Category: 2343-22-8

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 5-Fluoroindoline, is researched, Molecular C8H8FN, CAS is 2343-22-8, about Discovery of Novel Thiazole Carboxamides as Antifungal Succinate Dehydrogenase Inhibitors, the main research direction is thiazole carboxamide preparation antifungal succinate dehydrogenase inhibitor; fungicide; molecular docking; succinate dehydrogenase inhibitor; thiazole carboxamide.Category: piperazines.

To contribute mol. diversity for novel fungicide development, a series of novel thiazole carboxamides were rationally designed, synthesized, and characterized with the succinate dehydrogenase (SDH) as target. Bioassay indicated that compound 6g showed the similar excellent SDH inhibition as that of Thifluzamide with IC50 of 0.56 mg/L and 0.55 mg/L, resp. Some derivatives displayed improved in vitro fungicidal activities against Rhizoctonia cerealis and Sclerotinia sclerotiorum with EC50 of 1.2-16.4 mg/L and 0.5-1.9 mg/L. Surprisingly, 6g showed promising in vitro fungicidal activities against R. cerealis and S. sclerotiorum with EC50 of 6.2 and 0.6 mg/L, resp., which was superior to Thifluzamide with the EC50 of 22.1 and 4.4 mg/L, resp. Addnl., compounds 6c and 6g displayed excellent in vivo fungicidal activities against S. sclerotiorum on Brassica napus L. leaves with protective activity of 75.4% and 67.3% at 2.0 mg/L, resp., while Thifluzamide without activity at 5.0 mg/L. Transcriptomic anal. of S. sclerotiorum treated with 6g by RNA sequencing indicated the down-regulation of succinate dehydrogenase gene SDHA and SDHB, and the inhibition of the TCA-cycle.

The article 《Discovery of Novel Thiazole Carboxamides as Antifungal Succinate Dehydrogenase Inhibitors》 also mentions many details about this compound(2343-22-8)Category: piperazines, you can pay attention to it, because details determine success or failure

Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 5-Fluoroindoline, is researched, Molecular C8H8FN, CAS is 2343-22-8, about DMSO/t-BuONa/O2-Mediated Aerobic Dehydrogenation of Saturated N-Heterocycles, the main research direction is quinoline preparation; tetrahydroquinoline sodium tert butoxide dimethyl sulfoxide oxidative dehydrogenation; isoquinoline preparation; tetrahydroisoquinoline sodium tert butoxide dimethyl sulfoxide oxidative dehydrogenation; indole preparation; indoline sodium tert butoxide dimethyl sulfoxide oxidative dehydrogenation.Application of 2343-22-8.

Aromatic N-heterocycles such as quinolines I [R1 = H, 8-Cl, 6-OMe, etc.; R2 = H, 3-Me, 4-Ph, etc. X = N; Y = CH2], isoquinolines I [R1 = H; R2 = H, 1-Ph; X = CH2; Y = N] and indoles II [R1 = H, 5-F, 4-Br, etc.; R2 = H, 2-Me; Y = CH2, N] were synthesized via a sodium tert-butoxide promoted oxidative dehydrogenation of the saturated heterocycles in DMSO solution This reaction proceeded under mild reaction conditions with a good functional group tolerance. Mechanistic studies suggested a radical pathway involved hydrogen abstraction of dimsyl radicals from the N-H bond or α-C-H of the substrates, and subsequent oxidation of the nitrogen or α-aminoalkyl radicals.

The article 《DMSO/t-BuONa/O2-Mediated Aerobic Dehydrogenation of Saturated N-Heterocycles》 also mentions many details about this compound(2343-22-8)Application of 2343-22-8, you can pay attention to it, because details determine success or failure

Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 5-Fluoroindoline, is researched, Molecular C8H8FN, CAS is 2343-22-8, about Discovery of Novel Thiazole Carboxamides as Antifungal Succinate Dehydrogenase Inhibitors, the main research direction is thiazole carboxamide preparation antifungal succinate dehydrogenase inhibitor; fungicide; molecular docking; succinate dehydrogenase inhibitor; thiazole carboxamide.Category: piperazines.

To contribute mol. diversity for novel fungicide development, a series of novel thiazole carboxamides were rationally designed, synthesized, and characterized with the succinate dehydrogenase (SDH) as target. Bioassay indicated that compound 6g showed the similar excellent SDH inhibition as that of Thifluzamide with IC50 of 0.56 mg/L and 0.55 mg/L, resp. Some derivatives displayed improved in vitro fungicidal activities against Rhizoctonia cerealis and Sclerotinia sclerotiorum with EC50 of 1.2-16.4 mg/L and 0.5-1.9 mg/L. Surprisingly, 6g showed promising in vitro fungicidal activities against R. cerealis and S. sclerotiorum with EC50 of 6.2 and 0.6 mg/L, resp., which was superior to Thifluzamide with the EC50 of 22.1 and 4.4 mg/L, resp. Addnl., compounds 6c and 6g displayed excellent in vivo fungicidal activities against S. sclerotiorum on Brassica napus L. leaves with protective activity of 75.4% and 67.3% at 2.0 mg/L, resp., while Thifluzamide without activity at 5.0 mg/L. Transcriptomic anal. of S. sclerotiorum treated with 6g by RNA sequencing indicated the down-regulation of succinate dehydrogenase gene SDHA and SDHB, and the inhibition of the TCA-cycle.

The article 《Discovery of Novel Thiazole Carboxamides as Antifungal Succinate Dehydrogenase Inhibitors》 also mentions many details about this compound(2343-22-8)Category: piperazines, you can pay attention to it, because details determine success or failure

Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 5-Fluoroindoline, is researched, Molecular C8H8FN, CAS is 2343-22-8, about DMSO/t-BuONa/O2-Mediated Aerobic Dehydrogenation of Saturated N-Heterocycles, the main research direction is quinoline preparation; tetrahydroquinoline sodium tert butoxide dimethyl sulfoxide oxidative dehydrogenation; isoquinoline preparation; tetrahydroisoquinoline sodium tert butoxide dimethyl sulfoxide oxidative dehydrogenation; indole preparation; indoline sodium tert butoxide dimethyl sulfoxide oxidative dehydrogenation.Application of 2343-22-8.

Aromatic N-heterocycles such as quinolines I [R1 = H, 8-Cl, 6-OMe, etc.; R2 = H, 3-Me, 4-Ph, etc. X = N; Y = CH2], isoquinolines I [R1 = H; R2 = H, 1-Ph; X = CH2; Y = N] and indoles II [R1 = H, 5-F, 4-Br, etc.; R2 = H, 2-Me; Y = CH2, N] were synthesized via a sodium tert-butoxide promoted oxidative dehydrogenation of the saturated heterocycles in DMSO solution This reaction proceeded under mild reaction conditions with a good functional group tolerance. Mechanistic studies suggested a radical pathway involved hydrogen abstraction of dimsyl radicals from the N-H bond or α-C-H of the substrates, and subsequent oxidation of the nitrogen or α-aminoalkyl radicals.

The article 《DMSO/t-BuONa/O2-Mediated Aerobic Dehydrogenation of Saturated N-Heterocycles》 also mentions many details about this compound(2343-22-8)Application of 2343-22-8, you can pay attention to it, because details determine success or failure

Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Kumaran, Elumalai; Leong, Weng Kee published an article about the compound: 5-Fluoroindoline( cas:2343-22-8,SMILESS:FC1=CC2=C(NCC2)C=C1 ).Reference of 5-Fluoroindoline. 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:2343-22-8) through the article.

Gold nanoclusters were good catalyst precursors for the catalytic dehydrogenation of indolines to obtain indoles I [R1 = H, 5-Me, 5-F, 5-Br, 5-NO2, 6-NO2; R2 = H, Me, CO2Me, CO2Et]. Furthermore, this method was used to synthesize quinolines and quinazolines II [R3 = H, 4-ClC6H4, 2-furyl, etc.; R4 = H, 6-Br, 6,8-di-Br; X = CH, N] from tetrahydroquinolines and tetrahydroquinazolines. The catalytically active species was presumably Au(0) nanoparticles.

The article 《Gold(0) catalyzed dehydrogenation of N-heterocycles》 also mentions many details about this compound(2343-22-8)Reference of 5-Fluoroindoline, you can pay attention to it, because details determine success or failure

Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 5-Fluoroindoline( cas:2343-22-8 ) is researched.Application In Synthesis of 5-Fluoroindoline.Jin, Ning; Pan, Changduo; Zhang, Honglin; Xu, Pan; Cheng, Yixiang; Zhu, Chengjian published the article 《Rhodium-Catalyzed Direct C7 Alkynylation of Indolines》 about this compound( cas:2343-22-8 ) in Advanced Synthesis & Catalysis. Keywords: triisopropylsilylethynylindolinylethanone preparation; acetylindoline TIPS EBX alkynylation rhodium catalyst. Let’s learn more about this compound (cas:2343-22-8).

An efficient rhodium(III)-catalyzed direct C7 alkynylation of indoline C-H bonds e.g., I with the alkynylated hypervalent iodine reagents II (R = triisopropylsilyl, t-butyldimethylsilyl, trimethylsilyl, triethylsilyl) has been developed. This reaction proceeds smoothly under mild conditions over a wide structural scope with high site-selectivity and excellent functional-group tolerance.

After consulting a lot of data, we found that this compound(2343-22-8)Application In Synthesis of 5-Fluoroindoline can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Chemistry – An Asian Journal called Syntheses of 1H-Indoles, Quinolines, and 6-Membered Aromatic N-Heterocycle-Fused Scaffolds via Palladium(II)-Catalyzed Aerobic Dehydrogenation under Alkoxide-Free Conditions, Author is Yoo, Hyung-Seok; Yang, Yo-Sep; Kim, Soo Lim; Son, Seung Hwan; Jang, Yoon Hu; Shin, Jeong-Won; Kim, Nam-Jung, which mentions a compound: 2343-22-8, SMILESS is FC1=CC2=C(NCC2)C=C1, Molecular C8H8FN, Application of 2343-22-8.

Aromatic N-heterocycle-fused scaffolds such as indoles and quinolines I (R1 = H, 5-Me, 6-NH2, etc.; R2 = H, 2-Me, 2-C6H5, etc.; X = C, N) are important core structures found in various bioactive natural products and synthetic compounds Recently, various dehydrogenation methods with the help of alkoxides, known to significantly promote dihydro- or tetrahydro-heterocycles to be oxidized, were developed for the heterocycle synthesis. However, these approaches are sometimes unsuitable due to resulting undesired side reactions such as reductive dehalogenation. Herein, expedient syntheses of 1H-indoles, quinolines, and 6-membered N-heterocycle-fused scaffolds from their hydrogenated forms through palladium(II)-catalyzed aerobic dehydrogenation under alkoxide-free conditions are reported. A total of 48 compounds were successfully synthesized with a wide range of functional groups including halogens (up to 99% yield). These methodologies provide facile routes for various privileged structures possessing aromatic N-heterocycles without the help of alkoxides, in highly efficient manners.

After consulting a lot of data, we found that this compound(2343-22-8)Application of 2343-22-8 can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

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.Wang, Xuan; Tang, Huanyu; Feng, Huijin; Li, Yuanchao; Yang, Yaxi; Zhou, Bing researched the compound: 5-Fluoroindoline( cas:2343-22-8 ).Recommanded Product: 5-Fluoroindoline.They published the article 《Access to Six- and Seven-Membered 1,7-Fused Indolines via Rh(III)-Catalyzed Redox-Neutral C7-Selective C-H Functionalization of Indolines with Alkynes and Alkenes》 about this compound( cas:2343-22-8 ) in Journal of Organic Chemistry. Keywords: diazepinoindoline preparation; pyridoindoline preparation; pyrroloquinolinone preparation; indoline derivative annulation alkene alkyne; acrylate aza Michael addition indoline derivative; alkenylation indoline derivative acrylate. We’ll tell you more about this compound (cas:2343-22-8).

We report herein a new strategy for the Rh(III)-catalyzed redox-neutral C7-selective C-H activation/annulation of indolines to rapidly access various privileged 1,7-fused indolines by utilizing an oxidizing-directing group. For example, a Rh(III)-catalyzed redox-neutral C7-selective C-H functionalization of indolines, e.g., I [R = OMe, O2CCMe3, R1 = H; R = OMe, R1 = Me-2, Me-3, (CH2)5-3,3, Me-4, Me-5, OMe-5, Cl-5, Br-5, CO2Me-5] with arylalkynes, e.g., II [R2 = H, Me-4, OMe-4, F-4, Me-3], is described to directly access 7-membered 1,7-fused indolines, e.g., III [R1 = Me-2, Me-3, (CH2)5-3,3, Me-4, Me-5, OMe-5, Cl-5, Br-5, CO2Me-5, R2 = H; R1 = H, R2 = H, Me-4, OMe-4, F-4, Me-3]. Moreover, an unprecedented intramol. addition of an alkenyl-Cp*Rh(III) species to a carbamoyl moiety occurred to give 1H-pyrroloquinolinones, e.g., IV [R1 = Me-2, Me-3, (CH2)5-3,3, Me-4, Me-5, OMe-5, Cl-5, Br-5, CO2Me-5, R3 = Et; R1 = H, R3 = Me, Pr, Bu], when employing alkyl alkynes, e.g., R3CCR3. Addnl., an efficient Rh(III)-catalyzed redox-neutral C7-selective C-H activation/alkenylation/aza-Michael addition of indolines is also developed to give 6-membered 1,7-fused indolines, e.g., V [R1 = H, Me-4, Me-5, OMe-5, Cl-5, Br-5, F-5, OMe-6, R4 = CO2Me; R1 = H, R4 = CO2Et, CO2Bu, CO2CMe3, CO2CH2Ph, SO2Ph, CN, P(:O)(OEt)2] . The advantages of these processes are as follows: (1) mild and simple reaction conditions; (2) no need for an external oxidant; (3) broad scope of substrates; and (4) valuable six- or seven-membered 1,7-fused indolines as products.

Although many compounds look similar to this compound(2343-22-8)Recommanded Product: 5-Fluoroindoline, numerous studies have shown that this compound(SMILES:FC1=CC2=C(NCC2)C=C1), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 5-Fluoroindoline( cas:2343-22-8 ) is researched.Electric Literature of C8H8FN.Shi, Yunkai; Chen, Chao; Yang, Yaxi; Bing, zhou published the article 《Rh(III)-catalyzed selective C7-H functionalization of indolines with 1,3-enynes enables access to six-membered 1,7-fused indolines》 about this compound( cas:2343-22-8 ) in Tetrahedron Letters. Keywords: fused indoline preparation diastereoselective; indoline enyne cyclization rhodium catalyst. Let’s learn more about this compound (cas:2343-22-8).

Herein a Rh(III)-catalyzed C7-selective C-H activation/annulation of indolines I (R = H, OMe, F; R1 = H, Me, Br, Cl, F, OMe; R2 = H, Me; R3 = H, Me; R4 = H; R3R4 = -(CH2)5-; R5 = H, Me; R4R5 = -CH=CH-CH=CH-) with 1,3-enynes R6CCCH=C(CH3)2 (R6 = n-Bu, cyclopropyl, Ph, etc.) to efficiently access various privileged 1,7-fused indolines II bearing an all-carbon quaternary stereogenic carbon center was described. Notably, the resulting products II (R = R1 = R2 = R3 = R4 = R5 = H; R6 = cyclopropyl) can be readily transformed into 1,7-fused indoles III, further widening the C-7 derivatization of indoles and highlighting the synthetic utility of this methodol.

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Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Related Products of 2343-22-8. 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-Fluoroindoline, is researched, Molecular C8H8FN, CAS is 2343-22-8, about Discovery and Optimization of Pyrimidone Indoline Amide PI3Kβ Inhibitors for the Treatment of Phosphatase and Tensin Homologue (PTEN)-Deficient Cancers.

Compelling mol. biol. publications have reported the implication of phosphoinositide kinase PI3Kβ in PTEN-deficient cell line growth and proliferation. These findings supported a scientific rationale for the development of PI3Kβ-specific inhibitors for the treatment of PTEN-deficient cancers. This paper describes the discovery of 2-[2-(2,3-dihydro-indol-1-yl)-2-oxo-ethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one and the optimization of this new series of active and selective pyrimidone indoline amide PI3Kβ inhibitors. 2-[2-(2-Methyl-2,3-dihydro-indol-1-yl)-2-oxo-ethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one (I), identified following a carefully designed Me scan, displayed improved physicochem. and in vitro pharmacokinetic properties. Structural biol. efforts enabled the acquisition of the first x-ray cocrystal structure of p110β with the selective inhibitor compound I bound to the ATP site. The nonplanar binding mode described herein is consistent with observed structure-activity relationship for the series. Compound I demonstrated significant in vivo activity in a UACC-62 xenograft model in mice, warranting further preclin. investigation. Following successful development, compound 28 entered phase I/Ib clin. trial in patients with advanced cancer.

Although many compounds look similar to this compound(2343-22-8)Related Products of 2343-22-8, numerous studies have shown that this compound(SMILES:FC1=CC2=C(NCC2)C=C1), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics