58219-97-9

Upstream product

• 374-01-6 1,1,1-trifluoroisopropanol 
• 98-59-9 p-toluenesulfonyl chloride 

Downstream Products

• 98120-52-6 1,1,1-trifluoro-2-phenylthiopropane 
• 421-49-8 2,2,2-Trifluoro-1-methylethanamine 
• 1350432-91-5 1,1-difluoroprop-1-en-2-yl 4-methylbenzenesulfonate 
• 1350432-93-7 2-[18F]fluoro-2,2-difluoroethyl tosylate 

Relevant academic research and scientific papers

Preparation method of 1, 1, 1-trifluoroisopropylamine

The invention discloses a preparation method of 1, 1, 1-trifluoroisopropylamine, which comprises the following steps: (1) reacting 1, 1, 1-trifluoroisopropanol serving as a raw material with a sulfonyl chloride compound under the action of organic alkali to obtain a 1, 1, 1-trifluoroisopropyl sulfonate compound; (2) carrying out amination reaction on the 1, 1, 1-trifluoroisopropyl sulfonate compound and ammonia gas in a polar aprotic solvent; and (3) rectifying the reaction liquid to obtain the 1, 1, 1-trifluoroisopropylamine. The method has the advantages of easily available raw materials, mild conditions, high yield and the like, and is suitable for industrial large-scale production.

POLYMYXIN ANALOGS USEFUL AS ANTIBIOTIC POTENTIATORS

The disclosure provides compounds of the formula (I) or a tautomer thereof, or a pharmaceutically acceptable salt of either of the foregoing. The variables A, R1, and R2 are defined in the disclosure. The disclosure further includes pharmaceutical compositions comprising a compound of formula I together with at least one pharmaceutically acceptable carrier. The disclosure also includes a method of sensitizing bacteria to an antibacterial agent, comprising administering to a patient infected with the bacteria, simultaneously or sequentially, a therapeutically effective amount of the antibacterial agent and a compound of formula (I).

Direct, nucleophilic radiosynthesis of [18F]trifluoroalkyl tosylates: Improved labelling procedures

A rapid and efficient protocol to afford the title compound 2-[ 18F]-fluoro-2,2-difluoroethyl tosylate ([18F]7b) is described. Starting from [18F]fluoride ion, labelling reagent 7b was obtained in good yields and a high specific radioactivity. Compound ([ 18F]7b) was then used to synthesise a prospective radiotracer for PET-imaging in dementia.

A simple, rapid procedure for nucleophilic radiosynthesis of aliphatic [18F]trifluoromethyl groups

A procedure for the radiosynthesis of aliphatic [18F] trifluoromethyl groups by reacting 1,1-difluorovinyl precursors with [ 18F]fluoride ions, resulting in the equivalent of direct nucleophilic addition of H[18F]F, has been developed. A variety of 18F-labelled model compounds were then obtained and two potential [18F]radiotracers were synthesised by a two step process starting from 1,1-difluorovin-2-yl 4-toluenesulfonate. The method is widely applicable for the synthesis of novel radiotracers in high radiochemical yields and good specific activity.

NOUVELLE VOIE D'ACCES STEREOSELECTIVE AUX ESTERS ACRYLIQUES SON APPLICATION EN CHIMIE DES SUCRES

Regio- and stereo-selective synthesis of an acryl residue by treatment of an allyl alcohol with (Z,E)-1-fluoro-1-methoxy-2-phenylsulfinylpropene was performed in three consecutive reactions in the same flask; displacement of F- by the alcohol, Claisen rearrengement, and dehydrosulfinylation.Thus, 1,5-anhydro-2-deoxy-4,6-O-isopropylidene-D-arabino-hex-1-enitol gave methyl 3,7-anhydro-6,8-benzylidene-2,4,5-trideoxy-2-C-methylene-D-ribo-oct-4-enonate and methyl 2-O-allyl-4,6-dideoxy-α-D-erythro-hex-4-enopyranoside gave methyl (methyl 2-O-allyl-3,4,6-trideoxy-5-C-methyl-6-C-methylene-α-L-threo-hept-3-enopyranosyd)uronate, which has a chiral quaternary C-5 atom.

AN EASY AND EFFICIENT SYNTHESIS OF α-METHYLENE-γ,δ-UNSATURATED ESTERS FROM ALLYLIC ALCOHOLS

A new method for the regio- and stereo-specific introduction of an acrylic ester unit, via a one pot reaction is described.