On March 19, 2020, Akahoshi, Issei; Sumikawa, Yoshitake; Furuta, Sadayoshi; Fukushima, Keiichiro; Imazu, Takuya; Kotaka, Ryota published a patent.Recommanded Product: 6-(Trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid The title of the patent was Preparation of heteroaromatic amide derivative for inhibiting Nav1.7. And the patent contained the following:
The present invention relates to a compound I [X-Y = N-C or C-N; Y1-Y4 = independently single bond, -CH2-, -CH2CH2-, etc.; Z1 = single bond, -O-, -S-, etc.; ring A = monocyclic aromatic ring or bicyclic aromatic ring; R1a, R1b = independently H, halo, hydroxy, etc.; R2 = H, halo, hydroxy, etc.; R3a, R3b, R3c = independently H, halo, cyano, etc.; combination of R5a, R5b, R5c, R6a, R6b and n is selected from (1), (2), (3), etc.; (1) R5b and R5c combine to form a single bond, -CH2-, -OCH2-, etc., R5a is H, alkyl, haloalkyl, etc., R6a and R6b each is H, halo, hydroxy, etc., and n is 1 or 2 (2) R5a and R6a combine to form -CH2-, -CH2CH2-, -CH2CH2O-, etc., R5b is H, alkyl or haloalkyl, R5c and R6b each is H, halo, hydroxy, etc. (or R5c and R6b may combine to form -(CH2)p-, -O(CH2)p-, -(CH2)pO-, etc. (p = 0-3)), and n is 1 (3) R5a is H, alkyl, haloalkyl, etc., R5b is H or alkyl, R5c is H, alkyl or halo, R6a and R6b each is H, halo, alkyl, etc. (or R6a and R6b, together with the carbon atom to which they are attached, may combine to form a monocyclic ring) and n is 1 or 2; or a salt thereof]. For example, compound II was prepared via cyclization of 5-(trifluoromethyl)pyridin-2-amine with Et bromopyruvate, hydrogenation, hydrolysis and HATU-mediated amidation with 6-fluorochroman-3-amine·HCl. Compound I shows selective inhibition of Nav1.7 over Nav1.5, and is useful for the treatment of pain and various Nav1.7-related disease. The experimental process involved the reaction of 6-(Trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid(cas: 1774893-22-9).Recommanded Product: 6-(Trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid
The Article related to heteroaromatic amide preparation voltage gated sodium channel blocker, analgesic heteroaromatic amide, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Recommanded Product: 6-(Trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem