On August 6, 2015, Kobayashi, Kaori; Suzuki, Tamotsu; Kawahira, Mizuki; Fujii, Tomohiro; Sugiki, Masayuki; Ohsumi, Koji; Okuzumi, Tatsuya published a patent.HPLC of Formula: 386704-04-7 The title of the patent was Preparation of heterocyclic sulfonamide derivatives as TRPA1 antagonists for treating pain, digestive diseases, and inflammatory diseases. And the patent contained the following:
The heterocyclic sulfonamide derivatives are represented by formula I [Q = O, S; A = 6-membered aromatic or heterocyclic ring, bicyclic aromatic or heterocyclic ring; A1 = C(Ra), N; A2 = C(Rb), N; A3 = C(Rc), N; A4 = C(Rd), N; Ra-Rd = H, halo, cyano, OH, C1-6 alkyl, etc.; least two of A1-A4 are not N; R1 = H, (un)substituted C1-6 alkyl; R2 = H, (un)substituted C1-6 alkyl or C2-6 alkenyl; R3-R5 = H, C1-6 alkyl; R1 and R2 may form (un)substituted heterocycle; R4 and R5 may form cycloalkane; X = (un)substitued C, (un)substited N, or S-containing Cy; Cy = (un)substituted and hetero-(un)containing saturated or unsaturated cyclic group; R6 = (un)substituted C1-6 alkyl, C2-6 alkenyl, halo, OH, amino, etc.; m = 0-3], excluding II. Thus, Mitsunobu reaction of (2S)-1-(benzofuran-2-ylsulfonyl)-N-[(3-hydroxyphenyl)methyl]pyrrolidine-2-carboxamide (preparation given) and 4-hydroxybenzonitrile (sic) gave (2S)-1-(benzofuran-2-ylsulfonyl)-N-[[3-[(4-cyanophenyl)methoxy]phenyl]methyl]pyrrolidine-2-carboxamide showing human transient receptor potential ankyrin 1 antagonistic activity (IC50) 0.0030 μM. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).HPLC of Formula: 386704-04-7
The Article related to heterocyclic sulfonamide preparation trpa1 antagonist pain digestive inflammatory, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.HPLC of Formula: 386704-04-7
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