Solid-phase synthesis of Eptifibatide in a multifunctional reactor

doi:10.3724/SP.J.1095.2012.00228

Chinese Journal of Applied Chemistry

• Full Papers • Previous Articles Next Articles

Solid-phase synthesis of Eptifibatide in a multifunctional reactor

SHENG Zecui¹, ZHOU Cheng¹, ZHANG Lingzhi³, ZHU Liangliang¹, JIANG Bo¹,
CHEN Yingwen¹, ZHU Shemin², SHEN Shubao^1*

(1.College of Biotechnology and Pharmaceutical Engineering,Nanjing University of Technology,Nanjing 210009;
2.College of Material Science and Engineering,Nanjing University of Technology,Nanjing;
3.Chemistry and Chemical Engineering Department,Xuzhou Normal University,Xuzhou)

Received:2011-05-26 Revised:2011-07-12 Published:2012-03-10 Online:2012-03-10

Abstract

Abstract: A home-made reactor possessing functions including reaction, blending, bubbling, protecting with N2 and filtration was fabricated. The effects of the type of resin, solvent, coupling reagent and reaction time on the yield of cyclic eptifibatide were investigated. The results showed the overall yield was up to 86.6%, using Rink Amide AM resin as solid supporter, HBTU/HOBt/DIEA as the coupling reagent, DMF as the solvent and reaction 2 hours in the reactor. The purity of the product as revealed by HPLC could reach 98%.

Key words: Eptifibatide, Solid-phase synthesis reactor, Fmoc method

CLC Number:

O621.3

SHENG Zecui1, ZHOU Cheng1, ZHANG Lingzhi3, ZHU Liangliang1, JIANG Bo1, CHEN Yingwen1, ZHU Shemin2, SHEN Shubao1*. Solid-phase synthesis of Eptifibatide in a multifunctional reactor[J]. Chinese Journal of Applied Chemistry, DOI: 10.3724/SP.J.1095.2012.00228.

[1]	YAO Yuanyong1,2, WU Lanyan1, SHU Hua1, TANG Bangcheng1, XUE Wei2. Synthesis of α-Aminophosphonates by Bronsted Acid Catalysis [J]. Chinese Journal of Applied Chemistry, 2014, 31(12): 1428-1433.
[2]	ZHOU Weijie, SUN Xiaoqiang, XI Haitao*. Synthesis and Fluorescence Properties of Hyaluronic Acid Derivatives Containing Fluorinated Coumarin [J]. Chinese Journal of Applied Chemistry, 2014, 31(08): 916-921.
[3]	YIN Zhigang*, GUO Haiyan, QIAN Hengyu, ZHANG Tongyan, QIN Jinwan, ZHANG Yingjun. Synthesis and Application of a Special Colorant Used in Preparing Yellow Polyurethane Elastic Membrane [J]. Chinese Journal of Applied Chemistry, 2014, 31(08): 901-910.
[4]	ZENG Wei, CHEN Fuxue*. Recent Advances in Radical Trifluoromethylation Reactions [J]. Chinese Journal of Applied Chemistry, 2014, 31(06): 627-641.
[5]	XIAO Liwei*, KONG jie, ZHOU Qiuxiang, HU Yueli. One Pot Synthesis of β-Amino Ketone Derivatives Catalyzed by Polystyrene-supported Ferric Chloride [J]. Chinese Journal of Applied Chemistry, 2014, 31(06): 715-720.
[6]	KE Fang1*, WU Wen2, LI Peng1, LIN Chen1. Microwave-assisted Synthesis of Benzothiazole Derivatives in Aqueous Solution [J]. Chinese Journal of Applied Chemistry, 2014, 31(06): 721-725.
[7]	FENG Cuilan*, XU Haiyun, LIU Lantao, WANG Jing, LIU Ying. Catalytic Synthesis of Diaryl Ethers with Magnetically Recoverable Fe₃O₄ Nanoparticles Under Solvent-free and Ligand-free Conditions [J]. Chinese Journal of Applied Chemistry, 2014, 31(05): 536-540.
[8]	ZHAO Xuejing, ZHU Jie, LU Ming*. Improvement of the Oxidation Process in the Synthesis of 2,6-Diamino-3,5-dinitropyrazine-1-oxide [J]. Chinese Journal of Applied Chemistry, 2014, 31(01): 41-49.
[9]	DUAN Zhifang, LI Chongbi*, WU Xufang, CHEN Gang. Solid Phase Grinding Synthesis and Plant Growth Activities of Arylureido-acylthiourea Derivatives [J]. Chinese Journal of Applied Chemistry, 2013, 30(12): 1429-1433.
[10]	LI Yanqin1*, YU Fengli2, ZHUANG Shengli1. Improved Synthetic Method and Characterization of Emedastine Difumarate [J]. Chinese Journal of Applied Chemistry, 2013, 30(11): 1285-1288.
[11]	ZHANG Feng1, FANG Zheng1, LI Xiaolin1, HE Wei1, YUAN Aibang2, GUO Kai2*. Applications of Ugi Reaction to the Synthesis of Natural Products [J]. Chinese Journal of Applied Chemistry, 2013, 30(11): 1237-1249.
[12]	GUO Wenyan1,2, CHEN Jianxin1*. A New Method for Synthesizing α-Aminoamide Compounds [J]. Chinese Journal of Applied Chemistry, 2013, 30(10): 1114-1119.
[13]	WANG Chaolei, WANG Zeqing, MA Tingli*. Synthesis of Porphyrin Dyes with Electron Donate-withdraw Structure and Their Applications in Dye-sensitized Solar Cells [J]. Chinese Journal of Applied Chemistry, 2013, 30(07): 757-763.
[14]	SHI Dongxin, CHEN Jiaojiao*, DU Xianli, WANG Lele, JIANG Yi, REN Rongrong. Synthesis of Chiral Functional Monomers Containing L-Amino Acid Groups and Their Copolymers with N-isopropylacrylamide [J]. Chinese Journal of Applied Chemistry, 2013, 30(07): 740-744.
[15]	WANG Weidong1,4*, SUN Guofu2, SHI Zhengchun3,4, SHIMO Tetsuro4. Photosynthesis of Two Oxa Macrocyclic Compounds [J]. Chinese Journal of Applied Chemistry, 2013, 30(04): 378-382.

Solid-phase synthesis of Eptifibatide in a multifunctional reactor

PDF

Knowledge

Abstract

Cite this article

share this article

References

Related Articles 15

Recommended Articles

Metrics

Comments