Synthesis method of 2, 5-disubstituted piperazine derivative

The invention relates to the field of chemical synthesis, and particularly discloses a synthesis method of a 2, 5-disubstituted piperazine derivative. The 2, 5-disubstituted piperazine derivative is shown as a formula I: # imgabs0. The preparation method comprises the following steps: reacting an in...

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Bibliographische Detailangaben
Hauptverfasser: SHUAI BAOKUI, KANG KANG, LI ZHANSHAN, NIU BOBO, SHAN YUQING
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to the field of chemical synthesis, and particularly discloses a synthesis method of a 2, 5-disubstituted piperazine derivative. The 2, 5-disubstituted piperazine derivative is shown as a formula I: # imgabs0. The preparation method comprises the following steps: reacting an initial raw material a with a sulfonyl protective reagent to generate an intermediate b; carrying out substitution reaction on the intermediate b and a raw material c under an alkaline condition to generate an intermediate d; reacting the intermediate d with an amino protection reagent to generate an intermediate e; the intermediate e is subjected to a Mitsunobu reaction under the action of triphenylphosphine and diethyl azodicarboxylate, and a compound I is generated. The invention develops a method for increasing a carbon chain, chiral amino alcohol with protected alcoholic hydroxyl group and amino group reacts with another molecule of chiral amino alcohol, the reaction condition is mild, new impurities are not int