The invention relates to a process for the preparation of a compound of formula I (I), wherein R.sub.1 is hydrogen, fluoro or chloro; which process comprises a) reacting a compound of formula II (II), wherein R.sub.1 is hydrogen, fluoro or chloro; with a nitration agent to the compound of formula (III), wherein R.sub.1 is hydrogen, fluoro or chloro; and b) reacting the compound of formula III with chlorine gas at temperature from 180° C. to 250° C. to the compound of formula I.

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The invention relates to compositions and methods for inhibiting Krüppel-like Factor 10 (KLF10) for modulation of T regulatory cells and cancer immunotherapy.

The invention relates to compositions and methods for inhibiting Krüppel-like Factor 10 (KLF10) for modulation of T regulatory cells and cancer immunotherapy.

The present invention relates to processes of preparing N-((1,2,3,4,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-1-iso-propyl-1H-pyrazole-3-sulfonamide and salts thereof. The present invention further relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3 inhibition.

The present invention relates to processes of preparing N-((1,2,3,4,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-1-iso-propyl-1H-pyrazole-3-sulfonamide and salts thereof. The present invention further relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3 inhibition.

The present invention discloses a method for preparing aldehydes or ketones via aerobic oxidation of alcohols with the copper salts and nitroxide radicals as catalysts. Both oxygen and air could be used as oxidants, after 4 to 48 hours of reaction in an organic solvent at room temperature, the alcohols are efficiently oxidized to the corresponding aldehydes or ketones. The present invention has the following advantages: easy to operate, refraining from using chlorides which are corrosive to equipment, readily available raw materials and reagents, mils reaction conditions, the broad substrate scope, good functional group tolerance, convenient purification, environmentally friendly and no pollution. Thus, the method is suitable for industrial production.

The present invention discloses a method for preparing aldehydes or ketones via aerobic oxidation of alcohols with the copper salts and nitroxide radicals as catalysts. Both oxygen and air could be used as oxidants, after 4 to 48 hours of reaction in an organic solvent at room temperature, the alcohols are efficiently oxidized to the corresponding aldehydes or ketones. The present invention has the following advantages: easy to operate, refraining from using chlorides which are corrosive to equipment, readily available raw materials and reagents, mils reaction conditions, the broad substrate scope, good functional group tolerance, convenient purification, environmentally friendly and no pollution. Thus, the method is suitable for industrial production.

There is provided an α-carbonyl alkenyl ester and a preparation method therefor, and the α-carbonyl alkenyl ester is further used to react with a primary or secondary amine to prepare an amide. The two reactions are combined to develop an amide bond and peptide bond formation method that directly use carboxylic acids and amines as starting materials and allenones as a condensing reagent. The α-carbonyl alkenyl ester corresponding to an α-amino acid serves as a peptide synthesis building block and is used in solid phase peptide synthesis. The method is carried out under mild reaction conditions, simple to operate, and has a high yield. Compared with existing amide bond condensation reagents, the allenones have the advantages of being simple to prepare, having good stability, a low molecular weight, not racemizing when activating α-chiral carboxylic acids, and is a novel amide bond and peptide bond condensing reagent.

There is provided an α-carbonyl alkenyl ester and a preparation method therefor, and the α-carbonyl alkenyl ester is further used to react with a primary or secondary amine to prepare an amide. The two reactions are combined to develop an amide bond and peptide bond formation method that directly use carboxylic acids and amines as starting materials and allenones as a condensing reagent. The α-carbonyl alkenyl ester corresponding to an α-amino acid serves as a peptide synthesis building block and is used in solid phase peptide synthesis. The method is carried out under mild reaction conditions, simple to operate, and has a high yield. Compared with existing amide bond condensation reagents, the allenones have the advantages of being simple to prepare, having good stability, a low molecular weight, not racemizing when activating α-chiral carboxylic acids, and is a novel amide bond and peptide bond condensing reagent.

Provided is a photo-oxidation reaction of benzylic C—H bonds of an aromatic compound under the catalysis of an acid catalyst. The method aims to synthesize aromatic acids and acetophenones. The acid catalyst is one of Bronsted acids, including one or a mixture of two or more selected from the group consisting of hydrochloric acid, phosphoric acid, sulfuric acid, p-toluenesulfonic acid, methanesulfonic acid, trifluoromethanesulfonic acid, trifluoroacetic acid, and potassium hydrogen sulfate, as well as N-propylsulfonate pyridinium hydrogensulfate, N-butylsulfonate pyridinium hydrogensulfate, N-propylsulfonate pyridinium trifluoromethanesulfonate, N-butylsulfonate pyridinium trifluoromethanesulfonate, N-propylsulfonate pyridinium tetrafluoroborate, and N-butylsulfonate pyridinium tetrafluoroborate. The oxidation reaction is conducted under mild conditions (normal temperature and pressure) using air or oxygen as the oxidant in the presence of recyclable catalyst and solvent.