(2016/12/23)
4-AMINO-6-(HETEROCYCLIC)PICOLINATES AND 6-amino-2-(HETEROCYCLIC)pyrimidine-4-carboxylates AND THEIR USE AS HERBICIDES
4-Amino-6-(heterocyclic)picolinic acids and their derivatives; 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives; and methods of using the same as herbicides.
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Paragraph 0306; 0307; 0308
(2014/09/29)
Gold(III)-catalyzed annulation of 2-alkynylanilines: A mild and efficient synthesis of indoles and 3-haloindoles
Gold(III)-catalyzed annulation of 2-alkynylanilines in EtOH or EtOH-water mixtures at room temperature gives indoles derivatives in good yields. One-flask protocol for the gold-catalyzed conversion of 2-alkynylanilines to 3-bromo and 3-iodoindoles is also reported.