On March 1, 2007, Urade, Yoshihiro; Shigeno, Kazuhiko; Tanaka, Yuki; Kuze, Jiro; Tsuchikawa, Michinori; Hosoya, Toshiyuki published a patent.Computed Properties of 29704-38-9 The title of the patent was Preparation of pyrimidine-5-carboxamide derivatives as prostaglandin D synthase inhibitors. And the patent contained the following:
The title compounds [I; R1 = (un)substituted 5- or 6-membered unsaturated heterocyclyl or Ph; R2 = unsaturated heterocyclyl containing 1-3 heteroatom(s) selected from N, O, and S atoms containing 0-2 number of R3(CH2)m group(s), Ph containing R3(CH2)m group(s) at one or both of 3- and 4-positions; m = 0-4; R3 = halo, cyano, NO2, (un)substituted and (un)saturated heterocyclyl, (un)substituted NH2, COR6, OR7, SR8; R6 = H,HO, (un)substituted C1-6 alkoxy or NH2; R7 = H, (un)substituted C1-6 alkyl, C2-6 alkenyl, (un)substituted carbonyl; R8 = H, (un)substituted C1-6 alkyl] or salts thereof are prepared These compounds exhibit high inhibitory effect on hematopoietic prostaglandin D synthase and are useful for the prevention and/or treatment of allergic diseases, inflammatory diseases, Alzheimer’s disease, or brain injury. Thus, 2-phenoxypyrimidine-5-carboxylic acid was condensed with 4-aminobenzoic acid tert-Bu ester using 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride and 1-hydroxybenzotriazole in pyridine at 60° for 16 h to give 47% 2-phenoxy-N-(4-tert-butoxycarbonylphenyl)-5-pyrimidinecarboxamide (II). II and 2-phenoxy-N-[4-[2-[[(thiophen-2-yl)carbonyl]amino]ethyl]phenyl]-5-pyrimidinecarboxamide showed IC50 of 0.260 and 0.141 μg/mL, resp., against human hematopoietic prostaglandin D. The experimental process involved the reaction of tert-Butyl 2-(4-nitrophenyl)acetate(cas: 29704-38-9).Computed Properties of 29704-38-9
The Article related to pyrimidinecarboxamide preparation hematopoietic prostaglandin d synthase inhibitor, allergy inflammation prevention treatment pyrimidinecarboxamide preparation, alzheimer disease brain injury prevention treatment pyrimidinecarboxamide preparation and other aspects.Computed Properties of 29704-38-9
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