Ritonavir properties
The melting point of 120-122 ° C
Flash point 2 ℃
Storage conditions - 20 ° C Freezer
: solubility DMSO soluble10mg/mL (the clear solution, warmed)
Powder form
Color white to beige
It is used as an antiviral
Use antiviral drugs. Peptide - like Hiv_1 protease inhibitor used in the treatment of AIDS.
Production methods of compound (Ⅰ) soluble in methylene chloride, under 15 ℃ and nitrogen protection to join compounds (Ⅱ) and triethylamine methylene chloride solution, stirring 2 h, containing compounds in the mixture (Ⅲ), applied directly to the next step response.
Slowly add triethylamine to the reaction solution, add the obtained mixture to dichloromethane solution of triphosphogas at -15 ~ -13℃, and react for 1.5h. Slowly add compound (Ⅳ) methylene chloride solution, reaction of 1 h. Add water, separate organic layer, wash with 10% citric acid solution, concentrate. The residue was purified by silica gel and the yield of compound (V) was 38%.
The compound (V) is soluble in acetic acid and hydrogenated under palladium catalysis. Filtration, decompression and concentration. The residue is dissolved in water and adjusted to a Ph of 8 with sodium hydroxide. With methylene chloride extraction, extraction with water after washing, vacuum concentration, get compounds (Ⅵ), applied directly to the next step response.
Compounds (Ⅶ) soluble in ethyl acetate, adding sodium bicarbonate solution, reaction after stratification. Will be added to the compound of organic layer (Ⅵ) ethyl acetate solution, in 60 ℃ for 12 h. Concentrate, add ammonia and stir for 1 hour. Separate the organic layers and wash them with 10% potassium carbonate and sodium chloride solution respectively. Reduced pressure concentration, the residue was purified with silica gel, and the yield in compound (V) was 27%.
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