Synthesis method of Se-deuterated methyl-thiolidazine compound
Through a series of specific chemical reaction steps, the Se-deuterated methyl-thioridazine compounds were successfully synthesized, solving the problem of lack of synthetic methods in the prior art and achieving efficient and stable improvement of drug activity.
CN119751437APending Publication Date: 2025-04-04ZHEJIANG UNIV OF TECH
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Patent Information
- Application Number
- CN202411920093.X
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2024-12-25
- Publication Date
- 2025-04-04
AI Technical Summary
Technical Problem
There is a lack of a practical and versatile method for synthesizing Se-deuterated methyl-thioridazine compounds in the prior art, which limits its application in drug development.
Method used
The Se-deuterated methyl-thioridazine compound was obtained by a series of specific steps, including the substitution reaction of compound 1 with TsCl, the reaction with 2-chlorophenothiazine, the treatment in trifluoroacetic acid, the reaction in formaldehyde and sodium triacetoxyborohydride, and the catalytic reaction in tetrahydroxydiborane, and finally the treatment in TsSeCD3.
Benefits of technology
The efficient synthesis of Se-deuterated methyl-thioridazine compounds was achieved, with mild reaction conditions and high yields, providing a new idea to improve drug activity.
✦ Generated by Eureka AI based on patent content.
Abstract
The invention discloses a synthetic method of Se-deuterated methyl-thiolidazine compounds, which comprises the following specific operation processes: carrying out substitution reaction on a compound 1 and TsCl by # imgabs0 # under the action of alkali a to obtain a compound 2; dissolving the compound 2 and 2-chlorophenothiazine in a solvent A, and reacting under the action of alkali b and an additive to generate a compound 3; adding the compound 3 into a mixed solution of trifluoroacetic acid and a solvent B, and reacting to obtain a compound 4; dissolving the compound 4 in a solvent C, and reacting under the action of formaldehyde and sodium triacetoxyborohydride to generate a compound 5; dissolving the compound 5 and tetrahydroxydiborane in a solvent D, and reacting under the action of a catalyst i, a ligand I and alkali c to obtain a compound 6; dissolving the compound 6 and TsSeCD3 in a solvent E, and reacting under the action of a catalyst ii, a ligand II and alkali d to obtain a compound I; the method has the advantages of mild reaction conditions, easily available raw materials, simple reaction operation, high yield, economy and practicability, and provides opportunities for drug discovery.
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