On October 2, 2008, Boehm, Jeffrey Charles; Busch-Petersen, Jakob; Fu, Wei; Jin, Qi; Kerns, Jeffrey K.; Li, Huijie; Lin, Guoliang; Lin, Xichen; Neipp, Christopher E. published a patent.COA of Formula: C10H10BrNO2 The title of the patent was Preparation of indolecarboxamide derivatives for use as IKK2 inhibitors. And the patent contained the following:
Title compounds I [R1 = YZ; R2 = bicyclo group or (un)substituted heterocycloalkyl containing S, S(O), or SO2; R3 and R4 independently = H or F; Y = bond, alkylene, alkenylene, or alkynylene; Z = (un)substituted aryl or heteroaryl; m = 0 or 1; with provisions], and their pharmaceutically acceptable salts, are prepared and disclosed as IKK2 inhibitors. Thus, e.g., II was prepared by bromination of 1-(1,1-dimethylethyl) 7-Me 2,3-dihydro-1H-1,7-dicarboxylate (preparation given) followed by deprotection, oxidation, condensation with tetrahydro-4H-thiopyran-4-one, protection, oxidation, deprotection/hydrolysis, amidation with ammonia, and coupling with phenylboronic acid. Select I were evaluated in IKK2 assays and demonstrated a pIC50 of about 5.0 to about 8.5. I were disclosed as therapeutic agents for the inhibition of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, such as rheumatoid arthritis, asthma, rhinitis, and chronic obstructive pulmonary disease. The experimental process involved the reaction of Methyl 5-bromoindoline-7-carboxylate(cas: 860624-88-0).COA of Formula: C10H10BrNO2
The Article related to indolecarboxamide derivative preparation ikk2 inhibitor rheumatoid arthritis asthma rhinitis, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.COA of Formula: C10H10BrNO2
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