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Dapagliflozin intermediate compound crystal form and preparation method thereof

A technology for compounds and intermediates, applied in the field of dapagliflozin intermediate compound crystal forms and their preparation, can solve problems such as unfavorable subsequent reactions, unfavorable solvent recovery and reuse, and achieve the effects of high quality and good stability

Pending Publication Date: 2022-05-27
ZHEJIANG MENOVO PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there are still deficiencies in the removal of impurities, and the existence of these impurities is still unfavorable to subsequent reactions.
At the same time, the synthesis process and crystallization process of this compound have adopted two different alcohols (ethanol and n-propanol), which is unfavorable for the recovery and reuse of the solvent

Method used

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  • Dapagliflozin intermediate compound crystal form and preparation method thereof
  • Dapagliflozin intermediate compound crystal form and preparation method thereof
  • Dapagliflozin intermediate compound crystal form and preparation method thereof

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Embodiment Construction

[0042] The present invention will be further described in detail below with reference to the embodiments of the accompanying drawings.

[0043] The crystal form A of the intermediate compound of Dapagliflozin in this example, the chemical name is (2S,3R,4S,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl) -6-(Hydroxymethyl)-2-propoxytetrahydro-2H-pyran-3,4,5-triol, the structural formula is:

[0044]

[0045] like Figure 10 As shown, its X-ray powder diffraction pattern has the following characteristic diffraction peaks: 5.7±0.2°, 13.1±0.2°, 15.0±0.2°, 18.3±0.2°, 20.5±0.2°, 20.8±0.2°, 21.6±0.2°, 23.1±0.2° and 24.5±0.2°.

[0046] The crystalline form of the above-mentioned dapagliflozin intermediate compound is an oily substance when no alcohol solvent or water is involved in the crystallization.

[0047]The compound crystal contains 1% to 20% of the crystallization solvent, preferably 3.5 to 15% of the crystallization solvent.

[0048] The above-mentioned crystallization so...

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Abstract

The invention relates to a dapagliflozin intermediate compound crystal form and a preparation method thereof, and the chemical name of a dapagliflozin intermediate compound is (2S, 3R, 4S, 5S, 6R)-2-(4-chloro-3-(4-ethoxybenzyl) phenyl)-6-(hydroxymethyl)-2-propoxy tetrahydro-2H-pyran-3, 4, 5-triol. The compound (2S, 3R, 4S, 5S, 6R)-2-(4-chloro-3-(4-ethoxybenzyl) phenyl)-6-(hydroxymethyl)-2-propoxytetrahydro-2H-pyran-3, 4, 5-triol and the crystal form thereof are suitable for substrates with different masses, and the obtained intermediate is high in quality and good in stability, can be stored for a long time under the room temperature condition, can be used for preparing dapagliflozin, and can be used for preparing dapagliflozin. And the method has important significance on industrial large-scale production of dapagliflozin.

Description

technical field [0001] The invention relates to the field of medicine and chemical industry, in particular to a crystal form of an intermediate compound of Dapagliflozin and a preparation method thereof. Background technique [0002] Dapagliflozin, chemical name: (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(hydroxymethyl)tetrahydro - 2H-pyran-3,4,5-triol, the structural formula is: [0003] [0004] Dapagliflozin Dapagliflozin is a sodium-glucose cotransporter 2 inhibitor, the U.S. Food and Drug Administration (FDA) announced on January 8, 2014 that it approved the use of dapagliflozin for type 2 diabetes. treatment, while requiring manufacturers to conduct post-marketing studies on drug-related risks. [0005] There are multiple routes for the synthesis of dapagliflozin. Route 1 is reported in the literature J.Med.Chem.2014,57,1236-1251. The synthetic route is as follows figure 1 ; The synthetic route that route 2 is reported by patent EP1506211B1 is such...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/04C07H1/06
CPCC07H1/06C07H15/04C07B2200/13Y02P20/55
Inventor 李卫鹏王哲姚显睿黄想亮石展
Owner ZHEJIANG MENOVO PHARMA
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