CAJ | 학술논문

目的：对利托那韦的合成工艺进行优化研究，以获得一条适宜于工业化生产的合成工艺路线。方法使用（2S，3S，5S）－2－胺基－3－羟基－5－（叔丁氧羰基胺基）－1，6－二苯基己烷的丁二酸盐作为起始原料，经过酰胺化、氨基脱保护和再酰胺化三步反应，最终制得目标产物利托那韦。结果经过相应的优化研究之后，最终成功地以较高的收率合成了高纯度的利托那韦产品（总收率57％，纯度＞99％）。结论获得了一条较优的利托那韦合成工艺路线，该工艺路线具有高效、简洁以及绿色等特点，能够满足工业化生产的需要，具有广阔的应用前景。
목적：대리탁나위적합성공예진행우화연구，이획득일조괄의우공업화생산적합성공예로선。방법사용（2S，3S，5S）－2－알기－3－간기－5－（숙정양탄기알기）－1，6－이분기기완적정이산염작위기시원료，경과선알화、안기탈보호화재선알화삼보반응，최종제득목표산물리탁나위。결과경과상응적우화연구지후，최종성공지이교고적수솔합성료고순도적리탁나위산품（총수솔57％，순도＞99％）。결론획득료일조교우적리탁나위합성공예로선，해공예로선구유고효、간길이급록색등특점，능구만족공업화생산적수요，구유엄활적응용전경。
Objective To optimize the synthesis of ritonavir,in order to obtain a suitable synthetic routes for industrial production. Methods Ritonavir was finally synthesized via three steps including amidation,deprotection of amine,amidation from (2S,3S,5S)-2-amino-3-hydroxy-5-(tert-butoxycarbonyl amino)-1,6-diphenyl hexane succinate.Results After the study of optimization,ritonavir was synthesized with high yield and high purity (overall yield 57%,purity >99%).Conclusions An efficient,simple,green synthesis route of ritonavir is available,which makes it suitable for industrial production.