Chloroquine diphosphate synthesis

Yield:50-63-5 80.32%

Reaction Conditions:

with phosphoric acid in ethanol

Steps:

1.3; 1.4; 2.3; 2.4; 33; 3.4; 5.3; 5.4; 1.3; 1.4; 2.3; 2.4; 3.3; 3.4 (3) Preparation of chloroquine phosphate
338.5 g of chloroquine (1.06 mol) and 90 mL of ethanol were mixed, 150 mL of phosphoric acid (85%, 1.30 mol) was added dropwise, and the reaction was incubated. After the reaction was completed, 502.3 g of crude chloroquine phosphate was obtained by filtration. (4) Refining of chloroquine phosphate 502.3 g of crude chloroquine phosphate was heated to dissolve in 200 ml of ethanol, stirred in an ice-water bath to crystallize, filtered and dried to obtain 458.2 g of chloroquine phosphate with a yield of 80.32% and a liquid chromatography purity (HPLC): 98.44%.

References:

CN112300071, 2021, A Location in patent:Paragraph 0043; 0048-0053; 0058-0062; 0067-0070; 0076-0077

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