36192-61-7Relevant articles and documents
Dual Role of Anthranils as Amination and Transient Directing Group Sources: Synthesis of 2-Acyl Acridines
Kim, Saegun,Han, Sang Hoon,Mishra, Neeraj Kumar,Chun, Rina,Jung, Young Hoon,Kim, Hyung Sik,Park, Jung Su,Kim, In Su
, p. 4010 - 4014 (2018)
The transient directing group promoted C(sp2)-H functionalization of benzaldehydes with anthranils by a cationic rhodium(III) catalyst is described. Notably, anthranils have been used as both transient directing groups and amination sources to afford 2-acyl acridines through direct C-H amination followed by acid-mediated cyclization. A range of substrate scopes and functional group tolerance were observed.
Synthesis of 1-Amino-2,2,2-trifluoroalkylphosphonates from Alkene-Tethered Trifluoroacetimidoyl Chlorides
Rodríguez, José F.,Zhang, Anji,Arora, Ramon,Lautens, Mark
supporting information, p. 7540 - 7544 (2021/10/12)
The reaction of alkene-tethered trifluoroacetimidoyl chlorides with trialkyl phosphites furnishes 1-amino-2,2,2-trifluoroalkylphosphonates. The products were generated in moderate to good yields, and the scalability of this process was showcased. Partial hydrolysis of the phosphonate moiety was achieved. The cyclization is proposed to occur via formation of an imidoyl phosphonate intermediate that becomes susceptible to nucleophilic attack at nitrogen through the strong electron-withdrawing groups at the imidoyl carbon.
Novel 2-acyl Acridine derivatives, preparation method thereof, and pharmaceutical compositions for the prevention or treatment of cancer containing the same as an active ingredient
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Paragraph 0050; 0155; 0167; 0168, (2020/04/24)
The present invention relates to a novel 2-acyl acridine derivative having an anticancer activity and an anti-inflammatory activity, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient. The novel 2-acyl acridine derivative is a 2-acyl acridine derivative represented by chemical formula 1, an isomer of the 2-acyl acridine derivative, or a pharmaceutically acceptable salt of the 2-acyl acridine derivative. As results of taking keenly to the study of 2-acyl acridine to use 2-acyl acridine in treatment of various viruses, cancer, leukemia and others, the present inventors have found that a 2-acyl acridine derivative can be efficiently produced by intramolecular cyclization in addition to C-H amination due to catalyzation of aldimine and rhodium (III) along with anthranyl, and the 2-acyl acridine derivative produced through such a process has an excellent effect of treating cancer and inflammation. Therefore, it is expected that the 2-acyl acridine derivative can be used as a pharmaceutical composition for prevention or treatment of cancer or inflammation. Further, it is expected that a preparation method of the 2-acyl acridine derivative using a rhodium (III) catalyst, as a reaction which can be applied to or introduced into a wide range of functional groups and has regioselectivity and chemical selectivity, is very useful in the synthesis of a new drug or a compound having biological activities.COPYRIGHT KIPO 2020