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专利信息
专利号:WO-2008022467-A1
优先权日:2006-08-25
标 题 :2-substituted azain doles and 2 substituted thienopyrroles, their precursors and novel processes for the preparation thereof
发明人:LAUTENS MARK; YUEN JOSEPHINE; FANG YUANQING
权利人:LAUTENS MARK; YUEN JOSEPHINE; FANG YUANQING
摘要:The present invention relates generally to processes for the chemical synthesis of azaindole and thienopyrrole compounds, in particular azaindole and thienopyrrole compounds that are substituted at the 2-position of the azaindole or thienopyrrole ring, and optionally at additional locations of the azaindole or thienopyrrole ring such as the 1- and/or 3-position, compounds prepared by such processes, and synthetic precursors of such processes. More particularly, the present invention relates to the preparation of 2- substituted azaindoles from an ortho-gem-dihalovinylaminopyridine or from an ortho- gem-dihalovinylaminopyridine N-oxide compound and an organoboron reagent using a palladium metal pre-catalyst, base and a ligand. The present invention also relates to the preparation of 2-substituted thienopyrroles from an ortho-gem-dihalovinylthiophene compound and an organoboron reagent using a palladium metal pre-catalyst, base and a ligand. The present invention also relates to processes for the production of ortho-gem- dihalovinylaminopyridines which are useful as starting materials in the production of 2- substituted azaindoles, and novel compounds prepared by the processes. The present invention also relates to processes for the production of ortho-gem-dihalovinylthiophenes which are useful as starting materials in the production of 2-substituted thienopyrroles, and novel compounds prepared by the processes. Formulae (V) and (VII).