摘要 |
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. |
申请人 |
MERCK SHARP & DOHME CORP. |
发明人 |
PISSARNITSKI, DMITRI A.;ZHAO, ZHIQIANG;BURNETT, DUANE A.;JIN, YAN;WU, WEN-LIAN;SASIKUMAR, THAVALAKULAMGARA K.;MCNAMARA, PAUL;BARA, THOMAS A.;DOMALSKI, MARTIN S.;WONG, JESSE K.;LI, HONGMEI;CLADER, JOHN W.;XU, RUO;LIANG, XIAN;JOSIEN, HUBERT B. |