- Synthetic method of ammonium acetate-mediated benzothiazole compound
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The invention discloses a synthetic method of an ammonium acetate-mediated benzothiazole compound . The synthetic method comprises the steps: adding an o-haloaniline derivative, potassium sulfide, dimethyl sulfoxide, a catalyst, an additive 1 and an additive 2 into a reaction tube, carrying out a stirring reaction at the temperature of 130-150 DEG C, cooling to room temperature after the reactionis finished, and separating and purifying the product to obtain the benzothiazole compound. The invention provides the synthetic method of the benzothiazole compound by taking K2S as a sulfur source,DMSO as a carbon source and an oxidizing agent, an o-haloaniline derivative as a substrate and an ammonium acetate mediated three-component one-pot method. The method has the advantages of fewer reaction steps, mild reaction conditions, good functional group tolerance and the like.
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Paragraph 0072-0074
(2020/11/23)
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- K2S as Sulfur Source and DMSO as Carbon Source for the Synthesis of 2-Unsubstituted Benzothiazoles
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We describe a three-component reaction of o-iodoanilines with K2S and DMSO that provides 2-unsubstituted benzothiazoles in moderate to good isolated yields with good functional group tolerance. Electron-rich aromatic amines and o-phenylenediamines instead of o-iodoanilines provided 2-unsubstituted benzothiazoles and 2-unsubstituted benzimidazoles with and without K2S under similar conditions. Notably, DMSO plays three vital roles: carbon source, solvent, and oxidant.
- Deng, Guobo,Kuang, Daizhi,Liang, Yun,Yang, Yuan,Yu, Jiangxi,Zhang, Fuxing,Zhu, Xiaoming
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supporting information
p. 3789 - 3793
(2020/06/04)
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- A thiazole pyridine compound and its preparation method
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The invention relates to a thiazole pyridine compound and its preparation method. The compound is thiazolo(4,5-b)pyridine. The preparation method comprises the following steps: (1) a compound 13-bromine-2-aminopyridine is used as a starting material to react in the presence of benzoyl chloride and ammonium thiocyanate so as to obtain a benzoyl-protected thiourea-containing derivative compound 2; (2) the compound 2 undergoes hydrolysis to obtain a thiourea derivative compound; (3) the compound 3 undergoes ring closure under the action of NaH to generate a compound 4; and (4) the compound 4 undergoes deamination by the use of isoamyl nitrite to obtain a target product compound 5. According to the method, raw materials are cheap and easily available. The synthetic method is simple. The preparation method meets requirements of large-scale industrial production.
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Paragraph 0028
(2017/05/23)
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