Procaine synthesis

11synthesis methods

Product Name:Procaine
CAS Number:59-46-1
Molecular formula:C13H20N2O2
Molecular Weight:236.31

Procaine, its hydrochloride is called novocain, is suitable for infiltration anesthesia, conduction anesthesia, subarachnoid anesthesia, epidural anesthesia, and also used for local closure of peripheral nerves. Nitrocaine is obtained by refluxing esterification of p-nitrobenzoic acid and diethylaminoethanol in xylene, which is then reduced to procaine with iron powder, and then the finished product is obtained with hydrochloride.

13456-39-8 Synthesis

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59-46-1
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Yield:59-46-1 95.6%

Reaction Conditions:

with hydrogen;nickel in acetic acid butyl ester at 35; under 1520.1 Torr; for 12 h;Solvent;Reagent/catalyst;Temperature;

Steps:

10 Example 10

S1: in the reactor, 53.3 g of nitrocaine, 450 mL of butyl acetate and 0.6 g of an amorphous nickel catalyst were sequentially added,S2: At the same time of stirring, hydrogen gas is introduced to replace the air in the reaction system 3-4 times, Controlling the hydrogen pressure to 2 atmospheres Pressure, the reaction was stirred at 35 degrees Celsius for 12 hours to achieve catalytic hydrogenation;S3: Filtering under reduced pressure, washing the filter cake with the same solvent as in Step S1 to collect the amorphous nickel catalyst;S4: The filtrate obtained in step S3 was concentrated under reduced pressure to obtain a solid, which is the crude product of novocaine; S5: The resulting product was recrystallized from dichloromethane to give the product 44.8g, yield 95.6%,

References:

CN106905173,2017,A Location in patent:Paragraph 0023; 0024; 0025