Method for preparing paricalcitol

A technology of paricalcitol and chemical reaction, which is applied in the field of 1-α-hydroxy-19-desmethylene vitamin D2, a drug for treating osteoporosis, can solve the problem that paricalcitol is uneconomical and has many steps. , complex operation and other problems, to achieve the effect of improving yield, simplifying process flow, and high yield
CN103451238AInactive Publication Date: 2013-12-18SOUTHWEST JIAOTONG UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SOUTHWEST JIAOTONG UNIV
Publication Date
2013-12-18
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a method for preparing a medicine paricalcitol treating osteoporosis. According to the method, vitamin D2 is taken as a raw material, and a target object is obtained through steps of chemical reaction and biological reaction. Expensive toxic double hydroxylation reagent is not used, and the double-hydroxylation broken bond of a cheap and effective oxidized reagent potassium permanganate solution is adopted for preparing ketone. The method comprises the following steps of preparing olefin in an alkaline reagent through isomerism; carrying out hydroboration through a hydroboration reagent 9-BBN and borane; introducing 1-OH, thereby obtaining 19-demethylation vitamin D2 through ring opening; and by taking Pseudonocardia autotrophica SWJTUQL-3721021 (autotrophy Pseudonocardia CGMCC 5098) as hydroxylation bacterium, carrying out direct hydroxylation on 25-OH through a biological conversion method, thereby obtaining the paricalcitol through extraction and separation. According to the method, 27 public known reaction steps are reduced to 9 reaction steps through combining the chemical conversion and biological conversion, so that the total recovery is improved, the process route is shortened, and the method provides a new process route for industrial preparation of the paricalcitol.
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Description

technical field

[0001] The invention relates to chemical and biopharmaceuticals, especially 1-alpha-hydroxyl-19-demethylene vitamin D for treating osteoporosis 2 technology field. Background technique

[0002] Paricalcitol is a new type of active vitamin drug developed by Abbott in 1998. Its trade name is Zemplar, which has been approved by the FDA and is clinically used to prevent and treat animals with secondary hyperparathyroidism. Experimental and clinical studies have shown that paricalcitol has relatively selective pharmacological effects, can safely and effectively inhibit the secretion of parathyroid hormone and hyperplasia of parathyroid glands, and rarely cause hypercalcemia and hyperphosphatemia, and can replace calcitriol (calcitriol) for uremia is especially suitable for the treatment of secondary hyperparathyroidism in long-term hemodialysis patients.

[0003] 1-alpha-Hydroxy-19-demethylene vitamin D 2 (1α-19-nor-VD 2 ), that is, the known synthesis of pari...

Claims

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