124705-25-5Relevant academic research and scientific papers
Anticancer-Active N-Heteroaryl Amines Syntheses: Nucleophilic Amination of N-Heteroaryl Alkyl Ethers with Amines
Wang, Xia,Yang, Qiu-Xia,Long, Cheng-Yu,Tan, Yan,Qu, Yi-Xin,Su, Min-Hui,Huang, Si-Jie,Tan, Weihong,Wang, Xue-Qiang
, p. 5111 - 5115 (2019)
A mild amination protocol of N-heteroaryl alkyl ethers with various amines is described. This transformation is achieved by utilizing simple and readily available base as promoter via C-O bond cleavage, offering a new amination strategy to access several anticancer-active compounds. This work is highlighted by the excellent functional group compatibility, scalability, wide substrate scope, and easy derivatization of a variety of drugs.
Synthesis method of aza-arylamine compound and aza-arylamine compound
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Paragraph 0056; 0057; 0058; 0075, (2019/04/26)
The invention provides a synthesis method of an aza-arylamine compound as shown in a formula (I). The synthesis method comprises the following steps: an aza aromatic hydrocarbon compound as shown in aformula (II) reacts with an amine compound as shown in a formula (III) in presence of alkali and under a heating condition, so that u X substituent groups on an A ring of the compound as shown in theformula (II) are substituted by NRR in the compound as shown in the formula (III), and the compound as shown in the formula (I) is obtained, wherein A is an aza six-membered aromatic ring or five-membered aromatic ring, and is an independent single ring or is fused with a ring B; X refers to that the A ring has at least n X substituent groups, each X substituent group is independently selected from the group consisting of F, Cl, Br, I, CN, alkoxy of C and alkylthio of C, and n is a positive integer selected from 1-5; and the alkali is one or a mixture of more selected fromof BuOK, BuONa, BuONa, KHMDS, NaHMDS and LiHMDS. The synthesis method provided by the invention does not need the use of transition metal catalysts, is simple and convenient to operate, is economical and practical and is environmentally friendly. In addition, the invention also provides the aza-arylamine compound prepared by the method.
