320337-15-3

Upstream product

• 191602-86-5 1-(benzyloxy)-2-bromo-4-nitrobenzene 
• 5847-59-6 2-bromo-4-nitrophenol 
• 100-39-0 benzyl bromide 
• 1223466-37-2 N-(4-benzyloxy-3-bromophenyl)acetamide 
• 103-90-2 4-acetaminophenol 
• 6329-78-8 N-(3-bromo-4-hydroxyphenyl)acetamide 
• 100-02-7 4-nitro-phenol 

Downstream Products

• 320337-19-7 (6-iodo-((4-benzyloxy)-3-bromophenyl)-quinazolin-4-yl)amine 
• 16750-67-7 4-amino-2-bromophenol 
• 1223466-37-2 N-(4-benzyloxy-3-bromophenyl)acetamide 
• 1318802-86-6 C₂₁H₂₆BrNO₅ 
• 1318802-67-3 C₁₅H₁₈N₄O₃ 
• 1318802-89-9 C₂₅H₂₉ClN₄O₅ 
• 1318802-88-8 C₂₆H₃₂N₄O₅ 
• 1318802-87-7 C₂₁H₂₈BNO₇ 
• 1318802-82-2 C₂₀H₂₇N₅O₃ 
• 1318802-81-1 C₁₉H₂₅N₅O₃ 
• 1318802-80-0 C₂₀H₂₈N₆O₄ 
• 1318802-79-7 C₁₉H₂₆N₆O₃ 
• 1318802-78-6 C₁₈H₂₃N₅O₄ 
• 1318802-77-5 C₁₆H₂₁N₅O₃ 

Relevant academic research and scientific papers

A practical nickel-catalyzed reductive alkylation of amidophenyl bromides

A modified Weix's reductive coupling for alkylation of amidoaryl bromides based on Ni(COD)2 precatalyst and 2,2′-dipyridyl ligand was developed. This reaction is reliable for amidophenyl bromides and gives yields up to 87%, and is potentially useful in the synthesis of amidophenyl-containing molecules.

Discovery of a novel class of 2-aminopyrimidines as CDK1 and CDK2 inhibitors

A series of new 2-(2-aminopyrimidin-4-yl)phenol derivatives were synthesized as potential antitumor compounds. Substitution with pyrrolidine-3,4-diol at the 4-position of phenol provided potent inhibitory activity against CDK1 and CDK2. X-ray crystal structural studies were performed to account for the effect of the substituent on both the enzymatic and cell growth inhibitory activities.

Functionalized alkoxy arene diazonium salts from paracetamol

Arene diazonium tetrafluoroborates can be synthesized from aromatic acetamides via a sequence of deacetylation, diazotation and precipitation, induced by anion exchange. The reaction is conducted as a convenient one-flask transformation with consecutive addition of the appropriate reagents. Exchange of solvents or removal of byproducts prior to isolation of the product is not required. The arene diazonium salts are isolated from the reaction mixture by simple filtration. Two complementary protocols are presented, and the utility of the reaction is exemplified for a synthesis of the diarylheptanoid natural product de-O-methyl centrolobine.

PYRROLIDINE DERIVATIVES AS ERK INHIBITORS

Disclosed are the ERK inhibitors of Formula (1.0): and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of Formula (1.0).

Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series

Synthetic modifications on a 6-furanylquinazoline scaffold to optimize the dual ErbB-1/ErbB-2 tyrosine kinase inhibition afforded consistent SAR whereby a 4-(3-fluorobenzyloxy)-3-haloanilino provided the best enzyme potency and cellular selectivity. Changes made to the 6-furanyl group had little impact on the enzyme activity, but appeared to dramatically affect the cellular efficacy. The discovery of lapatinib emerged from this work.

Anilinoquinazolines as protein tyrosine kinase inhibitors

Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.

Anilinoquinazaolines as protein tyrosine kianse inhibitors

Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.