C07C255/50

Aryl-n-aryl derivatives for treating a RNA virus infection

A compound: ##STR00001##
wherein X.sup.1 represents an alkenylene group, a —NH—CO— group, a —CO—NH— group, Y.sup.1 represents an aryl group selected from pyridyl, pyrazinyl or pyrimidinyl, X.sup.2 represents —O—, —CO—NH—, —NH—CO—NH—, —OCH.sub.2—, —NH—CO—, a divalent 5-membered heteroaromatic ring comprising 1 to 4 heteroatoms or —SO.sub.2—NH—, and Y.sup.2 represents a hydrogen atom, a hydroxyl group, a morpholinyl group, a piperidinyl group, optionally substituted by a (C.sub.1-C.sub.4)alkyl group, a piperazinyl group, optionally substituted by a (C.sub.1-C.sub.4)alkyl group, or —CR.sup.1R.sup.2R.sup.3 or alternatively X.sup.2—Y.sup.2 represents —CONR.sub.cR.sub.d, wherein R.sub.c and R.sub.d form, together with the nitrogen atom a heterocyclic ring, optionally substituted by one or two (C.sub.1-C.sub.4)alkyl group, by a cyclopentyl group thus forming a spirocyclopentyl, or by a trifluoromethyl group, or any of its pharmaceutically acceptable salt, for use in the treatment and/or prevention of a RNA virus infection caused by a RNA virus belonging to group IV or V of the Baltimore classification.

Process of Fluorinating Inorganic Compounds by Direct Fluorination

The invention relates to a use of a fluorination gas, and the elemental fluorine (F.sub.2) is present in a high concentration, for example, in a concentration of elemental fluorine (F.sub.2), especially of equal to much higher than 15 or even 20% by volume, and to a process for the manufacture of a fluorinated compound by direct fluorination employing a fluorination gas, wherein the elemental fluorine (F.sub.2) is present in a high concentration. The process of the invention is directed to the manufacture of a fluorinated compound, for the exception of fluorinated benzene, by direct fluorination. Especially the invention is of interest in the preparation of fluorinated organic compounds, final products and as well intermediates, for usage in agro-, pharma-, electronics-, catalyst, solvent and other functional chemical applications. The fluorination process of the invention may be performed batch-wise or in a continuous manner.

Process of Fluorinating Inorganic Compounds by Direct Fluorination

The invention relates to a use of a fluorination gas, and the elemental fluorine (F.sub.2) is present in a high concentration, for example, in a concentration of elemental fluorine (F.sub.2), especially of equal to much higher than 15 or even 20% by volume, and to a process for the manufacture of a fluorinated compound by direct fluorination employing a fluorination gas, wherein the elemental fluorine (F.sub.2) is present in a high concentration. The process of the invention is directed to the manufacture of a fluorinated compound, for the exception of fluorinated benzene, by direct fluorination. Especially the invention is of interest in the preparation of fluorinated organic compounds, final products and as well intermediates, for usage in agro-, pharma-, electronics-, catalyst, solvent and other functional chemical applications. The fluorination process of the invention may be performed batch-wise or in a continuous manner.

PROCESS FOR PREPARATION OF HALOGENATED BENZYLAMINE AND INTERMEDIATES THEROF

The present invention provides an improved process for the preparation of halogenated benzylamine having the formula I from halogenated benzonitriles, Formula I wherein, X.sub.1 is selected from group consisting of hydrogen, chloro or fluoro, provided at least one X.sub.1 is chloro or fluoro.

##STR00001##

PROCESS FOR PREPARATION OF HALOGENATED BENZYLAMINE AND INTERMEDIATES THEROF

The present invention provides an improved process for the preparation of halogenated benzylamine having the formula I from halogenated benzonitriles, Formula I wherein, X.sub.1 is selected from group consisting of hydrogen, chloro or fluoro, provided at least one X.sub.1 is chloro or fluoro.

##STR00001##

Method for aromatic fluorination

Disclosed is a fluorination method comprising providing an aryl fluorosulfonate and a fluorinating reagent to a reaction mixture; and reacting the aryl fluorosulfonate and the fluorinating reagent to provide a fluorinated aryl species. Also disclosed is a fluorination method comprising providing, a salt comprising a cation and an aryloxylate, and SO.sub.2F.sub.2 to a reaction mixture; reacting the SO.sub.2F.sub.2 and the ammonium salt to provide a fluorinated aryl species. Further disclosed a fluorination method comprising providing a compound having the structure Ar—OH to a reaction mixture; where Ar is an aryl or heteroaryl; providing SO.sub.2F.sub.2 to the reaction mixture; providing a fluorinating reagent to the reaction mixture; reacting the SO.sub.2F.sub.2, the fluorinating reagent and the compound having the structure Ar—OH to provide a fluorinated aryl species having the structure Ar—F.

Method for aromatic fluorination

Disclosed is a fluorination method comprising providing an aryl fluorosulfonate and a fluorinating reagent to a reaction mixture; and reacting the aryl fluorosulfonate and the fluorinating reagent to provide a fluorinated aryl species. Also disclosed is a fluorination method comprising providing, a salt comprising a cation and an aryloxylate, and SO.sub.2F.sub.2 to a reaction mixture; reacting the SO.sub.2F.sub.2 and the ammonium salt to provide a fluorinated aryl species. Further disclosed a fluorination method comprising providing a compound having the structure Ar—OH to a reaction mixture; where Ar is an aryl or heteroaryl; providing SO.sub.2F.sub.2 to the reaction mixture; providing a fluorinating reagent to the reaction mixture; reacting the SO.sub.2F.sub.2, the fluorinating reagent and the compound having the structure Ar—OH to provide a fluorinated aryl species having the structure Ar—F.

Synthesis of 1:1:1 co-crystal of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(β-D-glucopyranos-1-yl)-benzene, L-proline and water

The invention relates to a process for the manufacture of the crystalline compound according to formula (I) comprising the steps (a) deacetylating the final intermediate (FI), (b) forming the crystalline compound according to formula (I) by reacting the deacetylated final intermediate of step (a) with L-proline and water and isolating the final reaction product; processes of manufacturing intermediates thereof; process intermediates and their uses in the processes according to the present invention.

Synthesis of 1:1:1 co-crystal of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(β-D-glucopyranos-1-yl)-benzene, L-proline and water

The invention relates to a process for the manufacture of the crystalline compound according to formula (I) comprising the steps (a) deacetylating the final intermediate (FI), (b) forming the crystalline compound according to formula (I) by reacting the deacetylated final intermediate of step (a) with L-proline and water and isolating the final reaction product; processes of manufacturing intermediates thereof; process intermediates and their uses in the processes according to the present invention.

NITRATION
20220009875 · 2022-01-13 · ·

A process for preparing a nitrated compound, including the step of reacting a compound (A) including at least one substituted or unsubstituted aromatic or heteroaromatic ring, wherein the heteroaromatic ring includes at least one heteroatom selected from the group consisting of oxygen, sulfur, phosphor, selenium and nitrogen, with a compound of formula (I)

##STR00001##

wherein Y is selected from the group consisting of hydrogen and nitro.