On May 13, 2004, Bit, Rino Antonio; Giblin, Gerard Martin Paul; Hall, Adrian; Hurst, David Nigel; Kilford, Ian Reginald; Miller, Neil Derek; Scoccitti, Tiziana published a patent.Application In Synthesis of Ethyl 2-bromo-6-fluorobenzoate The title of the patent was Preparation of benzoic acids and related compounds as EP1 receptor antagonists for the treatment of prostaglandin mediated diseases.. And the patent contained the following:
Title compounds I [A = (un)substituted aryl, 5 or 6-membered heterocyclyl ring, bicyclic heterocyclyl; B = Ph, pyridyl; Z = O, S, SO, etc.; R1 = CO2R4, CN, CONR5R6, etc.; R2a, R2b = H, halogen, (un)substituted alkyl, etc.; Rx = (un)substituted alkyl, CQaQb-heterocyclyl, CQaQb-bicyclic heterocyclyl, etc.; R4, R5 = H, (un)substituted alkyl; R6 = H, (un)substituted alkyl, heteroaryl, etc.; R8, R9 = H, Cl, F, etc.; Qa, Qb = H, CH3] and their pharmaceutically acceptable derivatives were prepared For example, the Suzuki coupling of Et 2′-bromobiphenyl-3-carboxylate and 2-benzyloxy-5-chlorophenylboronic acid, e.g., prepared from 3-ethoxycarbonylphenylboronic acid, followed by hydrolysis afforded compound I [A-R1 = 3-carboxyphenyl; Z = O; R2a = H, R2b = 5-Cl; R8, R9 = H] in 39% overall yield. In human prostanoid EP1 receptor binding assays, 90-examples of compounds I exhibited pIC50 values ranging from 6.0->9.0 at the EP1 receptor and pIC50 values of <6.0 at the EP3 receptor. Of note, no toxicol. effects are indicated/expected (sic) when the compounds I are administered at the assay concentration of 3 nM. Compounds I are claimed useful for the treatment of prostaglandin mediated diseases, e.g., inflammation, pain, etc. The experimental process involved the reaction of Ethyl 2-bromo-6-fluorobenzoate(cas: 1214362-62-5).Application In Synthesis of Ethyl 2-bromo-6-fluorobenzoate
The Article related to benzoic acid derivative preparation ep1 receptor antagonist prostaglandin disease, antiinflammatory agent benzoic acid derivative preparation ep1 receptor antagonist, analgesic benzoic acid derivative preparation ep1 receptor antagonist and other aspects.Application In Synthesis of Ethyl 2-bromo-6-fluorobenzoate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary