1246495-15-7

Upstream product

• 1246495-08-8 2,4-dichloro-N-((1-(1-methyl-1H-imidazol-4-ylsulfonyl)azetidin-3-yl)(phenyl)methyl)benzamide 
• 1379079-60-3 (S)-(1-((1-methyl-1H-imidazol-4-yl)sulfonyl)azetidin-3-yl)(phenyl)methanamine 
• 89-75-8 2,4-dichlorobenzoyl chloride 
• 1379079-58-9 (S)-tert-butyl((1-((1-methyl-1H-imidazol-4-yl)sulfonyl)azetidin-3-yl)(phenyl)methyl) carbamate 
• 1379079-54-5 (S)-tert-butyl (azetidin-3-yl(phenyl)methyl)carbamate 
• 1379079-52-3 (S)-benzyl 3-(((tert-butoxycarbonyl)amino)(phenyl)methyl)azetidine-1-carboxylate 
• 1379079-51-2 (R)-benzyl 3-((tert-butoxycarbonylamino)(phenyl)methyl)-3-nitroazetidine-1-carboxylate 

Relevant academic research and scientific papers

Chiral proton catalysis of secondary nitroalkane additions to azomethine: Synthesis of a potent GlyT1 inhibitor

The first enantioselective synthesis of a potent GlyT1 inhibitor is described. A 3-nitroazetidine donor is used in an enantioselective aza-Henry reaction catalyzed by a bis(amidine)-triflic acid salt organocatalyst, delivering the key intermediate with 92% ee. This adduct is reductively denitrated and converted to the target through a short sequence, thereby allowing assignment of the absolute configuration of the more potent enantiomer.

SULFONYL-AZETIDIN-3-YL-METHYLAMINE AMIDE ANALOGS AS GLYT1 INHIBITORS, METHODS FOR MAKING SAME, AND USE OF SAME IN TREATING PSYCHIATRIC DISORDERS

In one aspect, the invention relates to compounds which are useful as as inhibitors of glycine type 1 transporter (GIyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GIyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.