Über neue und über verbesserte Wege zum Aufbau von pharmakologisch wichtigen Aminen. XII. Mitteilung: Über Dihydro- und Tetrahydro-benzo-isochinoline als Protozoengifte
[EN] FORMAMIDE DERIVATIVES USEFUL AS ADRENOCEPTOR<br/>[FR] DERIVES DE FORMAMIDE UTILES COMME RECEPTEURS ADRENERGIQUES
申请人:PFIZER LTD
公开号:WO2005092840A1
公开(公告)日:2005-10-06
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
construction of a rich chemical space of arylethylamine motif. In this report, a practical protocol for the synthesis of arylethylamine functionality common in pharmaceutical chemicals has been developed. It proceeds by Mn-catalyzed anti-Markovnikov hydroarylation of electron-rich enamides under mild conditions without the use of ligands. In spite of mismatched electronic effects during the manganese-mediated
We present the first synthesis of bridged bicycles through the dearomatization of sterically and electronically unbiased aryl fragments. The visible-light promoted method occurs at room temperature and has ample functional-group tolerance. The key to the difunctionalization of the aryl partner is the use of naphthalene as an additive, which stabilizes transient (bi)radicals through its extended π cloud