Acetyl isovaleryl tylosin amide, preparation method and application
A technology of acetylisovaleryl tylosin amine and compound, which is applied in the field of novel acetylisovaleryl tylosin amide, and achieves the effects of simple preparation method, mild conditions and high yield
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Embodiment 1
[0037] Example 1: Preparation formula 2 Shown-NR 1 R 2 =-N(C 2 h 5 ) 2 Derivatives( 2-a )
[0038] take compound 1 (416mg, 0.4mmol), diethylamine (62μl, 0.6mmol) was dissolved in 5ml of methanol, after heating to 40°C, formic acid (31μl, 1.5mmol) was added, after constant temperature reaction for 8h, after the system was concentrated, 20ml of water was added Dissolve the residue, then adjust the pH with aqueous sodium hydroxide solution until no precipitation occurs, then filter with suction, dry and weigh the filter cake to obtain the compound 2-a (350mg), yield 80.61%, off-white solid.
Embodiment 2
[0039] Example 2: Preparation formula 2 Shown-NR 1 R 2 =-N(n-C 4 h 9 ) 2 Derivatives( 2-b )
[0040] take compound 1 (416mg, 0.4mmol), di-n-butylamine (101μl, 0.6mmol) was dissolved in 5ml of methanol, after heating to 60°C, sodium borohydride (23mg, 1.5mmol) was added, and after constant temperature reaction for 8h, the system was concentrated, Add 20ml of water to dissolve the residue, then adjust the pH with aqueous sodium hydroxide solution until no precipitation occurs, then filter with suction, dry and weigh the filter cake to obtain the compound 2-b (320mg), yield 70.08%, off-white solid.
Embodiment 3
[0041] Embodiment 3: Preparation formula 2 Shown-NR 1 R 2 =-NC 5 h 10 (tetrahydropyrrolyl) derivatives ( 2-d )
[0042] take compound 1 (416mg, 0.4mmol), tetrahydropyrrole (50μl, 0.6mmol) was dissolved in 5ml ethanol, after heating to 60°C, formic acid (31μl, 1.5mmol) was added, after constant temperature reaction for 8h, the system was concentrated, and 20ml of water was added Dissolve the residue, then adjust the pH with aqueous sodium hydroxide solution until no precipitation occurs, then filter with suction, dry and weigh the filter cake to obtain the compound 2-d (300mg), yield 69.22%, off-white solid.
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