On August 13, 2020, Genung, Nathan; Guckian, Kevin M.; Vessels, Jeffrey; Zhang, Lei; Gianatassio, Ryan; Lin, Edward Yin Shiang; Xin, Zhili published a patent.Quality Control of 3-Chloro-6-fluorobenzo[d]isoxazole The title of the patent was Preparation of heteroaryloxypyrrolidinylmethylthiazolylacetamide derivatives and analogs for use as O-GlcNAcase inhibitors. And the patent contained the following:
Title compounds I [R1 = halo, alkyl, haloalkyl, or alkoxy; R3 = H or alkyl; R4 = H, alkyl, haloalkyl, or cycloalkyl; or R3 and R4 are taken together with their intervening atoms to form an (un)substituted heterocyclyl; R5 = (un)substituted bicyclic aryl, bicyclic heteroaryl, bicyclic cycloaliphatic, or bicyclic heterocyclyl; each Y independently = CH, C(halo), N, etc. wherein at least one is N; Z = C(O), CH2C(O), (CH2)2, etc.; n = 0 to 8; p = 0 or 1; with provisions], and their pharmaceutically acceptable salts, are prepared and disclosed as O-glycoprotein-2-acetamido-2-deoxy-3-D-glucopyranosidase (O-GlcNAcase) inhibitors. Thus, e.g., II was prepared by a multistep procedure (preparation given). I were evaluated in OGA enzyme inhibition biochem. assays, e.g., II demonstrated an IC50 value of <1.0 nM. The experimental process involved the reaction of 3-Chloro-6-fluorobenzo[d]isoxazole(cas: 374554-89-9).Quality Control of 3-Chloro-6-fluorobenzo[d]isoxazole
The Article related to thiazolylacetamide heteroaryloxypyrrolidinylmethyl preparation oglcnacase oga inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Quality Control of 3-Chloro-6-fluorobenzo[d]isoxazole
Referemce:
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics