1-(tert-ブトキシカルボニル)ピペラジン

外観

白色～うすい黄色～うすい黄赤色粉末～結晶

溶解性

水、エタノール及びアセトンに溶ける。

用途

有機合成原料。

用途

医薬中間体.

化学的特性

Waxy Solid

使用

1-Boc-piperazine undergoes Buchwald-Hartwig amination with various aryl halides to form corresponding amine derivatives. It can be used to synthesize monosubstituted piperazine intermediates of many bioactive molecules and piperazine containing drug substances, such as trazodone.

主な応用

Tert-Butyl 1-piperazinecarboxylate, also known as Olaparib Impurity 7, is an impurity of Olaparib. Olaparib is used alone or in combination with bevacizumab (Avastin) to help maintain the response of certain types of ovarian (female reproductive organs where eggs are formed), fallopian tube (tube that transports eggs released by the ovaries to the uterus), and peritoneal (layer of tissue that lines the abdomen) cancer in people who have completely responded or partially responded to their first or later chemotherapy treatments. Olaparib is also used to treat certain types of breast cancer that has spread to other parts of the body and has not improved or has worsened after treatment with other therapies. It is also used to treat certain types of early breast cancer in people who have already been treated with other chemotherapy treatments.

一般的な説明

1-Boc-piperazine is an N-Boc protected piperazine. Crosscoupling of 1-Boc-piperazine with aryl iodides using CuBr/1,1′-bi-2-naphthol (catalyst) and K₃PO₄ (base) has been reported. 1-Boc-piperazine undergoes Buchwald-Hartwig coupling reactions with aryl halides. 1-Boc-piperazine can be prepared in 80% yield via solvent-free N-Boc protection catalyzed by iodine.