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Method for synthesizing fluorenylmethoxycarbonyl-2,3-dehydrovaline
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Paragraph 0009, (2019/08/07)
The invention relates to a method for synthesizing fluorenylmethoxycarbonyl-2,3-dehydrovaline. The method mainly solves the technical problem of lack of effective synthesis methods. The synthesis method includes the following steps: reacting Boc-alpha-phosphonomethylglycine trimethyl ester with acetone in a dichloromethane solution under the catalysis of DBU through an HWE to generate a compound 1; heating and hydrolyzing the compound 1 and sodium hydroxide in a mixed solution of methanol and water to generate a compound 2; removing, by the compound 2, a protecting group in the dichloromethanesolution of trifluoroacetic acid to generate a compound 3; and reacting the compound 3, 9-fluorenylmethyl-N-succinimidyl carbonate with sodium bicarbonate in a mixed solution of tetrahydrofuran and water to generate a target compound 4. The fluorenylmethoxycarbonyl-2,3-dehydrovaline, as an amino acid derivative, is mainly used as a pharmaceutical intermediate and in the synthesis of polypeptidesand the like.
