On September 18, 2003, Albaugh, Pamela Ann; Ammenn, Jochen; Burkholder, Timothy Paul; Clayton, Joshua Ryan; Conner, Scott Eugene; Cunningham, Brian Eugene; Engler, Thomas Albert; Furness, Kelly Wayne; Henry, James Robert; Li, Yihong; Malhotra, Sushant; Tebbe, Mark Joseph; Zhu, Guoxin published a patent.SDS of cas: 52537-00-5 The title of the patent was Preparation of 3-(indol-3-yl) 4-heteroaryl substituted pyrrole-2,5-diones as GSK-3β inhibitors. And the patent contained the following:
The title compounds [I; Ar = (un)substituted benzofuryl, indolyl, quinolinyl, etc.; R1 = H, alkoxy, halo, etc.; R2 = H, alkyl, (un)substituted piperidin-4(or 3)-yl, etc.; R3 = H, halo, alkyl, cyclopropyl; or R2 and R3 taken together = CH2CH2CH(CH2OH)CH2; R4, R5 = H, halo], useful for treating GSK-3β mediated diseases such as diabetes and Alzheimer’s disease, were prepared Thus, reacting 2-[1-(3-hydroxypropyl)-1H-indol-3-yl]acetamide with Me (1-methyl-1H-indol-4-yl)oxoacetate in the presence of tert-BuOK in DMF afforded 54% I [Ar = 1-methyl-1H-indol-4-yl; R1, R3-R5 = H; R2 = 3-hydroxypropyl] which showed IC50 of 0.1757 μM against GSK-3β. Pharmaceutical composition comprising the compound I was claimed. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).SDS of cas: 52537-00-5
The Article related to indolyl heteroaryl pyrroledione preparation gsk3beta inhibitor antidiabetic alzheimer’s disease, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.SDS of cas: 52537-00-5
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles