42245-42-1Relevant articles and documents
Pentazocine prodrug as well as preparation method and application thereof
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Paragraph 0040; 0056-0057, (2020/07/15)
The invention discloses a pentazocine prodrug shown as a formula (I), a preparation method thereof and medical application of a pharmaceutical preparation containing the pentazocine prodrug, wherein Ris hydrogen or deuterium. The water solubility of the prodrug compound is improved by 20 times or above at room temperature, the prodrug compound is chemically stable, the onset time is delayed, thedrug effect is prolonged, meanwhile, the same parent drug blood concentration is generated at a low dosage, and the prodrug compound has a wide clinical application prospect.
Efficient Preparation of Alkaloids Polycarpine and Polycarpaurines A and C
Guo, Pengbin,Yan, Shuang,Hu, Zeliang,Zhuang, Weihui,Xiong, Yan,Zhang, Lanya,Wang, Ziwen,Wang, Qingmin
, p. 121 - 124 (2017/02/05)
An efficient method for the preparation of alkaloids polycarpine and polycarpaurines A and C via microwave-assisted three-step one-pot reaction as the key step has been developed. This is the first report about the synthesis of polycarpaurines A and C. Starting from commercially available p-methoxybenzaldehyde, polycarpine and polycarpaurine A were obtained over seven steps with 40 and 24 % overall yield, respectively. Polycarpine could convert to polycarpaurine C in 72% yield in the presence of NaHSO3. The structure of polycarpine and polycarpaurines A and C was confirmed by1H NMR,13C NMR, and HRMS.
Bioresolution production of (2R,3S)-Ethyl-3-phenylglycidate for chemoenzymatic synthesis of the taxol C-13 side chain by galactomyces geotrichum ZJUTZQ200, a new epoxide-hydrolase-producing strain
Wei, Chun,Ling, Jinlong,Shen, Honglei,Zhu, Qing
, p. 8067 - 8079 (2014/07/08)
A newly isolated Galactomyces geotrichum ZJUTZQ200 strain containing an epoxide hydrolase was used to resolve racemic ethyl 3-phenylglycidate (rac-EPG) for producing (2R,3S)-ethyl-3-phenylglycidate ((2R,3S)-EPG). G. geotrichum ZJUTZQ200 was verified to be able to afford high enantioselectivity in whole cell catalyzed synthesis of this chiral phenylglycidate synthon. After the optimization of the enzymatic production and bioresolution conditions, (2R,3S)-EPG was afforded with high enantioselectivity (e.e.S > 99%, E > 49) after a 8 h reaction. The co-solvents, pH buffer solutions and substrate/cell ratio were found to have significant influences on the bioresolution properties of G. geotrichum ZJUTZQ200. Based on the bioresolution product (2R,3S)-EPG, taxol's side chain ethyl (2R,3S)-3-benzoylamino-2-hydroxy- 3-phenylpropionate was successfully synthesized by a chemoenzymatic route with high enantioselectivity (e.e.S > 95%).