On March 17, 2016, Nagamochi, Masatoshi; Gotanda, Kentoku; Noguchi, Tetsuji; Goto, Taiji; Sasaki, Junko; Torihata, Munefumi; Yoshino, Toshiharu; Isobe, Takashi; Ramadass, Venkataramanan published a patent.Recommanded Product: 4-Bromo-5-methoxy-2-methylaniline The title of the patent was Preparation of carboxylic acid derivatives as RORγt (retinoic acid receptor-related orphan receptor γt) inhibitors. And the patent contained the following:
Title compounds I [R1 = alkyl, cycloalkyl or phenyl; R2 = H, halo, alkyl, etc.; R3 = H, carboxy-alkyl or hydroxy; R4 = halo or alkyl; R5 = H or alkyl; R6 = H, halo or alkyl; R7 = H, halo, alkyl, etc.; R8 = hydroxy, alkoxy, monoalkylamino, etc.; L = single bond, methylene or oxygen atom; E = phenylene (optionally substituted with halo, alkyl or alkylsulfonyl), pyridinylene (optionally substituted with halo, alkyl or alkylsulfonyl), thienylene, etc.; Q1 = nitrogen atom or CH; Q2 = nitrogen atom or CH; -U-T- = -CH2CH2- or -CH:CH-; Y = methylene or oxygen atom; V = nitrogen atom or C(R9); R9 = H, alkyl, cycloalkyl, etc.; or pharmaceutically acceptable salts thereof], useful for the treatment of psoriasis, psoriatic arthritis, etc., were prepared For example, EDCI-mediated amidation of II [R = OH] (prepared from 1-bromo-4-iodo-2-methylbenzene in a multi-step process) with methylamine·HCl afforded compound II [R = NHMe]. In IL-17 production inhibition assay, 81-example of I showed IC50 values (nM) ranging from 4.48 to 1110, e.g., IC50 of II [R = NHMe] was 4.48 nM. Pharmaceutical compositions comprising I are disclosed. The experimental process involved the reaction of 4-Bromo-5-methoxy-2-methylaniline(cas: 152626-77-2).Recommanded Product: 4-Bromo-5-methoxy-2-methylaniline
The Article related to carboxylic acid preparation ror gamma t inhibitor, psoriasis psoriatic arthritis treatment ror gamma t inhibition, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 4-Bromo-5-methoxy-2-methylaniline
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem