94258-13-6Relevant academic research and scientific papers
Copper-Catalyzed Synthesis of β- And δ-Carbolines by Double N-Arylation of Primary Amines
Van Phuc, Ban,Do, Ha Nam,Quan, Nguyen Minh,Tuan, Nguyen Ngoc,An, Nguyen Quang,Van Tuyen, Nguyen,Anh, Hoang Le Tuan,Hung, Tran Quang,Dang, Tuan Thanh,Langer, Peter
, p. 1004 - 1008 (2021/04/12)
Two efficient and practical approaches are reported for the synthesis of β- and δ-carbolines from 3,4-dibromopyridine. The synthesis is based on site-selective Cu-catalyzed double C-N coupling reactions and subsequent annulations by twofold Pd-catalyzed C-N coupling with amines.
Efficient access to β- and γ-carbolines from a common starting material by sequential site-selective Pd-catalyzed C–C, C–N coupling reactions
Hung, Tran Quang,Hieu, Do Trung,Van Tinh, Dinh,Do, Ha Nam,Nguyen Tien, Tuan Anh,Van Do, Dang,Son, Le Thanh,Tran, Ngoc Han,Van Tuyen, Nguyen,Tan, Vu Minh,Ehlers, Peter,Dang, Tuan Thanh,Langer, Peter
, (2019/09/07)
Two efficient and practical approaches are reported for the synthesis of β- and γ-carboline derivatives from 3,4-dibromopyridine as a common starting material. The β-carbolines were prepared by site-selective Pd-catalyzed C–C coupling with o-bromophenylboronic acid and subsequent cyclization by double C–N coupling with amines. γ-Carbolines were prepared from the same starting material by C–N coupling with anilines and subsequent annulation by domino C–C/C–N coupling with o-bromophenylboronic acid.
Beta and gamma carboline derivatives as potential anti-Alzheimer agents: A comparison
Otto, Robert,Penzis, Robert,Gaube, Friedemann,Winckler, Thomas,Appenroth, Dorothea,Fleck, Christian,Tr?nkle, Christian,Lehmann, Jochen,Enzensperger, Christoph
, p. 63 - 70 (2015/01/09)
Nine novel β2- and 3-carboline derivatives bearing either methyl-, propargyl- or phenethyl-residues at the indole nitrogen were synthesized and tested as potential anti-Alzheimer drugs. Antagonism of recombinantly expressed NMDA receptors, inhibition of cholinesterases, and radical scavenging properties were determined for all compounds. Some were additionally tested in vivo for their ability to reverse scopolamine-induced cognitive impairment in an 8-arm radial maze experiment with rats. For the most promising candidates, the interaction with muscarinic M1receptors was also investigated. With this set of compounds assays the influence of the scaffold itself and the substituents can be investigated separately. 5-Methyl-β3-carboline (6) was the most potent (0.25 1/4mol/100 g b.w.) compound in the in vivo test and might be a good starting point for the development of novel anti-Alzheimer drugs.
