916887-25-7

Upstream product

• 111-34-2 -butyl vinyl ether 
• 83-38-5 2,6-dichlorobenzaldehyde 
• 949-99-5 4-nitro-3-phenyl-L-alanine 
• 17193-40-7 (S)-4-nitrophenylalanine methyl ester hydrochloride 
• 42521-08-4 2,6-dichloroisonicotinoyl chloride 
• 623144-30-9 methyl (2S)-2-[(tert-butoxycarbonyl)amino]-3-[2-(2,6-dichlorophenyl)-6-quinolinyl]-propanoate 
• 229328-97-6 3,5-dichloroisonicotinoyl chloride 

Relevant academic research and scientific papers

Efficient Multikilogram Synthesis of a VLA-4 Antagonist via a Povarov Reaction

Herein we describe the practical synthesis of a novel VLA-4 antagonist 1 as a potential treatment for multiple sclerosis. The key step is based on the Povarov reaction of an imine with an alkene to access a tetrahydroquinoline intermediate, leading to the corresponding quinoline core after an oxidative aromatization step. The development of the synthesis of 1 led to decreased complexity and the elimination of chromatographic purifications. These improvements were demonstrated at scale by the production of 32 kg of 1 in high yield with excellent purity.

2,6 QUINOLINYL DERIVATIVES, PROCESSES FOR PREPARING THEM AND THEIR USE AS MEDICAMENT

The present invention concerns 2.6-quinolinyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceu ticals. For example, the compounds according to the invention are useful for the treatment of a