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A kind of preparation method of prednisolone

A technology of prednisolone and compound, applied in steroids, organic chemistry and other directions, can solve the problems of complex operation, easy decomposition, heavy metal residues, etc., and achieve simple separation and purification operation, high material utilization rate, and few reaction steps. Effect

Active Publication Date: 2016-03-02
李竞
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  • Application Information

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Problems solved by technology

However, chromium is used in the reduction step, which causes heavy metal residues; in addition, the cost of iodo is relatively high, and the intermediate is unstable and easy to decompose, so it must be stored in the dark under nitrogen; during this period, the intermediate is separated many times, and the operation is complicated. Facilitate large-scale industrial production

Method used

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  • A kind of preparation method of prednisolone
  • A kind of preparation method of prednisolone

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Experimental program
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Effect test

Embodiment 1

[0028] (1) Add 10g of raw material (I), 50ml of acetone, and 20ml of glacial acetic acid into the reactor, stir, cool down to 0°C, add 30ml of acetone dissolved with 9g of NBS within 30 minutes, and react at 5-10°C for 2 hours. Acetone was distilled off.

[0029] (2) Add 30-50ml of ether into the reactor, slowly add 3.8g-4.2g of zinc powder, and carry out the reduction at room temperature for 2h. Stirring was continued for 15 minutes after the end of the TLC detection reaction.

[0030] (3) Add 0.1g catalyst AlCl to the reactor 3 , Stir at -5~0°C, slowly add 30ml of diethyl ether solution containing 5.5g of bromine within 30 minutes; keep the reaction temperature constant, and react for 2h.

[0031] (4) Use sodium hydroxide to adjust the pH of the reaction solution to be neutral, filter, add the filtrate to water, separate the liquid, extract the water phase with 10ml ether, extract three times, combine all the ether solutions, evaporate to dryness and dissolve in 50ml aceto...

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Abstract

The application relates to a method for synthetizing prednisolone. Double bond bromination, reductive debromination, bromination and hydrolysis reaction are carried out on a compound with a structure of formula I so as to generate the prednisolone. The method is high in yield, is easy to operate, and is applicable to industrial production.

Description

technical field [0001] The present invention relates to a kind of preparation method of steroid compound, especially relate to the preparation of prednisolone acetate. Background technique [0002] Prednisolone English name: Prednisolone, is a middle-effect adrenal cortex hormone drugs. It has various pharmacological effects such as anti-inflammation, anti-allergy and immune suppression, and is mainly used for severe bacterial infections and severe allergic diseases, various thrombocytopenic purpura, neutropenia, severe skin diseases, and immune rejection of organ transplantation reactions, tumor therapy, and ocular inflammation sensitive to glucocorticoids. [0003] The preparation method about prednisolone in the prior art has following several routes: [0004] 1. Using hydrocortisone as the starting material, using Arthrobacter simplex for biological dehydrogenation. The conversion rate of the biotransformation method is low, generally no more than 80%, extraction and ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J5/00
Inventor 李竞
Owner 李竞
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