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Preparation method of paricalcitol

A technology of paricalcitol and its compounds, which is applied in the field of new synthesis of chemical drugs, and can solve problems such as the lack of application experience in patients with hepatic insufficiency

Inactive Publication Date: 2014-07-02
湖南华腾制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

No experience in patients with severe hepatic insufficiency

Method used

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  • Preparation method of paricalcitol
  • Preparation method of paricalcitol
  • Preparation method of paricalcitol

Examples

Experimental program
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Effect test

Embodiment 1

[0036] (1) Synthesis of compound 2

[0037] 60 g of Nandrolone and 45 g of pyridinium chlorochromate were added to 400 ml of dichloromethane, stirred at room temperature, filtered, the mother liquor was concentrated under reduced pressure, and the residue was separated by a chromatographic column to obtain 49 g of the product.

[0038] (2) Synthesis of compound 3

[0039] 49g of compound 2 and 21g of (3S,6R,E)-6-(diphenylphosphine)-2,3-dimethylhept-4-en-2-ol were added to 350ml of tetrahydrofuran, cooled to - 78oC, slowly add 14g of sodium amide, stir for 5 hours, naturally rise to room temperature, add saturated ammonium chloride, then add ethyl acetate for extraction, collect the organic phase, concentrate, and the residue is separated by a chromatographic column to obtain 52g of product.

[0040] (3) Synthesis of compound 4

[0041] Add 52g of compound 3 to 300ml of dichloromethane, cool to 0°C, slowly add 35g of TBSCl, stir for 3 hours, add ice water, then add ethyl acet...

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Abstract

The invention discloses a method for preparing paricalcitol. Nandrolone is taken as a raw material, oxidation, Wittig reaction, hydroxyl protection, bromination, rearrangement, hydrogen bromide removal, addition, oxidation, reduction, hydroxyl deprotection and ring opening are carried out, so that the paricalcitol is obtained. The paricalcitol is used for preventing and treating secondary hyperparathyroidism.

Description

technical field [0001] The invention relates to a novel synthesis method of chemical drugs, in particular to a synthesis method of the compound paricalcitol. technical background [0002] The compound Paricalcitol, the English name is Paricalcitol, CAS: 131918-61-1, the structural formula is: [0003] [0004] Paricalcitol is a synthetic, biologically active vitamin D analog modified with two groups on the calcidol side chain to selectively activate the vitamin D receptor (VDR). Paricalcitol selectively upregulates calcium-sensing receptors (CaSR) in the thyroid. Therefore, paricalcitol can reduce PTH levels by inhibiting thyroid proliferation, reducing PTH synthesis and secretion, thereby restoring calcium and phosphorus homeostasis. Metabolic bone disease associated with chronic kidney disease can be prevented or treated. No age- or sex-related differences in pharmacokinetics were observed in the adult patients studied, and no differences in pharmacokinetics between ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C401/00
Inventor 邓泽平其他发明人请求不公开姓名
Owner 湖南华腾制药有限公司
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