Category: 84163-13-3

Electric Literature of 84163-13-3, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.84163-13-3, Name is 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride, molecular formula is C12H14ClFN2O. In a Article，once mentioned of 84163-13-3

The synthesis of a series of 3-(1-substituted-4-piperidinyl)-1,2-benzisoxazoles is described.The neuroleptic activity of the series was evaluated by utilizing the climbing mice assay and inhibition of <3H>spiroperidol binding.Structure-activity relationships were studied by variation of the substituent on the benzisoxazole ring with concomitant variation of four different 1-piperidinyl substituents.Maximum neuroleptic activity was realized when there was a 6-fluoro substituent on the benzisoxazole ring.The 1-piperidinyl substituent appeared less significant, although in most cases, the (1,3-dihydro-2-oxo-2H-benzimidazol-1-yl)propyl group imparted maximum potency.The most potent compound in both assays was 6-fluoro-3-<1-<3-(1,3-dihydro-2-oxo-2H-benzimidazol-1-yl)propyl>-4-piperidinyl>-1,2-benzisoxazole (11b).

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 84163-13-3 is helpful to your research. Electric Literature of 84163-13-3

Reference：
Piperidine – Wikipedia,
Piperidine | C5H20986N – PubChem

 

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent， Quality Control of: 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride, Which mentioned a new discovery about 84163-13-3

The present invention relates to an improved and industrially viable process for the preparation of high purity ? 99.8% chemical of paliperidone of formula-I (3-[2-[4-(6-fluoro-l,2-benzisoxazol-3-yl)-l-piperidinyl]ethyl]-6,7,8,9-tetra-hydro-9-hydroxy-2- methyl-4H-pyrido[l,2-a]pyrimidin-4-one), involving the novel intermediate, 3-(2- hydroxyethyl)-2-methyl-9-(phenylmethoxy)-4H-Pyrido[l,2-a]pyrimidin-4-one of formula-II. All intermediates encountered in the synthetic pathway of present invention are isolated by simple crystallization techniques in high pure. Paliperidone is useful as anti-psychotic agent in the treatment of psychotic disorders and is marketed under the brand name INVEGA.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 84163-13-3, help many people in the next few years.Quality Control of: 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride

Reference：
Piperidine – Wikipedia,
Piperidine | C5H21000N – PubChem

 

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬ Application In Synthesis of 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride, Which mentioned a new discovery about 84163-13-3

PROCESS FOR THE PREPARATION OF PALIPERIDONE

The present invention provides a process for the preparation of paliperidone or a pharmaceutically acceptable salt thereof, wherein the process comprises condensing a compound of formula (II) with a compound of formula (III) or a salt thereof, in a suitable solvent and a base, in the presence of a catalyst and an inhibiting agent, wherein the inhibiting agent is added to the reaction system before the compound of formula (II) and compound of formula (III) have reacted or as the reaction of the compound of formula (II) and compound of formula (III) is initiated, and optionally converting the paliperidone to a salt thereof, wherein X is a suitable leaving group. The present invention also provides substantially pure paliperidone or a salt thereof, paliperidone or a salt thereof as prepared by the process and uses of the paliperidone or salt thereof.

Because enzymes can increase reaction rates by enormous factors and tend to be very specific, Application In Synthesis of 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 84163-13-3

Reference£º
Piperidine – Wikipedia,
Piperidine | C5H21013N – PubChem

 

Related Products of 84163-13-3, In heterogeneous catalysis, the catalyst is in a different phase from the reactants. At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 84163-13-3, name is 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride. In an article£¬Which mentioned a new discovery about 84163-13-3

Discovery of 4-benzoylpiperidine and 3-(piperidin-4-yl)benzo[d]isoxazole derivatives as potential and selective GlyT1 inhibitors

Regulation of glycine transporter 1 (GlyT1) activity is a currently investigated strategy in drug discovery for schizophrenia. This study developed a series of new 4-benzoylpiperidine derivatives as GlyT1 inhibitors by bioisosteric replacement and mimicking of the pyridine ring of RG1678. Among the 4-benzoylpiperidine derivatives, 23q showed an IC50 of 30 nM. Preliminary optimization of the blood-brain barrier penetration led to the discovery of 3-(piperidin-4-yl)benzo[d]isoxazole derivatives. Both series showed good selectivity over GlyT2, D1, D2, D3, 5-HT1A and 5-HT2A receptors. Moreover, behavioral testing showed 23q (40 mg kg-1, intragastric) can inhibit the hyperlocomotion induced by acute treatment of phencyclidine, and improve the impaired negative and cognitive symptoms in chronic phencyclidine-induced C57BL/6J mice. An interesting finding showed that 3-(piperidin-4-yl)benzo[d]isoxazole was a privileged scaffold of atypical antipsychotic agents but exhibited high selectivity and potency as a GlyT1 inhibitor.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.84163-13-3. In my other articles, you can also check out more blogs about 84163-13-3

Reference£º
Piperidine – Wikipedia,
Piperidine | C5H21041N – PubChem

 

Related Products of 84163-13-3, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.84163-13-3, Name is 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride, molecular formula is C12H14ClFN2O. In a Patent£¬once mentioned of 84163-13-3

A process for the preparation of the Iraqi pan Litong (by machine translation)

The invention provides a preparation method of iloperidone, and the invention comprises the reaction of 1-[4-(3-substituted oxypropyl)-3-methoxyphenyl] ethyl ketone and 6-fluoro-3-(4-piperidyl)-1,2-benzisoxazole hydrochloride in a mixed solution of ester and amide to obtain iloperidone. The method has a high yield and less impurities, improves product colors, and is suitable for industrial production.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 84163-13-3

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Piperidine – Wikipedia,
Piperidine | C5H21030N – PubChem

 

84163-13-3, 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,84163-13-3

A mixture of 6-fluoro-3- (4-piperidinyl) -1,2-benzisoxazole hydrochloride was added to 400 mL of DMF, and potassium carbonate35 g, 3.5 g of potassium iodide and 33.5 g of 3-methoxy-4- (3-chloropropoxy) acetophenone were added and heated for about 7 h. Cold to room temperature, pumpingFilter, the filtrate stirring into the 1000mL cold water, stirring about 2h, pumping, washing, drying, light yellow crude 53g. EthanolAfter recrystallization, 28 g of iloperidone was obtained and the content of ILPI-07 was 0.12%.

The synthetic route of 84163-13-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Beijing Pharmaceutical Group Co., Ltd.; Wang Qichang; Liu Moyi; Liu Qingliang; Zou Jiang; Yang Yan; (9 pag.)CN106831742; (2017); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

84163-13-3,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.84163-13-3,6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride,as a common compound, the synthetic route is as follows.

General procedure: To Boc-Xaa-OH (0.005 mol) and HOBt (0.765 g, 0.005 mol) dissolved in DMF (10 mL/g of peptide) and cooled to 0 C was added NMM (0.55 mL, 0.005 mol). EDCI (0.956 g, 0.005 mol) was added under stirring while maintaining the temperature at 0 C. The reaction mixture was stirred for an additional 10 min and pre-cooled solution of [3-(4-piperidinyl)-6-fluoro-1,2-benzisoxazole]HCl (1.285 g, 0.005 mol) and NMM (0.55 mL, 0.005 mol) in DMF (13 mL) was added slowly (Scheme 4). After 20 min, pH of the solution was adjusted to 8 by the addition of NMM and the reaction mixture was stirred overnight at room temperature. DMF was removed under reduced pressure and the residue was poured into about 200 mL ice-cold 90% saturated KHCO3 solution and stirred for 30 min. The precipitated product was taken into CHCl3 and washed with 5% NaHCO3 solution (2 ¡Á 20 mL), water (2 ¡Á 20 mL), 0.1 N cold HCl solution (2 ¡Á 20 mL) and finally brine solution (2 ¡Á 20 mL). The CHCl3 layer was dried over anhydrous Na2SO4 and the solvent was removed under reduced pressure. The products so obtained were recrystallized from ether/petroleum ether to get white colored desired conjugates (16-25).

84163-13-3 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride 11334359, apiperidines compound, is more and more widely used in various fields.

Reference£º
Article; Suhas; Chandrashekar; Gowda, D. Channe; European Journal of Medicinal Chemistry; vol. 46; 2; (2011); p. 704 – 711;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

84163-13-3, 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

84163-13-3, 10g of reactant 6-fluoro-3-(4-piperidinyl)-1,2-benzoisoxazole hydrochloride and 10.4g of reactant 1-[4-(3-chloropropoxyl)-3-inethoxyphenyl]ethyl ketone were placed in a 250ml reaction flask, and a solution prepared with 17.9g potassium carbonate and 120ml water was added thereto. The reaction mixture was heated to 80-90 C and stirred for 1.5 hours, then naturally cooled to room temperature under stirring and filtered. The filter cake was washed twice with water, and then washed twice with methanol, and dried in vacuum at 50 C to obtain 15.1g crude iloperidone. The yield was 91.0%. The crude product was decolored by active carbon, then recrystallized with toluene to obtain iloperidone. The purity was 99.5% (determined by HPLC), and the melting point was 118~120C.

84163-13-3 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride 11334359, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Zhejiang Huahai Pharmaceutical Co., Ltd.; EP2479176; (2012); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem