1201687-03-7

Basic information

• Product Name: (R)-2-(4-fluorophenyl)-2-(trimethylsilyloxy)acetyl chloride
• Synonyms: (R)-2-(4-fluorophenyl)-2-(trimethylsilyloxy)acetyl chloride
• CAS NO: 1201687-03-7
• Molecular Weight: 260.768
• Mol File: 1201687-03-7.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: (R)-2-(4-fluorophenyl)-2-(trimethylsilyloxy)acetyl chloride(CAS DataBase Reference)
• NIST Chemistry Reference: (R)-2-(4-fluorophenyl)-2-(trimethylsilyloxy)acetyl chloride(1201687-03-7)
• EPA Substance Registry System: (R)-2-(4-fluorophenyl)-2-(trimethylsilyloxy)acetyl chloride(1201687-03-7)

Safety Data

• Hazardous Substances Data: 1201687-03-7(Hazardous Substances Data)

Upstream product

• 75-77-4 chloro-trimethyl-silane 
• 32222-45-0 (R)-2-(4-fluorophenyl)-2-hydroxyacetic acid 
• 32222-45-0 4-fluoromandelic acid 

Downstream Products

• 1201686-75-0 (3S)-N-[5-chloro-2-(1H-tetrazol-1-yl)benzyl]-2-[(2R)-2-(4-fluorophenyl)-2-hydroxyacetyl]isoxazolidine-3-carboxamide 
• 32222-45-0 (R)-2-(4-fluorophenyl)-2-hydroxyacetic acid 
• 1201686-45-4 (5S)-N-[5-chloro-2-(1H-tetrazol-1-yl)benzyl]-1-[(2R)-2-(4-fluorophenyl)-2-hydroxyacetyl]-4,5-dihydro-1H-pyrazole-5-carboxamide 
• 1201687-05-9 (S)-1-((R)-2-(4-fluorophenyl)-2-hydroxyacetyl)-4,5-dihydro-1H-pyrazole-5-carboxylic acid 
• 1201687-04-8 ethyl (S)-1-((R)-2-(4-fluorophenyl)-2-hydroxyacetyl)-4,5-dihydro-1H-pyrazole-5-carboxylate 

Relevant articles and documents

A one-pot asymmetric synthesis of a N-acylated 4,5-dihydropyrazole, a key intermediate of thrombin inhibitor AZD8165

A short, chromatography-free, and scalable synthetic route to thrombin inhibitor 1, the active metabolite of the propionic ester prodrug AZD8165, has been developed. The key synthetic step involved cycloaddition of TMS-diazomethane and ethyl acrylate to give an intermediate racemic dihydropyrazole which was reacted with enantiomerically pure 4-fluoro mandelic acid chloride in a one-pot dynamic kinetic resolution (DKR) process.

Novel Compounds 148

This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containi