Synthesis of sulfomycin derivant
The present invention discloses a method for synthesizing a thienamycin derivative, which uses (3S, 4R)-3-[(1R)-1-(t-butyldilnethylsilyloxy)ethyl]-4-{2-[2-(Boc-amino)ethylsuleenyl]carboxyethyl}-2-azetidinone as a starting material and the commercialized triethyl phosphite as Wittig reagent and adopt...
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Main Authors | , , , |
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Format | Patent |
Language | Chinese English |
Published |
18.02.2009
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Subjects | |
Online Access | Get full text |
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Summary: | The present invention discloses a method for synthesizing a thienamycin derivative, which uses (3S, 4R)-3-[(1R)-1-(t-butyldilnethylsilyloxy)ethyl]-4-{2-[2-(Boc-amino)ethylsuleenyl]carboxyethyl}-2-azetidinone as a starting material and the commercialized triethyl phosphite as Wittig reagent and adopts two steps of reactions (acylation reaction and intramolecular Wittig reaction) to synthesize the thienamycin derivative; because the Wittig reagent does not need to be synthesized independently, the synthesization steps can be simplified, and the reaction cost can be reduced; and the starting material can be prepared from the commercialized (3S, 4R)-3-[(1R)-1-(t-butyldilnethylsilyloxy)ethyl]-4-acetoxy-2-azetidinone by three steps of reactions (allylation reaction, oxidation reaction and esterification reaction). The synthesis method has the advantages of short route, mild reaction conditions, ready availability of materials and low cost, and the obtained thienamycin derivative, which can be used as a midbody, is |
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Bibliography: | Application Number: CN20081232808 |