Double-effect anesthetic
A technology for drugs and compounds, applied in the field of medicine, can solve problems such as inconvenience of use, and achieve the effect of reducing the number of administrations
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Embodiment 1
[0021] Example 1 Synthesis of Compound 2
[0022]
[0023] 4.12 g (10 mmol) of remifentanil was added to 20 mL of water, and under stirring at room temperature, 50 mL of 10% NaOH was added dropwise and stirred for 1 h. The reaction solution was added to toluene with water to obtain a white solid, which was compound 1, and was directly sent to the next step without purification. 1.8 g (10 mmol) of propofol was dissolved in 50 mL of dichloromethane, 1.92 g (10 mmol) of EDC hydrochloride, 0.25 g (2 mmol) of DMAP, and compound 1 were added to the reaction solution and reacted at room temperature for 3 h. The reaction solution was poured into 50 mL of water, separated, the organic phase was dried over anhydrous magnesium sulfate, the solvent was removed under reduced pressure, and 2.4 g of the target product was obtained by column chromatography, with a total yield of 48%.
[0024] MS: 523.50 (ES + ), 1 H-NMR (400MHz, CDCl 3 ): 7.42-7.12(m,8H), 3.81(s,3H), 2.94(m,2H), 2.79-2...
Embodiment 2
[0025] Example 2 Synthesis of Compound 4
[0026]
[0027] Add 4.12 g (10 mmol) of remifentanil to 20 mL of water, add 50 mL of 10% NaOH dropwise under stirring at room temperature, and react at 100 °C for 4 h. The reaction solution was added to toluene with water to obtain a white solid, which was compound 3, which was directly sent to the next step without purification. 3.6 g (20 mmol) of propofol was dissolved in 50 mL of dichloromethane, 3.84 g (20 mmol) of EDC hydrochloride, 0.50 g (4 mmol) of DMAP, and compound 3 were added to the reaction solution and reacted at room temperature for 3 h. The reaction solution was poured into 50 mL of water, separated, the organic phase was dried over anhydrous magnesium sulfate, the solvent was removed under reduced pressure, and 2.3 g of the target product was obtained by column chromatography with a total yield of 35%.
[0028] MS: 669.53 (ES + ), 1 H-NMR (400MHz, CDCl 3 ): 7.40-7.11(m,11H), 2.98(m,4H), 2.79-2.70(m,6H), 2.45(t,...
Embodiment 3
[0029] Example 3: Pharmacodynamic studies
[0030] 1. Test material
[0031] Kunming mice, weighing 18-22 g, were provided by the Experimental Animal Center of the Fourth Military Medical University; Propofol (P) and remifentanil (R) were provided by Yichang Renfu Pharmaceutical Co., Ltd., and P-R were self-made; Mb -4a digital display constant temperature electric heating plate, Beijing Kewei Yongxing Instrument Co., Ltd.
[0032] 2. Test plan and results
[0033] (1) Analgesic effect:
[0034] The analgesic effect was evaluated by the hot plate method. The average value of the second pain response before the drug was used as the basic pain threshold, and the mice with the basic pain threshold within 10-30 s were used for the experiment. Sixty female mice with qualified pain threshold were randomly divided into the following 6 groups (n=10): (1) Negative control group: given normal saline (10ml / kg, i.v.); (2) Group P: given P (15mg / kg) 1 min before pain induction kg, i.v...
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