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A kind of synthetic method of fondaparinux sodium intermediate
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A technology for fondaparinux sodium and a synthetic method, which is applied in chemical instruments and methods, preparation of sugar derivatives, sugar derivatives, etc., can solve problems such as high reaction cost and long reaction steps, and achieve simplified synthetic routes and reduced production cost effect
Active Publication Date: 2016-09-07
PHARMA SHANGHAI
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[0009] The synthetic method of above-mentioned technique synthetic reaction cost is high, and reaction step is longer
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Embodiment 1
[0020] The preparation process of compound 6 is:
[0021] Compound 3 (40 g, 0.13 mol) was dissolved in pyridine (240 mL, 2.98 mol), and acetic anhydride (80 ml, 0.85 mol) was added. The reaction solution was stirred at 20°C for 1-3 hours, and concentrated to obtain compound 6 (43 g, 94.5%).
[0022] The reaction equation is: .
Embodiment 2
[0024] The preparation process of compound Monomer C ring is:
[0025] Compound 6 (42.5 g, 0.12 mol) was dissolved in acetonitrile (475 mL) and water (55 ml), cerium ammonium nitrate (166 g, 0.3 mol) was added at 0°C, and the reaction solution was reacted at 20°C for 1-3 Hours, after the reaction was completed, it was filtered, extracted, washed with aqueous sodium bicarbonate solution, dried, concentrated and passed through the column to obtain compound C ring (21.5 g, 78%).
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Abstract
The invention discloses a method for synthesizing an intermediate of fondaparinux sodium, comprising the steps of: taking compound 3 as a raw material, acetylating the hydroxyl group to obtain compound 6, and dep-methoxybenzyl compound 6 with cerium ammonium nitrate (PMB), get the Monomer C ring. Through the above method, the synthesis method of the fondaparinux sodium intermediate of the present invention simplifies the synthesis route of the Monomer C ring compared with the original 5-step synthesis of the Monomer C ring, reduces production costs, and is suitable for large-scale industrial production.
Description
technical field [0001] The invention relates to the field of medicine and chemical industry, in particular to a method for synthesizing 1,6-anhydro-2-azido,3-acetyl-β-D-glucose, an important intermediate of fondaparinux sodium. Background technique [0002] Fondaparinux sodium (Fondaparinux sodium) is the world's first fully chemically synthesized pentosan compound, and the first indirect inhibitor of antithrombin-dependent factor Xa developed and produced by Sanofi Winthrop Industrie in France, CAS No. It is 114870-03-0, the Chinese name is: methyl O-(2-deoxy-6-O-sulfonic acid group-2-sulfonamido-α-D-glucopyranose)-(1→4)-O -(β-D-glucopyranose)-(1→4)-O-(2-deoxy-3,6-O-disulfonic acid-2-sulfonamido-α-D-glucopyranose )-(1→4)-O-(2-O-sulfonic acid group-α-L-pyraniduronic acid)-(1→4)-2-deoxy-6-O-sulfonic acid group- 2-Sulfonamido-α-D-glucopyranoside decasodium salt, molecular formula C 31 h 43 N 3 Na 10 o 49 S 8 , the molecular weight is 1728, and the structure is: . ...
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