33 results about "Trifluoroethylamine" patented technology

The invention relates to a new process for the manufacture of fluoroaryl compounds and derivatives thereof, in particular of fluorobenzenes and derivatives thereof, and especially wherein said manufacture relates to an environmentally friendly production of the said compounds. Thus, the present invention overcomes the disadvantages of the prior art processes, and in a surprisingly simple and beneficial manner, and as compared to the prior art processes, in particular, the invention provides a more efficient and energy saving processes, and also provides a more environmentally friendly process, for the manufacture of nuclear fluorinated aromatics, and preferably of nuclear fluorinated fluorobenzenes. Accordingly, in one aspect of the invention, an industrially beneficial process for preparing fluorobenzenes from halobenzene precursors using HF to form hydrogen halide is provided by the present invention. A beneficial and surprisingly simple use of chlorobenzene as an industrially interesting starting material in the manufacture of fluorobenzene is provided.

The invention belongs to the technical field of cathepsin K inhibitors, and particularly relates to novel nitrile cathepsin K inhibitors using cathepsin K as target protein and trifluoroethylamino groups as P2-P3 linkers and having different P3 position structures. The P2-P3 linkers are trifluoroethylamino groups, P3 positions are aryl groups comprising a bromophenyl group, a p-biphenyl group, a p-terphenyl group and a p-methyl biphenyl group. The nitrile inhibitors have the advantages that the structures are simple relatively, the synthesis is convenient, and the yield is high; inhibition constants (Ki) of the compounds (the inhibitors) to cathepsin K are in the picomole level, so that the effective inhibiting ability to the cathepsin K is reflected; when the P3 position is the P-terphenyl group, the inhibiting ability and the selectivity of the inhibitor to the Cat K (the cathepsin K) are better than those of corresponding amide inhibitors. In vitro cytotoxicity tests show that the inhibitors are free of cytotoxicity, and have the possibility of being applied to clinical trials and being used as potential anti-osteoporosis drug.

The invention relates to fatty trifluoroethyl ester compounds and a preparation method thereof. Wherein, the definition of fatty acid trifluoroethyl ester compound is the same as that in the claims. The preparation method includes the following steps: under low temperature conditions, add 2,2,2-trifluoroethylamine and tert-butyl nitrite into an organic solution in which fatty acids are dissolved, stir evenly, and continue to react at room temperature to obtain fatty acid three Fluoroethyl ester products. Wherein, the molar ratio of fatty acid to 2,2,2-trifluoroethylamine and tert-butyl nitrite is 1:(1-2.5):(1-2.5). The method of the present invention can obtain the target product without adding catalysts and other additives, has simple operation, mild reaction conditions, low cost, high yield, and is environmentally friendly, and can obtain trifluoroethyl esters of fats and drug molecule carboxylic acids Compounds are widely used.

The invention discloses a preparation method of trifluoroethylamine hydrochloride. First, trifluoroethylamine and hydrochloric acid are neutralized in an ethanol-water azeotropic or near-azeotropic system to obtain trifluoroethylamine hydrochloride The solution after the reaction, and the trifluoroethylamine hydrochloride obtained after desolvation and removal of water and ethanol by distillation under reduced pressure. The method provided by the invention is safe in technology, and the prepared product has high purity and low water content.

The present invention provides a process for producing highly pure fluoro-compounds by making use of N-(2-chloro-1,1,2-trifluoroethyl)diethylamine. The process produces little or no chlorinated by-products. The present invention provides a process for producing a fluoro-compound, comprising fluorinating an alcohol derivative represented by the following general formula (I): R1R2R3COH (I), (wherein R1 represents a hydrogen atom, a substituted or unsubstituted alkyl group, aryl group, alkylcarbonyl group, alkoxycarbonyl group, arylcarbonyl group or aryloxycarbonyl group; and R2 and R3 are each independently a substituted or unsubstituted alkyl group, aryl group, alkylcarbonyl group, alkoxycarbonyl group, arylcarbonyl group or aryloxycarbonyl group, wherein at least two of R1, R2 and R3 may together form part of a ring structure, either with or without a heteroatom) with N,N-diethyl-2-chloro-1,1,2-trifluoroethylamine to form a fluoro-compound represented by the following general formula (2): R1R2R3CF (2), (wherein R1, R2 and R3 are as defined above), the process being characterized in that an alcohol derivative represented by the following general formula (3): R4OH (3), (wherein R4 represents a substituted or unsubstituted alkyl group or aryl group) is added to the reaction system.

The present invention provides a synthetic method for upatinib, which uses compound 1 as a starting material to obtain compound formula 4 through chlorination, coupling, hydrolysis, and hydrogenation into a salt, and then derivatizes and halogenates with McBurney's acid to obtain intermediate Body compound 6. Next, we use 2-bromo-5-p-toluenesulfonyl-5H-pyrrolo[2,3-b]pyrazine compound 7 as raw material to obtain intermediate compound 9 through ammonolysis reaction and amino protection. The docking reaction of compound 6 and compound 9 obtained chemical formula 10, and then the key nucleus 11 of upadatinib was obtained by cyclization with trifluoroacetic anhydride. Finally, the docking reaction of trifluoroethylamine was optimized, and upadatinib was obtained by both methods. These improvements have greatly improved the route efficiency, reduced the process steps of using noble metal catalysts, reduced the process cost, and greatly reduced the generation of by-chiral products, which is conducive to improving the purity of the final product. The route is:

The present invention relates to a process for producing an optically active 1-alkyl-substituted 2,2,2-trifluoroethylamine, which is an important intermediate of medicines and agricultural chemicals, and which is represented by the formula [3] [in the formula R represents a lower alkyl group of a carbon and * represents an asymmetric carbon], or its salt by subjecting an optically active imine represented by the formula [1] to an asymmetric reduction under hydrogen atmosphere using a metal catalyst of Group VIII to convert it into an optically active secondary amine represented by the formula [2] and then by subjecting the secondary amine or its salt to hydrogenolysis.[Chem. 23]