77123-63-8

Upstream product

• 77123-61-6 2-fluoro-5-nitro-1-<(trimethylsilyl)ethynyl>benzene 
• 1066-54-2 trimethylsilylacetylene 
• 701-45-1 2-bromo-1-fluoro-4-nitrobenzene 
• 1072-85-1 o-fluorobromobenzene 
• 656-64-4 3-bromo-4-fluoroaniline 

Downstream Products

• 1188417-67-5 N-(3-ethynyl-4-fluorophenyl)-6,7-bis(2-(methoxy-d3)-2,2-d2-ethoxy)quinazolin-4-amine 
• 1012057-63-4 4-((3-ethynyl-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl acetate 
• 1012057-64-5 4-((3-ethynyl-4-fluorophenyl)amino)-7-methoxyquinazolin-6-ol 
• 77123-60-5 3-ethynyl-4-fluoroaniline 

Relevant academic research and scientific papers

Quinazoline derivatives

no abstract published

This new pharmaceutical use (6-1, 6-dihydro-2-yl) amide derivative, as the inhibitor of this preparation and AKT (PKB) phosphoenzyme

The invention relates to the novel materials of formula (I), wherein each of the substituents R, R1, R2, R3, R4 and R5 is as defined herein. The materials are useful as inhibitors of AKT(PKB) phosphorylation.

FORMULATION OF QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY

The present invention relates to a composition comprising an inclusion complex of a cyclodextrin and quinazoline containing zinc-binding moiety based derivatives. The cyclodextrin is preferable a β-cyclodextrin or a derivative thereof. The quinazolines have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.

TARTRATE SALTS OF QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY

The present invention relates to tartrate salts of quinazoline containing zinc-binding moiety based derivatives that are inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The tartrate salts may further act as HDAC inhibitors.

MULTI-FUNCTIONAL SMALL MOLECULES AS ANTI-PROLIFERATIVE AGENTS

The present invention relates to the compositions, methods, and applications of a novel approach to selective inhibition of several cellular or molecular targets with a single small molecule. More specifically, the present invention relates to multi-functional small molecules wherein one functionality is capable of inhibiting histone deacetylases (HDAC) and the other functionality is capable of inhibiting a different cellular or molecular pathway involved in aberrant cell proliferation, differentiation or survival.

Facile Synthesis of Ethynylated Benzoic Acid Derivatives and Aromatic Compounds via Ethynyltrimethylsilane

The coupling reaction between an aromatic halide and ethynyltrimethylsilane under the catalysis of palladium(0) generated in situ, followed by treatment of the (trimethylsilyl)ethynyl product with potassium carbonate in methanol at ambient temperatures, provides a simple approach to various ethynylated benzoic acid derivatives and other aromatic compounds.The conditions for the removal of the trimethylsilyl group were very mild, so that base-sensitive functionalities on the aromatic moiety could be tolerated.