392-24-5Relevant articles and documents
2-(2-ACRYLOYL-2,6-DIAZASPIRO[3.4]OCTAN-6-YL)-6-(1H-INDAZOL-4-YL)-BENZONITRILE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF G12C MUTANT KRAS PROTEIN FOR INHIBITING TUMOR METASTASIS
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Page/Page column 141, (2020/05/28)
The present invention provides e.g. 2-(2-acryloyl-2,6- diazaspiro[3.4]octan-6-yl)-6-(lH-indazol-4-yl)-benzonitrile and e.g. 2-(2-acryloyl-2,7-diazaspiro[3.5]nonan-7-yl)-6-(1H-indazol-4-yl)- benzonitrile derivatives and related compounds of formula (I) as inhibitors of G12C mutant KRAS protein for treating tumor metastasis. The present description discloses exemplary compounds (e.g. pages 53 to 90; table 1; compounds I-1 to I-141), pharmacological data (e.g. page 125 to 128; table 2; example 1) and synthesis thereof (e.g. pages 129 to 143; examples 2 to 7). Exemplary compounds are e.g. 2-(2-acryloyl-2,6- diazaspiro[3.4]octan-6-yl)-6-(5-methyl-1H-indazol-4-yl)-4- morpholinobenzonitrile (example 2; compound I-1) and 6-(2- acryloyl-2,7-diazaspiro[3.5]nonan-7-yl)-3-methoxy-2-(5-methyl-1H- indazol-4-yl)-4-morpholinobenzonitrile (example 7; compound I-84).
Formation of Nonaromatic Products in the Chlorination of Simple Substituted Aromatic Ethers
Watson, William David
, p. 5270 - 5276 (2007/10/02)
The neat chlorination of 4-chloroanisole produces 1,3,4,5,6-pentachloro-4-methoxycyclohexene in 35percent yield.Mono- and dichlorinated anisoles and a variety of simple substituted anisoles were chlorinated to determine the generality of nonaromatic product formation. 3,4-Dichloroanisole, 4-fluoroanisole, 4-bromoanisole, 4-methylanisole, and 4-chlorophenetole form similar products based on their spectral properties.These products are proposed to form by a cis-1,2-chlorine addition followed by rapid cis-1,4 chlorine addition.On the basis of the NMR data, a predominate configuration is proposed.