Substituted Benzylidene-3-Oxo-3,4-Dihydro-2H-Benzo[b][1,4]thiazine-6-Carboxylic Acid Analogs as Dynamin GTPase Inhibitors.
Sign Up to like & getrecommendations! Published in 2025 at "ChemMedChem"
DOI: 10.1002/cmdc.202500377
Abstract: Screening identified 2‐hydroxy‐3‐oxo‐3,4‐dihydro‐2H‐benzo[b][1,4]oxazine‐6‐carboxylic acid (1) as a 55 µM dynaminGTPase inhibitor. Synthesis of three 1‐based libraries shows no potency enhancement. However, S‐isostere‐based 3‐oxo‐3,4‐dihydro‐2H‐benzo[b][1,4]thiazine‐6‐carboxylic acid (16) gives rise to Libraries 4–6. Library 4 retains the C6‐ester of… read more here.
Keywords: carboxylic acid; benzo thiazine; oxo dihydro; dihydro benzo ... See more keywords
Synthesis of New Derivatives of 4-(4,7,7-Trimethyl-7,8-dihydro-6H-benzo [b]pyrimido[5,4-e][1,4]thiazin-2-yl)morpholine
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Heterocyclic Chemistry"
DOI: 10.1002/jhet.2556
Abstract: Cyclocondensation of 5-amino-6-methyl-2-morpholinopyrimidine-4-thiol (1) and 2-bromo-5,5-dimethylcyclohexane-1,3-dione (2) under mild reaction condition afforded 4,7,7-trimethyl-2-morpholino-7,8-dihydro-5H-benzo[b]pyrimido[5,4-e][1,4]thiazin-9(6H)-one (3). The 1H and 13C NMR data of compound (3) are demonstrated that this compound exists primarily in the enamino ketone form.… read more here.
Keywords: benzo pyrimido; trimethyl dihydro; pyrimido thiazin; dihydro benzo ... See more keywords
Carbon-based leaving group capability of Meldrum’s acid in substitution reactions: a new strategy toward the synthesis of 4-phenyl-3, 4-dihydro-2H-benzo[g]chromene-2, 5, 10-triones
Sign Up to like & getrecommendations! Published in 2017 at "Journal of the Iranian Chemical Society"
DOI: 10.1007/s13738-017-1129-6
Abstract: An efficient and straightforward method for the synthesis of new 5,5′-(2-benzylidenemalonyl)bis(2,2-dimethyl-1,3-dioxane-4,6-dione) derivatives by the reaction of Meldrum’s acid and aldehydes under mild reaction conditions is reported. Furthermore, the leaving group potency of Meldrum’s acid molecules… read more here.
Keywords: leaving group; meldrum acid; toward synthesis; synthesis ... See more keywords
Synthesis and structure activity relationships of DCLK1 kinase inhibitors based on a 5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one scaffold.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c00596
Abstract: Doublecortin-like kinase 1 (DCLK1) is a serine/threonine kinase that is overexpressed in gastrointestinal cancers, including esophageal, gastric, colorectal and pancreatic cancers. DCLK1 is also used as a marker of tuft cells, which regulate Type II… read more here.
Keywords: activity relationships; benzo pyrimido; kinase; structure activity ... See more keywords
In(OTf)3-Catalyzed Synthesis of 2,3-Dihydro-1H-benzo[e]indoles and 2,3-Dihydrobenzofurans via [3 + 2] Annulation.
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DOI: 10.1021/acs.orglett.0c02729
Abstract: An In(OTf)3-catalyzed intermolecular [3 + 2] annulation for the synthesis of 2,3-dihydro-1H-benzo[e]indoles and 2,3-dihydrobenzofurans from readily available substrates has been achieved. This approach takes advantage of oxetane and para-quinone methide as important functional units in… read more here.
Keywords: indoles dihydrobenzofurans; otf catalyzed; annulation; benzo indoles ... See more keywords
Temperature Tunable Synthesis of Tetrahydro-4H-pyrrolo[3,2-c]quinolin-4-ones and Dihydro-1H-benzo[b]azepines from 2-Aminobenzonitriles and Donor-Acceptor Cyclopropanes.
Sign Up to like & getrecommendations! Published in 2022 at "Organic letters"
DOI: 10.1021/acs.orglett.2c03674
Abstract: Tetrahydro-4H-pyrrolo[3,2-c]quinolin-4-ones and dihydro-1H-benzo[b]azepines are efficiently synthesized from 2-aminobenzonitriles and donor-acceptor cyclopropanes mediated by SnCl4 in moderate to good yields. The reaction involves the initial ring opening of a cyclopropane ring due to activation by SnCl4… read more here.
Keywords: tetrahydro pyrrolo; ones dihydro; benzo azepines; dihydro benzo ... See more keywords
Dual Pathways, One Framework: Theoretical Insights into the Benzimidazole × Benzodiazepine Crossroads from o‑Phenylenediamine and 2‑Cyanoacrylate Derivatives
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DOI: 10.1021/acsomega.5c05925
Abstract: Ketene dithioacetals represent a significant class of molecules with a pivotal role in organic synthesis, particularly as versatile building blocks for the development of novel pharmaceutical compounds. We employed density functional theory (DFT) calculations in… read more here.
Keywords: framework theoretical; dihydro benzo; dual pathways; one framework ... See more keywords
Efficient Synthesis of 7,8-Dihydro-6H-benzo[c]chromen-6-one Derivatives by Base-Mediated Chemoselective Annulation of Alkylidene Malononitriles with α,β-Unsaturated Coumarins
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DOI: 10.1055/s-0040-1706012
Abstract: An efficient and chemoselective synthesis of biologically valuable 7,8-dihydro-6H-benzo[c]chromen-6-ones is described. In this method, neither a metal catalyst nor expensive starting materials are needed, and the products can be purified by simple filtration and washing… read more here.
Keywords: benzo chromen; dihydro benzo; efficient synthesis;
New method for the synthesis of 4-aryl-3,4-dihydro-2H-benzo[g]chromene-2,5,10-triones
Sign Up to like & getrecommendations! Published in 2019 at "Synthetic Communications"
DOI: 10.1080/00397911.2019.1646286
Abstract: Abstract We report herein a new method for the synthesis of 4-aryl-3,4-dihydro-2H-benzo[g]chromene-2,5,10-triones 4 that proceeds in good yields (74–86%) and mild reaction conditions between readily available 2-amino-4-aryl-5,10-dioxo-5,10-dihydro-4H-benzo[g]chromene-3-carbonitriles 1, and formic acid (88%), at reflux for… read more here.
Keywords: benzo chromene; aryl; dihydro benzo;
A facile approach to the synthesis of 3,4-dihydro-2H-benzo[4,5]imidazo[2,1-b][1,3,4]thiadiazines
Sign Up to like & getrecommendations! Published in 2024 at "Journal of Sulfur Chemistry"
DOI: 10.1080/17415993.2024.2394627
Abstract: An efficient approach to the synthesis of novel 2,3-diaryl-3,4-dihydro-2H-benzo[4,5]imidazo[2,1-b][1,3,4]thiadiazines via a base-catalyzed intramolecular cyclization of 2-arylmethylthio-N-arylidene-1H-benzo[d]imidazol-1-amines has been developed. The use of alkali is critical for the annulation of the thiadiazine ring. In the absence… read more here.
Keywords: dihydro benzo; approach synthesis; benzo imidazo; benzo ... See more keywords
2-[(4-Chlorophenyl)selanyl]-3,4-dihydro-2H-benzo[h]chromene-5,6-dione: crystal structure and Hirshfeld analysis
Sign Up to like & getrecommendations! Published in 2017 at "Acta Crystallographica Section E: Crystallographic Communications"
DOI: 10.1107/s2056989017007605
Abstract: A step-like conformation about the pyranyl ring is found for the molecular structure of the title compound. The three-dimensional packing is sustained by π–π, C—Cl⋯π and C—H⋯O interactions. read more here.
Keywords: selanyl dihydro; chromene dione; benzo chromene; chlorophenyl selanyl ... See more keywords