2941-17-5

Upstream product

• 2843-17-6 3-bromo-2,2-dimethylpropionic acid 
• 4835-90-9 3-Hydroxy-2,2-dimethylpropanoic acid 

Downstream Products

• 23695-27-4 C₁₃H₁₅BrCl₂N₂O₃ 
• 69635-70-7 3-bromo-2,2-dimethyl-N-[4-(4-methyl-6-oxo-1,4,5,6-tetrahydro-pyridazin-3-yl)-phenyl]-propionamide 
• 4613-11-0 2,3-diphenylbutane 

Relevant academic research and scientific papers

NON-SYSTEMIC TGR5 AGONISTS

Compounds of structure (I), or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, R3, R4, R8, R9, R10, R11, R12, A1, A2, X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided.

OXADIAZOLE SUBSTITUTED INDAZOLE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE (S1P) AGONISTS

The present invention provides compounds of formula (I) or salts thereof, having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders mediated by S1P1 receptors.

Converting gem-dimethyl groups into cyclopropanes via Pd-catalyzed sequential C-H activation and radical cyclization

(Diagram presented) A novel route to the synthesis of cyclopropane derivatives is described. 1,1-Dimethyls in 2-(1,1-dimethylalkyl) dimethyloxazolines are first converted into 1,3-diiodide derivatives via Pd-catalyzed sequential C-H activation and then radically cyclized to provide 2-(1-alkylcylclopropyl)-dimethyloxazolines. The use of EtOAc as a solvent is crucial for the diiodination of the functionalized substrates.

REGIOSELECTIVE FORMATION OF AMIDOCARBOXY-SUBSTITUTED FREE RADICALS

Factors affecting the production of amidocarboxy-substituted free radicals have been investigated by examining reactions of derivatives of valine and sarcosine.Variations in the regioselectivity of reactions of these compounds are exemplified by the reactions of N-benzoylvaline methyl ester (4a) and N-benzoylsarcosine methyl ester (12a) with sulphuryl chloride and N-bromosuccinimide.Whereas the reaction of (4a) with sulphuryl chloride involves hydrogen-atom transfer from the β-position of (4a) with subsequent chlorine incorporation to give (4g), in direct contrast the reaction with N-bromosuccinimide proceeds via hydrogen-atom abstraction from the α-position of (4a) and yields the dibromide (4d).N-benzoylsarcosine methyl ester (12a), reacts with N-bromosuccinimide to give the α-bromosarcosine derivative (12b), whereas with sulphuryl chloride the product is the N-chloromethylglycine derivative (12c).These studies indicate that amidocarboxy-substituted radicals such as (3a) and (13) are considerably more stable than the tertiary alkyl radical (1a) and the amidosubstituted radical (14), respectively, but hydrogen-atom transfer reactions may afford the less stable products if electrophilic radicals are involved in the hydrogen-atom abstraction and if there is little development of radical character in the reaction transition state.