892413-92-2Relevant academic research and scientific papers
Continued Exploration of Trifunctional Alkyl 4-Chloro-2-diazo-3-oxobutanoates: Streamlined Entry into [1,2,3]Triazolo[5,1- c ][1,4]benzoxazines and [1,2,3]Triazolo[5,1- c ][1,4]benzoxazepines
Budeev, Anton V.,Kantin, Grigory,Dar'In, Dmitry,Krasavin, Mikhail
, p. 2155 - 2166 (2021/02/22)
Further exploration of the trifunctional character of previously introduced alkyl 4-chloro-2-diazo-3-oxobutanoates in reactions with N -protected substituted o -aminophenols followed by deprotection provided a convenient entry into [1,2,3]triazolo[5,1- c ][1,4]benzoxazines, which are of high medicinal importance, as documented in the literature. The same approach applied to N -protected substituted o -(aminomethyl)phenols afforded [1,2,3]triazolo[5,1- c ][1,4]benzoxazepines, which are practically unexplored compounds from a medicinal chemistry perspective. The syntheses start with S N 2-type alkylation of the phenol. Removal of the protecting group triggers imine formation followed by Wolff 1,2,3-triazole synthesis.
An Expedient Synthesis of 2-Aryl-1,4-benzoxazin-3-ones via Tandem Anionic Cyclisation/Alkylation Reactions of N -Boc- O -benzyl-2-aminophenols
Bodero, Olga,Spivey, Alan C.
supporting information, p. 471 - 474 (2017/02/24)
A one-pot, tandem anionic cyclization/alkylation reaction of N-Boc-O-benzylated-2-aminophenols to give 2-aryl-1,4-benzoxazin-3-ones is described. The Boc protecting group plays a crucial role in the process, as the tert-butoxide liberated in the cyclisati
Compound containing benzo[b]thiophene structure, and derivative, preparation method and application
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Paragraph 0098; 0099; 0100, (2017/04/28)
The invention discloses a micromolecular organic compound as shown in a structural formula (I) and containing a benzo[b]thiophene structure and a micromolecular organic compound as shown in a structural formula (II) and containing a 3-bromobenzo[b]thiophe
DIHYDRO 1,4-BENZOXAZINES AND METHOD OF SYNTHESIZING THE SAME USING SULFONIUM SALTS
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Paragraph 0052; 0053, (2014/11/11)
Exemplary embodiments of the present invention relate to benzoxazines having various N-protecting groups. An R1 functional group is at least one selected from the group consisting of H and a halogen, an R2 functional group is at least one selected from the group consisting of H, an amide, or a carbamate, and a Z functional group is at least one selected from the group consisting of a phenyl, substituted phenyl group, methyl, and t-butyl group. The exemplary embodiments provide compounds with benzoxazines having various cleavable protecting groups such as amides and carbamates.
Pyrazolopyrrolidine compounds
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Page/Page column 212, (2013/06/27)
The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
NOVEL AROMATIC HETEROCYCLIC CARBOXYLIC ACID AMIDE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS
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Page/Page column 20; 23, (2009/01/20)
This invention relates to novel aromatic heterocyclic carboxylic acid amide derivatives of formula (I) that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse
2,4 (4,6) PYRIMIDINE DERIVATIVES
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Page/Page column 87, (2010/11/08)
The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z1 and Z2 represent NH; Y represents -C3-9alkyl-, -C3-9alkenyl-, -C1-5alkyl-NR6-C1-5alkyl-, -C1-5alkyl-NR7-CO-C1 -5alkyl-, -C1-6alkyl-CO-NH-, -C1-6alkyl-NH-CO-, -C1-2alkyl-CO-Het10-CO-, -C1-3alkyl-NH-CO-Het3-, -Het4-C1-3alkyl-CO-NH-C1-3alkyl-, -C1-2alkyl-NH-CO-L1-NH-, -NH-CO-L2-NH-, -C1-2alkyl-CO-NH-L3-CO-, -C1-2alkyl-NH-CO-L1-NH-CO-C1-3alkyl-, -C1-2alkyl-CO-NH-L3-CO-NH-C1-3alkyl-, -C1-2alkyl-NR11-CH2-CO-NH-C1-3alkyl-, Het5-CO-C1-2alkyl-, -C1-5alkyl-CO-NH-C1-3alkyl-CO-NH-, -C1-5alkyl-NR13-CO-C1-3alkyl-NH-, -C1-3alkyl-NH-CO-Het27-CO-, or -C1-3alkyl-CO-Het28-CO-NH-; X1 represents a direct bond, O, -O-C1-2alkyl-, -CO-C1-2alkyl-, -NR16-C1-2alkyl-, -CO-NR17-, Het23-C1-2alkyl- or C1-2alkyl; X2 represents a direct bond, O, -O-C1-2alkyl-, -CO-C1-2alkyl-, -NR18-C1-2alkyl-, -CO-NR19-, Het24-C1-2alkyl- or C1-2alkyl; R1 and R5 each independently represent hydrogen, halo, C1-6alkyloxy- or C1-6alkyloxy- substituted with Het1 or C1-4alkyloxy-; R2 and R4 each independently represent hydrogen or halo; R3 represents hydrogen or cyano; R6, R7, R13, R17 and R19represent hydrogen; R11 represents hydrogen or C1-4alkyl; R16and R18 represent hydrogen, C1-4alkyl or Het17-C1-4alkyl-; L1, L2 and L3each independently represents C1-8alkyl optionally substituted with one or where possible two or more substituents selected from phenyl, methylsulfide, cyano, polyhaloC1-4alkyl-phenyl-, C1-4alkyloxy, pyridinyl, mono- or di(C1-4alkyl)-amino- or C3-6cycloalkyl; Het1 , Het2, Het17 each independently represent morpholinyl, oxazolyl, isoxazolyl, or piperazinyl; Het3, Het4, Het5 each independently represent morpholinyl, piperazinyl, piperidinyl or pyrrolidinyl; Het10 represents piperazinyl, piperidinyl, pyrrolidinyl or azetidinyl; Het22 represents morpholinyl, oxazolyl, isoxazolyl or piperazinyl wherein said Het22 is optionally substituted with C1-4alkyl; Het23 and Het24 each independently represent a heterocycle selected from pyrrolidinyl, piperazinyl or piperidinyl wherein said Het23 or Het24 are optionally substituted with Het22-carbonyl; Het27 and Het28 each independently represent a heterocycle selected from morpholinyl, piperazinyl, piperidinyl or pyrrolidinyl.
