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Synthesis method of 6alpha-methylprednisolone

A technology of methylprednisolone and synthetic methods, applied in the direction of steroids, organic chemistry, fermentation, etc., can solve the problems of low reaction yield, difficult to eliminate selenium, large pollution, etc., achieve high yield, avoid dramatic The use of toxic chemicals, the effects of three wastes treatment and pressure relief

Active Publication Date: 2015-04-29
浙江晟创制药有限公司
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Problems solved by technology

The dehydrogenation process in the prior art generally uses selenium dioxide for dehydrogenation. Selenium dioxide is a highly toxic substance, causing large pollution and low reaction yield. The residual selenium dioxide in the product is difficult to eliminate
[0004] At present, there are more than ten synthetic methods of methylprednisolone, many of which were developed in the 1960s, but all of them have low yield and high cost

Method used

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  • Synthesis method of 6alpha-methylprednisolone
  • Synthesis method of 6alpha-methylprednisolone
  • Synthesis method of 6alpha-methylprednisolone

Examples

Experimental program
Comparison scheme
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Embodiment

[0055] etherification reaction

[0056]Add 40ml of tetrahydrofuran into the four-neck flask, then add 10g of compound I, after nitrogen replacement, add 3ml of ethanol and 7ml of triethyl orthoformate; after raising the temperature to 36-38°C, add 0.2g of p-toluenesulfonic acid to continue the reaction 3 hours; TLC follow-up, cool down slightly to 30 after the reaction finishes + 1°C for use.

[0057] methylation reaction

[0058] Add 4gN-methylaniline and 37% formaldehyde 3g in the last step reactant; Slightly warm up to 40 + 1°C, keep warm for 3 hours; TLC detects the reaction status, after the reaction, the system cools down to about 15°C; concentrated hydrochloric acid adjusts the pH value of the system to 1-2; after the dropwise addition, the temperature rises to 25°C + 1°C, hydrolysis reaction for 2 hours; after adding 100ml of water dropwise into the reaction system, the system cooled down to 5 + After stirring at 1°C for 1 hour, after standing still for 5 hours, su...

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Abstract

The invention discloses a synthesis method of 6alpha-methylprednisolone. A compound I used as an initial raw material is subjected to etherification, methynation, hydrogenation, fermentation dehydrogenation, bromination and debromination to obtain the 6alpha-methylprednisolone. The reaction route is disclosed in the specification. Compared with the prior art, the synthesis method disclosed by the invention has the advantages of short synthesis route, high yield, environment friendliness and high production sustainability, can easily implement mass production, has very high commercial value, and is an excellent 6alpha-methylprednisolone synthesis scheme.

Description

technical field [0001] The invention relates to a production process method of methylprednisolone, in particular to a synthesis method of 6a-methylprednisolone. Background technique [0002] 6a-Methylprednisolone is a kind of highly effective anti-immune stress response adrenergic corticosteroid, which is widely used in clinical anti-immune stress response. 6a-Methylprednisolone has anti-inflammatory, anti-endotoxin, anti-immune, anti-shock and other pharmacological effects, and can be made into clinical injections, which can be used for organ transplantation, immune suppression, and acute adrenal insufficiency and postoperative shock. [0003] Because the production process of methylprednisolone drug is complex and the production cycle is long, it is a technology-intensive finished product. Wherein the 21-position upper acetate and the 1-position dehydrogenation process are key steps in the production process of methylprednisolone, which directly affects the quality and y...

Claims

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Application Information

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IPC IPC(8): C12P33/08C12P33/06C07J5/00
Inventor 徐润星王勇张学忠简双喜汪德喜
Owner 浙江晟创制药有限公司
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