A Cost-Effective Method to Prepare Pure Vildagliptin

被引：4
作者：
Peng, Jun [1 ]
Feng, Yue [1 ]
Tao, Zhu [1 ]
Chen, Yingjie [1 ]
Hu, Xiangnan [1 ]
机构：
[1] Chongqing Med Univ, Dept Pharm, Chongqing 400016, Peoples R China
来源：
LETTERS IN ORGANIC CHEMISTRY | 2013年 / 10卷 / 03期
关键词：
Vildagliptin; cost-effective; TCT; DIPEPTIDYL PEPTIDASE-IV; GLUCAGON-LIKE PEPTIDE-1; INHIBITOR; POTENT;
D O I：
10.2174/1570178611310030003
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A cost-effective synthetic approach to prepare vildagliptin under gentle experimental conditions has been reported with good yield and high purity. It was initiated with L-proline via successful reaction with chloroacetyl chloride in THF (Tetrahydrofuran) to give the 1-(2-chloroacetyl)-pyrrolidine-2-carboxylic acid, which was then treated by TCT (2, 4, 6-trichloro-1, 3, 5-triazine) in DCM (dichloromethane), and converted into 1-(2-chloroacetyl)-pyrrolidine-2-carboxamide, then further converted into 1-(2-chloroacetyl)-pyrrolidine-2-carbonitrile after dehydrated by TCT in DMF (N, N-dimethylformamide), the latter product was reacted with 3-aminoadamantanol to get vildagliptin. The total yield of vildagliptin was about 48%, the purity was about 99%.
引用
收藏
页码：159 / 163
页数：5
相关论文
共 50 条
  • [31] Electrostatic repellent dispersion method for green and cost-effective aqueous radiative cooling paint
    Fei, Jipeng
    Han, Di
    Zhou, Kai
    Koh, See Wee
    Ge, Junyu
    Tan, Jun Yan
    Ng, Bing Feng
    Chen, Zhong
    Cai, Lili
    Li, Hong
    BUILDING AND ENVIRONMENT, 2025, 269
  • [32] Measuring mental health in a cost-effective manner
    Harpham, T
    Reichenheim, M
    Oser, R
    Thomas, E
    Hamid, N
    Jaswal, S
    Ludermir, A
    Aidoo, M
    HEALTH POLICY AND PLANNING, 2003, 18 (03) : 344 - 349
  • [33] A Cost-Effective Recommender System for Taxi Drivers
    Qu, Meng
    Zhu, Hengshu
    Liu, Junming
    Liu, Guannan
    Xiong, Hui
    PROCEEDINGS OF THE 20TH ACM SIGKDD INTERNATIONAL CONFERENCE ON KNOWLEDGE DISCOVERY AND DATA MINING (KDD'14), 2014, : 45 - 54
  • [34] Which method of distal pancreatectomy is cost-effective among open, laparoscopic, or robotic surgery?
    Rodriguez, Maylis
    Memeo, Riccardo
    Leon, Piera
    Panaro, Fabrizio
    Tzedakis, Stylianos
    Perotto, Ornella
    Varatharajah, Sharmini
    de'Angelis, Nicola
    Riva, Pietro
    Mutter, Didier
    Navarro, Francis
    Marescaux, Jacques
    Pessaux, Patrick
    HEPATOBILIARY SURGERY AND NUTRITION, 2018, 7 (05) : 345 - 352
  • [35] A Facile and Cost-Effective Method to Prepare Biodegradable Poly(ester urethane)s with Ordered Aliphatic Hard-Segments for Promising Medical Application as Long-Term Implants
    Bi, Jingjing
    Liu, Yifan
    Liu, Jiaxu
    POLYMERS, 2022, 14 (09)
  • [36] Method Towards Service Composition Optimization on Cost-effective using Mixed Flower Pollination Algorithm
    Wu, Jiakai
    Tan, Wenan
    PROCEEDINGS OF THE 2021 IEEE 24TH INTERNATIONAL CONFERENCE ON COMPUTER SUPPORTED COOPERATIVE WORK IN DESIGN (CSCWD), 2021, : 37 - 42
  • [37] An environmentally friendly and cost-effective method to fabricate superhydrophobic PU sponge for oil/water separation
    Zhang, Jichao
    Liu, Xin
    Chen, Faze
    Liu, Jiyu
    Chen, Yang
    Zhang, Fan
    Guan, Naiqiao
    JOURNAL OF DISPERSION SCIENCE AND TECHNOLOGY, 2020, 41 (08) : 1136 - 1144
  • [38] Multiple Sclerosis: Systemic Challenges to Cost-Effective Care
    Weinstein, David R.
    Owens, Gary M.
    Gandhi, Ankit
    AMERICAN HEALTH AND DRUG BENEFITS, 2022, 15 (01) : 13 - 20
  • [39] Cost-Effective, Integrated In Vitro Phantoms for Cardiac MRI
    Chikop S.A.
    Konar A.S.
    Reddy N.S.L.
    Vajuvalli N.
    Keelara D.S.
    Kumnoor A.
    Raghuraman S.
    Venkatesan R.
    Geethanath S.
    Critical Reviews in Biomedical Engineering, 2021, 49 (03) : 7 - 16
  • [40] Cost-Effective Hearing Conservation: Regulatory and Research Priorities
    Dobie, Robert A.
    EAR AND HEARING, 2018, 39 (04) : 621 - 630
12345