Method for producing arbekacin through one-pot process continuous flow

• Main Authors: CHANG BAOLEI, YANG QINGKUN, LI DECAI, WU KE, CHEN ZHONGNAN, ZHOU XIANGUO
• Format: Patent
• Language: Chinese; English
• Published: 04.07.2017
• Subjects: CHEMISTRY; DERIVATIVES THEREOF; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; SUGARS

The invention provides a method for producing arbekacin through one-pot process continuous flow. The method is characterized in that a silanization product of dibekacin and active thioester undergo a reaction in a microreactor as initial raw materials. The combination of the active thioester and the advantage of the high selectivity of a microchannel reactor reduces a hydrazine hydrolysis process, improves the selectivity of the reaction, improves the product conversion rate to 70% or above, greatly reduces the difficulty of subsequent purification and separation and reduces the discharge of waste liquids and waste residues. The method for producing arbekacin through continuous flow technology one-pot process well solves the problems of tedious operation, long technologic process, much labor and large waste liquid discharge volume in traditional multi-step chemical synthesis. 本发明提供了锅法连续流生产阿贝卡星的方法。该方法以地贝卡星的硅烷化物和活性硫酯为起始原料在微反应器中进行反应。本发明采用活性硫酯结合微通道反应器高选择性的优势，不仅减少了步肼解工序，而且还提高了反应的选择性，产品转化率提高至70％以上，极大地降低了后续纯化分离的难度，减