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Crystal form of amantadine compound, and preparation method thereof

A technology for compounds and crystal forms, applied in the field of crystal forms of amantadine compounds and their preparation, can solve problems such as difficulty in research and production, use process, inability to detect and determine microscopic morphology, unfavorable research on pharmaceutical preparations, etc.

Inactive Publication Date: 2020-09-15
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After research, the inventor found that the white solid of the compound represented by the aforementioned formula (I) was prepared according to the method disclosed in Example 7 of the patent application WO2017193870 (compound 4), which was a waxy substance whose microscopic form could not be detected and determined. Moreover, this waxy substance is unfavorable for the transfer in production and the research of pharmaceutical preparations, and is difficult to be used in subsequent research and production and use processes.

Method used

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  • Crystal form of amantadine compound, and preparation method thereof
  • Crystal form of amantadine compound, and preparation method thereof
  • Crystal form of amantadine compound, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0146] Example 1: Preparation of ((((1r,3R,5S,7r)-3,5-dimethyladamantan-1-yl)carbamoyl)oxy)methyl palmitate crystal form A

[0147] Add 1.0 g of ((((1r,3R,5S,7r)-3,5-dimethyladamantan-1-yl)carbamoyl)oxy)methyl palmitate into 10 mL of methanol and 10 mL of acetonitrile , stirred at room temperature to obtain a clear solution, cooled to 0°C, a solid was precipitated, filtered with suction and vacuum-dried in a drying oven at room temperature to constant weight to obtain 0.85 g of crystals. The obtained crystals were confirmed to be Form A by XRD and DSC detection.

Embodiment 2

[0148] Example 2: Preparation of ((((1r,3R,5S,7r)-3,5-dimethyladamantan-1-yl)carbamoyl)oxy)methyl palmitate crystal form A

[0149] Add 1.0 g of ((((1r,3R,5S,7r)-3,5-dimethyladamantan-1-yl)carbamoyl)oxy)methyl palmitate to 10 mL methanol and 10 mL trifluoro In ethanol, stirred at room temperature to obtain a clear solution, cooled to 0°C, a solid precipitated, filtered with suction and vacuum-dried at room temperature in a drying oven to obtain 0.88 g of crystals. The obtained crystals were confirmed to be Form A by XRD and DSC detection, see attached figure 1 - attached image 3 .

Embodiment 3

[0150] Example 3: Preparation of ((((1r,3R,5S,7r)-3,5-dimethyladamantan-1-yl)carbamoyl)oxy)methyl palmitate crystal form A

[0151] Add 500 mg of ((((1r,3R,5S,7r)-3,5-dimethyladamantan-1-yl)carbamoyl)oxy)methyl palmitate into 5 mL of ethanol to obtain a clear solution, Then 10 mL of water was added dropwise, and a solid precipitated out, which was filtered by suction and vacuum-dried in a drying oven at room temperature to obtain 430 mg of crystals. The obtained crystals were confirmed to be Form A by XRD and DSC detection.

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PUM

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Abstract

The invention relates to a crystal form of an amantadine compound, and a preparation method of the crystal form, and belongs to the field of medicinal chemistry. The crystal form disclosed by the invention has good properties in the aspects of stability, solubility, dissolution, pharmacology and the like, and can be used for preparing pharmaceutical preparation production.

Description

technical field [0001] The invention relates to a crystal form of amantadine compounds and a preparation method thereof, and belongs to the field of medicinal chemistry. Specifically, the invention relates to ((((1r,3R,5S,7r)-3,5-dimethyl Adamant-1-yl)carbamoyl)oxy)methyl palmitate and ((((1r,3R,5S,7r)-3,5-dimethyladamantan-1-yl)carbamoyl ) crystal form of oxy)methyl stearate and a preparation method thereof. Background technique [0002] Most of the intersynaptic excitatory transmission uses glutamate as the neurotransmitter for fast signal transduction. N-methyl-D-aspartate receptors (NMDARs) are a class of ionotropic glutamate receptors whose functions are mainly involved in the refinement of neural circuits and triggering various forms of synaptic plasticity during development. It plays an important physiological role in the process of learning, memory and emotion regulation. More and more studies have found that NMDAR is involved in a variety of pathological processe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C269/08C07C271/24A61K31/27A61P25/00A61P25/28
CPCC07C269/08C07C271/24A61P25/00A61P25/28C07B2200/13C07C2603/74
Inventor 徐巾超叶辉青李英龙张杰林碧悦寇景平陈勇罗忠华黄芳芳
Owner SUNSHINE LAKE PHARM CO LTD
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