Halogen-substituted tetrazole carboxylic acid compounds, and preparation method and application thereof
A compound and halogen technology, applied to the active ingredients of heterocyclic compounds, metabolic diseases, organic chemistry, etc., can solve problems such as obvious side effects and weight gain
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Embodiment 1
[0024]
[0025] 2.61g (10mmol) compound A-1 and 1.24g (10mmol) compound B-1 are dissolved in 10mL DMF, add 4.15g (30mmol) K 2 CO 3 , and then stirred overnight at 120 °C under nitrogen protection. The reaction mixture was cooled slightly and poured into 100 mL of ice water, stirred, adjusted to pH=3-4 with concentrated hydrochloric acid, extracted with 50 mL×3 dichloromethane, combined the extract phases, washed once with brine, dried over anhydrous sodium sulfate, and evaporated on a rotary evaporator. The solvent was evaporated to obtain a residue, and then purified by column chromatography to obtain the pure product of C-1, ESI-MS, m / z=318 ([M+NH 4 ] + ).
[0026] Dissolve 2.43g (8mmol) of compound C-1 in 10mL of dry toluene, stir slowly under cooling in an ice-water bath, and slowly add 2.71g (10mmol) of PBr dropwise 3 Dissolve in 2 mL of dry dichloromethane solution. After the dropwise addition, the reaction mixture was stirred at room temperature for half an hour,...
Embodiment 2-8
[0029] According to the method of Example 1, the compounds of general formula I shown in the table below were prepared.
[0030]
[0031]
Embodiment 9
[0033] The sample was prepared into a suspension of 5 mg / mL concentration with 1% sodium carboxymethyl cellulose, and the administration volume was 0.4 mL / 20 g body weight, which was equivalent to a dose of 100 mg / kg.
[0034] Healthy ICR mice, half male and half male, weighing 20-24g, meet the first-class standard. Animals were fasted for 16 hours, administered intragastrically with the compound to be tested for 15 minutes, and then intraperitoneally injected with 2 g / kg of glucose saline solution. At 0.5h, 1h, 15.h and 2h after modeling, the capillary was regularly taken from the retrobulbar venous plexus of the mouse. Blood was collected, the serum was separated by centrifugation, and the serum glucose content at each time point was determined by the glucose oxidase method. The blank mice were given neither glucose nor the test compound, and the model mice were only given glucose without the test compound.
[0035]
[0036] It can be seen from the data in the above tabl...
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