ChemicalBook CAS DataBase List Vilanterol Trifenatate

Vilanterol Trifenatate synthesis

6synthesis methods

Product Name:Vilanterol Trifenatate
CAS Number:503070-58-4
Molecular formula:C44H49Cl2NO7
Molecular Weight:774.78

Vilanterol trifenatate is synthesized by incorporation of an oxygen atom at the homobenzylic position of the right-hand side phenyl ring of (R)-salmeterol and has suitable chemical properties for inhaled administration. The combination in fluticasone furoate (FF) and vilanterol trifenatate (VI) in a single inhaler is the first once daily combination available on the market for the treatment of stable COPD.

503068-34-6 Synthesis

503068-34-6
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503070-58-4
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Yield:503070-58-4 92%

Reaction Conditions:

in dichloromethane;tert-butyl alcohol at 5 - 66; for 4 h;Solvent;

Steps:

1-5 Example 1:
The virantra base (8g) and triphenylacetic acid (4.75g) were added to a mixed solvent of 33mL of dichloromethane and 167mL of t-butanol, and the stirring was started to adjust the rotation speed to 400 rpm, using a low temperature thermostat (Shanghai Bilang Instrument Manufacturing Co., Ltd.) is heated to 66 ° C to dissolve, the speed is adjusted to 90 rev / min, set the cooling program, from 66 ° C to 30 ° C process, the cooling rate is 0.3 ° C / min, 30 ° C for 1 hour; The process was carried out at 30 ° C to 5 ° C, the cooling rate was 0.2 ° C / min, and the temperature was kept at 5 ° C for 3 hours. Filtration and drying under vacuum at 40 ° C gave 11.7 g of a white solid, yield 92%, and chemical purity 99.9%.

References:

Anhui Dexinjia Bio-pharmaceutical Co., Ltd.;Xu Kun;Li Xuekun;Lin Jianhua;Zhang Qilong;Wang Honglei CN109574861, 2019, A Location in patent:Paragraph 0013-0022

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