On February 4, 2010, Mikamiyama, Hidenori; Ni, Chiyou; Shao, Bin; Tafesse, Laykea published a patent.Application In Synthesis of Ethyl 2-(4-(trifluoromethoxy)phenyl)acetate The title of the patent was Preparation of tetrahydropyridine and dihydropyrrole compounds as calcium channel blockers for treatment of pain and other disorders. And the patent contained the following:
The invention relates to tetrahydropyridinyl and dihydropyrrolyl compounds of formula I (wherein X = CO, CH2, or is part of a bridge; R9 = H or is part of a bridge; Hy = a 6- or 5-membered heteroaromatic ring, or a 5-membered heterocyclic ring; Z = SO2-aryl; SO2-cycloalkenyl, CH2-aryl, etc.; R1 = CN, OH-alkyl, CO2H, etc.; R2 = alkyl, alkenyl, alkynyl, etc.; m = 0-3; n = 0-1) and pharmaceutically acceptable salts, prodrugs, or solvates thereof. The invention is also directed to the use of compounds of formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain. Exemplary methods for synthesizing compounds of the invention were described, e.g., II was prepared by a multi-step synthesis involving the preparation of intermediate N-cyclopropyl-6-(1,2,3,6-tetrahydropyridin-4-yl)picolinamide and subsequent reaction with 4-trifluoromethoxybenzaldehyde to give II. Compounds of the invention were tested as N-type calcium channel (NTCC) blockers, and II demonstrated an IC50 value of 0.03 μM. II was also tested in the calcium mobilization assay for L-type calcium channel (LTCC) blocking activity and it showed an LTCC IC50 value of >20 μM in that assay. The experimental process involved the reaction of Ethyl 2-(4-(trifluoromethoxy)phenyl)acetate(cas: 1206550-93-7).Application In Synthesis of Ethyl 2-(4-(trifluoromethoxy)phenyl)acetate
The Article related to tetrahydropyridine dihydropyrrole compound preparation pain calcium channel disorder treatment, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Application In Synthesis of Ethyl 2-(4-(trifluoromethoxy)phenyl)acetate
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