50675-18-8Relevant articles and documents
SULFONYL-SUBSTITUTED BICYCLIC COMPOUND WHICH ACTS AS ROR INHIBITOR
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Paragraph 0184; 0185; 0494; 0495, (2020/08/16)
Provided is a sulfonyl-substituted bicyclic compound (A) which acts as a RORγ inhibitor, said compound has good RORγ inhibitory activity and is expected to be used for treating diseases mediated by a RORγ receptor in mammals.
Synthesis method of 4-ethynyl-tetrahydropyran or 4-ethynyl piperidine
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, (2020/01/12)
The invention relates to the technical field of organic synthesis. For solving the problems that a conventional synthesis method of 4-ethynyl-tetrahydropyran and 4-ethynyl piperidine is complex in operation, high in cost and unsuitable for industrial production in the prior art, the invention provides a synthesis method of 4-ethynyl-tetrahydropyran or 4-ethynyl piperidine, wherein the synthesis method comprises the following steps: carrying out Wittig reaction on carbonyl of a compound represented by the formula (I) and phosphorus ylide salt under the action of a strong alkali to generate a compound represented by the formula (II), wherein the reaction temperature is 0-50 DEG C; (2) hydrolyzing the compound represented by the formula (II) to generate a compound represented by the formula (III), wherein the reaction temperature is 20-60 DEG C; (3) carrying out a Corey-Fuchs reaction on the compound represented by the formula (III) to obtain a compound represented by the formula (IV), wherein the reaction temperature is -20 to 40 DEG C; and (4) carrying out a reaction of the compound represented by the formula (IV) with a strong alkali, and carrying out a reaction with a silica reagent to generate a compound represented by the formula (V), wherein the reaction temperature is -70 to 20 DEG C. The method has the advantages of simple and accessible raw materials, low cost, simple synthesis steps and high yield, and is suitable for laboratory small-scale preparation and industrial production.
Polysubstituted-indazole compounds and application of same as IDO inhibitors
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Paragraph 0139-0141, (2018/11/04)
The invention discloses polysubstituted-indazole compounds as shown in a formula (I) which is described in the specification, a preparation method for the compounds, and application of the compounds as IDO inhibitors. The compounds provided by the invention can be used for preventing and/or treating a plurality of diseases, such as Alzheimer's disease, cataract, infections related to cellular immune activation, autoimmune diseases, AIDS, cancers, depression, the metabolic disorder of tryptophan or the like.