On February 7, 2013, Baloglu, Erkan; Ghosh, Shomir; Lobera, Mercedes; Schmidt, Darby R. published a patent.Quality Control of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Preparation of substituted phenylacetamides as novel retinoid-related orphan receptor gamma (RORγ) modulators. And the patent contained the following:
The title compounds I [m = 0-2; n = 1-3; X1-X5 = N, N(O), CH, CR5; one of Y1 and Y2 = O or NR8 and the other is bond; or X1 = CR5, Y1 = NR8, Y2 = a bond, and R5 and R8, taken together with the atoms to which they are attached, form (un)substituted 5-7 membered ring, optionally containing an addnl. heteroatom selected from O, N and S; Cy = (un)substituted cycloalkyl, hetreocycloalkyl, Ph or 5-6 membered heteroaryl; Z = O, S, SO2, C(O), NR6, a bond; A1-A5 = N, N(O), CH, CR10; R1 = alkyl, haloalkyl, cycloalkyl, etc.; R2 = H, alkyl, haloalkyl; or R1 and R2 taken together with the carbon atom to which they are attached form (un)substituted 3-8 membered ring, optionally containing a heteroatom selected from O, N, and S; R3 and R31 = H, OH, alkyl, etc.; R4 = H, halo, alkyl, etc.; R41 = H, halo, OH, NH2, alkyl; or R4 and R41 taken together with the carbon atom to which they are attached form (un)substituted 3-8 membered ring, optionally containing a heteroatom selected from O, N, and S; R5 = alkyl, haloalkyl, cycloalkyl, etc.; R6 = H, alkyl, haloalkyl, etc.; R8 = H, alkyl, haloalkyl; R10 = alkyl, haloalkyl, cycloalkyl, etc.; with the provisos], useful as novel retinoid-related orphan receptor gamma (RORγ) modulators in the treatment of diseases mediated by RORγ, were prepared E.g., a multi-step synthesis of II, starting from 2-chloro-4-methylbenzonitrile and phenylmagnesium bromide, was described. Exemplified compounds I were tested in the dual FRET assay and were found to have a pIC50 between 5 and 9. Pharmaceutical composition comprising the compound I was disclosed. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Quality Control of Methyl 2-(2-aminothiazol-4-yl)acetate
The Article related to phenylacetamide preparation retinoid related orphan receptor gamma rorgamma modulator, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.Quality Control of Methyl 2-(2-aminothiazol-4-yl)acetate
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica