C07C253/14

Process for the preparation of teriflunomide

The present invention provides a process for the preparation of Teriflunomide (Formula-I). The present invention describes the synthesis of Teriflunomide without isolating the intermediate Leflunomide. Teriflunomide is prepared from 5-Methyl isoxazole-4-carboxylic acid by converting to its acid chloride and coupling with 4-trifluoromethyl aniline to obtain Leflunomide (which is not isolated) followed by ring opening reaction using aq. Sodium Hydroxide to form Teriflunomide. In other words, the process is telescoped from 5-methylisoxazole-4-carbonyl chloride. ##STR00001##

Method of making perfluorocyclobutane-containing monomer

The invention pertains to a multi-step process for making polyfunctional aromatic compounds comprising two phenyl rings bearing reactive groups susceptible of polycondensation reaction to provide polycondensed polymers, said method using economic raw materials, and possessing high selectivity and overall yield.

Method of making perfluorocyclobutane-containing monomer

The invention pertains to a multi-step process for making polyfunctional aromatic compounds comprising two phenyl rings bearing reactive groups susceptible of polycondensation reaction to provide polycondensed polymers, said method using economic raw materials, and possessing high selectivity and overall yield.

NOVEL NAMPT ENZYME AGONIST AND PREPARATION AND USE THEREOF

The present invention provides a class of novel NAMPT enzyme agonist and preparation and use thereof, which has a structural formula as shown in formula I or formula II. The present invention screens the NAMPT agonist NAT from the chemical small molecule library, and the NAT exhibits a good cytoprotective effect and a good anti-neurodegeneration effect in animal models of neurodegeneration. We studied the binding of NAT to enzymes, and then carried out multiple rounds of structure optimization based on the chemical structure characteristics of NAT and its enzyme activity properties, and obtained a relatively defined structure-activity relationship. The present patent not only lays the foundation for developing innovative drugs for anti-aging and neurodegenerative diseases, but also theoretically provides a proof-of-concept that enhancing NAMPT enzyme activity plays an important role in neuroprotection.

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Method for synthesizing 2-alkyl-4-trifluoromethyl-3-alkylsulfonylbenzoic acids

A process for preparing 2-alkyl-4-trifluoromethyl-3-alkylsulfonylbenzoic acids of the formula (I) is described. ##STR00001##
Here, the substituents are radicals such as alkyl and substituted phenyl.

Method for synthesizing 2-alkyl-4-trifluoromethyl-3-alkylsulfonylbenzoic acids

A process for preparing 2-alkyl-4-trifluoromethyl-3-alkylsulfonylbenzoic acids of the formula (I) is described. ##STR00001##
Here, the substituents are radicals such as alkyl and substituted phenyl.

Method for synthesizing 2-alkyl-4-trifluoromethyl-3-alkylsulfonylbenzoic acids

A process for preparing 2-alkyl-4-trifluoromethyl-3-alkylsulfonylbenzoic acids of the formula (I) is described. ##STR00001##
Here, the substituents are radicals such as alkyl and substituted phenyl.

Process for preparing cyanoacetates

This invention relates to a process for producing cyanoacetates involving contacting a salt of an alkyl, alkenyl, alkynyl or aryl formyl acetate with a hydroxyl amine acid under appropriate conditions and for a time sufficient to yield a cyanoacetate.

Process for preparing cyanoacetates

This invention relates to a process for producing cyanoacetates involving contacting a salt of an alkyl, alkenyl, alkynyl or aryl formyl acetate with a hydroxyl amine acid under appropriate conditions and for a time sufficient to yield a cyanoacetate.

Process to prepare 3-methyl-2-nitrobenzoic acid by air oxidation
10155718 · 2018-12-18 · ·

A method for preparing 3-methyl-2-nitrobenzoic acid is disclosed wherein 1,3-dimethyl-2-nitrobenzene is combined with an oxidation catalayst in the presence of an oxygen source and an initiator, provided that less than 99% of the 1,3-dimethyl-2-nitrobenzene is oxidized. A method for preparing compounds of Formula 7 and Formula 11 is also disclosed wherein the method is characterized by using 3-methyl-2-nitrobenzoic acid as prepared by the method disclosed above ##STR00001## wherein R.sup.1 is C.sub.1-C.sub.7 alkyl, C.sub.3-C.sub.6 cycloalkyl or C.sub.4-C.sub.7 alkylcycloalkyl.