852927-43-6Relevant articles and documents
Iron-Mediated Electrophilic Amination of Organozinc Halides using Organic Azides
Gra?l, Simon,Singer, Johannes,Knochel, Paul
supporting information, p. 335 - 338 (2019/11/22)
A wide range of alkyl-, aryl- and heteroarylzinc halides were aminated with highly functionalized alkyl, aryl, and heterocyclic azides. The reaction proceeds smoothly at 50 °C within 1 h in the presence of FeCl3 (0.5 equiv) to furnish the corresponding secondary amines in good yields. This method was extended to peptidic azides and provided the arylated substrates with full retention of configuration. To demonstrate the utility of this reaction, we prepared two amine derivatives of pharmaceutical relevance using this iron-mediated electrophilic amination as the key step.
Preparation method for arylamine benzamides compounds and N-aryl-arylamine benzamides compounds
-
Paragraph 0087; 0088; 0089; 0090, (2018/01/03)
The invention provides a preparation method for arylamine benzamides compounds and N-aryl-arylamine benzamides compounds and belongs to the technical field of refining. According to the method provided by the invention, carbon nitrogen coupling reaction is performed by using arylboronic acid (or borate) as an aryl reagent under a copper-catalyzed condition, the reaction is performed at 10-35 DEG C and the selective arylation of aminophenamide is realized. Compared with the present Buchwald-Hartwig carbon nitrogen coupling reaction under palladium-catalyzed condition, the carbon nitrogen coupling reaction has the advantages that the catalyst is low in cost and low in toxicity, the raw materials are simple, easily acquired, stable and low-toxicity, the reaction temperature is greatly reduced, inert gas atmosphere protection is not required, the stirring reaction can be directly performed in an opening reaction flask under a room temperature condition, the condition is mild and the operation is easy, aniline locally has high-selective arylation reaction, the reaction yield is high, the product is easily purified and the atom economy is high.
DIPHENYLAMINE DERIVATIVES
-
Page/Page column 27, (2010/02/11)
The invention relates to compounds of the formula (I) in which: i and j=1; R1 is in position 3 or 4 on the phenyl ring and represents a cyano group, an alkoxy group substituted by halogen, a thioalkyl group, an alkylcarbonyl group or an alkylsulfonyl group; and R2 represents a carboxyl group, an aikoxycarbonyl group, an alkylcarbonyl group, an unsubstituted amide group or a linear or branched alkyl group substituted by a cyano, hydroxyl, carboxyl, aikoxycarbonyl or unsubstituted amide group; and also the pharmaceutically acceptable derivatives, salts, solvates and stereoisomers thereof, including mixtures thereof in all propor-tions.