200949-32-2

Upstream product

• 131270-08-1 (R)-3-amino-4-phenylbutanoic acid 
• 24424-99-5 di-tert-butyl dicarbonate 
• 145149-49-1 (R)-tert-butyl (1-cyano-3-phenylpropan-2-yl)carbamate 
• 126301-19-7 (2R)-2-[(tert-butoxycarbonyl)amino]-3-phenylpropyl methanesulfonate 
• 106454-69-7 N-tert-butoxycarbonyl-D-Phenylalaninol 
• 884344-37-0 (4S)-4-benzylazetidin-2-one 
• 884344-34-7 (R)-4-benzyl-1-hydroxymethylazetidin-2-one 
• 884344-44-9 2-benzyl-4-oxo-azetidine-1-carboxylic acid tert-butyl ester 
• 101555-61-7 (R)-3-t-butoxycarbonylamino-4-phenylbutyric acid 

Downstream Products

• 200949-34-4 4-{(S)-2-Benzyloxycarbonylamino-2-[(S)-1-((R)-1-carbamoylmethyl-2-phenyl-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-ethyl}-imidazole-1-carboxylic acid benzyl ester 
• 200949-35-5 Boc-D-Phe-Gln-Trp-Ala-Val-Gly-His-Leu-β-homo-D-Phe-NH2 
• 1026500-44-6 (S)-2-[(S)-2-Amino-3-(1H-imidazol-4-yl)-propionylamino]-4-methyl-pentanoic acid ((R)-1-carbamoylmethyl-2-phenyl-ethyl)-amide 
• 145149-49-1 (R)-tert-butyl (1-cyano-3-phenylpropan-2-yl)carbamate 
• 200949-33-3 [(S)-1-((R)-1-Carbamoylmethyl-2-phenyl-ethylcarbamoyl)-3-methyl-butyl]-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

SEVEN-MEMBERED SULFONAMIDES AS MODULATORS OF RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ, NR1F3)

The invention provides modulators for the orphan nuclear receptor RORγ and methods for treating RORγ mediated diseases by administration of these novel RORγ modulators to a human or a mammal in need thereof. Specifically, the present invention provides compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof as well as pharmaceutical compositions comprising said compounds as an active ingredient.

Lipase-involved strategy to the enantiomers of 4-benzyl-β-lactam as a key intermediate in the preparation of β-phenylalanine derivatives

A simple chemoenzymatic method for the preparation of the enantiomers of 4-benzyl-β-lactam (4-benzylazetidin-2-one) from allylbenzene has been described. The enantiomers of this key intermediate have been used to produce the corresponding enantiomers of β-phenylalanine and N-Boc-protected β-phenylalanine amide through the simple cleavage of the lactam ring by acid-catalyzed hydrolysis and by ammonolysis, respectively. Burkholderia cepacia lipase-catalyzed kinetic double resolution techniques were responsible for achieving enantiopurity in the products. This was performed through the acylation of N-hydroxymethylated β-lactam followed by the butanolysis of the obtained (S)-ester. Direct lipase-catalyzed cleavage of the β-lactam ring has also been studied.

Syntheses and biological activities of bombesin analogs modified in the C-terminal dipeptide part

Bombesin receptor antagonists are possible therapeutic agents due to their ability to act as inhibitors of cellular proliferation. On the basis of our hypothesis on the mechanism of action of gastrin associating an activating enzyme system to the receptor and on the results reported in the litterature, we have synthesized bombesin analogues which have been modified in the C-terminal Leu13-Leu14 amide part. We have shown that modification in the C-terminal part of the bombesin strongly affected the biological activity in rat pancreatic acini. The most potent compound which is described here, H-D-Phe-Gln-Trp-Ala-Val-Gly-His-Leu-Ψ/(CH2)Leu-NH2, was able to recognize the bombesin receptor on rat pancreatic acini (Ki 4.3 nM) and antagonized the bombesin stimulated amylase secretion (Ki 7.7 nM).