Month: April 2022

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 4-Methyl-1-phenyl-2,3-dihydro-1H-phosphole 1-oxide, is researched, Molecular C11H13OP, CAS is 707-61-9, about Research and development of phospha sugar anti-cancer agents with anti-leukemic activity.Quality Control of 4-Methyl-1-phenyl-2,3-dihydro-1H-phosphole 1-oxide.

We have synthesized three deoxybromophospha sugar analogs, 4-bromo-3-methyl-1-phenyl-2-phospholene 1-oxide (MBMPP (2)), 2,3-dibromo-3-methyl-1-phenylphospholane 1-oxide (DBMPP (3)), the 2,3,4-tribromo-3-methyl-1-phenylphospholane 1-oxide (TBMPP (4)), by the reaction of 3-methyl-1-phenyl-2-phospholene 1-oxide (1b) and/or 2 with bromine, and investigated their potentials as anti-leukemic agents against human leukemia cell lines of K562 and U937. Cells’ growth inhibition was determined by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) in vitro assay. All agents showed inhibitory effects on leukemia cell proliferation, indicating that inhibition appeared to be dependent on number of bromine substituent in the heterocyclic structure. Further, the phospha sugar derivatives did not show any inhibitory effects on normal cell proliferation. These agents may facilitate the development of new strategies in mol. targeting anti-leukemic therapy.

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1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 6,7-Dichlorobenzo[d]thiazol-2-amine( cas:25150-27-0 ) is researched.Name: 6,7-Dichlorobenzo[d]thiazol-2-amine.Baldaniya, B. B. published the article 《Synthesis, characterization and biological activity of 5-arylidene-3-(6,7-dichloro-1,3-benzothiazol-2-yl)-phenyl-3,5-dihydro-4H-imidazol-4-ones》 about this compound( cas:25150-27-0 ) in E-Journal of Chemistry. Keywords: arylidene oxazolone condensation benzothiazolamine; imidazolone arylidene benzothiazolyl preparation antibacterial antifungal activity. Let’s learn more about this compound (cas:25150-27-0).

Some novel 5-arylidene-3-(6,7-dichloro-1,3-benzothiazol-2-yl)-2-phenyl-3,5-dihydro-4H-imidazol-4-ones were synthesized and characterized by elemental analyses, IR, NMR, and mass spectra. The products were evaluated for antibacterial and antifungal activities against different strains of bacteria and fungi.

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1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Application of 4360-63-8. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 2-Bromomethyl-1,3-dioxolane, is researched, Molecular C4H7BrO2, CAS is 4360-63-8, about Nickel-Catalyzed Cross-Electrophile Reductive Couplings of Neopentyl Bromides with Aryl Bromides. Author is Biswas, Soumik; Qu, Bo; Desrosiers, Jean-Nicolas; Choi, Younggi; Haddad, Nizar; Yee, Nathan K.; Song, Jinghua J.; Senanayake, Chris H..

5-Cyanoimidazole was identified as an inexpensive ligand for nickel-catalyzed cross-electrophile couplings by screening a diverse set of pharmaceutical compound library. A strategic screening approach led to the discovery of this novel ligand, which was successfully applied in the preparation of various alkylated arene products with good to high yields. Furthermore, the properties of this ligand allowed expanding the scope of reductive couplings to challenging substrates, such as sterically hindered neopentyl halides, which are known to generate motifs that are prevalent in biol. active mols.

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1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 7524-52-9, is researched, Molecular C12H15ClN2O2, about Synthesis and antimalarial activity of (S)-methyl-(7-chloroquinolin-4-ylthio)acetamidoalquilate derivatives, the main research direction is methyl chloroquinolinylthio acetamidoalquilate preparation antimalarial activity SAR.COA of Formula: C12H15ClN2O2.

The synthesis of five new (S)-methyl-(7-chloroquinolin-4-ylthio)acetamidoalquilate derivatives I (R = Me, propan-2-yl, 2-methylpropyl, benzyl,1H-indol-3-ylmethyl) is carried out under a modified version of the Steglich esterification reaction between different L-amino acid Me esters (S)-H2NCH(R)C(O)OCH3.HCl and 2-(7-chloroquinolin-4-ylthio)acetic acid. Two of the compounds showed significant inhibition (>50%) of β-hematin formation. The two active structures were tested in vivo as potential antimalarials in mice infected with Plasmodium berghei ANKA, a chloroquine susceptible strain. Compounds I (R = propan-2-yl, 1H-indol-3-ylmethyl) exhibited antimalarial activity comparable to that of chloroquine.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Yun, Fan; Cheng, Chunhui; Zhang, Jing; Li, Jingxuan; Liu, Xia; Xie, Rui; Tang, Pingwah; Yuan, Qipeng published the article 《Boric Acid Catalyzed Direct Amidation between Amino-Azaarenes and Carboxylic Acids》. Keywords: azaarylamide preparation green chem chemoselective; aminoazaarene carboxylic acid boric acid tetramethylpropanediamine catalyst amidation.They researched the compound: 5-Chloropyridin-3-amine( cas:22353-34-0 ).Computed Properties of C5H5ClN2. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:22353-34-0) here.

A novel and facile boric acid-catalyzed direct amidation between amino-azaarene compounds and carboxylic acids was developed. The amidation proceeded cleanly and provided good to excellent yields of the desired amides. Boric acid is a green and inexpensive catalyst. It was also found that N,N,N’,N’-tetramethylpropane-1,3-diamine acted as an additive accelerating this boric acid-catalyzed amidation. A mixed acid anhydride was postulated to be the active intermediate responsible for this successful amidation. This direct amidation was an atom- and step-economical reaction.

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1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Computed Properties of C34H22NO2P. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 5-(11bR)-Dinaphtho[2,1-d:1′,2′-f][1,3,2]dioxaphosphepin-4-yl-5H-dibenz[b,f]azepine, is researched, Molecular C34H22NO2P, CAS is 1265884-98-7, about Enantio- and Diastereodivergent Dual Catalysis: α-Allylation of Branched Aldehydes. Author is Krautwald, Simon; Sarlah, David; Schafroth, Michael A.; Carreira, Erick M..

An important challenge in asym. synthesis is the development of fully stereodivergent strategies to access the full complement of stereoisomers of products bearing multiple stereocenters. In the ideal case, where four products are possible, applying distinct catalysts to the same set of starting materials under identical conditions would in a single step afford any given stereoisomer. Herein, the authors describe the realization of this concept in a fully stereodivergent dual-catalytic synthesis of γ,δ-unsaturated aldehydes bearing vicinal quaternary/tertiary stereogenic centers. The reaction is enabled by chiral iridium and amine catalysts, which activate the allylic alc. and aldehyde substrates, resp. Each catalyst exerts high local stereocontrol irresp. of the other’s inherent preference.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 6,7-Dichlorobenzo[d]thiazol-2-amine, is researched, Molecular C7H4Cl2N2S, CAS is 25150-27-0, about Synthesis, characterization and antibacterial activity of 3-(6,7 substituted-1,3-benzothiazol-2-yl)-4-(4-substituted phenyl)-1,3-thiazolidin-2-one derivatives.Electric Literature of C7H4Cl2N2S.

Disubstituted 2-aminobenzothiazole derivatives (2) have been prepared from disubstituted aniline (1) in presence of potassium thiocynate, bromine, glacial acetic acid and ammonia solution It has been reacted with various aromatic aldehydes (3a-g) to afford Schiff’s base derivatives (4a-g). Further, these schiff’s bases are refluxed with thioglycolic acid in presence of DMF to afford 3-(6,7-substituted-1,3-benzothiazol-2-yl)-4-(4-substituted phenyl)-1,3-thiazolidin-2-one derivatives (5a-g, 6a-g, 7a-g, 8a-g, 9a-g, 10a-g). The title compounds and their derivatives have been characterized by their spectral data. The synthesized compounds were screened for their antibacterial activity against Staphylococcus aureus, Bacillus substilis, Escherichia coli and Pseudomonas aeruginosa.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

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.He, Zhi-Tao; Zhao, Yi-Shuang; Tian, Ping; Wang, Chuan-Chuan; Dong, Han-Qing; Lin, Guo-Qiang researched the compound: 5-(11bR)-Dinaphtho[2,1-d:1′,2′-f][1,3,2]dioxaphosphepin-4-yl-5H-dibenz[b,f]azepine( cas:1265884-98-7 ).Synthetic Route of C34H22NO2P.They published the article 《Copper-Catalyzed Asymmetric Hydroboration of α-Dehydroamino Acid Derivatives: Facile Synthesis of Chiral β-Hydroxy-α-amino Acids》 about this compound( cas:1265884-98-7 ) in Organic Letters. Keywords: dehydroamino acid preparation asym hydroboration copper catalyst; hydroxy amino acid asym preparation. We’ll tell you more about this compound (cas:1265884-98-7).

The Cu-catalyzed asym. conjugate hydroboration reaction of β-substituted α-dehydroamino acid derivatives has been established, affording enantio-enriched syn- and anti-β-boronate-α-amino acid derivatives with excellent combined yields (83-99%, dr ≈ 1:1) and excellent enantioselectivities (92-98% ee). The hydroboration products were expediently converted into valuable β-hydroxy-α-amino acid derivatives, which were widely used in the preparation of chiral drugs and bioactive mols.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Application of 1265884-98-7. 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: 5-(11bR)-Dinaphtho[2,1-d:1′,2′-f][1,3,2]dioxaphosphepin-4-yl-5H-dibenz[b,f]azepine, is researched, Molecular C34H22NO2P, CAS is 1265884-98-7, about Iridium-catalyzed enantioselective synthesis of (-)- and (+)-aurantioclavine.

A new protocol for generating indoleazepine I via an Ir-catalyzed intramolecularly asym. amination of secondary allylic alc. II in the presence of Carreira ligand and Sc(OTf)3 is described. This methodol. has been exploited in the facile synthesis of natural (-)-aurantioclavine (III), a biosynthetical precursor of communesins, and its unnatural enantiomer (+)-aurantioclavine (ent-III).

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Safety of 4-Methyl-1-phenyl-2,3-dihydro-1H-phosphole 1-oxide. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 4-Methyl-1-phenyl-2,3-dihydro-1H-phosphole 1-oxide, is researched, Molecular C11H13OP, CAS is 707-61-9, about NMR and uv spectral studies of some 1-aryl-substituted 3-methyl-2-phospholene oxides. Author is Kerek, F.; Ostrogovich, G..

The NMR and uv spectra of 7 1-aryl-3-methyl-2-phospholene oxides (I, R = H, Me, NMe2, etc.) are discussed. The value of 25 cps for the coupling constants of the P atom with vinylic protons indicates a Δ2,3 position of the phospholene ring double bond. The linear correlation of the bathochromic shift values with substituent constants (σ°) shows a low conjugative interaction between the benzene ring and the phosphoryl group.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem