104617-49-4Relevant articles and documents
Dopamine autoreceptor agonists: Resolution and pharmacological activity of 2,6-diaminotetrahydrobenzothiazole and an aminothiazole analogue of apomorphine
Schneider, Claus S.,Mierau, Joachim
, p. 494 - 498 (1987)
The enantiomers of the aminothiazole analogues of the known dopaminergic agonists apomorphine (1) and 2-aminohydroxytetralin (2) have been prepared. The absolute configurations of the enantiomers of 2,6-diaminotetrahydrobenzothiazole have been established by X-ray crystallographic analysis. Dopamine (DA) autoreceptor agonist activities of the compounds were evaluated. Testing revealed (-)-5, the S enantiomer, to be the most active compound tested (inhibition of GBL accelerated dopamine synthesis and inhibition of α-methyltyrosine-induced decline of DA). In addition (-)-5 does not exhibit stereotyped behavior, suggesting a pronounced selectivity for DA autoreceptors.
Preparation method of high-purity pramipexole
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Paragraph 0059-0061; 0068-0070, (2021/04/07)
The invention relates to the technical field of pharmacy, and provides a preparation method of high-purity pramipexole. According to the invention, raceme 2, 6-diamino 4, 5, 6, 7-tetrahydrobenzothiazole is used as an initial raw material, and pramipexole is obtained through a three-step chemical reaction, so the introduction of uncontrollable factors of drug quality is reduced, and the requirements of drug application are better met; the market price of the initial raw materials is low, so that the preparation cost of pramipexole can be greatly reduced; the solvent used in the method is green, environmentally friendly, cheap, easy to obtain and suitable for industrial production, the HPLC purity of the obtained pramipexole can reach 99.86%, and the isomer purity can reach 99.89%.
Industrial preparation method of 2,6-diamino-4,5,6,7-tetrahydro-benzothiazole
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Paragraph 0025-0045, (2020/07/15)
The invention discloses a preparation method of 2,6-diamino-4,5,6,7-tetrahydro-benzothiazole suitable for industrial production, wherein 2,6-diamino-4,5,6,7-tetrahydro-benzothiazole is prepared by using p-acetamido cyclohexanone as a raw material through a one-pot method. According to the method, liquid bromine and acetic acid are not used in the production and preparation process, the 6-acetamido-2-amino-4,5,6,7-tetrahydro-benzothiazole can be prepared through a one-pot method, post-treatment operation is easy and convenient, the labor cost is saved, and the production cost is greatly reduced. The 2,6-diamino-4,5,6,7-tetrahydro-benzothiazole prepared by the method is high in yield, good in purity and suitable for industrial production.
Alkali separation method of (S)-2,6-diamino-4,5,6,7-tetrahydrobenzothiazole * L-tartrate
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Paragraph 0023-0042, (2020/01/25)
The invention relates to an alkali precipitation method of (S)-2,6-diamino-4,5,6,7-tetrahydrobenzothiazole * L-tartrate, water is used as a solvent, and a mixed aqueous solution of sodium hydroxide and potassium hydroxide is dropped into an aqueous solution of (S)-2,6-diamino-4,5,6,7-tetrahydrobenzothiazole * L-tartrate to precipitate (S)-2,6-diamino-4,5,6,7-tetrahydrobenzothiazole. The method hasthe advantages that (1) the blazing slag residue of the obtained product can be reduced, and the quality level of the product is improved; (2) the amount of the reaction solvent water is reduced, thereby reducing the discharge amount of waste water and being beneficial to environmental protection; (3) Because the (S)-2,6-diamino-4,5,6,7-tetrahydrobenzothiazole is soluble in water, the loss of theproduct is reduced and the yield of the product is also improved after the amount of water is reduced.