On November 22, 2018, Boss, Christoph; Corminboeuf, Olivier; Fretz, Heinz; Lyothier, Isabelle; Pozzi, Davide; Richard-Bildstein, Sylvia; Siendt, Herve; Sifferlen, Thierry published a patent.Category: chlorides-buliding-blocks The title of the patent was Preparation of benzofuran and benzothiophene derivatives as PGE2 receptor modulators. And the patent contained the following:
The title compounds I [R1 = (independently) alkyl, alkoxy, halo, etc.; n = 1-3; R2 =H, alkyl, halo, or cyano; X = S or O; R3 = H, Me or CF3; R41 and R42 = (independently) H, Me; or R41 and R42, together with the carbon atom to which they are attached, represent a cycloprop-1,1-diyl group; R51 and R52 = (independently) H, Me; or R51 and R52, together with the carbon atom to which they are attached, represent a cycloprop-1,1-diyl group; Ar1 = (un)substituted Ph, or 5-6 membered heteroaryl, 8-10 membered bicyclic heteroaryl, etc.] or pharmaceutically acceptable salts thereof, useful in the treatment of cancer by modulating an immune response comprising a reactivation of the immune system in the tumor, were prepared E.g., a multi-step synthesis of {6-[4-Ethoxy-5-(1H-tetrazol-5-yl)-thiophen-2-yl]-pyrimidin-4-yl}-[2-(5-fluoro-2,7-dimethylbenzo[b]thiophen-3-yl)ethyl]amine, starting from Me 3-ethoxythiophene-2-carboxylate, was described. Exemplified compounds I were evaluated for EP2 and EP4 antagonistic activities (data given). The invention further relates to novel benzofurane and benzothiophene derivatives I and their use as pharmaceuticals, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds I, and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4. The experimental process involved the reaction of Methyl 4-bromo-2-chloro-6-methylbenzoate(cas: 877149-10-5).Category: chlorides-buliding-blocks
The Article related to benzofuran benzothiophene pyrimidinylamino preparation prostaglandin ep2 ep4 receptor antitumor, immune response modulator cancer benzofuran benzothiophene pyrimidinylamino preparation and other aspects.Category: chlorides-buliding-blocks
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics