On November 30, 2000, Mavunkel, Babu J.; Chakravarty, Sarvajit; Perumattam, John J.; Dugar, Sundeep; Lu, Qing; Liang, Xi published a patent.Electric Literature of 256935-86-1 The title of the patent was Preparation of 5-[4-benzylpiperidinyl(piperazinyl)]-indolecarboxamides as inhibitors of p38 kinase. And the patent contained the following:
The title compounds [I; one Z2 = CA, CR8A and the other = CR1, CR12, NR6, N (wherein R1, R6, R8 = H, noninterfering substituent; A = WiCOXjY; Y = COR2, an isostere; R2 = H, noninterfering substituent; W, X = spacer of 2-6Å; i, j = 0-1); Z3 = NR7, O; R3 = noninterfering substituent; n = 0-3; L1, L2 = linker; R4 = noninterfering substituent; m = 0-4; Z1 = CR5, N (R5 = H, noninterfering substituent); l, k = 0-2, wherein the sum of l and k = 0-3; Ar = aryl substituted with 0-5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; the distance between the atom of Ar linked to L2 and the center of the α ring is 4.5-24Å] which inhibit p38-α kinase (biol. data given), were prepared Thus, treating 6-methoxy-(4-benzylpiperidinyl)-indole-5-carboxamide with oxalyl chloride in CH2Cl2 afforded the indole-5-carboxamide II. 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 indolecarboxamide benzylpiperidinyl benzylpiperazinyl preparation p38 kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) 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