764650-43-3Relevant academic research and scientific papers
Small Molecule Inhibitors of KRAS G12C Mutant
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Paragraph 0455-0456, (2021/04/30)
The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, M, L, Cy, Cz, R1, R2, R3, R4, R2a, Rs
DEUTERATED N-(5-(2,3-DIHYDROBENZO[B][1,4]DIOXINE-6-CARBOXAMIDO)-2-FLUOROPHENYL)-2-((4-ETHYLPIPERAZIN-1 -YL)METHYL)QUINOLINE-6-CARBOXAMIDE
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Paragraph 00224-00225, (2018/04/21)
The present invention relates to N-(5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-fluorophenyl)-2-((4-ethylpiperazin-1-yl)methyl)quinoline-6-carboxamide, or a pharmaceutically acceptable salt or solvate thereof, wherein at least one hydrogen atom ha
HYDROXYETHYLAMINO SULFONAMIDE DERIVATIVES
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Page/Page column 44-45, (2010/05/13)
This invention relates to novel hydroxyethylamino sulfonamides and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound with the ability to act as an HIV (human immunodeficiency virus) protease inhibitor.
Syntheses of D-labelled oxidative metabolites of acrylamide and acrylonitrile for the quantification of their toxicities in humans
Belov, Vladimir N.,Korneev, Sergei M.,Angerer, Juergen,De Meijere, Armin
scheme or table, p. 4417 - 4425 (2009/05/07)
Syntheses of the labelled oxidative metabolites of acrylamide and acrylonitrile - reference compounds for the evaluation of human exposure to important toxicants - are reported. For that, L-cystine tert-butyl ester was acetylated and the product reductively cleaved to L-cysteine tert-butyl ester, which reacted with carbamoyl[D3]oxirane (obtained from [D 3]acrylonitrile and 30% aq. H2O2 at pH = 7.0-7.5) and afforded a separable mixture of tert-butyl N-acetyl-S-(2-hydroxy-2- carbamoyl[ D3]ethyl)cysteinate and tert-butyl N-acetyl-S-(1- carbamoyl-2-hydroxy[D3]ethyl)cysteinate (ca. 9:1). Removal of the tert-butyl group in these intermediates with aq. HCl gave the final deuterated internal standards with carbamoyl residues. Protection of the secondary hydroxy group in the major intermediate with tBuMe2SiCl/imidazole in DMF followed by dehydration of the carbamoyl group (trifluoroacetic anhydride/pyridine in CH2Cl2) and stepwise removal of the tert-butyl and tBuMe2Si protecting groups (TFA, Et3SiH, CH2Cl2; aq. HF in MeCN) yielded N-acetyl-S-(2-cyano-2- hydroxy[D3]ethyl)cysteine. Monoprotection of [D4]ethylene glycol with tBuMe2SiCl and NaH in THF, oxidation to tBuMe 2SiOCD2CDO, conversion to tBuMe2SiOCD 2CD(OH)CN and tBuMe2SiOCD2CD(OTs)CN followed by nucleophilic substitution of the tosyloxy group with N-acetyl-L-cysteine (MeOD, Et3N) and deprotection with 4 M HCl in dioxane resulted in N-acetyl-S-(1-cyano-2-hydroxy[D3]ethyl)cysteine. All transformations (except the last but one) gave the respective products in good yields. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
