5552-85-2

Upstream product

• 100-69-6 2-vinylpyridine 
• 2739-98-2 ethyl 2-(pyridinyl-2)acetate 
• 74-88-4 methyl iodide 
• 77-78-1 dimethyl sulfate 
• 100-71-0 2-Ethylpyridine 

Relevant academic research and scientific papers

PYRROLIDINE-PYRAZOLES AS PYRUVATE KINASE ACTIVATORS

The subject matter described herein is directed to pyruvate kinase activating compounds of Formula I and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds and methods of administering the compounds for the treatment of diseases associated with PKR and/or PKM2, such as pyruvate kinase deficiency, sickle cell disease, and beta-thalassemia.

Stereodivergent Construction of Tertiary Fluorides in Vicinal Stereogenic Pairs by Allylic Substitution with Iridium and Copper Catalysts

Although much effort has been spent on the enantioselective synthesis of tertiary alkyl fluorides, the synthesis of compounds containing such a stereogenic center within an array of stereocenters, particularly two vicinal ones, remains a synthetic challenge, and no method to control the configuration of each stereogenic center independently has been reported. We describe a strategy to achieve such a stereodivergent synthesis of vicinal stereogenic centers, one containing a fluorine atom, by forming the connecting carbon-carbon bond with a catalyst system comprising an iridium complex that controls the configuration at the electrophilic carbon and a copper catalyst that controls the configuration at the nucleophilic fluorine-containing carbon. These reactions occur with alkyl- and aryl-substituted allylic esters and the unstabilized enolates of azaaryl ketones, esters, and amides in high yield, diastereoselectivity, and enantioselectivity (generally >90% yield, >20:1 dr, 97-99% ee). Access to all four stereoisomers of products demonstrates the precise control of the two configurations independently. This methodology extends to the stereodivergent construction of vicinal quaternary and tertiary stereocenters in similarly high yield and selectivity. DFT calculations uncover the origin of stereoselectivity of copper enolate in allylic substitution.

PYRIDINE, BICYCLIC PYRIDINE AND RELATED ANALOGS AS SIRTUIN MODULATORS

The present invention provides novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders relating to aging or stress, diabetes, obesity, neurodegenerative disease, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorder that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. The compounds are of general formula (III) wherein R1, R2, R", X, Y, W, Z1 and Z2 are as defined in the specification.

GAMMA SECRETASE MODULATORS

The present invention provides compounds that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions conta

AMINOPYRAZOLE DERIVATIVES AS GSK-3 INHIBITORS

The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs, wherein R1, R2, and R3 are as defined herein; pharmaceutical compositions thereof; combinations thereof; and uses thereof in the treatment of, inter alia, conditions, diseases, and symptoms including, inter alia, Alzheimer's Disease, cancer, dementia, depression, diabetes, hair loss, schizophrenia, and stroke.