858104-55-9

Basic information

• Product Name: Glycine, N-[[4-[(2R,3R)-1-(4-fluorophenyl)-3-[[2-(4-fluorophenyl)-2-oxoethyl]thio]- 4-oxo-2-azetidinyl]phenoxy]acetyl]-
• CAS NO: 858104-55-9
• Molecular Formula: C27H22F2N2O6S
• Molecular Weight: 540.544
• Mol File: 858104-55-9.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: Glycine, N-[[4-[(2R,3R)-1-(4-fluorophenyl)-3-[[2-(4-fluorophenyl)-2-oxoethyl]thio]- 4-oxo-2-azetidinyl]phenoxy]acetyl]-(CAS DataBase Reference)
• NIST Chemistry Reference: Glycine, N-[[4-[(2R,3R)-1-(4-fluorophenyl)-3-[[2-(4-fluorophenyl)-2-oxoethyl]thio]- 4-oxo-2-azetidinyl]phenoxy]acetyl]-(858104-55-9)
• EPA Substance Registry System: Glycine, N-[[4-[(2R,3R)-1-(4-fluorophenyl)-3-[[2-(4-fluorophenyl)-2-oxoethyl]thio]- 4-oxo-2-azetidinyl]phenoxy]acetyl]-(858104-55-9)

Safety Data

• Hazardous Substances Data: 858104-55-9(Hazardous Substances Data)

Upstream product

• 858105-05-2 C₃₁H₃₀F₂N₂O₆S 
• 276884-77-6 tert-Butyl (4-formylphenoxy)acetate 
• 858104-46-8 tert-butyl (4-{(1R)-1-[(4-fluorophenyl)amino]-2-[(4-methoxybenzyl)thio]-3-oxo-3-[(4S)-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]propyl}phenoxy)acetate 
• 858104-49-1 (3R,4R)-1-(4-fluorophenyl)-3-[(4-fluorobenzoyl)methylthio]-4-[4-(t-butoxycarbonylmethoxy)phenyl]azetidin-2-one 
• 858104-48-0 (3R,4R)-1-(4-fluorophenyl)-3-[(3-nitropyridin-2-yl)dithio]-4-[4-(t-butoxycarbonylmethoxy)phenyl]azetidin-2-one 
• 858104-47-9 (3R,4R)-1-(4-fluorophenyl)-3-(4-methoxybenzylsulphanyl)-4-[4-(t-butoxycarbonylmethoxy)phenyl]azetidin-2-one 
• 858104-44-6 tert-butyl (4-{[(4-fluorophenyl)imino]methyl}phenoxy)acetate 
• 73620-18-5 methyl (4-formylphenoxy)acetate 
• 403-29-2 2-bromo-4'-fluoroacetophenone 
• 123-08-0 4-hydroxy-benzaldehyde 
• 1387445-08-0 C₄₀H₄₀F₂N₂O₈S 
• 1387472-99-2 C₂₄H₂₆FNO₅S 
• 1387445-04-6 C₁₅H₁₉FO₄S 
• 1152629-06-5 ethyl 2-[2-(4-fluorophenyl)-2-oxoethyl]sulfanylacetate 

Downstream Products

• 858103-95-4 N-{[4-((2R,3R)-1-(4-fluorophenyl)-3-{[2-(4-fluorophenyl)-2-oxoethyl]thio}-4-oxoazetidin-2-yl)phenoxy]acetyl}glycyl-D-valine 
• 858103-97-6 N-{[4-((2R,3R)-1-(4-fluorophenyl)-3-{[2-(4-fluorophenyl)-2-oxoethyl]thio}-4-oxoazetidin-2-yl)phenoxy]acetyl}glycyl-L-asparagine 
• 1033750-47-8 C₃₂H₃₂F₂N₂O₆S 
• 858104-67-3 C₃₅H₃₇F₂N₃O₇S₂ 

Relevant articles and documents

Selection and development of a route for cholesterol absorption inhibitor AZD4121

The development of a synthetic route to the cholesterol absorption inhibitor AZD4121 is presented. Key steps are a highly enantioselective CBS reduction, a stereospecific Staudinger reaction, an amine/lithium chloride mediated ester hydrolysis, and a resolution of a 50:50 diastereomeric mixture by recrystallization. The synthesis was accomplished in 10 linear steps, and the overall yield, when compared with the lead optimization (LO) route, was improved from 1% to 20%. All purifications of intermediates through preparative HPLC or silica gel chromatography were avoided. This was possible since many of the intermediates along the route could be used as such in the next step until an intermediate with suitable crystalline properties could be identified and purified through crystallization.

DIPHENYLAZETIDINONE DERIVATES POSSESSING CHOLESTEROL ABSORPTION INHIBITORY ACTIVITY

Compounds of formula (I) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.