192314-93-5Relevant articles and documents
A seven-membered heterocyclic compound or a salt thereof. Preparation method and application thereof
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Paragraph 0037; 0053-0055, (2021/10/13)
The invention discloses a seven-membered heterocyclic compound or a salt thereof as well as a preparation method and application thereof. The invention provides a seven-membered heterocyclic compound represented by a formula 7a or a salt thereof. The inve
Iclaprim p-toluenesulfonate and preparation method and application thereof
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Page/Page column 0380-0394, (2020/03/06)
The invention discloses an iclaprim p-toluenesulfonate and a preparation method and application thereof. The preparation method of the iclaprim p-toluenesulfonate as shown in a formula 7a is disclosed. The preparation method comprises the following steps that in an aprotic solvent and under the action of p-toluenesulfonic acid, a benzodihydropyran compound as shown in a formula 6 is subjected to an elimination reaction to obtain the iclaprim p-toluenesulfonate as shown in the formula 7a. The aprotic solvent is one or more of tetrahydrofuran, methyltetrahydrofuran, acetone, dimethylformamide and dimethylsulfoxide. By using the iclaprim p-toluenesulfonate as an intermediate to prepare iclaprim, a reagent used is more economical, a route is short, the yield is high, the preparation cost is low, the aftertreatment is simple, and the iclaprim p-toluenesulfonate is suitable for industrial production.
Iclaprim intermediate and applications thereof
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, (2020/03/02)
The invention discloses an iclaprim intermediate and applications thereof. The invention discloses a benzodihydropyrone compound shown as formula 5 or a salt thereof. The benzopyrone compound as shownin formula 5 or the salt thereof is used as a new intermediate of iclaprim for preparing iclaprim. A preparation method comprises the following steps: in an organic solvent, under the action of a reduction reagent, carrying out reduction reaction on the benzodihydropyrone compound as shown in formula 5 and/or a salt of the benzodihydropyrone compound as shown in formula 5 to obtain a benzodihydropyrane compound shown as formula 6, wherein the reducing reagent is sodium borohydride and/or potassium borohydride. When the iclaprim intermediate is used for preparing iclaprim, the used reagents are more economical, the route is short, the yield is high, the preparation cost is low, the post-treatment is simple, and the iclaprim intermediate is suitable for industrial production.