364066-92-2

Upstream product

• 352-11-4 1-chloromethyl-4-fluorobenzene 
• 22321-46-6 trans-2,5-dimethylpiperazine monohydrochloride 
• 2815-34-1 2,5-dimethyl-piperazine 

Downstream Products

• 685534-40-1 (5-chloro-2-[(E)-3-[(2R,5S)-4-(4-fluorobenzyl)-2,5-dimethylpiperazin-1-yl]-3-oxopropenyl]-phenyl)-carbamic acid tert-butyl ester 
• 685534-97-8 N-(5-chloro-2-[(E)-3-[(2R,5S)-4-(4-fluorobenzyl)-2,5-dimethylpiperazin-1-yl]-3-oxopropenyl]-4-methoxyphenyl)-acetamide 
• 685534-99-0 N-(5-chloro-2-[(E)-3-[(2R,5S)-4-(4-fluorobenzyl)-2,5-dimethylpiperazin-1-yl]-3-oxopropenyl]-4-methoxyphenyl)-methanesulfonamide 
• 431062-01-0 4-(4-fluoro-benzyl)-2R,5S-dimethyl-piperazine-1-carboxylic acid tert-butyl ester 
• 217648-11-8 2-chloro-1-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-ethanone 
• 217645-80-2 5-chloro-2-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-benzaldehyde 
• 680208-34-8 (6-amino-5-iodo-2-methoxy-pyridin-3-yl)-[4-(4-fluoro-benzyl)-2R,5S-dimethyl-piperazin-1-yl]-methanone 
• 680208-36-0 N-{5-[4-(4-fluorobenzyl)-2R,5S-dimethyl-piperazine-1-carbonyl]-3-iodo-6-methoxy-pyridin-2-yl}-acetamide 
• 680208-38-2 N-{5-[4-(4-fluorobenzyl)-2R,5S-dimethyl-piperazine-1-carbonyl]-6-methoxy-3-trimethylsilanylethynyl-pyridin-2-yl}-acetamide 
• 680208-31-5 (6-amino-2-fluoro-pyridin-3-yl)-[4-(4-fluoro-benzyl)-2R,5S-dimethyl-piperazin-1-yl]-methanone 
• 680208-33-7 (6-amino-2-methoxy-pyridin-3-yl)-[4-(4-fluoro-benzyl)-2R,5S-dimethyl-piperazin-1-yl]-methanone 

Relevant academic research and scientific papers

Design and synthesis of piperazine-indole p38α MAP kinase inhibitors with improved pharmacokinetic profiles

Derivatives of the 4-fluorobenzyl dimethylpiperazine-indole class of p38α MAP kinase inhibitors are described. Biological evaluation of these compounds focused on maintaining activity while improving pharmacokinetic (PK) properties. Improved properties were observed for structures bearing substitutions on the benzylic methylene.

Route development and bulk synthesis of CP-865,569

The synthesis of zwitterionic CP-865,569 by three different synthetic routes is described. The first two routes differ in the method of introducing the sulfonic acid at the penultimate step: by sulfite displacement of a benzylic chloride and by oxidation of a benzylic thioacetate. The third route is a convergent route to the drug candidate. The synthesis strategy was primarily driven by the need to introduce the sulfonic acid functionality at the final stage of the synthesis due to the high water solubility and low organic solubility of the desired product.

AZAINDOLE DERIVATIVES AS INHIBITORS OF P38 KINASE

The invention is directed to methods to inhibit p38 kinase, preferably p38-α using compounds which are azaindoles wherein the azaindoles are coupled through an azacyclic linker to another cyclic moiety.

PIPERAZINE DERIVATIVES AND THEIR USE AS ANTI-INFLAMMATORY AGENTS

This invention is directed to acyl piperazine derivatives of formula (Ia): wherein R 1a, R 2, R 3, R 4, R 5and R 6 are defined herein, which are useful as anti-inflammatory agents. This invention is also directed to other acyl piperazine derivatives, pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.