(S)-N-Didemethyl Dapoxetine synthesis
- Product Name:(S)-N-Didemethyl Dapoxetine
- CAS Number:147199-40-4
- Molecular formula:C19H19NO
- Molecular Weight:277.36
41198-42-9
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147199-40-4
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Yield:147199-40-4 98%
Reaction Conditions:
with hydrogenchloride;pyridoxal 5'-phosphate;isopropylamine;triethylamine in water;dimethyl sulfoxide at 25; pH=8; for 16 h;Enzymatic reaction;Solvent;Reagent/catalyst;Concentration;
Steps:
1-4 Preparation of Compound (1)
At 25 ° C,The reaction solvent was added to the reaction vessel, then an ammonia source was added, the pH was adjusted to 8.0 with hydrochloric acid, and then PLP and biological enzymes (S152E, L161V, A194S, A201N) were added.Stir slowly until all dissolved, then add compound (4) and react for 16 hours.After the end of the reaction, the pH was adjusted to 2.0 with hydrochloric acid, and extracted with isopropyl acetate to leave an aqueous phase. The pH was adjusted to 12.0 with aqueous sodium hydroxide and extracted with isopropyl acetate.Isopropyl acetate was concentrated under reduced pressure to give Compound (1).
The reaction solvent was water and dimethyl sulfoxide, and the volume ratio of the two was 1:1.
The ammonia source was isopropylamine and triethylamine in a reaction solvent concentration of 0.5 M, and the molar ratio of the two was 1:1.
The mass concentration of the compound (4) in the reaction solvent was 120 g/L.
The mass concentration ratio of the compound (4) and the biological enzymes (S152E, L161V, A194S, A201N, and ABJ05767 are mutated together) is 40:1.
The obtained intermediate compound (1) was obtained by the method described above, and the mass yield was 98%, and the purity by HPLC was 99.81%.
References:
CN110078632,2019,A Location in patent:Paragraph 0010; 0032; 0037-0045; 0046-0047; 0049-0050
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147199-40-4
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