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ChemicalBook CAS DataBase List 4,7-Dichloroquinoline
86-98-6

4,7-Dichloroquinoline synthesis

13synthesis methods
4,7-Dichloroquinoline is an important intermediate of antimalarial drugs such as chloroquine phosphate, hydroxychloroquine sulfate, and amodiaquine. It is usually obtained by chlorination and separation of 7-chloro-4-hydroxyquinoline.
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Yield:86-98-6 89.5%

Reaction Conditions:

with trichlorophosphateReflux;

Steps:

1-3 Synthesis of 4,7-dichloroquinoline (9) (chloro)

Add 120ml of phosphorus oxychloride to a 250mL three-necked flask, add 40g 4-hydroxy-7-chloroquinoline under stirring, and reflux for 1-2h until the reaction is complete. Cool to spin off the excess phosphorus oxychloride and slowly add the black oil Stir while adding in ice water, then neutralize the sodium bicarbonate aqueous solution to weak alkaline (pH 7-9), filter, wash with water, and crystallize with ethanol to obtain the product with a yield of 89.5%.

References:

CN111362872,2020,A Location in patent:Paragraph 0020; 0027-0028; 0029; 0036-0036; 0038; 0045-0046

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