主办:上海医药工业研究院
   中国药学会
   中国化学制药工业协会
ISSN 1001-8255   CN 31-1243/R   ZYGZEA

Archive

  • 2016 Volume 47 Issue 03
    Published: 10 March 2016
      

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  • YANG Zunhua1, LI Xiang2, HUANG Hesong2, LI Min1, FANG Yuanying2*
    Abstract ( )   Knowledge map   Save
    Isobutyronitrile and hydroxylamine hydrochloride were used as starting materials to synthesize [1-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-4-yl]methyl methanesulfonate(5) via condensation, cyclization, substitution and mesylation. 6-[4-(Methylsulfonyl)phenyl]pyridin-3-ol(8) was prepared from 2-bromo-5-
    hydroxypyridine by benzylation, Suzuki reaction and debenzylation. GSK-1292263, a GPR119 agonist, was synthesized from 5 and 8 by condensation in the presence of potassium carbonate with an overall yield of 40.6% based on 2-bromo-5- hydroxypyridine.
  • WANG Wuwei, CHEN Jie, HE Jia
    Abstract ( )   Knowledge map   Save
    In the quality study of paliperidone, five related substances were prepared and their structures were confirmed by MS, 1H NMR, and 13C NMR. These substances were paliperidone N-oxide(D), 3-[2-[4-(6- fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-7,8-dihydro-4H-pyrido[1,2-a]pyrimidin-4,9(6H)-
    dione(E), 3-(2-hydroxyethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one(F), 3-[2-[4-[(2,4-difluorophenyl)(hydroxyimino)methyl]piperidin-1-yl]ethyl]-9-hydroxy-2-methyl-6,7,8,9-tetrahydro- 4H-pyrido[1,2-a]pyrimidin-4-one(G), and 3-[2-[4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy-2- methyl-4H-pyrido[1,2-a]pyrimidin-4-one(H).
  • LI Yong, ZHU Tao, FAN Lingling, WANG Jianta, TANG Lei*
    Abstract ( )   Knowledge map   Save
    According to trilostane structure and its synthetic process, three related substances: 17β-hydroxy- 4α,5α-epoxy-androst-2-eno[3,2-c]isoxzole(A), 3,17β-dihydroxy-androst-2,4-diene-2-carbonitrile(B) and 4β,5β-epoxy- 17β-hydroxy-3-oxo-androst-2β-carbonitrile(C) were prepared and confirmed by MS, 1H NMR and 13C NMR. These substances were taken as the references for the quality control of trilostane.