90407-28-6Relevant academic research and scientific papers
INHIBITORS OF CYCLIN DEPENDNT KINASE 7 (CDK7)
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Paragraph 494, (2018/02/28)
The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
7-Substituted Benzothiophenes and 1,2-Benzisothiazoles. Part 2. Chloro and Nitro Derivatives
Rahman, Loay K. A.,Scrowston, Richard M.
, p. 385 - 390 (2007/10/02)
The 7-chloro and 7-nitro derivatives of benzothiophene and 1,2-benzisothiazole have been prepared from readily available precursors, which for each substituent are common to both ring systems. 7-Chlorobenzothiophene has been obtained from 3-chloro-2-mercaptobenzoic acid via 7-chlorobenzothiophen-3(2H)-one, or from 2,3-dichlorobenzaldehyde, either via β-(2,3-dichlorophenyl)-α-mercaptoacrylic acid (16) or, preferably, via 7-chlorobenzothiophene-2-carboxylic acid.Hexamethylphosphoric triamide is a particularly useful solvent in which to effect the selective nucleophilic replacement of the 2-chloro substituent in 2,3-dichlorobenzaldehyde. 7-Chloro-1,2-benzisothiazole is available by treatment of 3-chloro-2-mercaptobenzaldehyde with chloramine (57percent), or by heating 2,3-dichlorobenzaldehyde with sulphur and aqueous ammonia (46percent). 7-Nitrobenzothiophene has been obtained by treatment of 2-bromo-3-nitrobenzaldehyde with mercaptoacetic acid under alkaline conditions, followed by decarboxylation of the resulting 2-carboxylic acid.Cyclisation of 2-(n- or t-butylthio)-3-nitrobenzaldoxime with polyphosphoric acid gives 7-nitro-1,2-benzisothiazole in high yield. 3-Nitro-2-t-bytylthiobenzaldehyde behaves unexpectedly with chloramine, to give what is believed to be 7-nitro-2-t-butyl-1,2-benzothiazolium chloride (24) (73percent).
