Method for preparing tadalafil
A technology of tadalafil and its compounds, which is applied in the field of preparation of tadalafil, can solve problems such as difficult storage and transportation, unfavorable industrial production, inflammability and explosion, and achieve easy industrial production, low production cost and cheap price Effect
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Embodiment 1
[0029] Example 1 Preparation of Compound B
[0030] Compound B is prepared according to the method in patent WO2004011463. The prepared compound B has a purity of 97.00% and is HPLC.
Embodiment 2
[0032] Add 1200ml of purified water to 100g of compound B prepared in Example 1, add 4.66g of tetrabutylammonium bromide under stirring, slowly add 300ml of methylamine aqueous solution, and then heat the system to 80℃~85℃, keep warm for reaction After 6h, start the TLC dot plate. After the reaction is over, stop the reaction. Cool the system to 20℃~25℃, keep the temperature for 3.0h~4.0h, filter, wash the filter cake with 20ml purified water, scrape the filter cake, 65~70 After vacuum drying at ℃ for 7-8 hours, 88.48 g of tadalafil was obtained with a yield of 97.0% and a purity of 99.96% by HPLC.
Embodiment 3
[0034] Add 1500ml of purified water to 100g of compound B prepared in Example 1, add 4.80g of tetrabutylammonium bromide under stirring, slowly add 300mlg of methylamine aqueous solution, and then heat the system to 80℃~85℃, keep the temperature and react for 6h Start TLC and stop the reaction when the reaction is over. Cool the system to 20℃~25℃, keep for 3.0h~4.0h for crystallization, filter, wash the filter cake with 20ml purified water, scrape off the filter cake, and vacuum at 65~70℃ After drying for 7-8 hours, 88.50 g of tadalafil was obtained with a yield of 97.0% and an HPLC purity of 99.93%.
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