- Synthesis method of double different protected amino acids
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The invention relates to a synthesis method of double different protected amino acids.The technical problems of harsh reaction conditions, inapplicability of production enlarging and the like in an existing synthesis method are mainly solved. According to the technical scheme, the synthesis method of double different protected amino acids comprises the following steps: one of Boc20, Alloc-Cl or Cbz-Osuis added to amino alcohol under the action of an alkaline reagent to obtain a compound 1; the compound 1 reacts with methanesulfonyl chloride or paratoluensulfonyl chloride to obtain an intermediate, then a halide is added into acetone, heating and refluxing are executed to obtain a compound 2; the compound 2 is condensed with diethyl acetamidomalonate under the action of an alkaline agent togenerate a compound 3; the compound 3 is dissolved in alcohol and water, an inorganic base is added, heating, hydrolyzing and decarboxylating are executed to obtain a compound 4; acetylase is added into deionized water to obtain a compound 5 through enzymolysis; amino acid protection is executed, wherein one of Fmoc-Osu, Cbz-OSu, Alloc-Cl or Boc20 is added into thecompound 5 under the action of an alkaline agent to generatea target compound A.
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Paragraph 0014; 0019
(2019/07/04)
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- Allyl side chain protection in peptide synthesis
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A system for the protection of amino acid side-chain functional moieties during peptide synthesis, comprising the use of allyl protecting groups, such as, for example, allyl ether, allyl ester, allyl thioether allyloxycarbonyl and allyloxymethyl groups. The present allyl protecting groups do not exert adverse steric effects on peptide bond condensation, and are fully orthogonal to a variety of popular αN-protecting groups, including Fmoc and tBoc. Moreover, allyl deprotection is mild, and does not result in the formation of reactive carbonium ions. Allyl side-chain protection can be used alone or in conjunction with other types of side-chain protecting groups.
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