1450879-65-8

Upstream product

• 211108-48-4 tert-butyl 4-[(trimethylsilyl)oxy]-3,6-dihydropyridine-1(2H)-carboxylate 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 
• 373604-28-5 3-fluoro-4-hydroxypiperidine-1-carboxylic acid tert-butyl ester 
• 98-59-9 p-toluenesulfonyl chloride 
• 211108-50-8 tert-butyl-3-fluoro-4-oxopiperidine-1-carboxylate 
• 1174020-42-8 (-)-(3R,4S)-3-fluoro-4-hydroxypiperidine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

MODULATORS OF TREK (TWIK RELATED K+ CHANNELS) CHANNEL FUNCTION

Disclosed is a compound of formula (I): wherein all symbols are defined in the description. Also disclosed are pharmaceutical compositions comprising the compounds, methods of making the compounds, kits comprising the compounds and methods of using the compounds to prevent and/or treat disorders associated with dysregulation of TREK-1, TREK-2 or both TREK-1 and TREK-2 in a mammal.

PYRIMIDINE TBK/IKKε INHIBITOR COMPOUNDS AND USES THEREOF

The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.

COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK

The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.

COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK

The present invention relates to compounds of formula I in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.

Enantioselective synthesis of cis -3-fluoropiperidin-4-ol, a Building block for medicinal chemistry

The first enantioselective route to both enantiomers of cis-1-Boc-3-fluoropiperidin-4-ol, a highly prized building block for medicinal chemistry, is reported. An enantioselective fluorination is employed, taking advantage of the methodology reported by MacMillan, which uses a modified cinchona alkaloid catalyst. In studying the fluorination reaction, we have shown that the catalyst can be replaced by commercially available primary amines, including α-methylbenzylamine, with similar levels of enantioselectivity. The piperidinols are readily crystallized to obtain enantiopure material.