- Method for synthesizing benzothiazole by microwave radiation of benzothioamide compound in aqueous phase
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The invention discloses a method for synthesizing benzothiazole by microwave radiation of a benzothioamide compound in an aqueous phase. The method includes the steps: adding the benzothioamide compound into the aqueous phase under microwave conditions; performing cyclization under alkaline conditions to generate the benzothiazole. The method for preparing the benzothiazole is environmentally friendly, simple and convenient in operation, safe, cheap and efficient. Compared with the prior art, the method is applicable to a lot of functional groups, high in yield, few in by-products, simple in operation, safe, low in cost and environmentally friendly.
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Paragraph 0013; 0073
(2019/02/13)
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- STK4 INHIBITORS FOR TREATMENT OF HEMATOLOGIC MALIGNANCIES
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The application relates to compounds of Formula (I'): which modulate the activity of a kinase (e.g., STK4), a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease or disorder associated with the modulation of a kinase, such as STK4.
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- Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)- thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors
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4-(1,3-Benzothiazol-2-yl)thiophene-2-sulfonamide (4a) was found to be a moderately potent inhibitor of cyclin-dependent kinase 5 (cdk5) from a HTS screen. The synthesis and SAR around this hit is described. The X-ray coordinates of ligand 4a with cdk5 are also reported, showing an unusual binding mode to the hinge region via a water molecule.
- Malmstroem, Jonas,Viklund, Jenny,Slivo, Can,Costa, Ana,Maudet, Mickael,Sandelin, Catrin,Hiller, Goesta,Olsson, Lise-Lotte,Aagaard, Anna,Geschwindner, Stefan,Xue, Yafeng,Vasaenge, Mervi
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p. 5919 - 5923
(2012/11/07)
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- New Compounds Useful for Treating CNS Disorders
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The present invention provides new compounds of formula (I) as well as a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds
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Page/Page column 1
(2011/05/05)
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- INHIBITORS OF JUN N-TERMINAL KINASE
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The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula (I): or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
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Page/Page column 103
(2010/08/18)
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