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Monocholine salt of posaconazole phosphate, preparation method and applications thereof

A technology of posaconazole phosphate and choline salt, which is applied in the field of posaconazole phosphate monocholine salt and its preparation, can solve the problems of limiting the scope of clinical application of drugs, and achieve improved physical stability and easier handling , Low hygroscopicity effect

Active Publication Date: 2020-03-31
HC SYNTHETIC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The use of the excipient sulfobutyl ether-β-cyclodextrin greatly limits the scope of clinical application of the drug
The instructions for posaconazole injection specifically point out that the drug is not suitable for patients with moderate or severe renal impairment

Method used

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  • Monocholine salt of posaconazole phosphate, preparation method and applications thereof
  • Monocholine salt of posaconazole phosphate, preparation method and applications thereof
  • Monocholine salt of posaconazole phosphate, preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1: Preparation of posaconazole phosphate monocholine salt

[0038]

[0039] step 1

[0040]

[0041] Weigh posaconazole (10g, 14.28mmol) into a dry 250mL three-necked flask, add dichloromethane (100mL) under nitrogen protection, stir to dissolve, add triethylamine (5mL) at room temperature (25℃) ) The reaction was stirred at room temperature (25° C.) for 30 min, and phosphorus oxychloride (3 mL, 32.13 mmol) was slowly added, and the addition was completed in about 1 min. The reaction was completed for 6 hours and the reaction was completed. In-process HPLC judges whether the reaction is complete.

[0042] Chromatographic conditions:

[0043] Mobile phase: 6.8g / L potassium dihydrogen phosphate adjust pH to 3.0 with phosphoric acid: acetonitrile=60:40

[0044] Detection wavelength: 220nm Flow rate: 1.0ml / min Column temperature: 25℃

[0045] Sample concentration: 1mg / ml The dilution medium is 50% acetonitrile

[0046] The reaction solution was added dropwise to 150mL pure wa...

Embodiment 2

[0050] Example 2: Preparation of posaconazole phosphate monocholine salt

[0051]

[0052] step 1

[0053]

[0054] Take 40ml of phosphorus oxychloride and place it in a dry 250ml three-necked flask. Under the protection of nitrogen, cool to -5 to 5°C. Slowly add posaconazole (10g, 14.28mmol). After the addition, keep it warm and stir for 12 hours. The reaction is over. In-process HPLC judges whether the reaction is complete.

[0055] Chromatographic conditions:

[0056] Mobile phase: 6.8g / L potassium dihydrogen phosphate adjust pH to 3.0 with phosphoric acid: acetonitrile=60:40

[0057] Detection wavelength: 220nm Flow rate: 1.0ml / min Column temperature: 25℃

[0058] Sample concentration: 1mg / ml The dilution medium is 50% acetonitrile

[0059] The reaction solution was added dropwise to 800 mL of sodium hydroxide aqueous solution at 0°C, and the hydrolysis temperature was controlled to 0-5°C. After the hydrolysis was completed, the pH was adjusted to 3 to 4 with 10% hydrochloric acid....

Embodiment 3

[0063] Example 3: Preparation of posaconazole phosphate monocholine salt pentahydrate

[0064]

[0065] The same batch of posaconazole as in Example 1 was selected to repeat Steps 1 and 2 of Example 2 for the test, except that the drying method of Step 2 was changed to 35±5°C blast drying. The title compound is obtained as a white solid. (Related substances: 0.13%; moisture: 9.06%; content 99.87%).

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Abstract

The invention relates to a monocholine salt of posaconazole phosphate, a preparation method and applications thereof, wherein the monocholine salt of posaconazole phosphate has a structure representedby a formula (I), and n is an integer of 0-12, preferably an integer of 0-8, more preferably an integer of 0-6.

Description

Technical field [0001] The invention relates to a posaconazole phosphate monocholine salt and a preparation method and application thereof. Background technique [0002] Fungal infection is a common and frequently-occurring disease in clinic. Infection can be divided into two types: superficial fungal infection and deep fungal infection. Superficial fungal infections are caused by ringworm invading the skin, hair, nails and other body surface parts, with high incidence and low harm. Deep fungal infections are caused by fungi such as Candida, Aspergillus and Cryptococcus invading internal organs and deep tissues, which are very harmful. [0003] In recent years, with the continuous increase of immunosuppressed patients, the incidence of deep fungal infections has increased significantly. Fungal infections, especially deep fungal infections, have increasingly attracted widespread attention. However, current clinically used antifungal drugs have problems such as large side effects a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6558A61K31/675A61P31/10
CPCC07F9/65586A61P31/10
Inventor 杨成
Owner HC SYNTHETIC PHARMA CO LTD
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