Synthetic method of poly-substituted dimethyl amino phenyl acetic acid compound
The invention relates to a synthesis method of a poly-substituted dimethyl amino phenyl acetic acid compound. The synthesis method comprises the following steps: carrying out methyl esterification reaction on a compound shown in a formula I to obtain a co
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Paragraph 0129-0134
(2021/03/05)
Isotope derivatization reagent for labeling amino/phenolic hydroxyl and synthesis method thereof
The invention provides an isotope derivatization reagent for labeling amino/phenolic hydroxyl and a synthesis method thereof and belongs to the field of chemical synthesis. A homologous compound of p-aminophenylacetic acid containing amino, a benzene ring and carboxyl in a structure or a homologous compound of 4-(2-aminoethyl)benzoic acid is used as a raw material; and the amino is dimethylated and then the carboxyl in the product is subjected to esterification by adopting N-hydroxysuccinimide to obtain the isotope derivatization reagent. The isotope derivatization reagent has structure characteristics that one part of the isotope derivatization reagent is succinimidyl ester and the other part of the isotope derivatization reagent is dimethyl substituted tertiary amino; the succinimidyl ester is connected to dimethylamino through a carbon chain and a benzene ring; and the number of carbon atoms on the benzene ring and the carbon chain which is connected to the amino is 0 to 6. According to the isotope derivatization reagent provided by the invention, different D substituted or C substituted formaldehyde, or H or D substituted sodium cyanoborohydride are selected and a reactionroute is adjusted to obtain a series of isotope labeled reagents which can efficiently react with amino or phenolic hydroxyl and have different isotope substitutions. A starting raw material is changed, and the isotope labeled reagents with similar functions can be prepared through the method.
Effect of deuterated solvents toward 2,2,2-trichloroethyl esters with a benzylic methylene moiety
The indium-promoted chemoselective deprotection of 2,2,2-trichloroethyl esters containing a benzylic methylene was successfully achieved by employing deuterated solvents.