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Isoalantolactone derivative and application of salt of isoalantolactone derivative in preparation of medicine for treating thyroiditis

A kind of technology of xenotyrolactone and thyroiditis, which is applied in the direction of drug combination, medical formula, endocrine system diseases, etc., can solve the problems of easy recurrence and trouble clinical treatment, and achieve the effect of obvious therapeutic effect

Active Publication Date: 2017-03-08
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing treatment methods mostly adopt thyroid hormones (levothyroxine sodium tablets, etc.), replacement therapy, immunosuppressants (tripterygium glycosides tablets, etc.), surgical treatment, etc. Although there are certain clinical curative effects, there are still problems in safety. Not a small problem, such as drug-induced hyperthyroidism and other side effects still plague the clinical treatment, and it is easy to relapse once the drug is stopped

Method used

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  • Isoalantolactone derivative and application of salt of isoalantolactone derivative in preparation of medicine for treating thyroiditis
  • Isoalantolactone derivative and application of salt of isoalantolactone derivative in preparation of medicine for treating thyroiditis
  • Isoalantolactone derivative and application of salt of isoalantolactone derivative in preparation of medicine for treating thyroiditis

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Preparation of compound (II)

[0027]

[0028] 1) Preparation of Compound (1.1)

[0029]

[0030] 1) Isoaurinolide (1.0g, 4.3mmol) was dissolved in dichloromethane (16mL), and peroxybenzoic acid (1.1g, 5.2mmol) was slowly added to the system in batches, reacted at room temperature for 3 hours, saturated The reaction was quenched with sodium thiosulfate (16 mL), extracted with dichloromethane (16 mL×3), the organic phase was washed with saturated aqueous sodium bicarbonate (16 mL), dried and concentrated, and purified by column chromatography (petroleum ether: ethyl acetate=20: 1) Obtain compound 1.2 (white solid, 984 mg, yield 92.0%).

[0031] 2) preparation of compound (I-II),

[0032]

[0033] The compound 1.2 obtained in step 1) was dissolved in dichloromethane (98mL), potassium carbonate (16.4g, 118.9mmol) and dimethylamine hydrochloride (4.8g, 59.4mmol) were added to the system in turn, and the mixed system was stirred Reflux reaction for 3 hours, after...

Embodiment 2

[0039] Preparation of compound (III)

[0040]

[0041] 1) Preparation of Compound 1.3

[0042]

[0043] At 0°C, dissolve selenium dioxide (87.5mg, 0.75mmol) in dichloromethane (5mL), add tert-butanol peroxide (0.37mL), and stir for 30 minutes. , 2.15mmol) of dichloromethane (5mL) solution was slowly added to the above system, stirred at room temperature for 24 hours, quenched with saturated aqueous sodium thiosulfate (8mL), extracted with dichloromethane (8mL×3), dried Concentrate and purify by column chromatography (petroleum ether: ethyl acetate = 9:1 to 3:1) to obtain compound 1.23 (white solid, 350 mg, yield: 82.8%).

[0044] 2) Preparation of compound (I-III)

[0045]

[0046] The compound 1.3 obtained in the previous step was dissolved in dichloromethane (35mL), potassium carbonate (5.8g, 42.2mmol) and dimethylamine hydrochloride (1.7g, 21.1mmol) were added to the system successively, and the mixed system was stirred and refluxed Reacted for 3 hours. After th...

Embodiment 3

[0050] Preparation of Compound IV

[0051]

[0052] 1) Preparation of Compound 1.4

[0053]

[0054] Compound 1.3 (112mg, 0.45mmol) was dissolved in dichloromethane (1mL), and a solution of peroxybenzoic acid (100mg, 0.60mmol) in dichloromethane (1mL) was slowly added dropwise to the above system, and reacted at room temperature for 2 hours , quenched the reaction with saturated sodium thiosulfate (2 mL), extracted with dichloromethane (2 mL×3), dried and concentrated, and purified by column chromatography (petroleum ether: ethyl acetate = 4:1 to 1:1) to obtain compound 1.4 ( White solid, 89 mg, yield: 74.5%).

[0055] 2) Preparation of compound (I-IV)

[0056]

[0057] The compound 1.4 obtained in the previous step was dissolved in dichloromethane (35mL), potassium carbonate (5.8g, 42.2mmol) and dimethylamine hydrochloride (1.7g, 21.1mmol) were added to the system successively, and the mixed system was stirred and refluxed Reacted for 3 hours. After the reaction, ...

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Abstract

The invention discloses an isoalantolactone derivative and application of salt of the isoalantolactone derivative in preparation of a medicine for treating thyroiditis, and provides an isoalantolactone derivative as shown in formula (I); salifying acid is inorganic acid or organic acid; the inorganic acid is selected from hydrofluoric acid, hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, nitric acid, phosphoric acid, carbonic acid, boric acid, seleninic acid, phosphomolybdic acid, phosphorous acid and sulphurous acid; the organic acid is selected from citric acid, maleic acid, D-malic acid, L-malic acid, DL-malic acid, L-lactic acid, D-lactic acid, DL-acid, oxalic acid, methanesulfonic acid, valeric acid, oleic acid, lauric acid, p-toluene sulfonic acid, 1-naphthalenesulfonic acid, 2-naphthalene sulfonic acid, phthalic acid, tartaric acid, malonic acid, succinic acid, fumaric acid, glycollic acid, mercaptan acid, glycine, sarcosine, sulfonic acid, nicotinic acid, methyl pyridine acid, isonicotinic acid, benzoic acid or substituted benzoic acid.

Description

[0001] Technical field: [0002] The present invention relates to inulin derivatives and their salts and their application and preparation. [0003] Background technique: [0004] Inula helenium is a plant of the genus Inula in the family Compositae, a perennial herb whose roots are used for medicinal purposes. It has the functions of invigorating the spleen and harmonizing the stomach, regulating qi and relieving depression, relieving pain and preventing miscarriage. It is used for chest and flank, abdominal distension and pain, vomiting and diarrhea, chest and flank contusion, pain in the chest and flank, restless fetal movement and other diseases. The volatile oil of inulin contains iso-inuricolide, iso-inuricolide and other components. Its chemical structure is similar to that of Sandonian, and it has anthelmintic effect on pigs, dogs, and cats. Its curative effect is better than that of Sandonian, and its toxicity is lower. Low. [0005] Isoacarina lactone (CAS: 470-17-7...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P5/14C07D307/92C07D493/10
Inventor 杨诚杨光孙涛周红刚艾笑羽高险盛彭真刘双伟王常骅卢聘
Owner NANKAI UNIV
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