24345-85-5

Upstream product

• 7338-27-4 4-methoxy-2-methylene-4-oxobutanoic acid 
• 100-51-6 benzyl alcohol 
• 100-39-0 benzyl bromide 
• 97-65-4 2-methylenesuccinic acid 

Downstream Products

• 1040448-44-9 2,4-dibenzyl-1-methyl 5-oxohexane-1,2,4-tricarboxylate 
• 1361050-65-8 (E)-1-benzyl-4-methyl-2-(2,4,5-trifluorobenzylidene)succinate 
• 1361050-66-9 (Z)-1-benzyl-4-methyl-2-(2,4,5-trifluorobenzylidene)succinate 
• 1361050-68-1 (E)-4-methoxy-4-oxo-2-(2,4,5-trifluorobenzylidene)butanoic acid 
• 1361050-69-2 4-methoxy-4-oxo-2-(2,4,5-trifluorobenzyl)butanoic acid 
• 1361050-70-5 (R)-4-methoxy-4-oxo-2-(2,4,5-trifluorobenzyl)butanoic acid 
• 1361050-72-7 (S)-4-methoxy-4-oxo-2-(2,4,5-trifluorobenzyl)butanoic acid 
• 329978-18-9 methyl 4-(4-triisopropylsilyloxyphenyl)-3-(benzyloxycarbonyl)-3-butenoate 

Relevant academic research and scientific papers

Process for the production of sitagliptin

The present invention is directed to a process for the preparation of Sitagliptin, having formula (I)

Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: New insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7

(S)-Glutamic acid (Glu) is the major excitatory neurotransmitter in the central nervous system (CNS) activating the plethora of ionotropic Glu receptors (iGluRs) and metabotropic Glu receptors (mGluRs). In this paper, we present a chemo-enzymatic strategy for the enantioselective synthesis of five new Glu analogues 2a-f (2d is exempt) holding a functionalized substituent in the 4-position. Nine Glu analogues 2a-j are characterized pharmacologically at native 2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA), kainic acid (KA), and N-methyl-D-aspartic acid (NMDA) receptors in rat synaptosomes as well as in binding assays at cloned rat iGluR5-7 subtypes. A detailed in silico study address as to why 2h is a high-affinity ligand at iGluR57 (Ki = 3.81, 123, 57.3 nM, respectively), while 2e is only a high affinity ligand at iGluR5 (Ki = 42.8 nM). Furthermore, a small series of commercially available iGluR ligands are characterized in iGluR5-7 binding.

VITRONECTIN RECEPTOR ANTAGONISTS

Compounds of formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis wherein R is Het- or Ar; R is formula (a) or formula (b); or a pharmaceutically acceptable salt thereof.