On March 18, 2004, Chakravarty, Sarvajit; Dugar, Sundeep; Lu, Qing; Luedtke, Gregory R.; Mavunkel, Babu J.; Perumatam, John Joseph; Tester, Richland published a patent.Electric Literature of 256935-86-1 The title of the patent was Preparation of piperidinylcarbonyl- and piperazinylcarbonylindolamines as p38 kinase inhibitors.. And the patent contained the following:
Title compounds [I; 1 Z2 = CA, the other = CR1; R1, R2, R5, R6 = H, noninterfering substituent; A = WiCOXjY; Y = COR2; W, X = spacer of 2-6Å; i, j = 0, 1; 2 R6 may form a 5-6 membered ring; m = 0-4; n = 0-3; L1, L2 = linker; R4 = noninterfering substituent; Z1 = N, CR5; Ar = (substituted) (fused) Ph, thienyl], were prepared for treatment of pro-inflammation response (no data). Thus, 1-(4-fluorobenzyl)-2S,5R-dimethylpiperazine, 6-chloroindole-5-carboxylic acid (preparation given), TBTU, and Et3N were stirred in DMF overnight to give 92% amide, which in CH2Cl2 at 0° was treated with (COCl)2 followed by stirring at room temperature for 5 h. Pyrrolidine was added followed by stirring for 1 h to give 71% 1-[6-chloro-5-[4-(4-fluorobenzyl)-2R,5S-dimethylpiperazine-1-carbonyl]-1H-indol-3-yl]-2-pyrrolidin-1-ylethane-1,2-dione. This was stirred with NaH in THF for 30 min.; O-(diphenylphosphinyl)hydroxylamine was added followed by stirring for 10 h to give 1-[1-amino-6-chloro-5-[4-(4-fluorobenzyl)-2R,5S-dimethylpiperazine-1-carbonyl]-1H-indol-3-yl]-2-pyrrolidin-1-ylethane-1,2-dione. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).Electric Literature of 256935-86-1
The Article related to piperidinylcarbonylindolamine piperazinylcarbonylindolamine preparation p38 kinase inhibitor, indolyloxoacetamide amino piperazinylcarbonyl preparation p38 kinase inhibitor, pulmonary sarcosis silicosis cerebral malaria treatment aminoindole preparation, restenosis psoriasis cns reperfusion injury treatment aminoindole preparation and other aspects.Electric Literature of 256935-86-1
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