3474-90-6

Upstream product

• 23780-13-4 (2-phenylthiazol-4-yl)methanol 
• 20949-81-9 2-phenyl-thiazole-4-carbaldehyde 
• 141-82-2 malonic acid 
• 78359-00-9 4-(iodomethyl)-2-phenyl-1,3-thiazole 
• 4771-31-7 2-phenyl-4-chloromethylthiazole 
• 2227-79-4 benzenecarbothioamide 

Downstream Products

• 108175-81-1 2-Phenylthiazolo<5,4-c>pyridine-7(6H)-one 
• 108175-82-2 7-Chloro-2-phenylthiazolo<5,4-c>pyridine 

Relevant academic research and scientific papers

Tailored Mutants of Phenylalanine Ammonia-Lyase from Petroselinum crispum for the Synthesis of Bulky l- and d-Arylalanines

Tailored mutants of phenylalanine ammonia-lyase from Petroselinum crispum (PcPAL) were created and tested in ammonia elimination from various sterically demanding, non-natural analogues of phenylalanine and in ammonia addition reactions into the corresponding (E)-arylacrylates. The wild-type PcPAL was inert or exhibited quite poor conversions in both reactions with all members of the substrate panel. Appropriate single mutations of residue F137 and the highly conserved residue I460 resulted in PcPAL variants that were active in ammonia elimination but still had a poor activity in ammonia addition onto bulky substrates. However, combined mutations that involve I460 besides the well-studied F137 led to mutants that exhibited activity in ammonia addition as well. The synergistic multiple mutations resulted in substantial substrate scope extension of PcPAL and opened up new biocatalytic routes for the synthesis of both enantiomers of valuable phenylalanine analogues, such as (4-methoxyphenyl)-, (napthalen-2-yl)-, ([1,1′-biphenyl]-4-yl)-, (4′-fluoro-[1,1′-biphenyl]-4-yl)-, and (5-phenylthiophene-2-yl)alanines.

Kinase inhibitor, and preparation and application of kinase inhibitor

The invention provides a compound shown as a formula (I), or a stereoisomer, a tautomer, nitrogen oxide, metabolite, a prodrug, pharmaceutically acceptable salt or solvate of the compound, and application of the compound to preparing drugs or drug compositions for treating Pim kinase-mediated diseases.

The synthesis and activity of oxazole and thiazole analogues of urocanic acid

Direct exposure of human skin to sunlight leads to suppression of the immune system, believed to be mediated by urocanic acid. The synthesis of oxazole and thiazole analogues of urocanic acid is reported, as is their effect on biological markers of the hu