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To 1L four reaction flask was added 500g of toluene, then add 100g of starting material,Then add 1.01 ~ 1.05 equivalent of anhydrous potassium carbonate, then add 2% to 6% tetrabutylammonium bromide,Then add 1.1 to 1.3 times the equivalent of n-butyl bromide, and slowly warmed to 80 ~ 85 , incubated for 5 hours,Cooled to room temperature, filtered, the filtrate was transferred to a 1L four-necked flask,Hydrogen chloride gas is passed into the filtrate until it is no longer absorbed, filtered, the filter cake washed with toluene,Dried to give bupivacaine hydrochloride 132.84 ~ 141.70g,HPLC content> 99%, yield 90% ~ 96%.
80%
Take a step 1.75 g of dried DMF was added 20 g of a solvent, at roomtemperature solution of 1.2 g n-butylbromide, the addition was complete the reaction washeated to 80 degrees for 12 hours and 100 g of 8% after completion of the reactiondilute hydrochloric acid, and slowly cooled to room temperature, the precipitated solidwas filtered and dried to obtain the finished product 2.1 g (80% yield single-step).
In a three-neck flask add N-(2,6-dimethylphenyl)-2-piperidinecarboxamide BBKY-2, n-BUBr, potassium carbonate and twoThe methylformamide DMF was reacted at 90C for 1.5 hours, poured into 100 ml of ice water, filtered and dried to obtain bupivacaine;Because it is dissolved in isopropanol, hydrogen chloride gas is introduced into salt, filtered and dried to obtain bupivacaine hydrochloride.
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