Triaryldimethylpiperazine dihydrochloride polymorphic substance, preparation method and application thereof

A technology of dimethylpiperazine and ketone dihydrochloride, applied in the field of medicine, can solve problems such as inability to concentrate, sexual dysfunction, confusion, and narcolepsy

Inactive Publication Date: 2017-04-26
YUNNAN INST OF MATERIA MEDICA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

These drugs, while effective, often have problematic side effects, such as lethargy, confusion, inability to concentrate, and sex

Method used

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  • Triaryldimethylpiperazine dihydrochloride polymorphic substance, preparation method and application thereof
  • Triaryldimethylpiperazine dihydrochloride polymorphic substance, preparation method and application thereof
  • Triaryldimethylpiperazine dihydrochloride polymorphic substance, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0089] Example 1 (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl)(3-hydroxyphenyl) Preparation of polymorph B of methyl)phenyl)(4-methylpiperidin-1-yl)methanone dihydrochloride

[0090] Take 10g (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl)(3-hydroxyphenyl)methyl Base) phenyl) (4-methylpiperidin-1-yl) ketone into a glass bottle, add 200mL ethyl acetate to the glass bottle and stir evenly, then add 3.5mL concentrated hydrochloric acid with a volume percentage of 37.5%, at room temperature Stir, react for 3 hours, and dry in vacuo to obtain (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl ) (3-hydroxyphenyl)methyl)phenyl)(4-methylpiperidin-1-yl)methanone dihydrochloride polymorph B.

[0091] (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl)(3-hydroxy The XRPD pattern of polymorph B of phenyl)methyl)phenyl)(4-methylpiperidin-1-yl)methanone dihydrochloride is shown in figure 1 The peak information of its spectrum...

Embodiment 2

[0094] Example 2 (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl)(3-hydroxyphenyl) Preparation of polymorph C of methyl)phenyl)(4-methylpiperidin-1-yl)methanone dihydrochloride

[0095](4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl)( 3-Hydroxyphenyl) methyl) phenyl) (4-methylpiperidin-1-yl) polymorph B of ketone dihydrochloride was used as a starting sample, and 100 mL of acetonitrile was added to make the polymorph The sample of substance B was completely dissolved to obtain a clear solution. The obtained solution was slowly volatilized at room temperature, and the collected solid was polymorph C.

[0096] (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl)(3-hydroxy The XRPD pattern of polymorph C of phenyl)methyl)phenyl)(4-methylpiperidin-1-yl)methanone dihydrochloride is shown in image 3 The peak information of its spectrum is shown in Table 2. TGA and DSC diagrams of polymorph C Figure 4 shown by Figure 4 It can be se...

Embodiment 3

[0100] Example 3 (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl)(3-hydroxyphenyl) Preparation of polymorph C of methyl)phenyl)(4-methylpiperidin-1-yl)methanone dihydrochloride

[0101] (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl)( 3-hydroxyphenyl) methyl) phenyl) (4-methylpiperidin-1-yl) ketone dihydrochloride polymorph B as the starting sample, placed in an open glass bottle; add 100mL Acetonitrile to obtain a clear solution; continue to add mixed polymers (polycaprolactone, polyethylene glycol, polymethyl methacrylate, sodium alginate and hydroxyethyl cellulose mixed with quality); after fully stirring, place the sample Slowly volatilize at room temperature, and the obtained solid is polymorph C.

[0102] (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl)(3-hydroxy Phenyl) methyl) phenyl) (4-methylpiperidin-1-yl) XRPD figure, TGA and DSC figure of polymorph C of ketone dihydrochloride are respectively with image 3 and ...

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Abstract

The application discloses five polymorphic substances: B, C, A, M and I of (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazine-1-yl)(3-hydroxyphenyl)methyl)phenyl)(4-methylpiperidine-1-yl)methyl ketone dihydrochloride, a preparation method thereof, and applications thereof in preparation for medicines.

Description

technical field [0001] The present invention relates to but not limited to the technical field of medicine, in particular to but not limited to a polymorphic form of triaryldimethylpiperazine dihydrochloride and its preparation method and application. Background technique [0002] Depression is a common mental illness, mainly manifested as low mood, loss of interest, pessimism, slow thinking, lack of initiative, self-blame, poor diet and sleep, worry that you have various diseases, and feeling that you are suffering from various diseases in your body. Discomfort, and in severe cases, suicidal thoughts and behaviors may appear. In the fourth edition of the "Diagnostic and Statistical Manual of Mental Disorders" published by the American Psychiatric Association, depression is classified under mood disorders and is divided into three types: major depressive disorder, dysthymic disorder and other Unspecified depression. [0003] Factors causing depression include: genetic fact...

Claims

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Application Information

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IPC IPC(8): C07D401/10A61K31/496A61P25/24A61P25/22A61P25/04A61P1/04
CPCC07D401/10C07B2200/13
Inventor 王京昆宋鹤孙敏王泽人杨志苏敏刘红斌师冰毛勇刘慧浪李泽千崔涛赵春梅苏梅袁芳张天财刘勇张宽仁魏云林沈悦海
Owner YUNNAN INST OF MATERIA MEDICA
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