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ChemicalBook CAS DataBase List Tetracaine hydrochloride

Tetracaine hydrochloride synthesis

9synthesis methods
synthesis of tetracaine hydrochloride: To the reaction kettle, first add 320.0kg of methyl isobutyl ketone, then add 40.0kg (207mol) of p-butylaminobenzoic acid and 56.8kg of anhydrous potassium carbonate in turn, heat the oil bath to 116°C for reflux reaction for 4h, stop heating, and react for a while. Cool for 0.5h, then add 38.3kg (266mol) of 2-Dimethylaminoethyl Chloride Hydrochloride, continue to heat to 116°C for reflux reaction for 4h, and cool to below 30°C after the reaction is complete, then add deionized water 127.0 kg stirred for 30min, left standing for 1h, separated the organic layer, dried and concentrated to obtain an oily substance, then added 169.0kg of acetone and stirred, adjusted the pH value with concentrated hydrochloric acid to 3-4, and precipitated a large number of crystals, which continued to crystallize for 12h after freezing. , centrifugal filtration and drying to obtain 53.0kg of white solid which is tetracaine hydrochloride, the yield is 85.07%, and the HPLC purity is 99.34%.
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Yield:136-47-0 94%

Reaction Conditions:

with hydrogenchloride in water;ethyl acetate;

Steps:

4 preparation of tetracaine hydrochloride

(7) (0.019 mol) and 60 mL of ethyl acetate were placed in a 100 mL three-necked flask. The mixture was stirred to dissolve all, and 1.6 mL of concentrated hydrochloric acid was added dropwise. The mixture was stirred for 30 min. The solid appeared, stirred overnight The filter cake was dried in a vacuum oven at 40 ° C overnight to give 5.4 g of a white solid in 94% yield.

References:

CN106518697,2017,A Location in patent:Paragraph 0015

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