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    • 5. 发明申请
    • PROCESS FOR THE PREPARATION OF FONDAPARINUX
    • FONDAPARINUX的制备方法
    • WO2013011459A1
    • 2013-01-24
    • PCT/IB2012/053649
    • 2012-07-17
    • RANBAXY LABORATORIES LIMITEDPANDYA, BhargavNAGARAJU, P.
    • PANDYA, BhargavNAGARAJU, P.
    • C07H7/033
    • C07H7/033
    • The present invention relates to process for preparation of O-(2,3-Di-O-benzyl- β -D-glucopyranuronicacid)-(1→4)-3-O-acetyl-1,6-anhydro-2-azido-2-deoxy- β -D-glucopyranose represented by Formula (II) comprising oxidation of O-(2,3-Di-O-benzyl- β -D-glucopyranosyl)-(1→4)-3-O-acetyl-1,6-anhydro-2-azido-2-deoxy- β -D-glucopyranose represented by Formula (I) with N-bromosuccinamide (NBS), bisacetoxy iodobenzene (iodobenzene diacetate) or mixture thereof, optionally in presence of 2,2,6,6-tetramethylpiperidine-1-oxyl (hereinafter referred as TEMPO). The process of the invention are useful for the production of fondaparinux sodium, a heparin and blood clotting factor Xa inhibitor.
    • 本发明涉及制备O-(2,3-二-O-苄基-β-D-吡喃葡萄糖醛酸) - (1→4)-3-O-乙酰基-1,6-脱水-2-叠氮基 由式(II)表示的包含O-(2,3-二-O-苄基-β-D-吡喃葡萄糖基) - (1→4)-3-O-乙酰基的氧化的2-脱氧-β-D-吡喃葡萄糖 由式(I)代表的具有N-溴代琥珀酰胺(NBS),双乙酰氧基碘苯(二乙酸碘苯)或其混合物的-1,6-脱水-2-叠氮基-2-脱氧-β-D-吡喃葡萄糖, 2,6,6-四甲基哌啶-1-氧基(以下称TEMPO)。 本发明的方法可用于生产磺达肝素钠,肝素和凝血因子Xa抑制剂。