Merck Sharp + Dohme Corp.

Yan Jin

Duane A Burnett

John W Clader

Hubert B Josien

Wen-Lian Wu

Dmitri A Pissarnitski

Hongmei Li

Jesse K Wong

Zhiqiang Zhao

Thavalakulamgara K Sasikumar

Ruo Xu

Thomas A Bara

Martin Domalski

Paul E McNamara

Xian Liang

Martin S Domalski

Paul Mcnamara

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)&#x2014;O&#x2014;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)&#x2014;O&#x2014;C(O)-heteroaryl and a basic tertiary amine. 

Tetrahydropyranochromene gamma secretase inhibitors

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Princeton, NJ, United States of America

Yan Jin