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2005
Oxazine derivatives
R 0595
Discovery of Orally Active Prostaglandin D2 Receptor Antagonists. — The highly
potent prostaglandin D2 receptor antagonist (XII) is synthesized by modification of
03- 156 indomethacin
analogues. A previously used method to synthesize methylindoleacetic
acids is replaced by a more efficient synthesis consisting of palladium-catalyzed C2
homologation, cf. (VI)→(VIII), followed by hydroboration, cf. (VIII)→(X). The synthesis of (XII) is completed by using sequential procedures which include N-acylation,
aminolysis, Mitsunobu coupling with alcohol (V), and deprotection. Compound (XII)
displays the strongest human prostaglandin D2 receptor antagonist activity of all synthesized N-(p-alkoxy)benzoyl-2-methylindole-4-acetic acid analogues and good subtype selectivity, as well as in vivo prostaglandin D2 receptor antagonist activity. —
(TORISU*, K.; et al.; Bioorg. Med. Chem. Lett. 14 (2004) 19, 4891-4895; Minase
Res. Inst., Ono Pharm. Co., Ltd., Shimamoto, Osaka 618, Japan; Eng.) —
H. Hoennerscheid
2005
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