- Preparation method of high-purity tinidazole
-
The invention discloses a synthetic preparation method of high-purity tinidazole, and belongs to the technical field of chemical pharmacy. The method includes: taking beta-hydroxyethyl sulfide and 2-methyl-5-nitroimidazole as the raw materials, using 4-methyl-2-pentanone as a solvent, conducting dehydration condensation under the action of concentrated sulfuric acid to obtain a condensation compound 2-methyl-1-(2-ethylthioethyl)-5-nitro-1H-imidazole, and then under the catalysis of sodium molybdate, performing oxidization to generate a tinidazole crude product; and decoloring and refining thecrude product with water to obtain a tinidazole finished product with purity of greater than or equal to 99.98%. Compared with the prior art, the raw materials are easy to obtain, reaction is simple,and operation is easy and convenient; meanwhile, the incompletely reacted 2-methyl-5-nitroimidazole and the recycled 4-methyl-2-pentanone can be directly applied mechanically, so that the production cost is effectively reduced, the reaction period is shortened, pollution is reduced, and the yield and the product quality are improved.
- -
-
Paragraph 0021; 0022-0024; 0026-0027; 0028-0030; 0031-0032
(2020/10/04)
-
- Sulfoxide and sulfone compounds, as well as selective synthesis method and application thereof
-
The invention discloses a method for selectively synthesizing a sulfoxide compound shown as a formula (II) and a sulfone compound shown as a formula (III). In a reaction solvent, thioether (I) is usedas a reaction raw material and oxygen as an oxidation reagent, under the catalytic action of visible light and a photosensitive reagent; under the assistance of an additive, when a large-polarity proton-containing additive such as an acid and an alcohol or a solvent or an additive with excellent electron donating ability is used, a sulfoxide compound (II) is selectively generated; and when a small-polarity aprotic additive or a solvent is used, a sulfone compound (III) is selectively generated. The synthesis method has the advantages of easily available and cheap raw materials, simple reaction operation, mild reaction conditions, high yield and excellent functional group tolerance. According to the invention, synthesis and modification of some medicines are realized, and an efficient method for selectively constructing sulfoxide and sulfone compounds is provided for medicinal chemistry research.
- -
-
Paragraph 0049-0052; 0150-0153
(2019/12/02)
-
- Synthesis method of tinidazole
-
The invention belongs to the field of chemical pharmaceutical synthesis, and particularly relates to a synthesis method of tinidazole. According to the synthesis method of tinidazole, ethyl 2-hydroxyethyl sulfide and 2-methyl-5-nitroimidazole are used as raw materials, toluene is used as a solvent, a condensation reaction is carried out under the action of aluminum trichloride, quenching and filtration are carried out to obtain a condensate, and then the condensate is oxidized by dropwise adding hydrogen peroxide under catalysis of sodium molybdate to obtain a tinidazole crude product. In themethod, toluene is used as the solvent, aluminum trichloride is used as a dehydrating agent, sodium molybdate is used as an oxidation catalyst, the solvent is cheap and can be recycled, the cost is saved, and three wastes are reduced.
- -
-
Paragraph 0028-0047
(2020/01/08)
-
- Selective Late-Stage Oxygenation of Sulfides with Ground-State Oxygen by Uranyl Photocatalysis
-
Oxygenation is a fundamental transformation in synthesis. Herein, we describe the selective late-stage oxygenation of sulfur-containing complex molecules with ground-state oxygen under ambient conditions. The high oxidation potential of the active uranyl cation (UO22+) enabled the efficient synthesis of sulfones. The ligand-to-metal charge transfer process (LMCT) from O 2p to U 5f within the O=U=O group, which generates a UV center and an oxygen radical, is assumed to be affected by the solvent and additives, and can be tuned to promote selective sulfoxidation. This tunable strategy enabled the batch synthesis of 32 pharmaceuticals and analogues by late-stage oxygenation in an atom- and step-efficient manner.
- Li, Yiming,Rizvi, S. Aal-e-Ali,Hu, Deqing,Sun, Danwen,Gao, Anhui,Zhou, Yubo,Li, Jia,Jiang, Xuefeng
-
supporting information
p. 13499 - 13506
(2019/08/21)
-
- External preparation for skin diseases containing nitroimidazole
-
An external preparation for skin disease which comprises a nitroimidazole derivative represented by the following formula (I): wherein R1, R3 and R4 may be the same or different and represent a hydrogen atom, a nitro group, a lower alkyl group, a substituted lower alkyl group, a lower alkenyl group, or a substituted lower alkenyl group; and R2 represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group and a lower alkenyl group or a substituted lower alkenyl group, provided that any one of R1, R3 and R4 is a nitro group.
- -
-
-
- Chemical compounds having ion channel blocking activity for the treatment of immune dysfunction
-
The present invention relates to chemical compounds having inhibitory activity on an intermediate conductance Ca 2+ activated potassium channel (IK Ca), and the use of such compounds for the treatment or alleviation of diseases or conditions relating to immune dysfunction. Moreover, the invention relates to a method of screening a chemical compound for inhibitory activity on an intermediate conductance Ca 2+ activated potassium channel (IK Ca).
- -
-
-
- Process for production of 5-nitroimidazole derivatives
-
A process for preparing 5-nitroimidazole compounds of STR1 where R and R1 are each alkyl from 1 to 4 carbon atoms, A is oxygen and n is 1, allowing for improved yields of the final products, is described.
- -
-
-
- Treatment of rheumatoid arthritis and related diseases
-
It is believed that rheumatoid arthritis and related collagen and auto-immune diseases are an infection and that various species of free-living (limax) amoebae are the aetiological agent of these diseases. It has been discovered that tinidazole and related compounds, antimycotic drugs with anti-protozoal activity, are effective for the treatment of rheumatoid arthritis and other collagen and auto-immune (rheumatoid) diseases.
- -
-
-