- Synthesis method of (S)-2, 6-diamino-5-oxohexanoic acid
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The invention relates to a synthetic method of (S)-2, 6-diamino-5-oxohexanoic acid. The method mainly solves the technical problem of large-scale production of (S)-2, 6-diamino-5-oxohexanoic acid. The synthesis method comprises the following steps: reacting L-2-amino adipic acid with 9-fluorenylmethyl-N-succinimido carbonate in a mixed solution of water and acetone to generate a compound 1; under the catalysis of p-toluenesulfonic acid, reacting the compound 1 with paraformaldehyde in a toluene solution to generate a compound 2; reacting the compound 2 with di-tert-butyl dicarbonate, pyridine and ammonium carbonate in an ethyl acetate solution at room temperature to generate a compound 3; and reacting the compound 3 with lithium hydroxide in a mixed solution of ethanol and water to generate a target compound 4. As a derivative of (S)-2-amino adipic acid, (S)-2, 6-diamino-5-oxo hexanoic acid has become an important intermediate for the synthesis of alpha-amino adipic acid peptide.
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Paragraph 0008
(2021/04/14)
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- Synthetic method of terminal carboxylic acid
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The invention discloses a synthetic method of a terminal carboxylic acid. The synthetic method is characterized by comprising the steps of adding an olefin represented by a formula (3) shown in the description, formic acid, acetic anhydride, Pd(OAc)2 and a monophosphorus ligand TFPP into an organic solvent in a proportion, carrying out hydrogen carbonylation reaction on the olefin represented by the formula (3) shown in the description, formic acid and acetic anhydride at 80-90 DEG C for 48h-72h under the catalysis of the metal palladium salt Pd(OAc)2 and the monophosphorus ligand TFPP so as to obtain the terminal carboxylic acid represented by a formula shown in the description, and separating a target product, namely the terminal carboxylic acid after the reaction is finished, wherein olefin represented by the formula (3) is selected from cycloolefins, or linear olefins of which the R1 is electron donating groups. By virtue of the method disclosed by the invention, corresponding terminal carboxylic acid and a derivative thereof can be prepared through the reaction under mild conditions of low temperature and no high pressure; and the steps of the synthetic method are simple and convenient, the operation is convenient, the yield is high, the energy source can be greatly saved, and the synthetic efficiency can be greatly improved.
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Paragraph 0159-0162
(2019/11/21)
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- Pd-Catalyzed Highly Chemo- And Regioselective Hydrocarboxylation of Terminal Alkyl Olefins with Formic Acid
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An efficient Pd-catalyzed hydrocarboxylation of alkenes with HCOOH is described. A wide variety of linear carboxylic acids bearing various functional groups can be obtained with excellent chemo- and regioselectivities under mild reaction conditions. The reaction process is operationally simple and requires no handling of toxic CO.
- Ren, Wenlong,Chu, Jianxiao,Sun, Fei,Shi, Yian
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supporting information
p. 5967 - 5970
(2019/08/26)
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