(+)-2-methoxybornyl benzoate and its preparation method and application
A technology of methoxybenzoic acid and p-toluenesulfonic acid, which is applied in the fields of nervous system diseases, organic chemistry, and drug combination, and can solve problems such as limited application and unsatisfactory ability of borneol to penetrate the blood-brain barrier
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Embodiment 1
[0013] 1. Synthesis of (+)-2-methoxybornyl benzoate
[0014] Add 20g of natural borneol, 15g of 2-methoxybenzoic acid and 30ml of toluene into a 500ml round bottom flask; add 0.5g of p-toluenesulfonic acid dropwise, mix well; stir and reflux at 120°C for 8 hours. After the reaction, the catalyst, unreacted borneol, and solvent were removed to obtain the initial product. The primary product was separated with a silica gel column to obtain colorless crystals.
[0015] 2. Properties of (+)-2-methoxybornyl benzoate
[0016] The colorless crystals obtained in step 1 are poorly soluble in water, but easily soluble in chloroform, ethanol, acetone, and ethyl acetate. The melting point is 36.8-37.2°C.
[0017] 3. Identification of the compounds of the present invention:
[0018] 1. UV spectrum analysis: the compound of the invention is dissolved in methanol, and then scanned with a PDA-100 diode array detector (DAD), and the compound has ultraviolet absorption at 202.8nm, 235.1nm, ...
Embodiment 2
[0035] 1. Acute toxicity test of dextroborneol in mice
[0036] 1.1. Experimental animals
[0037] 60 Kunming white mice, half male and half male, body weight 20±2g. Provided by the Guangdong Provincial Laboratory Animal Center, certificate number: SCXK Yue 2008-0001 Yue Jian Zheng Zi 2007A013, used for the test after 3 days of adaptation.
[0038] 1.2. Experimental method
[0039] Mice were fasted overnight for 15 h before administration, and had free access to water. They were divided into 6 groups with 10 rats in each group. Groups 1 to 5 were given dextroborneol blended oil solution, and the dosages were 6170, 4319, 3023, 2116, 1481 mg / kg; Blend oil. According to the weight of the mice, the drug group was fed with dextroborneol at a dose of 0.2 mL / 10 g, and the control group was fed with the same volume of edible oil. Return to normal feeding 2 hours after administration, observe continuously for 14 days, observe the changes in the weight of the mice every day, whethe...
Embodiment 3
[0057] Experimental Study of (+)-2-Methoxybornyl Benzoate Penetrating the Blood Brain Barrier
[0058] 1. Test animals: SPF grade Kunming mice, half male and half male, weighing 20±2g. Provided by the Experimental Animal Center of the Guangdong Provincial Department of Health, certificate number: SCXK Yue 2008-0002, used for experiments after 3 days of adaptation. Kunming mice were fasted overnight for 15 hours before administration, and had free access to water.
[0059] 2. Method
[0060] 2.1 Liquid preparation
[0061] Accurately weigh 40mg of Evans blue and transfer it into a 10ml volumetric flask, add normal saline to the volume to obtain a 0.4% solution; mix acetone and normal saline (7:3) (v:v) to obtain a homogeneous solution slurry mixture.
[0062] 2.2 Evansland standard curve drawing
[0063] Prepare Evans blue multiple release series concentration solution 0.5ug / g, 10ug / g, 20ug / g, 50ug / g, 100ug / g with blank mouse brain plasma, and measure the absorbance at 620...
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