266337-25-1

Usage

Also known as

D-pipecolic acid

Natural occurrence

Synthesized by plants and animals

Pharmaceutical properties

Role in the synthesis of various drugs and as a potential therapeutic agent in the treatment of neurological disorders

Potential role

Development of new materials and in organic synthesis processes

Upstream product

• 87691-27-8 N-tert-butoxycarbonyl-L-cis-4-hydroxyproline 
• 87250-97-3 2’-methyl-2’-propanyl (1S,4S)-3-oxo-2-oxa-5-azabicyclo[2.2.1]heptane-5-carboxylate 

Downstream Products

• 129431-01-2 (4S)-4-hydroxy-L-prolinamide 

Relevant academic research and scientific papers

QUINAZOLINE DERIVATIVES

The invention concerns quinazoline derivatives of Formula (I) wherein each of R1, R3, R20, X1, X2, Z, W, (a) and (q) have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of turnours which are sensitive to inhibition of erbB receptor tyrosine kinases, particularly EGFR tyrosine kinase.

Synthesis and structure-activity relationships of potent 3- or 4-substituted-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors

A series of 3- or 4-substituted-2-cyanopyrrolidines were synthesized and evaluated as dipeptidyl peptidase IV inhibitors. Dipeptidyl peptidase IV (DPP-IV) inhibitors have attracted attention as potential drugs for use in the treatment of type 2 diabetes because they prevent degradation of glucagon-like peptide-1 (GLP-1) and extend its duration of action. A series of 2-cyanopyrrolidines are among the most potent of DPP-IV inhibitors. We focused our attention on substitutions at the 3- or 4-position of 2-cyanopyrrolidines and synthesized and evaluated various derivatives. Among them, the 4-fluoro derivative was found to exhibit better DPP-IV inhibitory activity and higher plasma drug concentrations after oral administration to rats than the 4-unsubstituted derivative. We report here on the synthesis and biological data of the aforementioned derivatives.