- Preparation method of neticonazole hydrochloride
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The invention discloses a preparation method of neticonazole hydrochloride. The preparation method comprises the following steps: (1) taking a compound as shown in a formula III and bromopentane as reaction raw materials, reacting under an alkaline condition, extracting a product obtained by the reaction, reacting the extracted and separated organic product with hydrogen chloride to form a salt soas to obtain neticonazole hydrochloride; optionally (2) refining the obtained neticonazole hydrochloride. According to the method disclosed by the invention, the reaction conditions for preparing each intermediate, the intermediate post-treatment process and the neticonazole hydrochloride refining process are strictly controlled, so that the prepared neticonazole hydrochloride is high in purity,very low in residual solvent and impurity content, and excellent in stability.
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- 4-amide substituted pyrimidine targeted DDR1 inhibitor as well as preparation and anti-tumor activity application thereof
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The invention discloses an N-substituted (5-chloro-6-(substituted phenoxy)pyrimidin-4-yl)benzamide targeted DDR1 small molecule inhibitor as well as preparation and application thereof. Provided is the N-substituted (5-chloro-6-(substituted phenoxy)pyrimidin-4-yl)benzamide target DDR1 inhibitor. The synthesized 45 compounds have low toxicity to normal lung cells, the best compound is C1 in 10 [mu]M DDR1 kinase preliminary screening, and the inhibition rate of the compound on DDR1 under 10 [mu] M is significantly superior to that of a lead compound YFQ07. In the aspect of cell experiments, theIC50 value of C1 to PC-9GR is significantly superior to that of YFQ07. In addition, it is found that the inhibition rate of the designed and synthesized compound on PC-9 cells (EGFR L858R mutation) mostly exceeds 50%, and the C1 can inhibit formation of lung cancer cell colonies and migration of tumor cells.
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Paragraph 0046; 0048; 0053
(2020/12/31)
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- Synthesis and antifungal activities of a series of (1,2-disubstituted vinyl)imidazoles
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A series of vinylimidazoles containing a hetero atom such as sulfur or oxygen at a β-position of the vinyl group was prepared and the antifungal activities were tested. It was found that sulfur-substituted derivatives such as (E)-1-[2-(methylthio)-1-[2-(p
- Ogawa,Matsuda,Eto,Asaoka,Kuraishi,Iwasa,Nakashima,Yamaguchi
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p. 2301 - 2307
(2007/10/02)
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