On March 20, 2003, Neya, Masahiro; Sawada, Akihiko; Ohne, Kazuhiko; Abe, Yoshito; Mizutani, Tsuyoshi; Ishibashi, Naoki; Inoue, Makoto published a patent.COA of Formula: C10H7BrN2 The title of the patent was Preparation of 2-(thiophenyl)thiopyran-1,1-dioxides as MMP or TNF-α inhibitors. And the patent contained the following:
Title compounds I [wherein R1 = (un)substituted Ph, naphthyl, bicyclic heterocyclyl, alkenyl, or alkynyl; R2 = CO2H or protected CO2H; or a salt thereof] were prepared as matrix metalloproteinase (MMP) or tumor necrosis factor α (TNF-α) inhibitors. For example, coupling of 2-(trimethylsilyl)ethyl (S)-[2-(5-bromothiophen-2-yl)-1,1-dioxo-3,4,5,6-tetrahydro-2H-thiopyran-2-yl]acetate and 2-(4′-cyano-4-biphenylyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane followed by deesterification gave II. Five compounds of the invention were tested for gelatinolytic activity against human MMP-9 and displayed inhibitory activity with IC50 values ranging from 1.37 nM to 16.0 nM. Thus, I are useful for treating and/or preventing diseases mediated by MMP or TNF-α (no data). The experimental process involved the reaction of 5-(4-Bromophenyl)pyrimidine(cas: 160377-42-4).COA of Formula: C10H7BrN2
The Article related to thiophenyl thiopyrandioxide preparation mmp tnf inhibitor, Heterocyclic Compounds (One Hetero Atom): Thiopyrans and Areno- and Diarenothiopyrans and other aspects.COA of Formula: C10H7BrN2
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia