ChemicalBook CAS DataBase List Desloratadine

Desloratadine synthesis

11synthesis methods

Product Name:Desloratadine
CAS Number:100643-71-8
Molecular formula:C19H19ClN2
Molecular Weight:310.82

Desloratadine is a tricyclic H1 antagonist that is used to treat allergies.According to previously published methods described above for cyproheptadine and azatadine, the 8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-one – ketone, was reacted with a Grignard reagent to give the corresponding tertiary carbinol, which was dehydrated in acidic media affording the 8-chloro-11-piperidinylidene derivative – 8-chloroazatadine. The last reacted with ethyl chloroformate on reflux in benzene to give the desired compound, loratadine.

79794-75-5 Synthesis

79794-75-5
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100643-71-8
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Yield:100643-71-8 98.5%

Reaction Conditions:

in ethanol;waterReflux;Inert atmosphere;Alkaline conditions;

Steps:

1.1 Preparation of desloratadine
40g of loratadine, 40g of sodium hydroxide, 500ml of absolute ethanol and 125ml of purified water were added to the reaction flask, The reaction solution was concentrated to a large amount of solid precipitated, filtered, washed and dried to obtain desloratadine 32 g, the yield was 98.5%. The reaction was carried out under nitrogen atmosphere. (Molar ratio of loratadine to alkali is 1: 20; the ratio of purified water to anhydrous ethanol is 1: 4)

References:

ZHUHAI KINHOO PHARMACEUTICAL CO., LTD;Shang, GuanQing CN103804357, 2016, B Location in patent:Paragraph 0041-0042

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38092-89-6 Synthesis