4-substituted chroman compounds, tablet thereof, and application of compounds in treatment of epilepsy
A compound, the technology of chroman, which is applied in the field of medicine, can solve the problems that 4-substituted chroman compounds have not been reported, etc.
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0020] Embodiment 1: the synthesis of compound 1
[0021] Under nitrogen protection, nickel perchlorate hexahydrate (Ni(ClO 4 ) 2 ·6H 2 O, 0.02mmoL), In-TOX (0.024mmoL), A mixture of molecular sieves (400 mg) and chlorobenzene (4.0 mL) was stirred at room temperature for 10 h. When the nickel salt was completely dissolved, (E)-methyl 4-(4-fluorophenyl)-2-oxo-3-enoate (0.3mmoL) was added immediately, followed by 3-dimethylaminophenol (0.2 mmol) and stirred at room temperature. After the completion of the reaction as monitored by TLC, the reaction solution was filtered through crude silica gel (100-200 mesh) and rinsed with ethyl acetate. The filtrate was concentrated under reduced pressure, and the crude product was purified by column chromatography (petroleum ether / ethyl acetate=3:1) to obtain compound 1. After structure confirmation, the synthesized compound 1 H-NMR and 13 The C-NMR data is consistent with the literature (Highly Enantioselective Nickel-Catalyzed Oxa-...
Embodiment 2
[0022] Embodiment 2: the synthesis of compound 2
[0023] Under nitrogen protection, nickel perchlorate hexahydrate (Ni(ClO 4 ) 2 ·6H 2 O, 0.02mmoL), In-TOX (0.024mmoL), A mixture of molecular sieves (400 mg) and chlorobenzene (4.0 mL) was stirred at room temperature for 10 h. After the nickel salt was completely dissolved, (E)-2-oxo-4-(thiophen-2-yl)butyric acid-3-enoic acid methyl ester (0.3mmoL) was added immediately, and then 3-dimethylaminophenol ( 0.2 mmol) and stirred at room temperature. After the completion of the reaction as monitored by TLC, the reaction solution was filtered through crude silica gel (100-200 mesh) and rinsed with ethyl acetate. The filtrate was concentrated under reduced pressure, and the crude product was purified by column chromatography (petroleum ether / ethyl acetate=4:1) to obtain compound 2. After structure confirmation, the synthesized compound 1 H-NMR and 13 The C-NMR data is consistent with the literature (Highly Enantioselective N...
Embodiment 3
[0025] 1. Prescription
[0026]
[0027]
[0028] 2. Process steps
[0029] 1. Adhesive preparation: take the povidone K30 (PVP-K30) of the prescribed amount, add it into a 50% ethanol solution, and configure a 5% povidone-ethanol solution as the adhesive;
[0030] 2. Mix compound 1, microcrystalline cellulose (MCC), dextrin, starch, and low-substituted hydroxypropyl cellulose (L-HPC) evenly, then add a binder to make soft materials, and granulate with a 40-mesh sieve. Dry at 40°C, sieve through a 30-mesh sieve, add magnesium stearate, mix well, and tablet.
PUM
Login to View More Abstract
Description
Claims
Application Information
Login to View More