950666-52-1

Upstream product

• 62-53-3 aniline 
• 950666-51-0 (2R,4R)-5-(4-fluorophenyl)-1-[2-(4-hydroxy-6-methoxytetrahydro-2-pyranyl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide 
• 100-39-0 benzyl bromide 

Downstream Products

• 950666-51-0 (2R,4R)-5-(4-fluorophenyl)-1-[2-(4-hydroxy-6-methoxytetrahydro-2-pyranyl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide 
• 950666-53-2 (2R,4R)-1-[2-(4-benzyloxy-6-hydroxytetrahydro-2-pyranyl)-ethyl]-5-(4-fluorophenyl)-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide 

Relevant academic research and scientific papers

Process for preparing C7 intermediates and their use in the preparation on N-substituted pyrrole derivatives

The present invention relates to a process for preparing C7 intermediates and their use in the preparation of pyrrole derivatives of a class that is effective at inhibiting the biosynthesis of cholesterol in humans, and more particularly to improved synthetic methods for preparing 3,5-dihydroxy-7-pyrrol-1-yl heptanoic acids. The invention further relates to intermediates in this process.

PROCESS AND INTERMEDIATE COMPOUNDS USEFUL IN THE PREPARATION OF STATINS, PARTICULARLY ATORVASTATIN

There is provided a process for the preparation of a compound of formula (7) or salts thereof: wherein R1 represents a hydrogen or a hydrocarbyl group, R2 represents a hydrogen or substituent group, R3 represents a hydrogen or a hydrocarbyl group, and X represents a hydrogen or substituent group which comprises a) cyanating a compound of formula (1): wherein Y represents a halo group, preferably CI or Br; P1 represents hydrogen or a protecting group, and W represents =0 or -OP2, in which P2 represents hydrogen or a protecting group, to give a compound of formula (2): b) reducing the compound of formula (2) to give a compound of formula (3): coupling the compound of formula (3) with a compound of formula (4): to give a compound of formula (5): when W represents -OP2, deprotecting and then oxidising the compound of formula (5) to give a compound of formula (6): and e) subjecting the compound of formula (5) when W represents =O, or compound of formula (6) to ring-opening, and removal of any remaining protecting groups, to give a compound of formula (7) or salts thereof.