7312-24-5Relevant articles and documents
Bromination of 3-substituted benzo[b]thiophenes: Access to Raloxifen intermediate
Liger, Fran?ois,Pellet-Rostaing, Stéphane,Popowycz, Florence,Lemaire, Marc
scheme or table, p. 3736 - 3739 (2011/08/06)
A practical route to prepare halogeno-derivatives is described, starting from easily available 3-cyano-benzo[b]thiophene. Main efforts have been devoted to the optimization of the experimental procedures (solvent, bromination) to promote selectivity. Synt
Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 2. 6,6-dimethylbicyclo[3.1.1]heptane derivatives
Mitsumori, Susumu,Tsuri, Tatsuo,Honma, Tsunetoshi,Hiramatsu, Yoshiharu,Okada, Toshihiko,Hashizume, Hiroshi,Inagaki, Masanao,Arimura, Akinori,Yasui, Kiyoshi,Asanuma, Fujio,Kishino, Junji,Ohtani, Mitsuaki
, p. 2446 - 2455 (2007/10/03)
In an earlier paper, we reported that novel prostaglandin D2 (PGD2) receptor antagonists having the bicyclo[2.2.1]heptane ring system as a prostaglandin skeleton were a potent new class of antiallergic agents and suppressed various allergic inflammatory responses such as those observed in conjunctivitis and asthma models. In the present study, we synthesized PGD2 receptor antagonists having the 6,6-dimethylbicyclo [3.1.1]heptane ring system. These derivatives have the amide moiety, in contrast to those with the bicyclo[2.2.1]heptane ring system, which have the sulfonamide group. The derivatives having the 6,6-dimethylbicyclo[3.1.1]heptane ring also exhibited strong activity in PGD2 receptor binding and cAMP formation assays. In in vivo assays such as allergic rhinitis, conjunctivitis, and asthma models, these series of derivatives showed excellent pharmacological profiles. In particular, compound 45 also effectively suppressed eosinophil infiltration in allergic rhinitis and asthma models. This compound (45, S-5751) is now being developed as a promising alternative antiallergic drug candidate.
