http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-110156823-A

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filingDate 2019-06-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ac70ece64c3a415ea7fbd3a7876a1e13
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publicationDate 2019-08-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-110156823-A
titleOfInvention A kind of nontoxic methotrexate prodrug and preparation method thereof
abstract The invention discloses a nontoxic methotrexate prodrug and a preparation method thereof, comprising the following two steps: (a) using 4-(hydroxymethyl) phenylboronic acid pinacol ester and p-nitrophenoxyformyl chloride As a raw material, it is dissolved in an organic solvent, and the reaction is fully stirred at 0 °C to synthesize an active small molecule that can be reversibly combined with methotrexate; (b) the active small molecule synthesized in the previous step, methotrexate and Triethylamine is dissolved in an organic solvent and fully reacted at room temperature and in the dark to prepare a methotrexate prodrug. The methotrexate prodrug prepared by the present invention itself has no toxicity, but can be decomposed to generate methotrexate under the action of reactive oxygen species (ROS), and exert its effect on the lesion site. The methotrexate prodrug prepared by the invention can be used for the treatment of diseases with a microenvironment rich in ROS such as tumors, which can not only have a therapeutic effect, but also avoid the toxic and side effects caused by the use of methotrexate, and has a very ideal disease treatment effect.
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Total number of triples: 42.