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
A novel and practical synthesis of Iclaprim
Liu, Weiyuan,Chen, Liang,Pan, Jing,Zhou, Ting,Lin, Kuaile,Zhou, Weicheng
, p. 410 - 418 (2020/10/19)
A novel and facile synthesis of Iclaprim was reported. Started from trimethoprim (TMP), the amino-protection and Friedel–Crafts acetylation with acetic anhydride were simultaneously completed in CH2Cl2 with SnCl4 as cataly
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 preparation method for iclaprim
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, (2020/02/14)
The invention discloses an iclaprim intermediate, and a preparation method for iclaprim, and provides a preparation method of a phenol compound represented by formula 8. An acetyl compound representedby formula 2 undergoes a selective demethylation reaction in an organic solvent in the presence of a Lewis acid to obtain the phenol compound of the formula 8. The invention also provides the acetylcompound of the formula 2, and a preparation method and an application thereof. The method for preparing iclaprim from the iclaprim intermediate has the advantages of economical reagents, short route,high yield, low preparation cost, simplicity in post-treatment, and suitableness 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.
Preparation method of iclaprim intermediate
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, (2020/01/12)
The invention discloses a preparation method of an iclaprim intermediate. The invention discloses a preparation method of an acetamide compound represented by a formula 1a, wherein the preparation method comprises the following steps: performing acetylati
Iclaprim intermediate and preparation method of iclaprim
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, (2020/02/14)
The invention discloses an iclaprim intermediate and a preparation method of iclaprim. The invention discloses the preparation method of the iclaprim shown as a formula 7, which comprises the following steps: in an aprotic solvent, and under the action of
Iclaprim intermediate, and preparation method of iclaprim
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, (2020/02/19)
The invention discloses an iclaprim intermediate, and a preparation method of iclaprim. A preparation method of phenol compounds represented by formula 4 is characterized in that acetylbenzene compounds represented by formula 3 undergo a selective demethy
Iclaprim intermediate, and preparation method for iclaprim
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Paragraph 0277-0296, (2020/02/14)
The invention discloses an iclaprim intermediate, and a preparation method for iclaprim. The invention provides a preparation method of dihydrocoumarin compounds represented by formula 5. The preparation method comprises the following steps: (1) carrying
Novel intermediate of Iclaprim as well as preparation method and application thereof
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, (2020/01/08)
The invention provides a new intermediate compound (formula I) of a dihydrofolate reductase inhibitor Iclaprim. According to the method and the intermediate compound shown as the formula I, the initial raw materials are easy to obtain and low in price, each step of reaction in the whole reaction step route is easy to control, the generation of impurities can be reduced, the obtained intermediate is solid and does not need to be purified, the total yield is high, and the production cost is greatly reduced.