33208-99-0Relevant articles and documents
Amino acid amide hydrochloride without inorganic ammonium salt and synthesis method thereof
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Paragraph 0036-0042, (2022/01/10)
The present invention discloses an amino acidamide hydrochloride without inorganic ammonium salts and a synthesis method thereof, comprising the following steps: S1, the amino acid under alkaline conditions, added di-tert-butyl dicarbonate to prepare tert-butoxycarbonyl - amino acid; S2, to the prepared tert-butoxycarbonyl - amino acid and then add di-tert-butyl dicarbonate, in the presence of N- methyl morpholine, ammonium bicarbonate, the preparation of tert-butoxycarbonyl - amino acid amide; S3, the tert-butoxycarbonyl - amino acid amide placed in the ethyl acetate / hydrogen chloride solution system, Crystallization is obtained immediately. The present invention is twice added di-tert-butyl dicarbonate, prepared under different conditions to give a high purity tert-butoxycarbonyl - amino acid amide, and finally in the ethyl acetate / hydrogen chloride solution conditions to obtain the final product, the present invention solves the problem of inorganic ammonium salts in the production of amino acid amide hydrochloride difficult to separate, reducing the amount of organic solvent.
Biosynthesis method and application of N-methyl-o-carborane-L-propionamide
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Paragraph 0010; 0022-0027, (2021/04/17)
The invention discloses a biosynthesis method of N-methyl-o-carborane-L-propionamide, which comprises the following steps: 1, synthesizing L-propionamide by using D,L-alanine and ammonia water as raw materials and laccase as a catalyst, filtering the reaction product to remove the laccase, and introducing hydrogen chloride gas to generate L-propionamide hydrochloride; 2, in an organic solvent or ionic liquid, reacting with 1-bromomethyl-o-carborane under an alkaline condition to obtain the corresponding o-carborane derivative. According to the invention, through the degradation characteristics of laccase on amines and alcohols, it is accidentally found that laccase has the function of synthesizing the L-propylamine amide, and has the characteristics of high yield, safety, no pollution and the like. Therefore, by chemically synthesizing and modifying o-carborane and a relatively hydrophilic group L-propionamide, the purpose of increasing the polarity and cell affinity of the compound is achieved, so that the technical effect of targeted enrichment and high concentration of boron ions in tumor cells is achieved.
BICYCLIC COMPOUNDS
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Paragraph 00727, (2020/06/01)
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
Method for preparing L-alaninamide hydrochloride
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Paragraph 0015-0017, (2018/06/04)
The invention relates to a method for preparing L-alaninamide hydrochloride. The method comprises the following specific steps: A. dissolving L-alanine in methanol and adding an appropriate amount ofchloride catalyst to undergo an esterification reaction; B. introducing an ammonia gas into the esterified product to undergo an aminolysis reaction; C. heating a reaction solution after aminolysis invacuum to remove ammonia, and then filtering out ammonium chloride; D. acidifying the filtered reaction solution to adjust the pH, and then adding an appropriate amount of ketone to precipitate a crystal, namely, L-alaninamide hydrochloride. The method for preparing the L-alaninamide hydrochloride provided by the invention has a simple route and relatively low cost, and is suitable for mass production.
Thermodynamic and Structural Investigation of Synthetic Actinide-Peptide Scaffolds
Safi, Samir,Jeanson, Aurélie,Roques, Jérome,Solari, Pier Lorenzo,Charnay-Pouget, Florence,Den Auwer, Christophe,Creff, Ga?lle,Aitken, David J.,Simoni, Eric
supporting information, p. 877 - 886 (2016/02/03)
The complexation of uranium and europium, in oxidation states +VI and +III, respectively, was investigated with pertinent bio-inorganic systems. Three aspartate-rich pentapeptides with different structural properties were selected for study to rationalize the structure-affinity relationships. Thermodynamic results, crosschecked by both isothermal titration calorimetry and time-resolved laser fluorescence spectroscopy, showed different affinity depending on the peptide for both Eu(III) and U(VI). The thermodynamic aspects were correlated to structural predictions, which were acquired by density functional theory quantum chemical calculations and from IR and extended X-ray absorption fine structure experiments. The combination of these microscopic properties revealed that carbonyl-metal interactions affected the entropy in the case of europium, while the larger uranyl cation was mostly affected by preorganization and steric effects, so that the affinity was enhanced through enthalpy. The approach described here revealed various microscopic aspects governing peptide actinide affinity. Highlighting these mechanisms should certainly contribute to the rational synthesis of higher affinity biomimetic aspartic ligands.
Synthesis of α-amino dithioesters and endothiodipeptides
Hartke, Klaus,Barrmeyer, Stephan
, p. 251 - 256 (2007/10/03)
The α-amino ester hydrochlorides (1) are converted into N-protected α-amino amides (3), α-amino thioamides (4) and α-amino dithiomethylesters (5). Condensation of 5 with the alkali salts of α-amino acids gives rise to the endothiodipeptide alkali salts (7). Johann Ambrosius Barth 1996.
