Molecular Formula | C32H47F5O3S |
Molar Mass | 606.77 |
Density | 1.201±0.06 g/cm3(Predicted) |
Melting Point | 104-106°C |
Boling Point | 674.8±55.0 °C(Predicted) |
Flash Point | 361.9°C |
Solubility | DMSO: >5mg/mL |
Vapor Presure | 3.95E-19mmHg at 25°C |
Appearance | powder |
Color | White |
pKa | 10.27±0.70(Predicted) |
Storage Condition | 2-8°C |
Stability | Stable for 2 years as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
Refractive Index | 1.521 |
WGK Germany | 3 |
RTECS | KG7623000 |
HS Code | 2937230000 |
The corresponding diketene compound was added to Grignard reagent (9-pentafluoropentylthio nonyl bromide was dissolved in tetrahydrofuran solution containing magnesium turnings, and a small amount of iodine was added to initiate the reaction to prepare Grignard reagent). Of the solution. After completion of the reaction, a solution of acetic acid in tetrahydrofuran was added to terminate the reaction. Water was added and tetrahydrofuran was distilled off, followed by further water and extraction with isohexane. After the extract was washed with aqueous potassium chloride, isohexane was distilled off, acetonitrile was added, and copper bromide, lithium bromide and acetic anhydride were slowly added. The reaction solution was placed in a mixture of thiourea, toluene and water, and cooled. The pH was adjusted to 3 with dipotassium hydrogen phosphate. The precipitated copper was removed by filtration. The filter cake was washed with toluene and the organic layers were combined and washed with an aqueous solution of sodium chloride. Toluene was distilled off, methanol was added, and aqueous sodium hydroxide was added and heated. The reaction solution was extracted with isohexane and neutralized with acetic acid. The methanol was distilled off and the resulting material was partitioned between water and ethyl acetate. The organic layer was concentrated, ethyl acetate, acetic acid and hydrogen peroxide were further added, and the reaction was stirred. Ethyl acetate was added and an aqueous solution of sodium sulfite was added to destroy the excess hydrogen peroxide. Neutralization with sodium hydroxide separated the organic layer and washed with water. The solvent was distilled off and seed crystals were added to promote crystallization. The crystals were washed with cold ethyl acetate and recrystallized from ethyl acetate to obtain fulvestrant.
developed by Astrazeneca pharmaceutical company. The US Food and Drug Administration (FDA) approved it for marketing in the US in 2002. Is a new type of ER inhibitor-ER under the prescription of breast cancer treatment drugs. It can bind competitively to ER and its affinity is comparable to that of estradiol. It can also block ER, inhibit its binding to estrogen, and stimulate the receptor to undergo morphological changes, reduce ER concentration, so that tumor cells are damaged. For the treatment of advanced breast cancer that has developed systemic metastasis, for the treatment of postmenopausal metastatic advanced breast cancer that has failed anti-estrogen therapy and is estrogen receptor (ER) positive.