647035-70-9

Upstream product

• 104-53-0 3-phenyl-propionaldehyde 
• 619-45-4 4-methoxycarbonyl aniline 
• 637-59-2 1-Bromo-3-phenylpropane 
• 619-44-3 methyl 4-iodobenzoate 
• 101954-72-7 N-(4-methoxycarbonylphenyl)-2-nitrobenzenesulfonamide 

Downstream Products

• 936571-61-8 C₃₃H₄₆N₄O₇ 
• 936571-59-4 4-{tert-butoxycarbonylmethyl-[5-(N,N'-bis-tert-butoxycarbonyl)guanidino-pentanoyl]amino}-benzoic acid methyl ester 
• 936571-78-7 2(S)-(2(S)-{4-[(5-guanidino-pentanoyl)-(3-phenyl-propyl)-amino]-benzoylamino}-3-methyl-butyrylamino)-3-phenyl-propionic acid 
• 1032374-62-1 C₃₂H₄₄N₄O₇ 

Relevant academic research and scientific papers

Efficient Synthesis of Trifluoromethyl Amines through a Formal Umpolung Strategy from the Bench-Stable Precursor (Me4N)SCF3

Reported herein is the one-pot synthesis of trifluoromethylated amines at room temperature using the bench-stable (Me4N)SCF3reagent and AgF. The method is rapid, operationally simple and highly selective. It proceeds via a formal umpolung reaction of the SCF3with the amine, giving quantitative formation of thiocarbamoyl fluoride intermediates within minutes that can readily be transformed to N-CF3. The mildness and high functional group tolerance render the method highly attractive for the late-stage introduction of trifluoromethyl groups on amines, as demonstrated herein for a range of pharmaceutically relevant drug molecules.

A mild inter- and intramolecular amination of aryl halides with a combination of CuI and CsOAc

A unique combination of CuI and CsOAc was found to catalyze aryl amination under mild conditions. The reaction takes place at room temperature or at 90 °C with broad functional group compatibility. The intramolecular reaction was able to form five-, six-, and seven-membered rings with various protecting groups on the nitrogen atom. The scope of the intermolecular amination, as well as its applications to unsymmetrical N,N′-dialkylated phenylenediamines, was investigated.

SUBSTRATE-MIMETIC AKT INHIBITOR

Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with 0 a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionallv homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterpartsand are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.

Modifications of the GSK3β substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics

Amplification, overexpression, and elevated activation of Akt have been detected in many human malignancies making it an important target for cancer therapy. The Akt substrate-binding site offers a large number of potential interactions to an appropriatel

Synthesis of Secondary Arylamines through Copper-Mediated Intermolecular Aryl Amination

(Equation presented) A mild intermolecular copper-mediated amination of aryl iodides has been developed. The reaction takes place at room temperature or heating at 90°C and tolerates halogens attached to the aromatic ring. Its synthetic applications include a synthetic protocol for unsymmetrical N,N′-dialkylated phenylenediamines and both a stepwise and a general synthetic method for N-aryl secondary amines via Ns-anilides (readily obtained by reaction of the Ns-amide).