120067-55-2

Upstream product

• 501-81-5 pyridyl-3-yl-acetic acid 
• 6419-36-9 3-pyridineacetic acid hydrochloride 

Downstream Products

• 105462-24-6 risedronic acid 
• 1124382-00-8 N-[5-(cyclohexylamino)[1,2,4]triazolo[1,5-a]pyridin-2-yl]-2-pyridin-3-ylacetamide 

Relevant academic research and scientific papers

Heteroarylacetyl chlorides and mixed anhydrides as intermediates in the synthesis of heterocyclic dronic acids

It has been recognised that there is no need for phosphorous acid during the conversion of 1-heteroarylacetic acids to the corresponding dronic acids, as phosphorus trichloride (PCl3) is the real reagent. We could prove that the first intermediate toward the formation Risedronic acid is 3-pyridylacetyl chloride that was prepared in different ways using inorganic halides in toluene or in methanesulfonic acid (MSA). The intermediate was then reacted with two equivalents of PCl3 to afford risedronic acid after hydrolysis and pH adjustment. The pyridylacetyl chloride intermediate was identified on the basis of its esterification and amidation reaction. In MSA as the solvent, mixed anhydrides may also be formed as the intermediates from which the dronic acids may be formed in reaction with PCl3. A similar situation was anticipated for the reaction sequence of Zoledronic acid.

Thiophene inhibitors of PDE4: Crystal structures show a second binding mode at the catalytic domain of PDE4D2

PDE4 inhibitors have been identified as therapeutic targets for a variety of conditions, particularly inflammatory diseases. We have serendipitously identified a novel class of phosphodiesterase 4 (PDE4) inhibitor during a study to discover antagonists of the parathyroid hormone receptor. X-ray crystallographic studies of PDE4D2 complexed to four potent inhibitors reveal the atomic details of how they inhibit the enzyme and a notable contrast to another recently reported thiophene-based inhibitor.

TRIAZOLOPYRIDINE COMPOUNDS AND THEIR USE AS ASK INHIBITORS

The present invention relates to triazolopyridine compounds according to Formula (I), their use as medicament, for treating autoimmune disorders, inflammatorydiseases, cardiovascular disceases and/or neurodegenerative diseases and a process for their preparation.

REAGENT AND USE THEREOF FOR THE PRODUCTION OF BISPHOSPHONATES

A new liquid reagent is disclosed in form of an ionic liquid containing phosphorous acid and a tertiary amine. The reagent can be used as a replacement of phosphorous acid, where the new reagent as a liquid reagent can be handled using usual equipment for handling liquids and the dosing of the reagent can therefore be controlled more precisely in industrial plants compared to phosphorous acid, which is a solid at ambient temperature. The new liquid reagent is particular suitable for the synthesis of bisphosphonates.

HETEROCYCLIC COMPOUNDS WITH AFFINITY TO MUSCARINIC RECEPTORS

The present invention relates to heterocyclic compounds of the formula (I) wherein - the heterocycle comprises two double bonds which may be present at several positions, represented by the dashed lines ( -- ); - the heterocycle contains two heteroatoms,

2, 6 BISHETEROARYL-4-AMINOPYRIMIDINES AS ADENOSINE RECEPTOR ANTAGONISTS

4-Aminopyrimidine derivatives of formula (I) FORMULA heteroaryl groups, including pharmaceutically acceptable salts thereof, wherein R1 and R2 are adenosine A2A receptor antagonists useful in the treatment of movement disorders such as Parkinson's disease.