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Novel thiazole derivative or salt, isomer, preparation method and application thereof
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A technology of tautomers and stereoisomers, which is applied in the therapeutic field to achieve the effects of fast absorption, low clearance rate and long half-life
Active Publication Date: 2021-02-09
CHENGDU EASTON BIOPHARMACEUTICALS CO LTD
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Opioid abuse is a major public health problem in the U.S. because of its pain-relieving effects; 78 people die from opioid overdose every day
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Embodiment 1
[0059] Example 1: Preparation of 4-{2-{[5-(naphthalene-2-yl)thiazol-2-yl]oxy}ethyl}morpholine
[0060]
[0061] Step 1, at room temperature, compound IIa (2.43g, 10mmol), compound VI (1.97g, 15mmol), Cs 2 CO 3 (9.75g, 30mmol) was added into DMF (30mL), heated to 100°C, reacted for 6h, and the raw materials were completely reacted. The reaction solution was cooled to room temperature, and H 2 O (30mL), extracted three times with ethyl acetate (50mL*3), the organic phase was washed with water and saturated brine successively, the organic phase was dried with anhydroussodiumsulfate, filtered, the filtrate was spin-dried, and the crude product was used as eluent petroleumether: Ethyl acetate=3:1 was passed through the column, spin-dried, and vacuum-dried to obtain 2.50 g of the product. Yield: 85.2%.
[0062] Step 2, at room temperature, compound Va (2.50g, 8.5mmol), compound naphthalene-2-ylboronic acid (1.76g, 10.2mmol), CsF (1.55g, 10.2mmol) were added to 1,4-dioxane / ...
Embodiment 2
[0065] Example 2: Preparation of 4-{2-{[5-phenylthiazol-2-yl]oxy}ethyl}morpholine
[0066]
[0067] According to the preparation method of Example 1, the 2-naphthylboronic acid in step 2 was replaced by an equimolar amount of phenylboronic acid to obtain the title compound with a yield of 80.4% and a purity of 99.46%.
[0070] Example 3: Preparation of 4-{2-{[5-(3,4-dichlorophenyl)thiazol-2-yl]oxy}ethyl}morpholine
[0071]
[0072] According to the preparation method of Example 1, the 2-naphthylboronic acid in step 2 was replaced by an equimolar amount of 3,4-dichlorophenylboronic acid to obtain the title compound with a yield of 82.5% and a purity of 99.77%.
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Abstract
The invention discloses a novel thiazole derivative or salt, an isomer, a preparation method and application thereof. A compound shown as a formula (I) has a Sigma 1 receptorantagonism effect, and has strong in vitro affinity to sigma 1R in the aspect of in vitroreceptor affinity. Meanwhile, in D2L radioactive ligand binding analysis and 5HT-1A receptor, CB1 receptor and CB2 receptor cAMP tests,the affinity to the receptors is poor, and high receptor selectivity is shown. Mouse acetic acid twisting tests show that the compound has an analgesic effect. Through rat oral administration pharmacokinetic experiments, it can be known that the compound is long in half-life period, low in clearance rate and large in AUClast; Cmax can be quickly reached after oral administration, and the compoundis extremely quick to absorb and suitable for medicine.
Description
technical field [0001] The present invention relates to the field of medicinal chemistry, in particular to thiazole derivatives or their salts, isomers, their preparation method and the application of their pharmaceutical composition in the preparation of treatment and prevention, especially in pain, drugaddiction, opioiddrug synergism , psychosis, etc. in the treatment of purposes. Background technique [0002] At present, the incidence rate of pain in the world is about 35-45%, and the incidence rate of the elderly is even higher, about 75%-90%. Pain is the third therapeutic field in the world, and the market is huge. Opioids are currently the most powerful and commonly used central analgesics. Past studies have shown that opioids (such as codeine, morphine, oxycodone, and fentanyl) can effectively relieve pain. They bind to opioid receptors in the brain, spinal cord, and gastrointestinal tract to relieve pain. Precisely because of their remarkable pain-relieving effec...
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