36458-24-9

Upstream product

• 421-83-0 trifluoromethane sulfonyl chloride 
• 64-04-0 phenethylamine 
• 121-44-8 triethylamine 
• 358-23-6 trifluoromethylsulfonic anhydride 
• 335-05-7 Trifluoromethanesulfonyl fluoride 

Downstream Products

• 193689-55-3 (Phenethyl-trifluoromethanesulfonyl-amino)-acetic acid ethyl ester 
• 1071494-16-0 C₉H₉F₃INO₂S 
• 1071493-74-7 N-(2,6-diiodophenethyl)-1,1,1-trifluoromethanesulfonamide 
• 1227829-51-7 C₁₁H₁₂F₃NO₄S 
• 1227829-56-2 C₁₃H₁₄F₃NO₆S 
• 1263209-31-9 N-(2-bromo-2-phenylethyl)trifluoromethanesulfonamide 

Relevant academic research and scientific papers

Trifluoromethanesulfonyl alkyne amide compound as well as preparation method and application thereof

The invention discloses a trifluoromethanesulfonyl alkyne amide compound as well as a preparation method and application thereof. Based on hydrosulfide reaction of the alkyne amide and sulfydryl, selective modification and marking of sulfydryl in polypept

Weak coordinated nitrogen functionality enabled regioselective C-H alkynylationviaPd(ii)/mono-N-protected amino acid catalysis

The exploration of weak coordinated amine derivative enabled regioselective C-H functionalization remains challenging due to the elusive achievement of reactivity and selectivity simultaneously. Herein, regioselective C-H alkynylation of various readily transformable nitrogen functionalities was developed with great efficiency, with the assistance of the mono-N-protected amino acid (MPAA) ligandviaPd(ii) catalysis proceedingvia5, 6 and 7-membered palladacycle intermediates.

Sulfoxide ligand metal catalyzed oxidation of olefins

The enantioselective synthesis of isochroman motifs has been accomplished via Pd(II)-catalyzed allylic C—H oxidation from terminal olefin precursors. Critical to the success of this goal was the development and utilization of a novel chiral aryl sulfoxide-oxazoline (ArSOX) ligand. The allylic C—H oxidation reaction proceeds with the broadest scope and highest levels asymmetric induction reported to date (avg. 92% ee, 13 examples ≥90% ee). Additionally, C(sp3)-N fragment coupling reaction between abundant terminal olefins and N-triflyl protected aliphatic and aromatic amines via Pd(II)/sulfoxide (SOX) catalyzed intermolecular allylic C—H amination is disclosed. A range of 52 allylic amines are furnished in good yields (avg. 76%) and excellent regio- and stereoselectivity (avg. >20:1 linear:branched, >20:1 E:Z). For the first time, a variety of singly activated aromatic and aliphatic nitrogen nucleophiles, including ones with stereochemical elements, can be used in fragment coupling stiochiometries for intermolecular C—H amination reactions.

C-H to C-N Cross-Coupling of Sulfonamides with Olefins

Cross-coupling of nitrogen with hydrocarbons under fragment coupling conditions stands to significantly impact chemical synthesis. Herein, we disclose a C(sp3)-N fragment coupling reaction between terminal olefins and N-triflyl protected aliphatic and aromatic amines via Pd(II)/SOX (sulfoxide-oxazoline) catalyzed intermolecular allylic C-H amination. A range of (56) allylic amines are furnished in good yields (avg. 75%) and excellent regio- and stereoselectivity (avg. >20:1 linear:branched, >20:1 E:Z). Mechanistic studies reveal that the SOX ligand framework is effective at promoting functionalization by supporting cationic π-allyl Pd.

Pd(II)-catalyzed o-C-H acetoxylation of phenylalanine and ephedrine derivatives with MeCOOOtBu/Ac2O

Pd(II)-catalyzed ortho C-H acetoxylation of triflate protected phenethyl- and phenpropylamines has been achieved with tert-butyl peroxyacetate as the stoichiometric oxidant and either DMF or CH3CN as the promoter. The reaction was found to tolerate a large variety of functional groups and could be combined with subsequent intramolecular amination to afford functionalized indoline derivatives.

Pd(II)-catalyzed amination of C-H bonds using single-electron or two-electron oxidants

(Chemical Equation Presented) Pd(II)-catalyzed intramolecular amination of arenes is developed using either a one- or two-electron oxidant. The reaction protocol tolerates a wide range of deactivating groups including acetyl, cyano, and nitro groups. This catalytic reaction allows expedient syntheses of broadly useful substituted indolines or indoles.

AMINOALCOHOL DERIVATIVES AND THEIR USE AS BETA-3 ADRENERGIC RECEPTOR AGONISTS

The present invention relates to a compound formula [I] or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.

Use of the triflamide group for friedel-crafts acylation of N-(β-phenethyl)amino acids to 3-benzazepine derivatives

Triflamides of N-(β-phenethyl)amino acids (1) were treated with P2O5 under the Friedel-Crafts acylation conditions to give the 3-benzazepines in good yields. N-(β-Phenethyl)-N-triflylvaline (1f) and phenylglycine (1g) were efficientl