申请人:Wu Wen-Lian
公开号:US20110236400A1
公开(公告)日:2011-09-29
Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.
本发明涉及一种新型伽马分泌酶抑制剂的公开。还公开了抑制伽马分泌酶的方法、治疗神经退行性疾病的方法和治疗阿尔茨海默病的方法。还公开了一种使用醛(或酮)和烷基取代的两个电子提取基团的混合物,在一步反应中制备烯烃的方法,并将该混合物与:(a)磺酰卤化物(例如磺酰氯)和碱性三级胺反应,或(b)磺酰酐和碱性胺反应,或(c)芳基-C(O)-卤和碱性三级胺反应,或(d)芳基-C(O)-O-C(O)-芳基和碱性三级胺反应,或(e)杂环芳基-C(O)-卤和碱性三级胺反应,或(f)杂环芳基-C(O)-O-C(O)-杂环芳基和碱性三级胺反应。