19155-24-9Relevant articles and documents
Quinazolinones. I. Synthesis of indolo[2,1-b]quinazolinones
Domanig
, p. 271 - 276 (1981)
-
Dirhodium(ii) tetraacetate catalysed reactions of diazo thioamides: Isolation and cycloaddition of anhydro-4-hydroxy-1,3-thiazolium hydroxides (thioisomuenchnones), an approach to analogues of dehydrogliotoxin
Moody, Christopher J.,Slawin, Alexandra M.Z.,Willows, David
, p. 2716 - 2722 (2003)
Dirhodium(II) tetraacetate catalysed reaction of the indoline diazo thioamide 8 gives the thioisomuenchnone 9, a stable characterisable solid. This masked thiocarbonyl ylide undergoes 1, 3-dipolar cycloaddition with N-methylmaleimide and maleic anhydride to give the exo-cycloadducts 10 and 11, characterised by X-ray crystallography. The thioisomuenchnone 18, derived from diazo thioamide 17, is an extremely stable crystalline mesoionic system which can be characterised by X-ray crystallography but fails to undergo intramolecular cycloaddition. The related thioisomnchnone 19 can be generated by reaction of indoline-2-thione 7 with bromoacetyl chloride in the presence of triethylamine, and undergoes cycloaddition, to give adducts 20 and 21.
Influenza virus replication inhibitors and uses thereof
-
Paragraph 0333-0337, (2021/07/01)
The invention belongs to the field of medicines, and particularly relates to novel compounds serving as an influenza virus replication inhibitor, a preparation method thereof, a pharmaceutical composition containing the compounds and application of the compounds and the pharmaceutical composition in treatment of influenza. The compounds are compounds as shown in a formula (I) or a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrugs of the stereoisomer, the tautomer, the nitrogen oxide, the solvate, the metabolite and the pharmaceutically acceptable salt of the compound as shown in the formula (I). The compounds not only can well inhibit influenza viruses, but also have lower cytotoxicity, excellent in-vivo pharmacokinetic property and the in-vivo pharmacodynamic property and good liver microsome stability.
NOVEL COMPOUNDS USEFUL AS POLY(ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS
-
Paragraph 216, (2021/11/06)
The present invention provides novel poly(ADP-ribose) polymerase (PARP) inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods for the treatment, prevention and/or amelioration of PARP mediated diseases or disorders using them. In particular, the compounds described herein are useful for the treatment of carcinoma of the breast, ovarian cancer, carcinoma of the liver, carcinoma of the lung, small cell lung cancer, esophageal cancer, gall bladder cancer, pancreatic cancer and stomach cancer.
NovelN-transfer reagent for converting α-amino acid derivatives to α-diazo compounds
Lu, Guan-Han,Huang, Tzu-Chia,Hsueh, Hsiao-Chin,Yang, Shin-Cherng,Cho, Ting-Wei,Chou, Ho-Hsuan
supporting information, p. 4839 - 4842 (2021/05/25)
A novel universalN-transfer reagent for direct and effective transformation of α-amino ketones, acetamides, and esters to the corresponding α-diazo products under mild basic conditions has been developed. This one-step synthetic approach not only allows for generation of α-substituted-α-diazo carbonyl compounds from α-amino acid derivatives but also permits preparation of α-diazo dipeptides fromN-terminal dipeptides (32 examples, up to 91%).