Aibomycin analogue, its preparation method, medicinal composition and use
A composition and drug technology, applied in the field of epothilone analogues, can solve problems such as weakening natural products
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Embodiment 1
[0179] 4-Oxo-pentanoyl chloride
[0180]
[0181] Dissolving 4-oxo-pentanoic acid in CH 2 Cl 2 , add 0.01 equivalent of DMF, and then add 1.1 equivalent of oxalyl chloride. The mixture was stirred at room temperature for 6 hours and concentrated to give the crude title compound which was used without further purification.
Embodiment 2
[0183] 1-(4-Benzyl-2-oxo-oxazolidin-3-yl)-pentan-1,4-dione
[0184]
[0185] 4-Benzyl-oxazolidin-2-one was dissolved in THF (tetrahydrofuran) at -78°C, and 1.1 equivalents of n-butyllithium dissolved in hexane was added. The mixture was stirred at -78°C for 10 minutes, followed by the addition of 1 equivalent of the product of Example 1 in THF. The resulting mixture was stirred for another 30 min and washed with NH 4 The reaction was quenched with Cl solution and extracted with EtOAc. use Na 2 SO 4 The EtOAc extracts were dried and concentrated. The residue was purified by silica gel chromatography to give the title compound.
Embodiment 3
[0187] 4-Benzyl-3-[3-(2-methyl[1,3]-dioxol-2-yl)-propionyl]-oxazolidin-2-one
[0188]
[0189] The product of Example 2 was dissolved in -40°C CH 2 Cl 2 1.2 equivalents of 1,2-bis-trimethylsiloxyethane and 0.05 equivalents of TMSOTf (trimethylsilyltrifluoromethanesulfonic acid) were added. Stir the mixture at -40°C for 6 hours, add 0.2 equivalent of Et 3 N(triethylammonium). The solvent was removed under reduced pressure to give the crude title compound which was used without further purification.
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