1152629-06-5

Upstream product

• 623-51-8 ethyl 2-sulfanylacetate 
• 403-29-2 2-bromo-4'-fluoroacetophenone 
• 64-17-5 ethanol 
• 403-42-9 1-(4-fluorophenyl)ethanone 

Downstream Products

• 1387473-11-1 C₃₁H₃₁F₂NO₆S 
• 1387473-21-3 C₂₆H₂₁F₂NO₅S 
• 858104-50-4 (4-{(2R,3R)-1-(4-fluoro-phenyl)-3-[(RS)-2-(4-fluoro-phenyl)-2-oxoethylsulfanyl]-4-oxo-azetidin-2-yl}-phenoxy)-acetic acid 
• 858105-05-2 C₃₁H₃₀F₂N₂O₆S 
• 1369489-34-8 C₃₆H₃₉F₂N₃O₇S 
• 1369489-35-9 tert-butylammonium (2R)-3-cyclohexyl-2-[[2-[[2-[4-[(2R,3R)-1-(4-fluorophenyl)-3-[(2R)-2-(4-fluorophenyl)-2-hydroxyethyl]thio-4-oxoazetidin-2-yl]phenoxy]acetyl]-amino]acetyl]amino]propanoate 
• 858104-55-9 (3R,4R)-1-(4-fluorophenyl)-3-[(4-fluorobenzoyl)methylthio]-4-{4-[N-(carboxymethyl)carbamoylmethoxy]phenyl}azetidin-2-one 
• 1387445-04-6 C₁₅H₁₉FO₄S 
• 1387472-99-2 C₂₄H₂₆FNO₅S 
• 1387445-08-0 C₄₀H₄₀F₂N₂O₈S 

Relevant academic research and scientific papers

An umpolung oxa-[2,3] sigmatropic rearrangement employing arynes for the synthesis of functionalized enol ethers

An oxa-[2,3] sigmatropic rearrangement involving arynes is reported featuring the umpolung of ketones, where the C=O bond polarity is reversed. The in situ-generated sulfur ylides from β-keto thioethers and arynes undergo efficient rearrangement allowing the facile and robust synthesis of functionalized enol ethers in high yields and excellent functional group compatibility. Preliminary mechanistic studies rule out the possibility of Pummerer-type rearrangement operating in this case.

INHIBITORS OF APOL1 AND METHODS OF USING SAME

The disclosure provides at least one entity chosen from compounds of formula (I), solid state forms of the same, compositions comprising the same, and methods of using the same, including use in treating focal segmental glomerulosclerosis (FSGS) and/or non-diabetic kidney disease (NDKD).

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.