O-carborane derivative for assisting BNCT and synthesis method thereof

The invention belongs to the technical field of organic synthesis, and discloses an o-carborane derivative capable of being used for assisting BNCT and a synthesis method of the o-carborane derivative. The preparation method comprises the following steps: reacting 1, 4-amino-3-phenyl butyric acid hy...

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Bibliographische Detailangaben
Hauptverfasser: ZHANG HONGDUO, WANG WEN, JIN CHENGFU, JIN TAO, LI XIANLUO, JIN FENG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention belongs to the technical field of organic synthesis, and discloses an o-carborane derivative capable of being used for assisting BNCT and a synthesis method of the o-carborane derivative. The preparation method comprises the following steps: reacting 1, 4-amino-3-phenyl butyric acid hydrochloride or 2-hydroxy-3-phenyl propiophenone with 1-bromomethyl o-carborane in an organic solventor ionic liquid under an alkaline condition to obtain the corresponding o-carborane derivative; or taking 2, 2, 2-dibromoacetophenone as an initial product, reacting with piperazine to generate 2, 2-dipiperazinyl acetophenone, and then reacting with 1-bromomethyl o-carborane in an organic solvent or ionic liquid under an alkaline condition to obtain the corresponding o-carborane derivative. Fluorine ions and relative hydrophilic groups are introduced through chemical synthesis for modification, the purpose of increasing the polarity and cell affinity of the compound is achieved, and thereforethe technical effect that