Method for synthesizing finasteride
A technology of finasteride and androsteroid, applied in the field of compound synthesis, can solve the problems of high synthesis cost, low reaction yield, expensive raw material and the like
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Embodiment 1
[0041] A kind of synthetic method of finasteride, its technical synthetic route schematic diagram is shown in figure 1 .
[0042] A synthetic method for finasteride, comprising the steps of:
[0043] (1), the synthesis of 3-carbonyl-4-androstene-17β-carboxylic acid
[0044] Progesterone (31.5 g, 100.0 mmol) was dissolved in dioxane (200 mL). At low temperature, top up with Br 2(15.78 g, 98.6 mmol) and 15% sodium hydroxide solution (40 mL). After dropping, react for 6 hours. Pour into ice water (70 mL), extract the aqueous layer with ethyl acetate (40 mL×3), combine the organic phases, wash with appropriate amount of saturated sodium bicarbonate solution and saturated sodium chloride solution, and dry over anhydrous sodium sulfate. The solvent was evaporated to dryness under reduced pressure, and the residue was recrystallized with ethyl acetate to obtain white crystal 3-carbonyl-4-androstene-17β-carboxylic acid (27.80 g, yield 88%), mp 246~247 ° C (document mp 245~248℃);...
Embodiment 2
[0058] A synthetic method for finasteride, comprising the steps of:
[0059] (1), the synthesis of 3-carbonyl-4-androstene-17β-carboxylic acid
[0060] Progesterone (3.2 g, 10.0 mmol) was dissolved in dioxane (20 mL). At low temperature, top up with Br 2 (1.52g, 9.5mmol) and 15% sodium hydroxide solution (4mL). After dropping, react for 6 hours. Pour into ice water (7 mL), extract the aqueous layer with ethyl acetate (10 mL×3), combine the organic phases, wash with appropriate amount of saturated sodium bicarbonate solution and saturated sodium chloride solution, and dry over anhydrous sodium sulfate. The solvent was evaporated to dryness under reduced pressure, and the residue was recrystallized from ethyl acetate to give white crystals of 3-carbonyl-4-androstene-17β-carboxylic acid (2.62g, yield 83%), mp 246~247°C (document mp 245~248℃);
[0061] (2), the synthesis of N-tert-butyl-3-carbonyl-4-androstene-17β-carboxamide
[0062] 3-carbonyl-4-androstene-17β-carboxylic a...
Embodiment 3
[0074] A synthetic method for finasteride, comprising the steps of:
[0075] (1), the synthesis of 3-carbonyl-4-androstene-17β-carboxylic acid
[0076] Progesterone (31.5 g, 100.0 mmol) was dissolved in dioxane (200 mL). At low temperature, top up with Br 2 (16.00 g, 100.0 mmol) and 15% sodium hydroxide solution (40 mL). After dropping, react for 6 hours. Pour into ice water (70 mL), extract the aqueous layer with ethyl acetate (40 mL×3), combine the organic phases, wash with appropriate amount of saturated sodium bicarbonate solution and saturated sodium chloride solution, and dry over anhydrous sodium sulfate. The solvent was evaporated to dryness under reduced pressure, and the residue was recrystallized from ethyl acetate to obtain white crystal 3-carbonyl-4-androstene-17β-carboxylic acid (28.10 g, yield 89%), mp 246~247 ° C (document mp 245~248℃);
[0077] (2), the synthesis of N-tert-butyl-3-carbonyl-4-androstene-17β-carboxamide
[0078] 3-carbonyl-4-androstene-17β...
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