Month: April 2022

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called I2/DMSO-catalyzed one-pot approach for the synthesis of 1,3,4-selenadiazoles, published in 2021, which mentions a compound: 21778-81-4, mainly applied to arylaldehyde hydrazide selenium iodine catalyst one pot cascade reaction; diaryl selenadiazole preparation; hetroarylaldehyde hydrazide selenium iodine catalyst one pot cascade reaction; diheteroaryl selenadiazole preparation, Reference of 5-Methoxy-1H-indole-2-carbaldehyde.

A three-component cascade reaction for the synthesis of 1,3,4-selenadiazoles and their derivatives from arylaldehydes, hydrazine, and elemental selenium by using mol. iodine wais reported. This strategy was operationally simple, well-suited to a wide range of functional groups, and provided the desired products in moderate to excellent yields. The proposed mechanism predicted that the reaction tolerated a radical process.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Kroth, Heiko; Oden, Felix; Molette, Jerome; Schieferstein, Hanno; Gabellieri, Emanuele; Mueller, Andre; Berndt, Mathias; Sreenivasachary, Nampally; Serra, Andreia Monica; Capotosti, Francesca; Schmitt-Willich, Heribert; Hickman, David; Pfeifer, Andrea; Dinkelborg, Ludger; Stephens, Andrew published the article 《PI-2620 Lead Optimization Highlights the Importance of Off-Target Assays to Develop a PET Tracer for the Detection of Pathological Aggregated Tau in Alzheimer′s Disease and Other Tauopathies》. Keywords: PET imaging tracer preparation Tau aggregation Alzheimer’s palsy Pick’s.They researched the compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride( cas:136725-55-8 ).Category: pyridazine. 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:136725-55-8) here.

The first candidate PI-2014 was tested in healthy controls and subjects with Alzheimer′s disease (AD). As PI-2014 displayed off-target binding to monoamine oxidase A (MAO-A), a new lead with improved binding to Tau and decreased MAO-A binding was required. For compound optimization, Tau binding assays based on both human AD brain homogenate and Tau-paired helical filaments were employed. Furthermore, two MAO-A screening assays based on (1) human-recombinant MAO-A and (2) displacement of 2-fluoro-ethyl-harmine from mouse brain homogenate were employed. Removing the N-Me group from the tricyclic core resulted in compounds displaying improved Tau binding. For the final round of optimization, the cyclic amine substituents were replaced by pyridine derivatives PI-2620 (2-(2-fluoropyridin-4-yl)-9H-pyrrolo[2,3-b:4,5-c′]dipyridine) emerged as a best candidate displaying high Tau binding, low MAO-A binding, high brain uptake, and fast and complete brain washout. Furthermore, PI-2620 showed Tau binding on brain sections from corticobasal degeneration, progressive supranuclear palsy, and Pick′s disease.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Name: 5-Methoxy-1H-indole-2-carbaldehyde. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 5-Methoxy-1H-indole-2-carbaldehyde, is researched, Molecular C10H9NO2, CAS is 21778-81-4, about Asymmetric Sequential Corey-Chaykovsky Cyclopropanation/Cloke-Wilson Rearrangement for the Synthesis of 2,3-Dihydrofurans. Author is Zhou, Yiming; Li, Ning; Cai, Wei; Huang, You.

The first sequential Corey-Chaykovsky cyclopropanation/Cloke-Wilson rearrangement between propargyl sulfonium salts and acrylonitrile derivatives was developed, affording the tetra-substituted 2,3-dihydrofurans in generally excellent yields (57-98%) with good diastereoselectivities (7:1-18:1). In addition, chiral propargyl sulfonium salt is also suitable for this strategy, giving the optically active 2,3-dihydrofurans with good enantioselectivities. This reaction sequence was designed upon in situ generated 10π-conjugated structures from the dearomatization of indole fragments and subsequent intramol. 1,6-addition

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 5-Methoxy-1H-indole-2-carbaldehyde( cas:21778-81-4 ) is researched.Related Products of 21778-81-4.Lorton, Charlotte; Voituriez, Arnaud published the article 《Phosphine-Promoted Synthesis of 9H-Pyrrolo[1,2-a]indole Derivatives via an γ-Umpolung Addition/Intramolecular Wittig Reaction》 about this compound( cas:21778-81-4 ) in Journal of Organic Chemistry. Keywords: pyrroloindole synthesis phoshine promoted Michael intramol Wittig indolecarbaldehyde allenoate. Let’s learn more about this compound (cas:21778-81-4).

The synthesis of substituted 9H-pyrrolo[1,2-a]indole products from 1H-indole-2-carbaldehydes and allenoates is described, using a phosphine-promoted Michael addition/intramol. Wittig reaction. This halide- and base-free methodol. provides an efficient access to different tricyclic nitrogen-containing heterocycles (18 examples, 32-88% isolated yields).

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – 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: 17739-45-6, is researched, Molecular C7H13BrO2, about Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development, the main research direction is dihydrodiazepino indolone derivative preparation pamiparib PARP inhibitor cancer.Reference of 2-(2-Bromoethoxy)tetrahydro-2H-pyran.

Poly (ADP-ribose) polymerase (PARP) plays a significant role in DNA repair responses; therefore, this enzyme is targeted by PARP inhibitors in cancer therapy. Here we have developed a number of fused tetra- or pentacyclic dihydrodiazepinoindolone derivatives with excellent PARP enzymic and cellular PARylation inhibition activities. These efforts led to the identification of pamiparib (BGB-290, 139), which displays excellent PARP-1 and PARP-2 inhibition with IC50 of 1.3 and 0.9 nM, resp. In a cellular PARylation assay, this compound inhibits PARP activity with IC50 = 0.2 nM. Cocrystal of pamiparib shows similar binding sites with PARP with other PARP inhibitors, but pamiparib is not a P-gp substrate and shows excellent drug metabolism and pharmacokinetics (DMPK) properties with significant brain penetration (17-19%, mice). The compound is currently being investigated in phase III clin. trials as a maintenance therapy in platinum-sensitive ovarian cancer and gastric cancer.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

COA of Formula: C10H9NO2. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 5-Methoxy-1H-indole-2-carbaldehyde, is researched, Molecular C10H9NO2, CAS is 21778-81-4, about Phosphine-Promoted Synthesis of 9H-Pyrrolo[1,2-a]indole Derivatives via an γ-Umpolung Addition/Intramolecular Wittig Reaction. Author is Lorton, Charlotte; Voituriez, Arnaud.

The synthesis of substituted 9H-pyrrolo[1,2-a]indole products from 1H-indole-2-carbaldehydes and allenoates is described, using a phosphine-promoted Michael addition/intramol. Wittig reaction. This halide- and base-free methodol. provides an efficient access to different tricyclic nitrogen-containing heterocycles (18 examples, 32-88% isolated yields).

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – 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.Zhang, Lei; Zheng, Mingyue; Zhao, Fei; Zhai, Yun; Liu, Hong researched the compound: 5-Methoxy-1H-indole-2-carbaldehyde( cas:21778-81-4 ).Name: 5-Methoxy-1H-indole-2-carbaldehyde.They published the article 《Rapid Generation of Privileged Substructure-Based Compound Libraries with Structural Diversity and Drug-Likeness》 about this compound( cas:21778-81-4 ) in ACS Combinatorial Science. Keywords: indolecarboxaldehyde amine carboxylic acid isonitrile Ugi intramol arylation cyclization; heterocyclic compound library preparation structural diversity drug likeness. We’ll tell you more about this compound (cas:21778-81-4).

A library of privileged-substructure-based, heterocyclic compounds was constructed by a sequence of Ugi four-component reactions incorporating the indole motif and microwave-assisted cyclizations in branched pathways. Cheminformatic anal. confirmed that the library exhibited a high degree of structural diversity and good drug-likeness.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Continuous-Flow Pd-Catalyzed Carbonylation of Aryl Chlorides with Carbon Monoxide at Elevated Temperature and Pressure, published in 2019, which mentions a compound: 39977-42-9, mainly applied to ester aryl preparation continuous flow; aryl chloride carbon monoxide methoxycarbonylation palladium catalyst; (hetero)aryl chlorides; Pd-catalyzed; carbon monoxide; carbonylation; continuous flow; gas-liquid transformation, Reference of Methyl 5-(hydroxymethyl)picolinate.

The development of a continuous-flow protocol for a palladium-catalyzed methoxycarbonylation of (hetero)aryl chlorides RCl (R = 4-cyanophenyl, quinolin-2-yl, pyrazin-2-yl, etc.) using carbon monoxide gas and methanol is described. (Hetero)aryl chlorides are the least expensive of the aryl halides, but are underutilized in carbonylation reactions due to their very poor reactivity. The described protocol exploits intensified conditions at elevated temperature and pressure, which are readily accessed within a continuous-flow environment, to provide moderate to excellent product yields RC(O)OCH3 (11 examples) in a short 16 min residence time. The continuous-flow protocol enables the safe and potentially scalable carbonylation of aryl chlorides using CO gas.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride(SMILESS: Cl.F[C@@H]1CCNC1,cas:136725-55-8) is researched.Application of 21778-81-4. The article 《Novel Human Neutral Sphingomyelinase 2 Inhibitors as Potential Therapeutics for Alzheimer’s Disease》 in relation to this compound, is published in Journal of Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:136725-55-8).

Neutral sphingomyelinase 2 (nSMase2) catalyzes the cleavage of sphingomyelin to phosphorylcholine and ceramide, an essential step in the formation and release of exosomes from cells that is critical for intracellular communication. Chronic increase of brain nSMase2 activity and related exosome release has been implicated in various pathol. processes, including the progression of Alzheimer’s disease (AD), making nSMase2 a viable therapeutic target. Recently, we identified phenyl(R)-(1-(3-(3,4-dimethoxyphenyl)-2,6-dimethylimidazo[1,2-b] pyridazin-8-yl) pyrrolidin-3-yl)-carbamate 1 (PDDC)(I), the first nSMase2 inhibitor which possesses both favorable pharmacodynamics and pharmacokinetic (PK) parameters, including substantial oral bioavailability, brain penetration and significant inhibition of exosome release from the brain in vivo. Herein we demonstrate efficacy of 1 (PDDC) in a mouse model of AD and detail extensive structure-activity relationship (SAR) studies with 70 analogs, unveiling several that exert similar or higher activity against nSMase2 with favorable pharmacokinetic properties.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Application of 21778-81-4. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 5-Methoxy-1H-indole-2-carbaldehyde, is researched, Molecular C10H9NO2, CAS is 21778-81-4, about Synthetic studies on mitomycins. Synthesis of aziridinopyrrolo[1,2-a]indoles. Author is Hirata, Tadashi; Yamada, Yasuhiro; Matsui, Masanao.

Conversion of the nitro compounds 2,4,5-Me(R1O)R2C6H2NO2 (R1, R2 = Me, H; Me, Me; PhCH2O, H; PhCH2O, Me) by a modified Reissert indole synthesis gave the esters I (R3 = CO2Et), m. 155-6, – , – , 141-2°, resp., reduced by LiAlH4 to the alcs. I (R3 = CH2OH), m. 83.5-5.0, 139-40, 103-4, 100-3°, resp., oxidized in turn by KMnO4 in Me2CO with poor yields (10-20%) or with yields up to 90% by CrO3-C5H5N of the corresponding aldehydes I (R3 = CHO), m. 136-7, 172-3, 178-9, 172-5°, resp. The aldehydes treated with NaH and H2C:CHPPh3Br in tetrahydrofuran (THF) gave 80-8% yields of 9H-pyrrolo[1,2-a]indoles (II) (R1, R2 = Me, H; PhCH2O, H; PhCH2O, Me), m. 80-1, 88-9, 88-9°, resp., with structures supported by uv and N.M.R. spectra. Acylation of II with KOCMe3 and Me2CO3 afforded 60-80% 3H-pyrrolo-[1,2-a]indoles (III) (R4 = OMe), m. 121-3, 122-3, 139-41°, resp. Similarly acylation with HCO2Et gave III (R4 = H; R1, R2 = Me, H; PhCH2O, Me), m. 135-41 (decomposition), and 138-42°, with structures supported by ir, uv, and N.M.R. spectra. Functionalization of the vinylic double bond of III for attachment of the aziridine moiety was achieved by iodine-azide addition giving 74-5% yields of iodo-azides (IV, R1, R2 = Me, H; PhCH2O, Me), m. 93.8-4.5, and 171-9°, ir, uv, and N.M.R. spectral data given. Catalytic hydrogenation of IV over Pd-C in MeOH containing HCl gave 60-90% yields of the corresponding iodo-amine hydrochlorides, m. >300, >300°, yielding the expected iodoamines, m. indefinite, 135-41° (decomposition), resp., ir bands (Nujol) given. Protection of the amine group with ClCO2Me furnished the iodo carbamates (V) (R5 = H; R1, R2 = Me, H; PhCH2O, Me) (VI, VII), m. 160-2 and 183-4°, resp. Cyclization with NaOMe in (MeOCH2)2 or THF gave VIII (R5 = H; R1 = Me, R2 = H), m. 210.5-14.5°, with structure confirmed by spectroscopic data, and VIII (R5 = H, R1 = PhCH2O, R2 = Me), m. 219.5-21.5°. Nitration of VI and VII gave the 8-nitro derivatives V (R5 = NO2, R1, R2 = Me, H; PhCH2O, Me), m. indefinite and 192-9°, resp. The location of the NO2 group was elucidated by N.M.R. spectral anal. The ring closure of the 8-nitro derivatives similarly gave the corresponding aziridines, VIII (R5 = NO2; R1, R2 = Me, H; PhCH2O, Me), m. 242-6, and 232-3.5°.

As far as I know, this compound(21778-81-4)Application of 21778-81-4 can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.

Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem