Category: 136725-55-8

Varghese, Swapna; Rahmani, Raphael; Russell, Stephanie; Deora, Girdhar Singh; Ferrins, Lori; Toynton, Arthur; Jones, Amy; Sykes, Melissa; Kessler, Albane; Eufrasio, Amanda; Cordeiro, Artur Torres; Sherman, Julian; Rodriguez, Ana; Avery, Vicky M.; Piggott, Matthew; Baell, Jonathan B. published an article about the compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride( cas:136725-55-8,SMILESS:Cl.F[C@@H]1CCNC1 ).Recommanded Product: 136725-55-8. 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:136725-55-8) through the article.

Trypanosoma brucei (T. brucei) and Trypanosoma cruzi (T. cruzi) are causative agents of parasitic diseases known as human African trypanosomiasis and Chagas disease, resp. Together, these diseases affect 68 million people around the world. Current treatments are unsatisfactory, frequently associated with intolerable side-effects, and generally inadequate in treating all stages of disease. In this paper, we report the discovery of N-ethylurea pyrazoles that potently and selectively inhibit the viability of T. brucei and T. cruzi. Sharp and logical SAR led to the identification of 54 as the best compound, with an in vitro IC50 of 9 nM and 16 nM against T. b. brucei and T. cruzi, resp. Compound 54 demonstrates favorable physicochem. properties and was efficacious in a murine model of Chagas disease, leading to undetectable parasitemia within 6 days when CYP metabolism was inhibited.

From this literature《Discovery of Potent N-Ethylurea Pyrazole Derivatives as Dual Inhibitors of Trypanosoma brucei and Trypanosoma cruzi》,we know some information about this compound(136725-55-8)Recommanded Product: 136725-55-8, but this is not all information, there are many literatures related to this compound(136725-55-8).

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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.Yamagami, Takafumi; Kobayashi, Ryo; Moriyama, Noriaki; Horiuchi, Hideki; Toyofuku, Eiji; Kadoh, Yoichi; Kawanishi, Eiji; Izumoto, Shinichi; Hiramatsu, Hajime; Nanjo, Takehiro; Sugino, Masuhiro; Utsugi, Masayuki; Moritani, Yasunori researched the compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride( cas:136725-55-8 ).Product Details of 136725-55-8.They published the article 《Scalable Process Design for a PDE10A Inhibitor Consisting of Pyrazolopyrimidine and Quinoxaline as Key Units》 about this compound( cas:136725-55-8 ) in Organic Process Research & Development. Keywords: PDE10A inhibitor pyrazolopyrimidine quinoxaline preparation. We’ll tell you more about this compound (cas:136725-55-8).

In this study, research and development for the synthetic process of a PDE10A inhibitor are described; in particular, an efficient regioselective construction of the quinoxaline unit, a cost-effective pyrazolo[1,5-a]pyrimidine formation, and a cost-saving approach in a nucleophilic aromatic substitution (SNAr) reaction by introducing oxazolidinone as an electron-withdrawing group to a chloropyrazolo[1,5-a]pyrimidine core are key points. The newly developed process has been successfully scaled up to 40 kg. Furthermore, a one-pot tandem reaction from aminopyrazole to dichloropyrazolo[1,5-a]pyrimidine by activating malonic acid with POCl3 was discovered. The finding contributed to avoiding isolation of the hygroscopic pyrazolo[1,5-a]pyrimidin-5(4H)-one intermediate, which caused complicated filtration and drying processes observed in the first scale-up campaign.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride, is researched, Molecular C4H9ClFN, CAS is 136725-55-8, about Discovery of novel 4-phenyl-2-(pyrrolidinyl)nicotinamide derivatives as potent Nav1.1 activators, the main research direction is phenyl pyrrolidinyl nicotinamide derivative preparation sodium channel CNS disease; Dravet syndrome phenyl pyrrolidinyl nicotinamide derivative preparation; BBB penetration; Dravet syndrome; Na(v)1.1 activator; Slow current decay of inactivation; Voltage-gated sodium channels.Formula: C4H9ClFN.

The voltage-gated sodium channel, Nav1.1, is predominantly expressed in parvalbumin-pos. fast spiking interneurons and has been genetically linked to Dravet syndrome. Starting from a high throughput screening hit isoxazole derivative 5, modifications of 5 via combinations of IonWorks and Q-patch assays successfully identified the nicotinamide derivative 4. Its increasing decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6 and acceptable brain exposure in mice was observed Compound 4 is a promising Nav1.1 activator that can be used to analyze pathophysiol. functions of the Nav1.1 channel towards treating various central nervous system diseases.

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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors》. Authors are Henderson, Scott H.; Sorrell, Fiona; Bennett, James; Fedorov, Oleg; Hanley, Marcus T.; Godoi, Paulo H.; Ruela de Sousa, Roberta; Robinson, Sean; Ashall-Kelly, Alexander; Hopkins Navratilova, Iva; Walter, Daryl S.; Elkins, Jonathan M.; Ward, Simon E..The article about the compound:(R)-(-)-3-Fluoropyrrolidine Hydrochloridecas:136725-55-8,SMILESS:Cl.F[C@@H]1CCNC1).HPLC of Formula: 136725-55-8. Through the article, more information about this compound (cas:136725-55-8) is conveyed.

Dual-specificity tyrosine-regulated kinase 1A (DYRK1A) regulates the proliferation and differentiation of neuronal progenitor cells during brain development. Consequently, DYRK1A has attracted interest as a target for the treatment of neurodegenerative diseases, including Alzheimer′s disease (AD) and Down′s syndrome. Recently, the inhibition of DYRK1A has been investigated as a potential treatment for diabetes, while DYRK1A′s role as a mediator in the cell cycle has garnered interest in oncol. indications. Structure-activity relationship (SAR) anal. in combination with high-resolution X-ray crystallog. leads to a series of pyrazolo[1,5-b]pyridazine inhibitors with excellent ligand efficiencies, good physicochem. properties, and a high degree of selectivity over the kinome. Compound 11 (I) exhibited good permeability and cellular activity without P-glycoprotein liability, extending the utility of 11 in an in vivo setting. These pyrazolo[1,5-b]pyridazines are a viable lead series in the discovery of new therapies for the treatment of diseases linked to DYRK1A function.

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Name: (R)-(-)-3-Fluoropyrrolidine Hydrochloride. 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: (R)-(-)-3-Fluoropyrrolidine Hydrochloride, is researched, Molecular C4H9ClFN, CAS is 136725-55-8, about 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.

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,
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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride( cas:136725-55-8 ) is researched.Safety of (R)-(-)-3-Fluoropyrrolidine Hydrochloride.Ai, Yong; Chen, Xiao-Gang; Shi, Ping-Ping; Tang, Yuan-Yuan; Li, Peng-Fei; Liao, Wei-Qiang; Xiong, Ren-Gen published the article 《Fluorine Substitution Induced High Tc of Enantiomeric Perovskite Ferroelectrics: (R)- and (S)-3-(Fluoropyrrolidinium)MnCl3》 about this compound( cas:136725-55-8 ) in Journal of the American Chemical Society. Keywords: manganese chloride fluoropyrrolidinium fluorine substitution enantiomeric perovskite ferroelec. Let’s learn more about this compound (cas:136725-55-8).

The past decade has witnessed much progress in designing mol. ferroelecs., whose intrinsic mech. flexibility, structural tunability, and easy processability are desirable for next-generation flexible and wearable electronic devices. However, an obstacle in expanding their promising applications in nonvolatile memory elements, capacitors, and sensors is effectively modulating the Curie temperature (Tc). Here, taking advantage of fluorine substitution on the reported mol. ferroelec., (pyrrolidinium)MnCl3, we present enantiomeric perovskite ferroelecs., namely, (R)- and (S)-3-(fluoropyrrolidinium)MnCl3. The close van der Waal’s radii and the similar steric parameters between H and F atoms ensure the min. disruption of the crystal structure, while their different electronegativity and polarizability can trigger significant changes in the phys. and chem. properties. As expected, the Tc gets successfully increased from 295 K in (pyrrolidinium)MnCl3 to 333 K in these two homochiral compounds Such a dramatic enhancement of 38 K signifies an important step toward designing high-Tc mol. ferroelecs. In the light of the conceptually new idea of fluorine substitution, one could look forward to a continuous succession of new mol. ferroelec. materials and technol. developments.

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Pyridazine – Wikipedia,
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Formula: C4H9ClFN. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride, is researched, Molecular C4H9ClFN, CAS is 136725-55-8, about Discovery of Potent N-Ethylurea Pyrazole Derivatives as Dual Inhibitors of Trypanosoma brucei and Trypanosoma cruzi. Author is Varghese, Swapna; Rahmani, Raphael; Russell, Stephanie; Deora, Girdhar Singh; Ferrins, Lori; Toynton, Arthur; Jones, Amy; Sykes, Melissa; Kessler, Albane; Eufrasio, Amanda; Cordeiro, Artur Torres; Sherman, Julian; Rodriguez, Ana; Avery, Vicky M.; Piggott, Matthew; Baell, Jonathan B..

Trypanosoma brucei (T. brucei) and Trypanosoma cruzi (T. cruzi) are causative agents of parasitic diseases known as human African trypanosomiasis and Chagas disease, resp. Together, these diseases affect 68 million people around the world. Current treatments are unsatisfactory, frequently associated with intolerable side-effects, and generally inadequate in treating all stages of disease. In this paper, we report the discovery of N-ethylurea pyrazoles that potently and selectively inhibit the viability of T. brucei and T. cruzi. Sharp and logical SAR led to the identification of 54 as the best compound, with an in vitro IC50 of 9 nM and 16 nM against T. b. brucei and T. cruzi, resp. Compound 54 demonstrates favorable physicochem. properties and was efficacious in a murine model of Chagas disease, leading to undetectable parasitemia within 6 days when CYP metabolism was inhibited.

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Reference:
Pyridazine – Wikipedia,
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Electric Literature of C4H9ClFN. 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: (R)-(-)-3-Fluoropyrrolidine Hydrochloride, is researched, Molecular C4H9ClFN, CAS is 136725-55-8, about Discovery of novel 4-phenyl-2-(pyrrolidinyl)nicotinamide derivatives as potent Nav1.1 activators. Author is Miyazaki, Tohru; Kawasaki, Masanori; Suzuki, Atsushi; Ito, Yuki; Imanishi, Akio; Maru, Takamitsu; Kawamoto, Tomohiro; Koike, Tatsuki.

The voltage-gated sodium channel, Nav1.1, is predominantly expressed in parvalbumin-pos. fast spiking interneurons and has been genetically linked to Dravet syndrome. Starting from a high throughput screening hit isoxazole derivative 5, modifications of 5 via combinations of IonWorks and Q-patch assays successfully identified the nicotinamide derivative 4. Its increasing decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6 and acceptable brain exposure in mice was observed Compound 4 is a promising Nav1.1 activator that can be used to analyze pathophysiol. functions of the Nav1.1 channel towards treating various central nervous system diseases.

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Pyridazine – Wikipedia,
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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Scalable Process Design for a PDE10A Inhibitor Consisting of Pyrazolopyrimidine and Quinoxaline as Key Units, published in 2019-04-19, which mentions a compound: 136725-55-8, Name is (R)-(-)-3-Fluoropyrrolidine Hydrochloride, Molecular C4H9ClFN, Reference of (R)-(-)-3-Fluoropyrrolidine Hydrochloride.

In this study, research and development for the synthetic process of a PDE10A inhibitor are described; in particular, an efficient regioselective construction of the quinoxaline unit, a cost-effective pyrazolo[1,5-a]pyrimidine formation, and a cost-saving approach in a nucleophilic aromatic substitution (SNAr) reaction by introducing oxazolidinone as an electron-withdrawing group to a chloropyrazolo[1,5-a]pyrimidine core are key points. The newly developed process has been successfully scaled up to 40 kg. Furthermore, a one-pot tandem reaction from aminopyrazole to dichloropyrazolo[1,5-a]pyrimidine by activating malonic acid with POCl3 was discovered. The finding contributed to avoiding isolation of the hygroscopic pyrazolo[1,5-a]pyrimidin-5(4H)-one intermediate, which caused complicated filtration and drying processes observed in the first scale-up campaign.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride, is researched, Molecular C4H9ClFN, CAS is 136725-55-8, about Highest-Tc organic enantiomeric ferroelectrics obtained by F/H substitution, the main research direction is organic enantiomeric ferroelec substitution phase transition temperature.Application of 136725-55-8.

Through the strategy of F/H substitution, we precisely designed the highest-Tc (phase transition temperature) organic enantiomeric ferroelecs., (R)- and (S)-(N,N-dimethyl-3-fluoropyrrolidinium) iodide, of which the Tc reaches up to 470 K, far beyond those of other enantiomeric ferroelecs. and also the com. ferroelec. BaTiO3.

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