Category: 924-99-2

Skugor, Maja Matanovic published the artcileSynthesis and biological activity of 4”-O-acyl derivatives of 14- and 15-membered macrolides linked to ω-quinolone-carboxylic unit, Name: Ethyl 3-(dimethylamino)acrylate, the publication is Bioorganic & Medicinal Chemistry (2010), 18(17), 6547-6558, database is CAplus and MEDLINE.

The synthesis and antimicrobial activity of a new class of macrolide antibiotics which consist of a macrolide scaffold and a quinolone unit covalently connected by an appropriate linker are described. Optimization of several synthetic steps and structural properties of lead compound 26 are discussed. Promising antibacterial properties of this compound and some of its analogs are reported.

Bioorganic & Medicinal Chemistry published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C9H17NO, Name: Ethyl 3-(dimethylamino)acrylate.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Gompper, Rudolf published the artcileThe allopolarization principle and its applications. 1. Acceptor-substituted allyl cations as ambifunctional electrophiles, Formula: C7H13NO2, the publication is Angewandte Chemie (1978), 90(10), 808-10, database is CAplus.

Vinamidinium salts [I; R = H, Me, Ph, CO₂Et, CO₂Me; R¹ = H, Me, Ph, Me₂N, Cl; R² = CO₂Et, CO₂Me, COPh, (MeO)₂CH] are stable to hydrolysis at room temperature Treatment of I [R = R¹ = H; R² = CO₂Et, COPh (II and III)] with NaBH₄ yields R²C(NMe₂):CHCH₂NMe₂ (R² = CO₂Et, COPh). R²C(NMe₂):CHCH:CPhCN (R² as above) are prepared by reaction of II and III with benzyl cyanide (EtOH/NaOEt). II reacts with [PhCH:NCHCO₂Et]^– K⁺ to yield IV.

Angewandte Chemie published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C7H13NO2, Formula: C7H13NO2.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Yu, Lu published the artcileRegio- and Enantioselective Formal Hydroamination of Enamines for the Synthesis of 1,2-Diamines, Computed Properties of 924-99-2, the publication is Angewandte Chemie, International Edition (2019), 58(25), 8551-8555, database is CAplus and MEDLINE.

The asym. formal hydroamination of enamines using a CuH catalyst is reported [e.g., enamine I + O-acylhydroxylamine II â†?diamine III (69%, 97:3 e.r.) in presence of (MeO)₂MeSiH as hydride source, Cu(OAc)₂ and (R)-DTBM-SEGPHOS]. The method provides a straightforward and efficient approach to the synthesis of chiral 1,2-dialkyl amines in good yields with high levels of enantioselectivities for a broad range of substrates, and should have significant value for the preparation of mols. bearing a 1,2-diamine motif.

Angewandte Chemie, International Edition published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C12H10O4S, Computed Properties of 924-99-2.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Yang, Feng V. published the artcileParallel synthesis of N-biaryl quinolone carboxylic acids as selective M₁ positive allosteric modulators, SDS of cas: 924-99-2, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(2), 531-536, database is CAplus and MEDLINE.

An iterative analog library synthesis approach was employed in the exploration of a quinolone carboxylic acid series of selective M₁ pos. allosteric modulators, and strategies for improving potency and plasma free fraction were identified.

Bioorganic & Medicinal Chemistry Letters published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C18H10F3NO3S2, SDS of cas: 924-99-2.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Zhu, Yun-fei published the artcileSynthesis of 5-amino-1-cyclopropyl-7-[3,5-dimethyl-1-piperazinyl]-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid (sparfloxacin), COA of Formula: C7H13NO2, the publication is Zhongguo Xinyao Zazhi (2008), 17(9), 757-759, database is CAplus.

A method for the synthesis of the title compound [i.e., 5-amino-1-cyclopropyl-7-(3,5-dimethyl-1-piperazinyl)-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid, fluoroquinolone antibacterial agent] is reported here. Said compound was prepared from 2,3,4,5-tetrafluorobenzoic acid via nitration and acyl chlorination before coupling with Et (dimethylamino)acrylate, cyclopropylamine displacement, cyclization, reduction, hydrolysis and condensation with 2,6-dimethylpiperazine. The overall yield was 34.2%. Compared to a known process, this synthetic sequence eliminates three reaction steps; di-Et malonate condensation, partial hydrolysis decarboxylation and tri-Et orthoformate condensation. Said process has advantages, such as short reaction time, mild reaction conditions, waste reduction, yield increase, and a good prospect for industrial application.

Zhongguo Xinyao Zazhi published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C5H10N2OS, COA of Formula: C7H13NO2.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Swellmeen, Lubna published the artcileStructure based drug design of Pim-1 kinase followed by pharmacophore guided synthesis of quinolone-based inhibitors, Name: Ethyl 3-(dimethylamino)acrylate, the publication is Bioorganic & Medicinal Chemistry (2017), 25(17), 4855-4875, database is CAplus and MEDLINE.

Over expression of Human phosphatidylinositol mannoside kinases isoform 1 (Pim-1 kinase) has been reported in several leukemia and solid tumors. The authors’ continuous interest to reveal the secrecies of the mysterious Pim-1 kinase binding pocket has led the authors to employ a structure based drug design procedure based on receptor-ligand pharmacophore generation protocol implemented in Discovery Studio 4.5 (DS 4.5). Subsequently, the authors collected 104 crystal structures of Pim-1 kinase from the Protein Data Bank (PDB) and used them to generate pharmacophores based on the anticipated co-crystallized ligand-Pim 1 kinase receptor interactions. All selected pharmacophoric features were enumerated and only those that had corresponding valuable receptor-ligand interactions were retained. This was followed by modeling all pharmacophore combinations and scoring them according to their Receiver Operating Characteristic (ROC) curve anal. parameters as well as a DS.4.5 built-in Genetic Function Algorithm (GFA) validating model. Accordingly, 111 pharmacophores resulted with acceptable ROC performances; 1XWS_2_04, 2BIK_2_06, and 1XWS_2_06 (ROC AUC value of: 0.770, 0.743 and 0.741 resp.) were the best pharmacophores. These pharmacophores were employed to guide the synthesis of new series of 7-[(2-Carboxyethyl)amino]-1-substituted-6-fluoro-8-nitro-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid and their reduced 8-amino derivatives The synthesized compounds were later evaluated for their Pim-1 kinase inhibitory potencies. Of which the most potent illustrated an IC₅₀ value of 0.29 μM against Pim-1 kinase.

Bioorganic & Medicinal Chemistry published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C12H6NNaO4, Name: Ethyl 3-(dimethylamino)acrylate.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Al-Hiari, Yusuf M. published the artcileSynthesis and biological evaluation of substituted tetrahydro-1H-quino[7,8-b][1,4]benzodiazepine-3-carboxylic derivatives, Computed Properties of 924-99-2, the publication is Farmacia (Bucharest, Romania) (2014), 62(3), 570-588, database is CAplus.

This research paper aims the preparation of substituted tetrahydroquino[7,8-b][1,4]benzodiazepine-3-carboxylic acids I (R = F, Me, H₂N). Reaction of 7-chloro-1-cyclopropyl-6-fluoro-8-nitro-1,4-dihydroquinoline-3-carboxylic acid with each of 2-amino-5-methylbenzoic acid, 2-amino-5-flourobenzoic acid, and 2-amino-5-nitrobenzoic acid yielded 8-nitro-7-substituted anilino-1,4-dihydroquinoline-3-carboxylic acids with low yields. Reduction of 8-nitro-7-substituted anilino-1,4-dihydroquinoline-3-carboxylic acids with sodium dithionite or stannous chloride resulted in the production of 8-amino-7-substituted aniline-1,4-dihydro-quinoline-3-carboxylic acids II. Polyphosphoric acid (PPA) catalyzed thermal lactamization of 8-amino-7-substituted aniline-1,4-dihydro-quinoline-3-carboxylic acids resulted in the production of I. The prepared targets and the intermediates have shown interesting antibacterial activity mainly against gram pos. strains. In particular, the reduced intermediates II showed good activity against standard S. aureus (MIC = 0.05 – 0.19 μg/mL). Intermediates II have also shown reasonable activity against resistant gram pos. strains. The targets I (R = F, H₂N) have comparable activity to the reference against standard gram pos. strains.

Farmacia (Bucharest, Romania) published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C7H13NO2, Computed Properties of 924-99-2.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Porter, Jacob published the artcileA novel, unusual acid catalyzed route to substituted 1,4-dihydropyridine via double decarboxylation, HPLC of Formula: 924-99-2, the publication is Letters in Organic Chemistry (2011), 8(9), 610-613, database is CAplus.

A simple and high yield route to 3,4,5-trisubstituted 1,4-dihydropyridine systems via an interesting intermol. condensation and double decarboxylation is described. Thus, in presence of AcOH, reaction of (E)-EtO₂CCH:CHNHBn and di-Et (ethoxymethylene)malonate gave 1,4-dihydropyridine derivative (I).

Letters in Organic Chemistry published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C7H13NO2, HPLC of Formula: 924-99-2.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Netz, Astrid published the artcileFacial diastereoselectivity in cationic propargylations with planar-chiral areneCr(CO)₃-substituted propargyl cations, Application In Synthesis of 924-99-2, the publication is European Journal of Organic Chemistry (2005), 1823-1833, database is CAplus.

The planar-chiral (o-methoxyphenyl)chromium tricarbonyl-substituted propargyl cation reacts with silyl enol ether derivatives with poor and with enamines with good facial diastereoselectivity to give rise to the (arene)carbonylchromium-substituted propargylated cyclohexan-2-ones, and carboxylic acid, γ-lactone, cyclopentan-2-one, and esters. Structural correlations were unambiguously deduced from x-ray structure. The origin of facial diastereoselectivity with this class of organometallic electrophiles lies in steric and stereoelectronic biases rather than in purely electronic nucleophilicity.

European Journal of Organic Chemistry published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C7H13NO2, Application In Synthesis of 924-99-2.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Bailie, Alexandra E. published the artcileSynthesis of quinolone antibiotic analogues: a multistep synthetic chemistry experiment for undergraduates, Related Products of esters-buliding-blocks, the publication is Journal of Chemical Education (2021), 98(10), 3333-3340, database is CAplus.

A multistep synthesis of quinolone antibiotic analogs was developed as a laboratory experiment for intermediate/advanced undergraduate students. Students can synthesize a range of desfluoroenoxacin analogs via a five-step sequence. The experiment includes a range of key practical laboratory techniques including thin-layer chromatog. (TLC), liquid-liquid extraction, trituration, recrystallization and the characterization of compounds by IR and NMR spectroscopy. The experiment provides an opportunity for students to carry out fundamental organic chem. transformations from the curriculum such as the preparation of acyl chlorides, 1,4-conjugate addition-elimination, heterocycle synthesis, nucleophilic aromatic substitution and ester hydrolysis. The five-step sequence does not require column chromatog. and can be adapted to a range of laboratory settings.

Journal of Chemical Education published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C7H13NO2, Related Products of esters-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics