2605-14-3Relevant articles and documents
Preparation method of 2-chloro-6-methoxybenzothiazole
-
Paragraph 0028; 0029; 0030, (2019/03/28)
The invention discloses a preparation method of 2-chloro-6-methoxybenzothiazole, and belongs to the field of medical intermediates. The method comprises the following steps: dissolving 2-amino-6-methoxybenzothiazole in an organic solvent, adding a hydrochloric acid solution, dropwise adding a sodium nitrite solution, and after completion of the reaction, adding a hydrochloric acid solution containing a catalyst, cooling, and recrystallizing to obtain a target product. The preparation method disclosed by the invention is simple, the raw materials are easy to obtain, the reagents and drugs usedin an operation process are relatively low in toxicity, reaction conditions are mild, the time is short, the yield is high, the cost is low, three wastes are little, and the target product is high incontent and high in purity, and the suitability for industrial production is achieved.
TYROSINE KINASE INHIBITOR AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
-
Paragraph 0326; 0327, (2018/03/25)
The present invention relates to a tyrosine kinase inhibitor and a pharmaceutical composition comprising same. The tyrosine kinase inhibitor of the present invention has the structures as shown in the following formula (I) or (II):
Synthesis and antibacterial evaluation of a novel series of 2-(1,2-dihydro-3-oxo-3H-pyrazol-2-yl)benzothiazoles
Stella, Alessandro,Segers, Kenneth,De Jonghe, Steven,Vanderhoydonck, Bart,Rozenski, Jef,Anne, Jozef,Herdewijn, Piet
experimental part, p. 253 - 265 (2011/09/30)
The 2-(1,2-dihydro-3-oxo-3H-pyrazol-2-yl)benzothiazole scaffold was selected as a central core structure for the discovery of novel antibacterial compounds. A systematic variation of the substituents on the oxo-pyrazole moiety, as well as on the benzo moiety, led to the creation of a small and focused library of benzothiazoles that was subjected to antibacterial screening. In a first round of screening, activity of the compounds against six representative microorganisms was established. For the most potent congeners, MIC values against S. aureus and P. aeruginosa were determined. The structure-activity relationship study clearly revealed that subtle structural variations influence the antibacterial activity to a large extent. The most potent congeners displayed MIC values of 3.30 μM.