871024-05-4

Upstream product

• 454685-58-6 4,6-diiodo-pyrimidine-5-amine 
• 108-95-2 phenol 

Downstream Products

• 871027-25-7 4-phenoxy-6-prop-1-yn-1-ylpyrimidin-5-amine 
• 871027-32-6 4-(3,3-diethoxyprop-1-yn-1-yl)-6-phenoxypyrimidin-5-amine 
• 1346176-26-8 2-[2-(6-cyano-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidin-5-yl)ethoxy]ethyl benzoate 
• 871027-37-1 4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine-6-carbonitrile 
• 871027-36-0 4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine-6-carboxamide 
• 871027-35-9 4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine-6-carboxylic acid 
• 871027-34-8 4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine-6-carbaldehyde 
• 871027-33-7 6-(diethoxymethyl)-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine 
• 871027-27-9 2-[2-(6-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidin-5-yl)ethoxy]ethyl benzoate 
• 871027-26-8 6-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine 

Relevant academic research and scientific papers

Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold

Dual inhibitors of human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR) have been investigated for breast, lung, gastric, prostate, and other cancers; one, lapatinib, is currently approved for breast cancer. To develop novel HER2/EGFR dual kinase inhibitors, we designed and synthesized pyrrolo[3,2-d]pyrimidine derivatives capable of fitting into the receptors' ATP binding site. Among the prepared compounds, 34e showed potent HER2 and EGFR (HER1) inhibitory activities as well as tumor growth inhibitory activity. The X-ray cocrystal structures of 34e with both HER2 and EGFR demonstrated that 34e interacts with the expected residues in their respective ATP pockets. Furthermore, reflecting its good oral bioavailability, 34e exhibited potent in vivo efficacy in HER2-overexpressing tumor xenograft models. On the basis of these findings, we report 34e (TAK-285) as a promising candidate for clinical development as a novel HER2/EGFR dual kinase inhibitor.

FUSED HETEROCYCLIC COMPOUND

The present invention relates to a compound represented by the formula: wherein W is C(R 1 ) or N, each A is an optionally substituted aryl group or a heteroaryl group, X 1 is -NR 3 -Y 1 -, -O-, -S-, -SO-, -SO 2 or -CHR 3 - wherein R 3 is a hydrogen atom or an optionally substituted aliphatic hydrocarbon group, or R 3 is optionally bonded to A to form an optionally substituted ring structure, R 1 is a hydrogen atom or an optionally substituted group bonded via a carbon atom, a nitrogen atom or an oxygen atom, R 2 is a hydrogen atom or optionally substituted group bonded via a carbon atom or a sulfur atom, or R 1 and R 2 , or R 2 and R 3 are optionally bonded to form an optionally substituted ring structure, or a salt thereof, and a tyrosine kinase inhibitor or an agent for the prophylaxis or treatment of cancer, which contains this compound or a prodrug thereof.