288254-71-7Relevant articles and documents
Triple-Bond Directed Csp2?N Bond Formation with N-Fluorobenzenesulfonimide as Aminating Source: One-Step Transformation of Aldehydes into Amines
Sushmita,Aggarwal, Trapti,Shibata, Norio,Verma, Akhilesh K.
, p. 16063 - 16067 (2019)
A metal-free, versatile triple-bond directed approach for the decarbonylative C?H amination of ortho-alkynyl quinoline/pyridine aldehydes using N-fluorobenzenesulfonimide as nitrogen source under mild reaction conditions has been described. The designed reaction strategy was triggered by trapping of fluorine by base with subsequent attack of bis(phenylsulfonyl)-λ2-azane on the carbonyl carbon of a heterocycle, which was gradually converted into the corresponding amine through a Curtius type rearrangement. This protocol provides a one-step approach for the conversion of aldehydes into amines in good yields. The synthesized amines were successfully transformed into biologically important pyrroloquinolines/pyridines.
AMIDE DERIVATIVES AND DRUGS
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Page 22, (2010/02/08)
The present invention provides an amide derivative represented by the following formula [1]: wherein n represents 0 or 1; X represents CR4 or N; Y represents CR6 or N; Z represents CR7 or N; R1 and R2 may be the same or different and each represents hydrogen, optionally substituted alkyl, acyl, optionally substituted aryl, or an optionally substituted aromatic heterocyclic group; R4, R5, R6 and R7 may be the same or different and each represents hydrogen, halogen, hydroxy, amino, alkyl, haloalkyl, alkoxy, monoalkylamino, dialkylamino, arylalkyl, cyano, or nitro; and R3 represents optionally substituted alkylamino, optionally substituted arylamino, or optionally substituted cyclic amino, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising them as an active ingredient. The compound of the present invention is useful as a TGF-β inhibitor.