Month: April 2022

Computed Properties of C5H5FN2. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Divergent Aminocarbonylations of Alkynes Enabled by Photoredox/Nickel Dual Catalysis. Author is Zhao, Xian; Feng, Xiaoliang; Chen, Fan; Zhu, Shengqing; Qing, Feng-Ling; Chu, Lingling.

A metallaphotoredox-catalyzed strategy for the selective and divergent aminocarbonylation of alkynes with amines and 1 atm of CO was reported. This synergistic protocol not only enables the Markovnikov-selective hydroaminocarbonylation of alkynes to afford α,β-unsaturated amides, but also facilitated a sequential four-component hydroaminocarbonylation/radical alkylation in the presence of tertiary and secondary alkyl boronate esters, which allowed for straightforward conversion of alkynes into corresponding amides. Preliminary mechanistic studied disclose that a photoinduced oxidative insertion of aniline and CO into nickel followed by a migratory insertion of (carbamoyl)nickel species was involved.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Recommanded Product: Ethyl oxazole-5-carboxylate. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Fluorogenic Behaviour of the Hetero-Diels-Alder Ligation of 5-Alkoxyoxazoles with Maleimides and their Applications. Author is Renault, Kevin; Jouanno, Laurie-Anne; Lizzul-Jurse, Antoine; Renard, Pierre-Yves; Sabot, Cyrille.

Fluorogenic reactions are largely underrepresented in the toolbox of chemoselective ligations despite their tremendous potential, particularly in chem. biol. and biochem. In this respect, we have investigated in full detail the fluorescence behavior of the azaphthalamide, a scaffold which is generated through a hetero-Diels-Alder reaction of 5-alkoxyoxazole and maleimide derivatives under mild conditions that are compatible with, among others, peptide chem. The scope and limitations of such a fluorogenic labeling strategy were examined through four distinct applications, which target enzymic activities or bioorthogonal reactions.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 4-Aminopyrimidine( cas:591-54-8 ) is researched.Computed Properties of C4H5N3.Abdelaziz, Ahmed M.; Basnet, Sunita K. C.; Islam, Saiful; Li, Manjun; Tadesse, Solomon; Albrecht, Hugo; Gerber, Cobus; Yu, Mingfeng; Wang, Shudong published the article 《Synthesis and evaluation of 2’H-spiro[cyclohexane-1,3′-imidazo[1,5-a]pyridine]-1′,5′-dione derivatives as Mnk inhibitors》 about this compound( cas:591-54-8 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: spiro cyclohexane imidazopyridine dione preparation chemoselective antitumor Mnk inhibitor; Anti-cancer; Inhibitor; Mnk; eFT508; eIF4E. Let’s learn more about this compound (cas:591-54-8).

A series of 2’H-spiro[cyclohexane-1,3′-imidazo[1,5-a]pyridine]-1′,5′-dione derivatives I (R = pyridin-4-yl, pyrimidin-4-yl, oxazol-2-yl, etc.) is presented as Mnk inhibitors. Some of them showed sub-micromolar to low nanomolar inhibitory activities against Mnk1/2 with a high level of selectivity for both kinases over CDKs. Biochem. assays revealed that compounds I (R = pyridin-4-yl, pyrimidin-4-yl) are non-ATP-competitive inhibitors of Mnks. Lead compound I (R = pyrimidin-4-yl) demonstrated a high selectivity for Mnk1/2 over a selection of 51 kinases, and displayed anti-proliferative activities against a panel of cancer cell lines. However, this compound in combination with our inhouse CDK4/6 inhibitor 83 did not show a synergistic effect in A2780 ovarian cancer cells, suggesting that caution be exercised in the selection of an agent to be combined with an Mnk inhibitor.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

SDS of cas: 2150-55-2. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Enzymatic syntheses of L-cysteine by sodium alginate/gelatin co-immobilized Pseudomonas sp. B-3. Author is Wang, Pu; Yin, Jiangfeng; He, Junyao; Liang, Fayong.

The immobilization of Pseudomonas sp. B-3 by sodium alginate/gelatin mixed gel and the biosynthesis of L-cysteine from DL-2-amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC) by immobilized cells were investigated. Suitable method for the immobilization of Pseudomonas sp. B-3 was selected by the comparison of eight immobilization methods. The influences of some key factors such as gel constitution, cells embedded and activation time on enzyme activity were optimized. Tween-60, N-carbamyl-L-cysteine amidohydrolase (L-NCC hydrolase) activator of Mn2+ and L-cysteine desulfhydrase inhibitor of hydroxylamine was added into reaction solution to improve L-cysteine productivity. Sodium alginate/gelatin co-immobilization showed both the highest enzyme activity and best gel strength. After 10 h activation for immobilized cells, the bioconversion was conducted at pH 8.0 and 42° for 10 h, 9.18 g/L-1 of L-cysteine was formed from 20 g/L-1 of DL-ATC/3H2O, with the molar conversion rate of 75.83%. An increase of 29.0% for L-cysteine production was obtained after catalyzed by immobilized cells in comparison with resting cells. After reused for four times, the relative molar conversion rate of L-cysteine remained 71.5% of the initial value. Sodium alginate/gelatin embedding method was suitable for immobilization of Pseudomonas sp. B-3. L-cysteine production was enhanced by the addition of Tween-60, Mn2+ and hydroxylamine hydrochloride in reaction solution

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: Ethyl oxazole-5-carboxylate( cas:118994-89-1 ) is researched.Reference of Ethyl oxazole-5-carboxylate.Piou, Tiffany; Slutskyy, Yuriy; Kevin, Nancy J.; Sun, Zhongxiang; Xiao, Dong; Kong, Jongrock published the article 《Direct Arylation of Azoles Enabled by Pd/Cu Dual Catalysis》 about this compound( cas:118994-89-1 ) in Organic Letters. Keywords: oxazole aryl halide palldium copper catalyst arylation; ethyl aryl oxazole carboxylate preparation. Let’s learn more about this compound (cas:118994-89-1).

A practical approach toward the synthesis of 2-arylazoles via direct arylation was described. The transformation relied on a Pd/Cu cocatalyst system that operated with low catalyst loadings. The reaction conditions were found to be tolerant of a wide range of functional groups and nitrogen-containing heterocycles commonly employed in a drug discovery setting.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Computed Properties of C4H6N2O2S. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Asymmetric synthesis of S-carboxymethyl-L-cysteine by a chemicoenzymic method.

A chemienzymic method is developed for production of S-carboxymethyl-L-cysteine (I) from DL-2-aminothiazoline-4-carboxylic acid (II) in the presence of ClCH2CO2H using a hydrolyzing system. The carboxymethylation of L-cysteine with ClCH2CO2H to I proceeded effectively at 26° and pH ≥8.0, the yield reaching nearly 100%. The carboxymethylation of II with ClCH2CO2H was not observed Next, the production of I from II in the presence of ClCH2CO2H was examined using rinsed cells of Pseudomonas desmolytica AJ-11898. About 10 g I/L was produced from 18 g II/L in 8 h, the molar yield being 45%. This finding shows that the aminothiazolinecarboxylate racemase in P. desmolytica AJ-11898 may be inhibited by the ClCH2CO2H added to the reaction mixture In fact, the II remaining in the reaction mixture was in the D-form. Moreover, the yield of L-cysteine from DL-II in the absence of ClCH2CO2H was ∼50% when cells of AJ-11898 pretreated with SH reagents were used as the enzyme source.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Category: pyrazines. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Synthesis of 6-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones via directed lithiation of 2-substituted 5-aminopyridine derivatives. Author is Rewcastle, Gordon W.; Denny, William A.; Winters, R. Thomas; Colbry, Norman L.; Showalter, H. D. Hollis.

Directed lithiation of Boc or pivaloyl derivatives of 2-substituted 5-aminopyridines I (R = Cl, F, OMe, R1 = COnCMe3, X = H, n = 1, 2) with BuLi-TMEDA in di-Et ether at -10°C gave 4-lithio derivatives which were quenched with CO2 to give the analogous C-4 carboxylic acids I (X = CO2H). Hydrolysis of the protecting groups with either TFA or aqueous KOH gave 2-substituted 5-aminopyridine-4-carboxylic acids I (R1 = H, X = CO2H) which were converted to 6-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones II by reaction with formamide or, more optionally, formamidine acetate. Boc protected aminopyridines provided the best overall results, with synthesis of these derivatives best achieved by direct reaction of the aminopyridine with di-tert-Bu dicarbonate in the absence of added base.

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Pyrazine – Wikipedia,
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Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 2150-55-2, is researched, SMILESS is O=C(C1N=C(N)SC1)O, Molecular C4H6N2O2SJournal, Biotechnology Letters called Kinetic properties of a L-cysteine desulfhydrase-deficient mutant in the enzymic formation of L-cysteine from D,L-ATC, Author is Pae, Ki Moon; Ryu, Ok Hee; Yoon, Hyun Sook; Shin, Chul Soo, the main research direction is cysteine manufacture aminothiazolinecarboxylate Pseudomonas mutant.Reference of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid.

A mutant strain lacking L-cysteine desulfhydrase was screened after UV treatment of Pseudomonas sp. CU6. The properties of the original and mutant strains were compared on the basis of parameter values estimated from kinetic simulation of the enzymic formation of L-cysteine from D,L-2-amino-Δ2-thiazoline-4-carboxylic acid (ATC). Both strains suffered from product inhibition, but inhibition was less for the mutant strain.

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Pyrazine – Wikipedia,
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Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 2150-55-2, is researched, SMILESS is O=C(C1N=C(N)SC1)O, Molecular C4H6N2O2SJournal, Article, Applied and Environmental Microbiology called Genes from Pseudomonas sp. strain BS involved in the conversion of L-2-amino-Δ2-thiazolin-4-carbonic acid to L-cysteine, Author is Shiba, Toshikazu; Takeda, Kohji; Yajima, Misako; Tadano, Makoto, the main research direction is Pseudomonas gene atcB atcC sequence; aminothiazoline carbonic acid hydrolase gene atcB sequence Pseudomonas; carbamoylcysteine amidohydrolase gene atcC sequence Pseudomonas.Application In Synthesis of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid.

DL-2-Amino-Δ2-thiazoline-4-carbonic acid (DL-ATC) is a substrate for cysteine synthesis in some bacteria, and this bioconversion has been utilized for cysteine production in industry. We cloned a DNA fragment containing the genes involved in the conversion of L-ATC to L-cysteine from Pseudomonas sp. strain BS. The introduction of this DNA fragment into Escherichia coli cells enabled them to convert L-ATC to cysteine via N-carbamoyl-L-cysteine (L-NCC) as an intermediate. The smallest recombinant plasmid, designated pTK10, contained a 2.6-kb insert DNA fragment that has L-cysteine synthetic activity. The nucleotide sequence of the insert DNA revealed that two open reading frames (ORFs) encoding proteins with mol. masses of 19.5 and 44.7 kDa were involved in the L-cysteine synthesis from DL-ATC. These ORFs were designated atcB and atcC, resp., and their gene products were identified by overproduction of proteins encoded in each ORF and by the maxicell method. The functions of these gene products were examined using extracts of E. coli cells carrying deletion derivatives of pTK10. The results indicate that atcB and atcC are involved in the conversion of L-ATC to L-NCC and the conversion of L-NCC to cysteine, resp. AtcB was first identified as a gene encoding an enzyme that catalyzes thiazoline ring opening. AtcC is highly homologous with L-N-carbamoylases. Since both enzymes can only catalyze the L-specific conversion from L-ATC to L-NCC or L-NCC to L-cysteine, it is thought that atcB and atcC encode L-ATC hydrolase and N-carbamoyl-L-cysteine amidohydrolase, resp.

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Pyrazine – Wikipedia,
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Zhang, Wen-Ze; Chen, Zhuang-Zhuang; Han, Xiu-Juan; Dong, Wen-Kui published an article about the compound: 4-Aminopyrimidine( cas:591-54-8,SMILESS:C1=CN=CN=C1N ).Recommanded Product: 591-54-8. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:591-54-8) through the article.

Two novel single-armed nitrogen-heterocyclic chemosensors with basically similar structures, PDNS and PZNS, were synthesized to specifically identify Al3+ in DMS:H2O (1:1 volume/volume) solution by fluorescence emission spectroscopy, and the color of PDNS and PZNS changed from yellow to colorless when Al3+ was added under daylight. This is the first time that nitrogen-heterocyclic is introduced into salamo-based chem. sensor. At excitation wavelengths of 361 and 365 nm, solutions of PDNS and PZNS changed to intense green-blue fluorescence. Furthermore, it was found that PDNS/PZNS and Al3+ have excellent binding capacity, the lower limit of detection (LOD = 6.25 x 10-9/1.26 x 10-9 mol·dm-3) is also calculated In addition, sensor PZNS can detect Al3+ in a solution system with up to 95% water content and applicable pH range is 3-12. Compared to other salamo-based sensors, PZNS and PDNS have broader detection conditions and wider utilities. PZNS can also identify CN- in fluorescence spectrum. PZNS can be used for detection of Al3+ in aqueous systems in daily production and life.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem