1541197-73-2

Upstream product

• 4530-20-5 BOC-glycine 
• 23039-28-3 3-(tert-butyl)benzaldehyde 
• 1541197-71-0 (S)-3-amino-3-(3-bromo-5-tert-butylphenyl)propionicacid ethyl ester 
• 1541197-69-6 (S)-3-amino-3-(3-bromo-5-tert-butylphenyl)propionic acid 
• 1541197-67-4 3-amino-3-(3-bromo-5-tert-butylphenyl)propionic acid ethyl ester hydrochloride salt 
• 1541197-65-2 3-amino-3-(3-bromo-5-tert-butylphenyl)propionic acid 
• 241155-85-1 3-bromo-5-formyl-tert-butylbenzene 
• 129316-09-2 1,3-dibromo-5-t-butylbenzene 
• 24424-99-5 di-tert-butyl dicarbonate 
• 1541197-63-0 (S)-3-(2-aminoacetylamino)-3-(3-bromo-5-tert-butylphenyl)propionic acid ethyl ester hydrochloride salt 

Downstream Products

• 1541198-84-8 (S)-ethyl 3-(3-bromo-5-(tert-butyl)phenyl)-3-(2-(3-guanidinobenzamido)acetamido)propanoate 
• 1541196-91-1 (S)-3-(3-bromo-5-(tert-butyl)phenyl)-3-(2-(3-guanidinobenzamido)acetamido)propanoic acid 
• 1541198-85-9 (S)-ethyl 3-(3-bromo-5-(tert-butyl)phenyl)-3-(2-(5-guanidinonicotinamido)acetamido)propanoate 
• 1541196-92-2 (S)-3-(3-bromo-5-(tert-butyl)phenyl)-3-(2-(5-guanidinonicotinamido)acetamido)propanoic acid 
• 1541198-86-0 (S)-tert-butyl 2-((3-((2-((1-(3-bromo-5-(tert-butyl)phenyl)-3-ethoxy-3-oxopropyl)amino)-2-oxoethyl)carbamoyl)phenyl)amino)-4,5-dihydro-1H-imidazole-1-carboxylate 
• 1541198-87-1 (S)-3-(3-bromo-5-(tert-butyl)phenyl)-3-(2-(3-((1-(tert-butoxycarbonyl)-4,5-dihydro-1H-imidazol-2-yl)amino)benzamido)acetamido)propanoic acid 
• 1541196-95-5 (S)-3-(3-bromo-5-(tert-butyl)phenyl)-3-(2-(3-((4,5-dihydro-1H-imidazol-2-yl)amino)benzamido)acetamido)propanoic acid 
• 1541198-88-2 (3S)-ethyl 3-(3-bromo-5-(tert-butyl)phenyl)-3-(2-(5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)nicotinamido)acetamido)propanoate 
• 1541196-98-8 (3S)-3-(3-bromo-5-(tert-butyl)phenyl)-3-(2-(5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)nicotinamido)acetamido)propanoic acid 
• 1541198-89-3 (S)-ethyl 3-(3-bromo-5-(tert-butyl)phenyl)-3-(2-(3-((4,5-dihydro-1H-imidazol-2-yl)amino)-5-hydroxybenzamido)acetamido)propanoate 
• 1541197-01-6 (S)-3-(3-bromo-5-(tert-butyl)phenyl)-3-(2-(3-((4,5-dihydro-1H-imidazol-2-yl)amino)-5-hydroxybenzamido)acetamido)propanoic acid 
• 1541199-05-6 (3S)-ethyl 3-(3-(tert-butyl)-5-cyanophenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido)propanoate 
• 1541197-08-3 (3S)-3-(3-(tert-butyl)-5-cyanophenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido)propanoic acid 
• 1541259-41-9 (S)-ethyl 3-(2-aminoacetamido)-3-(3-(tert-butyl)-5-(pyridin-3-yl)phenyl)propanoate 

Relevant academic research and scientific papers

Iridium-catalysed C-H borylation of β-aryl-aminopropionic acids

Iridium-catalysed catalytic, regioselective C-H borylation of β-aryl-aminopropionic acid derivatives gives access to 3,5-functionalised protected β-aryl-aminopropionic acid boronates. The synthetic versatility of these new boronates is demonstrated through sequential one-pot functionalisation reactions to give diverse building blocks for medicinal chemistry. The C-H borylation is also effective for dipeptide substrates. We have exemplified this methodology in the synthesis of a pan αv integrin antagonist.

BETA AMINO ACID DERIVATIVES AS INTEGRIN ANTAGONISTS

Disclosed herein are novel pharmaceutical agents which are useful as integrin receptor antagonists that mediate the pathologic processes of angiogenesis and fibrosis and as such are useful in pharmaceutical compositions and in methods for treating conditions mediated by these integrins by inhibiting or antagonizing these integrins. The novel pharmaceutical agents include those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods and intermediates useful for making the pharmaceutical agents and methods of using the pharmaceutical agents are also provided.