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Synthesis method for dapsone

A synthetic method, the technology of dapsone, applied in the field of medicinal chemistry, can solve the problems of slow reaction progress, unavailable reagents, high price, etc.

Inactive Publication Date: 2017-03-22
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The main disadvantage of this preparation method is that the reaction progress is slow, the reagents are not easy to get, and the price is expensive, and the final product is not easy to separate

Method used

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  • Synthesis method for dapsone
  • Synthesis method for dapsone
  • Synthesis method for dapsone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1: 4,4'-Dichlorodiphenylsulfone

[0016]

[0017] In a 100ml three-neck flask, add 11.26g (0.1mol) of compound I and 20.0ml of concentrated sulfuric acid, react at room temperature for 4 hours, TLC spotting test shows that the reaction is complete, add 20.0ml of pure water to precipitate a solid, filter it with a large amount of The filter cake was washed three times with pure water to obtain Compound II, which was dried overnight in a forced air oven at 40°C to obtain 27.29 g of a light yellow crystalline powder with a yield of 95.02%. MS(+1): 286.96.

Embodiment 2

[0018] Example 2: Dapsone

[0019]

[0020] Measure 50.0ml of ethanol into a 250ml three-neck flask, then slowly add 10.0g (40.27mmol) of 4,4'-dichlorodiphenyl sulfone, 4.30g (80.54mmol) of ammonium chloride solid, stir while adding, and then add 50.0ml of ethanol, heated and refluxed for 5 hours, TLC spotting test showed that the reaction was complete, 30ml of distilled water slowly quenched the reaction, stirred and lowered the temperature, waited for a large amount of solids to precipitate, filtered with suction, washed the filter cake with a small amount of ethanol three times, and blasted at 40 ℃ After drying, 7.9 g of white crystalline powder was obtained, yield: 91.9%. MS (+1): 249.30.

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Abstract

The invention belongs to the field of medical chemistry, and discloses a preparation method for dapsone, wherein the method comprises the following steps: with chlorobenzene as a raw material and sulfuric acid as a solvent, carrying out a dehydration reaction to obtain dichlorodiphenyl sulfone, and then adding an ammoniation reagent into the reaction system, to prepare dapsone. The dilute sulphuric acid is used as the solvent, no any ligand, no protection with inert gas or no separation is required, sodium hydrosulfite is added as a reducing agent, and dapsone can be prepared. The method can obviously improve the yield and quality of dapsone.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry and relates to a synthesis method of dapsone. Background technique [0002] Dapsone, chemical name 4,4'-sulfonyl dianiline, is used in combination with other leprosy inhibitors for the treatment of various types of leprosy and dermatitis herpetiformis caused by Mycobacterium leprae, and also for pustular dermatosis , pemphigoid, necrotizing pyoderma, relapsing polychondritis, granuloma annulare, certain skin lesions of systemic lupus erythematosus, actinomycetal mycomycosis, acne conglomerates, psoriasis, Treatment of herpes zoster. Pneumocystis may be treated in combination with trimethoprim. [0003] Its main preparation method is as follows at present: [0004] [0005] The main disadvantage of this preparation method is that the reaction progress is slow, the reagents are not easy to get, and the price is expensive, and the final product is not easy to separate. Contents of the inven...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C315/04C07C317/36
CPCC07C315/00C07C315/04C07C317/36C07C317/14
Inventor 李铁刘红悦赵国磊
Owner BEIJING VENTUREPHARM BIOTECH
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