Method for preparation of brinzolamide and intermediates thereof
A compound and amino protecting group technology, applied in the production of bulk chemicals, organic chemistry, etc., can solve the problems of high price risk, high price of 3-acetylthiophene, difficult production and operation, etc., and achieve low safety risk and cost, Cost-competitive and easy to synthesize
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[0056] Example 1
[0057] 1. Amination reaction
[0058] Add 1 g of the compound represented by formula (1) and 10 ml of tetrahydrofuran to the reaction vessel, cool to 0° C., add 0.8 mL of triethylamine, and stir overnight at this temperature. TLC follows the reaction result.
[0059] The temperature was lowered to -10°C, and 1 mL of 70% ethylamine aqueous solution was added, and the reaction was complete at room temperature.
[0060] Cool in an ice bath, add 11 mL of concentrated hydrochloric acid, control the inner temperature below 20°C, and stir for 1 hour.
[0061] Extract with dichloromethane 20 mL×2, dry with anhydrous sodium sulfate, filter, and concentrate the filtrate under reduced pressure.
[0062] The oily substance was dissolved in 20 mL of ethyl acetate, 20 mL of n-hexane was added, stirred, and filtered to obtain 0.8 g of a pale yellow solid represented by formula (2).
[0063] Mass spectrum (ESI) [M-HCl+1]=375.
[0064] 2. Introduce protecting group (benzyl)
[0065] 0.5 g...
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