171348-52-0

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 43163-94-6 2-amino-3-fluoro-3-methylbutanoic acid 
• 1609548-90-4 3-methylbut-2-en-1-yl (3,5-bis(trifluoromethyl)benzoyl)oxycarbamate 
• 1609549-18-9 4-(2-fluoropropan-2-yl)oxazolidin-2-one 
• 293305-66-5 tert-butyl 2-fluoro-1-(hydroxymethyl)-2-methylpropyl carbamate 
• 103723-65-5 3-methylbut-2-en-1-yl N-hydroxycarbamate 

Downstream Products

• 757242-20-9 (E)-(S)-4-({2-[(S)-2-(tert-Butoxycarbonyl-methyl-amino)-3-methyl-3-phenyl-butyrylamino]-3-fluoro-3-methyl-butyryl}-methyl-amino)-2,5-dimethyl-hex-2-enoic acid 

Relevant academic research and scientific papers

Iron(II)-catalyzed intramolecular olefin aminofluorination

An iron(II)-catalyzed diastereoselective olefin aminofluorination is reported (dr up to >20:1). This new transformation applies a functionalized hydroxylamine and Et3N·3HF as the nitrogen and fluorine source, which facilitates the efficient synthesis of β-fluoro primary amines and amino acids from allylic alcohol derivatives. Preliminary mechanistic studies reveal that an iron-nitrenoid is a possible intermediate and that its reactivity and enantioselectivity can be efficiently modulated by ligands.

BENZAMIDE TRPA1 ANTAGONISTS

Compounds of formula I, pharmaceutically acceptable salts thereof, diastereomers, enantiomers, or mixtures thereof: wherein R, X, Y, Z, n and A are as defined in the specification, as well as pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.

SUBSTITUTED IMIDAZOHETEROCYCLES

The present invention provides substituted imidazoheterocyclic compounds having the structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.

Tubulin inhibitors. Synthesis and biological activity of HTI-286 analogs with B-segment heterosubstituents

Modifications of the B-segment of HTI-286 (2) produced a class of analogs incorporating heteroatom-substituents. The structure-activity relationship was studied. Analogs bearing methylsulfide and fluoride groups exhibited potency comparable to that of the parent compound HTI-286 and to paclitaxel in cytotoxicity assays against KB-3-1 cell lines. These analogs were more potent than paclitaxel against P-glycoprotein expressing KB-8-5 and KB-V1 cell lines. Several analogs showed strong inhibition of tubulin polymerization.