On July 8, 2003, Mavunkel, Babu J.; Liu, David Y.; Schreiner, George F.; Lewicki, John A.; Perumattam, John J. published a patent.Reference of 6-Chloro-1H-indole-5-carboxylic acid The title of the patent was Preparation of indoles, benzimidazoles and benztriazoles for treating cardiac failure and other disorders. And the patent contained the following:
The title compounds I and II [Z1, Z2 = CR4, N; R4 = H, alkyl, aryl, each of said alkyl or aryl optionally including one or more heteroatoms selected from O, S and N and optionally substituted by one or more of halo, OR, SR, NR2, RCO, CO2R, CONR2, O2CR, NROCR, etc. and R = H, alkyl; R1 = Q and X1 = CO, SO, SO2, CHOH; m = 1; Y = alkyl, aryl, arylalkyl; YY = alkylene bridge; n = 0-2; Z3 = N; X2 = CH, CH2 or an isostere; Ar = one or two Ph moieties directly coupled to X2 optionally substituted by halo, nitro, alkyl, etc.; R2 = H, alkyl, aryl; R3 = H, halo, NO2, alkyl, alkenyl, etc.], useful as selective inhibitors of p38α kinase, were prepared Thus, amidation of benzimidazole-5-carboxylic acid with 4-benzylpiperidine in the presence of EDAC and DMAP in DMF afforded 47% 4-benzylpiperidinyl-benzimidazole-5-carboxamide which showed 85% inhibition of p38β at 50 μM. The compounds I were tested for their specificity for p38α as compared to p38β (data given). The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).Reference of 6-Chloro-1H-indole-5-carboxylic acid
The Article related to benzimidazole preparation p38 kinase inhibitor, heart failure benzimidazole benzotriazole indole preparation, benzotriazole preparation p38 kinase inhibitor, indole preparation p38 kinase inhibitor and other aspects.Reference of 6-Chloro-1H-indole-5-carboxylic acid
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