ChemicalBook CAS DataBase List ZANAMIVIR HYDRATE

ZANAMIVIR HYDRATE synthesis

10synthesis methods

Product Name:ZANAMIVIR HYDRATE
CAS Number:139110-80-8
Molecular formula:C12H20N4O7
Molecular Weight:332.31

1H-Pyrazole-3-carboximidamide Hydrochloride

166197-22-4
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4-amino-2-deoxy-2,3-didehydro-N-acetylneuraminic acid

130525-62-1
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$234.00/1g

139110-80-8
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$7.00/1mg

Yield:139110-80-8 74.9%

Reaction Conditions:

with sodium carbonate in water at 35; for 7 h;Industrial scale;Temperature;

Steps:

3.5 Synthesis of zanamivir (Formula I)
1.4 kg of 2,3-didehydro-4-amino-4-acety lneuraminic acid (Formula la) was added 30l of glass reactor , 15 kg of water was added , then 1.3 kg of sodium carbonate was added, and followed by the addition 800 g of imidopyridine hydrochloride at 40 ° C , and reaction was carried out for 6 hours. the 8 kg of water was concentrated and 13 kg of isopropyl alcohol was added and stirred to precipitate a solid powder. filtered , washed with isopropanol and dried to obtain 67 g of crude Zanamivir . then recrystallized from isopropanol-water , filtrated , and dried to obtain a pharmaceutical grade of zanamivir (formula I) 1. kg Yield: 74.9%

References:

Hubei Haoxin Pharmaceutical Co., Ltd.;Jin Peng;Pan Yajin;Wang Gongxian CN106632186, 2017, A Location in patent:Paragraph 0118; 0119

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