219323-43-0

Upstream product

• 59410-82-1 (S)-α-phenylglycine ethyl ester hydrochloride 
• 501-53-1 benzyl chloroformate 
• 64-17-5 ethanol 
• 394210-43-6 2,5-dioxo-4-phenyl-oxazolidine-3-carboxylic acid benzyl ester 
• 5840-78-8 4-phenyl-oxazolidine-2,5-dione 
• 2835-06-5 phenylglycin 
• 5491-18-9 (S)-N-(benzyloxycarbonyl)phenylglycine 
• 2935-35-5 (S)-2-phenylglycine 

Downstream Products

• 5491-18-9 (S)-N-(benzyloxycarbonyl)phenylglycine 
• 1027309-84-7 (S)-2-{(R)-2-[3-((S)-2-Benzyloxycarbonylamino-2-phenyl-acetylamino)-2-oxo-pentanoylamino]-4-methyl-pentanoylamino}-3-methyl-butyric acid tert-butyl ester 

Relevant academic research and scientific papers

COMPOUNDS USEFUL AS CSF1 MODULATORS

This invention relates to novel compounds and to pharmaceutical compositions comprising the novel compounds. More specifically, the invention relates to compounds useful as Colony Stimulating Factor 1 Receptor (cFMS) modulators (e.g. cFMS inhibitors). This invention also relates to processes for preparing the compounds, uses of the compounds in treatment and methods of treatment employing the compounds. Specifically, the invention relates to the use of the compounds for the treatment of cancer and autoimmune diseases.

Triphenylphosphine dibromide: a simple one-pot esterification reagent

We report a one-pot, expedient protocol for the conversion of carboxylic acids to their esters using excess triphenylphosphine dibromide, base, and the alcohol. The reaction gave the esterified product in moderate-to-high yields (30-95%). For chiral acids, the reaction proceeded with little or no racemization. Use of a chiral alcohol in this transformation gave the ester with retention of configuration of the stereogenic center. Information is presented indicating that esterification proceeds through the intermediate generation of an acyloxyalkoxyphosphorane and where steric interactions play an important role in the energetics of the reaction.

Development of a rapid, room-temperature dynamic kinetic resolution for efficient asymmetric synthesis of α-aryl amino acids

equation presented A rapid, highly efficient and general dynamic kinetic resolution (DKR) of racemic α-aryl UNCAs with the dual-function catalysis of modified cinchona alkaloid was accomplished at room temperature. This DKR led to the development of a highly enantioselective catalytic method for the practical synthesis of a wide range of α-aryl and α-heteroaryl amino acids in 89-92% ee and 86-95% yield from racemic UNCAs.

Poststatin, a new inhibitor of prolyl endopeptidase. V. Endopeptidase inhibitory activity of poststatin analogues

Thirty analogues of poststatin were synthesized, and their inhibitory activities against prolyl endopeptidase, human leukocyte elastase and cathepsin B were measured. The α-ketone was essential and the S configuration was preferable to the R configuration in the β-substituted-β-amino-α-oxopropionic acid moiety of poststatin analogues for endopeptidase inhibitory activity. The analogue in which the D-leucine residue of poststatin was replaced by L-leucine showed strong inhibitory activity to cathepsin B. Introduction of an aromatic group into the P4 position and proline into the P2 position increased inhibitory activity to elastase. Benzyloxycarbonyl-L-homophenylalanyl-(RS)-3-amino-2-oxovaleryl-D- leucyl-L-valine was about 6 times more active to prolyl endopeptidase than natural poststatin.