Method for synthesizing Seocalcitol

A technology of theocalcidol and a synthesis method, applied in the field of synthesizing theocalcidol, can solve the problems of difficulty in product purification and high production cost, and achieve the effects of low production price, reduced production cost and cost reduction.

Inactive Publication Date: 2010-09-15
HYDRAGON PHARMA
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Problems solved by technology

The purpose of the present invention is to provide a low-cost and efficient method for synthesizing Theocalcidol, which ...

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  • Method for synthesizing Seocalcitol
  • Method for synthesizing Seocalcitol
  • Method for synthesizing Seocalcitol

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Abstract

The invention provides a method for synthesizing Seocalcitol, which mainly solves the technical problem of high production cost, difficult product purification and the like in the conventional synthetic method. The method comprises the following steps of: performing a Wittig/Wittig-Horner Julia/Horner-Wadsworth-Emmons name reaction by utilizing an aldehyde intermediate 7 and a Ylide intermediate 2 under the action of an alkali to construct carbon-carbon double bonds so as to form a precursor compound 10 of Seocalcitol, and then performing an illumination reaction and a deprotection reaction to prepare Seocalcitol 11. The invention also provides a method for synthesizing the key Ylide intermediate 2. The method has the advantages of simple operation, no side reaction, convenient purification, high yield and low cost, and is suitable for preparing high-purity Seocalcitol products through industrial production.

Description

technical field The invention relates to a method for synthesizing ceocalcidol. Background technique Studies have shown that vitamin D analogs have therapeutic effects on many cancers (including prostate cancer, breast cancer, pancreatic cancer, colon cancer, skin cancer and brain tumors, etc.) can exhibit anticancer activity. However, the use of most vitamin D analogs can lead to hypercalcemia, which can be life-threatening in severe cases, which limits the use of large doses of vitamin D drugs to treat cancer. Theocalcitol (Seocalcitol, EB1089, CB1089) came into being under this background. Theocalcitol was developed by Leo Pharmaceutical Products Ltd. of Denmark and applied for compound patent and application patent in 1991. In 2005, Cougar Biotechnology of the United States obtained the global exclusive authorization to develop Theocalcidol from Leo Pharmaceuticals. Cougar Biotechnology Company research proves that Theocalcidol has a good curative effect on prostate...

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Application Information

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IPC IPC(8): C07C401/00C07F9/53
Inventor 程华威李晓勇刘哲生
Owner HYDRAGON PHARMA
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