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Synthetic method for rivaroxaban

A synthetic method, the technology of rivaroxaban, applied in the direction of organic chemistry, etc., can solve problems such as unfavorable safety production, toxicity, etc., and achieve the effects of safe storage and use, mild reaction conditions, and high reaction yield

Inactive Publication Date: 2016-06-15
PEKING UNIV FOUNDER GRP CO LTD +2
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] In the existing rivaroxaban preparation method, there is 4-(4-(5-(aminomethyl)-2-oxazolidin-3-yl)phenyl)morpholinyl-3-one and The substitution reaction of 2-chloro-formyl-5-chlorothiophene to obtain rivaroxaban, such as Chinese patent 00818966.8, uses methylamine in the reaction, which is toxic and can form explosive mixtures when mixed with air, which is not conducive to safe production

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  • Synthetic method for rivaroxaban
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Embodiment 1

[0021] Put 1.5kg of 4-(4-(5-(aminomethyl)-2-oxyoxazolidin-3-yl)phenyl)morpholino-3-one into a 50L reaction flask, add 10kg of acetone, Stir at 20~25℃ for 10min, add sodium carbonate solution (1kg sodium carbonate dissolved in 10kg water) under stirring, after addition, cool to 5~10℃, add dropwise the toluene solution of 5-chloro-thiophene-2-carboxylic acid chloride , Which contains 5kg of 5-chloro-thiophene-2-carboxylic acid chloride. After the addition is complete, add 4kg of acetone. After the addition is complete, stir at room temperature for 60 minutes, then stir at 50-55°C for 2 hours. After the reaction is complete, cool to below 15°C. After stirring for 1 hour, filter, the filter cake was washed with 10 kg of water, 10 kg of acetone, drained, and air-dried for 10 hours to obtain 1.82 kg of rivaroxaban, yield: 91%.

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Abstract

The invention discloses a synthetic method for rivaroxaban, which is mild in reaction conditions, employs required reaction reagents being low in cost and easy to obtain, is harmless to operators and environment, and has high reaction yield.

Description

Technical field [0001] The invention relates to a method for synthesizing rivaroxaban, belonging to the technical field of chemical drug synthesis. Background technique [0002] Rivaroxaban, English name Rivaroxaban, CAS number: 366789-02-8. Rivaroxaban tablets were launched in the United States by Bayer Pharmaceuticals in July 2011. It is a highly selective factor Xa inhibitor that can be taken orally directly. It interrupts the internal and external coagulation cascade system by inhibiting coagulation factor Xa. Pathway, thereby inhibiting thrombin generation and thrombosis. Rivaroxaban does not inhibit thrombin (activating factor II), nor has it proven to have an effect on platelets. [0003] Rivaroxaban is mainly used in adult patients with elective hip or knee replacement surgery to prevent venous thromboembolism (VTE). Venous thromboembolism, including deep vein thrombosis (DVT) and pulmonary embolism (PE), is one of the main causes of death in humans. Deep vein thrombosi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D413/14
Inventor 易崇勤李育巧刘秀洁邹明琛谢小飞郭欲晓
Owner PEKING UNIV FOUNDER GRP CO LTD