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Crystal form of fumarate of pyrrole derivative

A fumarate and crystallization technology, applied in the direction of organic chemistry, etc., to achieve the effect of high purity and good stability

Inactive Publication Date: 2015-02-04
SUNCADIA PHARM CO LTD +1
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0006] CN101300229A discloses 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3 base]-N-methylmethylamine monofumarate, but not involving its crystalline form

Method used

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  • Crystal form of fumarate of pyrrole derivative
  • Crystal form of fumarate of pyrrole derivative
  • Crystal form of fumarate of pyrrole derivative

Examples

Experimental program
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Embodiment 1

[0042] The preparation method of pyrrole derivative maleate with crystal form A is described in detail below.

[0043] Step 1: Synthesis of 5-(2-fluorophenyl)-1-(pyridine-3-sulfonyl)-1H-pyrrole-3-carbaldehyde

[0044] Compound II (260 mg) was dissolved in tetrahydrofuran (50 ml), 60% NaH was added, and the reaction was stirred at room temperature for 30 minutes. Then add 15-crown-5 (1.5g), stir at room temperature for 1 hour, then add pyridine-3-sulfonyl chloride, stir at room temperature for 2 hours until the reaction is complete by TLC, then add 20 mL of saturated brine to the reaction system , extracted with ethyl acetate (100mL×2), combined the organic phases, washed the organic phase with 50ml of saturated brine, dried with an appropriate amount of anhydrous sodium sulfate, filtered, and concentrated the filtrate under reduced pressure to obtain the crude compound IV (200mg) which was directly used in the next reaction.

[0045] Step 2: Synthesis of 1-[5-(2-fluorophenyl)...

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Abstract

The invention relates to a crystal form of fumarate of a pyrrole derivative, and concretely relates to a crystal form of 1-[5-(2-fluorophenyl)-1-(prindine-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethamide monofumarate and a preparation method thereof. An X-ray powder diffraction spectrum represented by 2theta angle and the interplanar distance by performing Cu-Ka radiation on the crystal form, and is shown as figure 1. The crystal form is high in purity and good in stability, is applicable to preparation technological process and long-term storage, and also has superiority in industrialized production.

Description

technical field [0001] The present invention relates to a kind of 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3 base]-N-methylmethylamine monofumarate Crystalline forms and methods for their preparation. Background technique [0002] In the development of pharmaceutical compositions, it is very important that the drug is in a form that can be easily handled and processed. In manufacturing, it is also very important to be able to provide the drug in the purest possible crystalline form. It would be desirable if an active pharmaceutical ingredient could be easily obtained in a stable crystalline form. Therefore, in producing commercially viable and pharmaceutically acceptable pharmaceutical compositions, whenever possible, the drug should be provided in a substantially crystalline and stable crystalline form. [0003] 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3yl]-N-methylmethylamine monofumarate was developed by Takeda Pharmaceutical Company A g...

Claims

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Application Information

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IPC IPC(8): C07D401/12
CPCC07D401/12
Inventor 孙飘扬吕小虎吴成龙孙绍光黄金昆张羽
Owner SUNCADIA PHARM CO LTD
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