- Preparation method of 2-alkyl substituted thiazole compound
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The invention discloses a preparation method of a 2-alkyl substituted thiazole compound, which comprises the following steps: oxidizing 2-alkyl thiothiazole into 2-alkyl sulfonyl thiazole, mixing the 2-alkyl sulfonyl thiazole with a Grignard reagent, reacting the mixture at 0-5 DEG C, heating the mixture to room temperature to continue the reaction; then adding an acid solution and continuously reacting the components at room temperature to obtain a 2-alkyl substituted thiazole compound, wherein the structural formula of the 2-alkyl thiothiazole is that a Grignard reagent of the 2-alkyl sulfonyl thiazole is RCH2MgX, R1 is selected from C1-C4 alkyl groups, R is selected from H and C1-C4 alkyl groups, and X is halogen. According to the present invention, the use of the expensive palladium catalyst and the ligand is avoided, the use of the poor safety butyl lithium reagent is avoided, the ultra-low temperature of-78 DEG C is not required, the cheap and easily available 2-alkylthiothiazole is adopted as the starting material, the 2-alkyl substituted thiazole compound can be prepared under the milder condition, and the method is suitable for the industrial production.
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Paragraph 0051-0054
(2021/06/06)
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- Epothilone analogs
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Novel analogs of epothilone A, epothilone B, and epothilone C are synthesized by Stille coupling thazole-stannanes to macrolactone intermediates. The synthetic epothilone analogs selectively prevent mitosis in cancer cells through the induction and stabilization of microtubulin assembly. Selected synthetic epothilone analogs are demonstrated to have greater bioactivity than their corresponding native compound.
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- Pharmaceutical compositions and methods of inhibiting gastric acid secretion
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Pharmaceutical compositions and methods of inhibiting gastric acid secretion by administering N-alkenyl and N-alkynyl thioamides.
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