124993-49-3

Upstream product

• 124993-48-2 2-<<4-(2-quinolinylmethoxy)phenoxy>methyl>benzyl chloride 
• 151-50-8 potassium cyanide 
• 124993-40-4 2-[(4-hydroxyphenoxy)methyl]quinoline 
• 187879-24-9 1-(4-Hydroxy-phenoxy)-3-(triphenyl-λ⁵-phosphanylidene)-propan-2-one 
• 612-12-4 o-Xylylene dichloride 
• 143-33-9 sodium cyanide 
• 773837-37-9 sodium cyanide 
• 91-63-4 2-methylquinoline 
• 3747-74-8 2-(chloromethyl)quinoline monohydrochloride 

Downstream Products

• 120128-20-3 2-[[4-[[2-(1H-tetrazol-5-ylmethyl)phenyl]methoxy]phenoxy]methyl]quinoline 

Relevant academic research and scientific papers

Therapeutic uses of tri-aryl acid derivatives

The use of triaryl acid derivatives of formula (I) and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.

The process development of RG 12525 (2-{[4-(Tetrazol-5-ylmethylphenyl)-methoxy]phenoxymethyl}quinoline)

This contribution describes process improvements to provide a practical and cost-effective synthesis for the manufacture of RG 12525 which resulted in a 3-fold increase in overall yield. Improved solvent systems for chlorination and azidation reactions are described. Adjustments to the tetrazole-forming step eliminated azide sublimation and minimised this risk on scale-up. A robust solvent system was found to control the polymorphic form during crystallisation, which had hitherto been difficult due to the near-equivalence of melting points (154 and 157 °C) of the two known forms.

Approaches to p-hydroxyphenoxymethylquinolines which avoid intermediate chloromethylquinolines for the synthesis of the LTD4 antagonist, RG 12525

As part of an effort to develop an industrial synthesis of the LTD4 antagonist RG 12525 (1), several approaches to the intermediate (2-quinolinylmethoxy)phenol 3 were investigated that avoided the generation of the lachrymatory sensitizer α-chloro-2-methylquinoline 2. Utilization of a cyclic sulfate in place of α,α'dichloro-o-xylene 4 showed promise as a selective dialkylating agent in the conversion of 3 to RO 12525 (1).

Development of a Novel Series of (2-quinolinylmethoxy)phenyl-Containing Compounds as High-Affinity Leukotriene D4 Receptor Antagonists. 2. Effects of an Additional Phenyl Ring on Receptor Affinity

This series of reports describe the development of orally active, highly potent, specific antagonists of the peptidoleukotrienes containing a (2-quinolinylmethoxy)phenyl moiety.The compounds reported in this paper contain an additional phenyl ring, which