On May 30, 2002, Dugar, Sundeep; Luedtke, Gregory; Tan, Xuefei published a patent.Application In Synthesis of 6-Chloro-1H-indole-5-carboxylic acid The title of the patent was Preparation of piperidinylcarbonyl- and piperazinylcarbonylindolylglyoxylates and -amides as inhibitors of p38-α kinase. And the patent contained the following:
[Title compounds I; dotted line = optional double bond; B = WiCOXjY; Y = COR2, isostere thereof; R2 = H, noninterfering substituent; W, X = spacer of 2-6 Å; i, j = 0, 1; R3 = noninterfering substituent; n = 0-3; Z3 = NR7, O; R7 = H, noninterfering substituent; 1 Z2 = C, CR8A, the other = CR1, C(R1)2, NR6, N; R1, R6, R8 = H, noninterfering substituent; A = Q1; Z1 = CR5, N; R5 = H, noninterfering substituent; p, q = 0-2; p+q = 0-3; Ar = aryl group substituted with 0-5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; R4 = noninterfering substituent; m is 0-4; L1, L2 = linker; the distance between the atom of Ar linked to L2 and the center of the Z2-containing ring = 4.5-24Å], were prepared as inhibitors of p38-α kinase (no data). Thus, title compound (II) was prepared in several steps starting from 4-nitrophenylglyoxylic acid. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).Application In Synthesis of 6-Chloro-1H-indole-5-carboxylic acid
The Article related to indolylglyoxylate piperidinylcarbonyl preparation p38 kinase inhibitor, piperazinylcarbonylindolylglyoxamide preparation p38 kinase inhibitor, proinflammation response treatment indolylglyoxamide preparation and other aspects.Application In Synthesis 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