663921-15-1Relevant articles and documents
Direct 3-Acylation of Indolizines by Carboxylic Acids for the Practical Synthesis of Red Light-Releasable Caged Carboxylic Acids
Watanabe, Kenji,Terao, Nodoka,Niwa, Takashi,Hosoya, Takamitsu
, p. 11822 - 11834 (2021/07/31)
To enhance the practicality of photouncaging system using 3-acyl-2-methoxyindolizines, direct acylation of indolizines with carboxylic acids was developed using condensation reagents, generally used for peptide coupling. This method allowed for caging a broad range of carboxylic acids with indolizines. The method enabled a facile synthesis of water-soluble caged bioactive carboxylic acids having an intramolecular photosensitizer. The efficient release of carboxylic acids from the synthesized caged compounds upon red light irradiation was confirmed in neutral buffered solutions.
Dar2 polypeptide radioactive drug and preparation method thereof
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Paragraph 0054; 0058, (2020/06/20)
The invention discloses a Dar2 polypeptide radioactive drug and a preparation method thereof. The drug comprises a Dar polypeptide dimer and a radioactive nuclide, wherein the radioactive nuclide canmark the Dar polypeptide dimer through a bifunctional chelating agent; the Dar polypeptide dimer is a polypeptide dimer which is synthesized through the steps of enabling GGG to be connected with twoDar polypeptide monomers and performing dimerization on the two Dar polypeptide monomers connected to the GGG; and each Dar polypeptide monomer is D type amino acid linear heptatomic polypeptide, andthe sequence is anedywr. According to the drug disclosed by the invention, the radioactive nuclide is marked on Dar polypeptide dimer molecules through the bifunctional chelating agent, the in vivo marked drug is concentrated to tumor positions through the targeting effects of Dar polypeptide, and through a single-photon emission computed tomography (SPECT) technique or a positron emission computed tomography (PET) technique of nuclear medicine, tomography diagnosis is performed on integrin alpha 6 positive tumor.
Preparation method of amino polyethylene glycol propionic acid
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, (2019/01/14)
The invention relates to the field of organic synthesis, in particular to a preparation method of amino polyethylene glycol propionic acid. The preparation method comprises the steps that catalytic hydrogenation is carried out on dibenzyl amino polyethylene glycol tert-butyl propionate shown in formula I-2 to obtain amino polyethylene glycol tert-butyl propionate shown in formula I-3; (2) the amino polyethylene glycol tert-butyl propionate shown in formula I-3 is hydrolyzed under the acidic condition to obtain amino polyethylene glycol propionic acid shown in formula I. The preparation methodof the amino polyethylene glycol propionic acid has the advantages that the defects in the prior art that the yield is low, the dangerousness is high, and the enlargement of production is difficult are overcome, the reaction conditions are mild, the operation is simple, an intermediate does not to be purified, the next reaction can be directly carried out, the whole yield reaches up to 87-92%, thepurity of end products reaches up to 97-99.5%, and a safe and efficient synthetic route is provided for the preparation of amino polyethylene glycol propionic acid.