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Process for synthesizing triamcinolone acetonide acetate

A technology of triamcinolone acetonide acetate and a synthetic method, which is applied in the field of pharmaceutical chemical synthesis, can solve problems such as no synthetic technology of triamcinolone acetonide acetate, and achieve the effects of low toxicity, low risk, and low pollution

Active Publication Date: 2013-01-09
BAOJI KANGLE BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, only Beijing Shuguang Pharmaceutical Co., Ltd., Zhejiang Xianju Pharmaceutical Co., Ltd., Zhanjiang Xiangyang Pharmaceutical Factory and Jiangsu Jintan Pharmaceutical Factory produce triamcinolone acetonide acetate raw materials in China, and there is no relevant literature on the synthesis process of triamcinolone acetonide acetate. to report

Method used

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  • Process for synthesizing triamcinolone acetonide acetate
  • Process for synthesizing triamcinolone acetonide acetate
  • Process for synthesizing triamcinolone acetonide acetate

Examples

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Embodiment 1

[0032] Step 1, take tetraenyl acetate as raw material, obtain oxide compound through oxidation reaction under the effect of formic acid and potassium permanganate, concrete process is:

[0033] 101. Add 20g tetraenyl acetate and 640mL reaction solvent acetone into the reactor, cool down to 0°C, then add 6mL formic acid into the reactor, stir for 15min, then add 150mL potassium permanganate solution into the reactor, stir for 6min Then add 100mL reducing solution (sodium sulfite aqueous solution with a concentration of 100g / L) to the reactor, stir and react for 10min, heat up the reaction system in the reactor to 38°C and filter to obtain filter cake and filtrate; the permanganic acid The potassium solution is a mixed solution of potassium permanganate, acetone and water, wherein the concentration of potassium permanganate is 65g / L, and the volume ratio of acetone and water is 1:14;

[0034] 102. Concentrate the filtrate described in 101 under reduced pressure until there is no...

Embodiment 2

[0044] Step 1, take tetraenyl acetate as raw material, obtain oxide compound through oxidation reaction under the effect of formic acid and potassium permanganate, concrete process is:

[0045] 101. Add 20g tetraenyl acetate and 600mL reaction solvent acetone into the reactor, cool down to -3°C, then add 5.7mL formic acid into the reactor, stir for 10min, then add 190mL potassium permanganate solution into the reactor, stir After reacting for 4 minutes, add 96 mL of reducing solution (sodium sulfite aqueous solution with a concentration of 80 g / L) to the reactor, stir and react for 5 minutes, heat up the reaction system in the reactor to 35 ° C and filter to obtain a filter cake and filtrate; Potassium manganate solution is a mixed solution of potassium permanganate, acetone and water, wherein the concentration of potassium permanganate is 50g / L, and the volume ratio of acetone and water is 1:12;

[0046] 102. Concentrate the filtrate described in 101 under reduced pressure un...

Embodiment 3

[0056] Step 1, take tetraenyl acetate as raw material, obtain oxide compound through oxidation reaction under the effect of formic acid and potassium permanganate:

[0057] 101. Add 20g tetraenyl acetate and 680mL reaction solvent acetone into the reactor, cool down to 6°C, then add 6.1mL formic acid into the reactor, stir for 20min, then add 148mL potassium permanganate solution into the reactor, and stir to react After 8 minutes, 110 mL of reducing solution (sodium sulfite aqueous solution with a concentration of 120 g / L) was added to the reactor, stirred for 15 minutes, and the reaction system in the reactor was heated to 40 ° C and then filtered to obtain a filter cake and filtrate; the high manganese The potassium permanganate solution is a mixed solution of potassium permanganate, acetone and water, wherein the concentration of potassium permanganate is 70g / L, and the volume ratio of acetone and water is 1:16;

[0058] 102. Concentrate the filtrate described in 101 under...

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Abstract

The invention discloses a process for synthesizing triamcinolone acetonide acetate. The process comprises the steps of firstly, taking an acetic acid tetraene material as a raw material, and obtaining an oxide through an oxidation reaction under the effect of methanoic acid and potassium permanganate; secondly, taking the oxide as a raw material, and obtaining a ring-reducing material through a ring-reducing reaction under the effect of perchloric acid and N-bromosuccinimide; thirdly, taking the ring-reducing material as a raw material, and conducting a fluorination reaction under the effect of fluorine hydride and dimethylformamide to obtain a triamcinolone acetonide acetate crude product; and fourthly, purifying the triamcinolone acetonide acetate crude product to obtain the triamcinolone acetonide acetate. The process is mild in reaction condition, easy to control, low in toxicity and dangerousness of used auxiliary materials, low in pollution and applicable to industrial production, the triamcinolone acetonide acetate which is synthesized by the process is subjected to high performance liquid chromatography (HPLC) detection, the purity can exceed 99%, and the yield is high.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical chemical synthesis, and in particular relates to a synthesis method of triamcinolone acetonide acetate. Background technique [0002] Triamcinolone acetonide acetate is a common drug for skin diseases. Its effect is similar to that of hydrocortisone, and its anti-inflammatory effect is 5-20 times that of hydrocortisone. Sodium retention is strong. Triamcinolone acetonide acetate is clinically divided into injections and ointments, which are suitable for various skin diseases, allergic rhinitis, joint pain, bronchial asthma, frozen shoulder, tenosynovitis, synovitis, acute sprain, rheumatoid arthritis, etc. . At present, only Beijing Shuguang Pharmaceutical Co., Ltd., Zhejiang Xianju Pharmaceutical Co., Ltd., Zhanjiang Xiangyang Pharmaceutical Factory and Jiangsu Jintan Pharmaceutical Factory produce triamcinolone acetonide acetate raw materials in China, and there is no relevant literatur...

Claims

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Application Information

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IPC IPC(8): C07J71/00
Inventor 王轶
Owner BAOJI KANGLE BIOTECH
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