Category: 21987-29-1

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 21987-29-1, name is 4,4-Difluoropiperidine, introducing its new discovery. category: piperidines

Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore

A series of tetrahydroisoquinolines acting as dual histamine H3/serotonin transporter ligands is described. A highly regio-selective synthesis of the tetrahydroisoquinoline core involving acid mediated ring-closure of an acetophenone intermediate followed by reduction with NaCNBH3 was developed. In vitro and in vivo data are discussed.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 21987-29-1 is helpful to your research. category: piperidines

Reference£º
Piperidine – Wikipedia,
Piperidine | C5H3116N – PubChem

 

Chemistry is an experimental science, Product Details of 21987-29-1, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 21987-29-1, Name is 4,4-Difluoropiperidine

Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3)

PRMT3 catalyzes the asymmetric dimethylation of arginine residues of various proteins. It is crucial for maturation of ribosomes and has been implicated in several diseases. We recently disclosed a highly potent, selective, and cell-active allosteric inhibitor of PRMT3, compound 4. Here, we report comprehensive structure-activity relationship studies that target the allosteric binding site of PRMT3. We conducted design, synthesis, and evaluation of novel compounds in biochemical, selectivity, and cellular assays that culminated in the discovery of 4 and other highly potent (IC50 values: ?10-36 nM), selective, and cell-active allosteric inhibitors of PRMT3 (compounds 29, 30, 36, and 37). In addition, we generated compounds that are very close analogs of these potent inhibitors but displayed drastically reduced potency as negative controls (compounds 49-51). These inhibitors and negative controls are valuable chemical tools for the biomedical community to further investigate biological functions and disease associations of PRMT3.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Product Details of 21987-29-1, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 21987-29-1, in my other articles.

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Piperidine – Wikipedia,
Piperidine | C5H3062N – PubChem

 

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.21987-29-1,4,4-Difluoropiperidine,as a common compound, the synthetic route is as follows.

Synthesis of methyl (3R)-4-[6-(4,4-difluoropiperidin-l-yl)-2-(methylsulfanyl)pyrimidin- 4-yl]-3-methylmorpholine: Into a 40-mL microwave and maintained with an inert atmosphere of nitrogen, was placed (3R)-4-[6-chloro-2-(methylsulfanyl)pyrimidin-4-yl]-3-methylmorpholine (1 g, 3.85 mmol, 1 equiv), 4,4-difluoropiperidine (932.7 mg, 7.70 mmol, 2.0 equiv), Pd2(dba)3 (352.5 mg, 0.38 mmol, 0.10 equiv), XantPhos (445.5 mg, 0.77 mmol, 0.20 equiv), Cs2C03 (2.5 g, 7.70 mmol, 2.00 equiv), dioxane(10 ml). The resulting solution was stirred for 1 hr at 90 ¡ãC. The solids were filtered out. The combined organic layer was concentrated. The residue was applied onto a silica gel column with ethyl acetate/petroleum ether (1 :3). This resulted in 180 mg (13.57 percent) of (3R)-4-[6-(4,4-difluoropiperidin- l-yl)-2-(methylsulfanyl)pyrimidin-4-yl]-3- methylmorpholine as a white solid. LC-MS-BLV-CY-232-2: (ES, m/z): 345 [M+H]+. H-NMR- BLV-CY-232-2: (300 MHz, d6-DMSO, ppm): delta 5.73 (s, 1H), 4.42-4.31 (m, 1H), 3.97-3.87 (m, 2H), 3.71-3.68 (m, 5H), 3.56 (dd, 7 = 11.4, 2.9 Hz, 1H), 3.41 (td, 7 = 11.8, 2.8 Hz, 1H), 3.04 (td, 7 = 12.8, 3.6 Hz, 1H), 2.38 (s, 3H), 2.02-1.89 (m, 4H), 1.13 (d, 7 = 6.7 Hz, 3H)., 21987-29-1

The synthetic route of 21987-29-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BLUEVALLEY PHARMACEUTICAL LLC; LI, Xiang; (99 pag.)WO2019/50889; (2019); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In a patent, 21987-29-1, molecular formula is C5H9F2N, introducing its new discovery., 21987-29-1

SUBSTITUTED PYRIDINES AND METHOD OF USE

The invention discloses compounds of Formula (I) wherein X, R1, R2, and R3 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.

21987-29-1, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 21987-29-1

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Piperidine – Wikipedia,
Piperidine | C5H3030N – PubChem

 

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.21987-29-1,4,4-Difluoropiperidine,as a common compound, the synthetic route is as follows.

A mixture of Intermediate B (879 mg, 3.30 mmol), 4,4-difluoropiperidine (400 mg, 3.30 mmol), Pd2(dba)3 (302 mg, 0.330 mmol), xantphos (382 mg, 0.660 mmol) and KO’Bu (748 mg, 6.60 mmol) in toluene (10 ml) was bubbled with argon for 10 min. The mixture was then heated at 100¡ãC for overnight. The reaction was quenched with 60percent NaHC03 aqueous solution. The aqueous phase was extracted with DCM/IPA (20 ml x3, V/V = 3/1 ). The combined organic phase was dried over anhydrous MgS04. Filtered and concentrated. The residue was purified by silica gel chromatography (eluted with 2percent MeOH in DCM) to give the title compound as yellow solid (270 mg, 31 percent yield). LCMS (method B): [M+H]+ = 265, tR = 1.79 min.

21987-29-1, 21987-29-1 4,4-Difluoropiperidine 2758352, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; CHEN, Chao; DENG, Haibing; GUO, Haibing; HE, Feng; JIANG, Lei; LIANG, Fang; MI, Yuan; WAN, Huixin; XU, Yao-Chang; YU, Hongping; ZHANG, Ji Yue (Jeff); WO2013/38362; (2013); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

21987-29-1, 4,4-Difluoropiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In a 100 mL flask was placed 4-[5-(2-tert-butyl-4-pyridyl)-3-thienyl]-3-chloro-benzoic acid (150 mg, 0.40 mmol, 1 eq.) in DMF (10 mL), followed by addition of DIPEA (0.37 mL, 1.61 mmol, 5 eq.) and HATU (307 mg, 0.80 mmol, 2 equiv), and the resulting mixture was stirred for 5 min at RT and 3,3-difluoropiperidine (196 mg, 1.61 mmol, 4 eq.) were added and the mixture stirred at RT under nitrogen atmosphere overnight. The progress of the reaction was monitored by TLC and LCMS. After completion of reaction, the mixture was diluted with water (100 mL) and extracted with EtOAc (2*100 mL), washed with water (4*100 mL) then dried over anhydrous sodium sulfate and the combined organic layer was concentrated under reduced pressure to give a viscous compound, which was purified by reverse phase HPLC process to afford [4-[5-(2-tert-butyl-4-pyridyl)-3-thienyl]-3-chloro-phenyl]-(4,4-difluoro-1-piperidyl) methanone (50 mg) as an off-white solid, the free base. 1H NMR (400 MHz, Methanol-d4) delta (ppm): 8.49 (d, J=5.2 Hz, 1H), 7.91 (s, 1H), 7.78 (s, 1H), 7.71-7.61 (m, 3H), 7.52 (d, J=5.2 Hz, 1H), 7.47 (d, J=7.9 Hz, 1H), 3.87 (t, 2H), 3.62 (t, 2H), 2.08 (t, 4H), 1.42 (s, 9H). LCMS: (M+1) 475.2.

21987-29-1, 21987-29-1 4,4-Difluoropiperidine 2758352, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Medivation Technologies LLC; Pujala, Brahmam; Jangir, Ramniwas; Guguloth, Rambabu; Shinde, Bharat Uttam; Rai, Roopa; Pham, Son Minh; Bernales, Sebastian; Lindquist, Jeffrey; Guha, Mausumee; Kallem, Satyanarayana; Bhatt, Bhawana; Bhagwat, Vikas Ramdas; (162 pag.)US2018/51013; (2018); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.21987-29-1,4,4-Difluoropiperidine,as a common compound, the synthetic route is as follows.

Step 8: N-(cis-3-{[(4,4-Difluoropiperidin-1-yl)sulfonyl]methyl}cyclobutyl)-N-methyl-7-[(4-methylphenyl)sulfonyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine To a mixture of 4,4-difluoropiperidine (77 mg, 0.64 mmol) and triethylamine (97 mg, 0.96 mmol) in tetrahydrofuran (20 mL) at 0¡ã C. was added dropwise a solution of cis-[3-(methyl{7-[(4-methylphenyl)sulfonyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}amino)cyclobutyl]methanesulfonyl chloride (150 mg, 0.320 mmol) in tetrahydrofuran (10 mL). The mixture was allowed to warm to room temperature overnight. The solvent was evaporated and the residue was taken up in ethyl acetate (80 mL). The solution was washed with brine (30 mL), dried over sodium sulfate and concentrated to afford the crude title compound (134 mg) as a white solid. LC/MS (exact mass) calculated for C24H29F2N5O4S2; 553.651. found (M+H+); 554.3., 21987-29-1

As the paragraph descriping shows that 21987-29-1 is playing an increasingly important role.

Reference£º
Patent; Pfizer Inc.; Brown, Matthew Frank; Fenwick, Ashley Edward; Flanagan, Mark Edward; Gonzales, Andrea; Johnson, Timothy Allan; Kaila, Neelu; Mitton-Fry, Mark J.; Strohbach, Joseph Walter; TenBrink, Ruth E.; Trzupek, John David; Unwalla, Rayomand Jal; Vazquez, Michael L.; US2014/243312; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.21987-29-1,4,4-Difluoropiperidine,as a common compound, the synthetic route is as follows.

Example 1683-(4-Cyclohexylamino-1H-pyrazolo[4,3-c]pyridin-3-yl)-1-(4,4-drfluoro-piperidin-1-yl)-propan-1-oneTo a solution of Intermediate 23 (35 mg, 0.12 mmol) in DMF (1.5 ml) was added HATU (48 mg, 0.13 mmol) and Lambda/,Lambda/-diisopropylethylamine (126 mul, 0.73 mmol). 4,4-difluoro0 piperidine (19 mul, 0.18 mmol) was then added and the resulting solution was left to stir at room temperature overnight. The volatiles were removed under reduced pressure and the crude product was re-dissolved in 10percent MeOH/DCM and eluted though an Isolute-NH2 cartridge. The crude product purified by flash chromatography eluting with 10percent MeOH/DCM to give a yellow gum (28 mg, 61percent). 1H NMR (400 MHz, DMSO-Cf6) delta ppm-5 1.14 – 1.26 (m, 1 H), 1.30 – 1.46 (m, 4 H), 1.60 – 1.72 (m, 1 H), 1.71 – 2.01 (m, 8 H), 2.87 (t, 2 H), 3.21 (t, J=6.4 Hz, 2 H), 3.49 – 3.60 (m, 4 H), 4.01 (br. s., 1 H), 6.67 (br. s., 1 H), 7.62 (d, J=6.0 Hz, 1 H); m/z (ES+APCl)+: 392 [M + H]+., 21987-29-1

As the paragraph descriping shows that 21987-29-1 is playing an increasingly important role.

Reference£º
Patent; MEDICAL RESEARCH COUNCIL TECHNOLOGY; MCIVER, Edward, Giles; SMILJANIC, Ela; HARDING, Denise, Jamilla; HOUGH, Joanne; WO2010/106333; (2010); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.21987-29-1,4,4-Difluoropiperidine,as a common compound, the synthetic route is as follows.

Example 1683-(4-Cyclohexylamino-1H-pyrazolo[4,3-c]pyridin-3-yl)-1-(4,4-drfluoro-piperidin-1-yl)-propan-1-oneTo a solution of Intermediate 23 (35 mg, 0.12 mmol) in DMF (1.5 ml) was added HATU (48 mg, 0.13 mmol) and Lambda/,Lambda/-diisopropylethylamine (126 mul, 0.73 mmol). 4,4-difluoro0 piperidine (19 mul, 0.18 mmol) was then added and the resulting solution was left to stir at room temperature overnight. The volatiles were removed under reduced pressure and the crude product was re-dissolved in 10percent MeOH/DCM and eluted though an Isolute-NH2 cartridge. The crude product purified by flash chromatography eluting with 10percent MeOH/DCM to give a yellow gum (28 mg, 61percent). 1H NMR (400 MHz, DMSO-Cf6) delta ppm-5 1.14 – 1.26 (m, 1 H), 1.30 – 1.46 (m, 4 H), 1.60 – 1.72 (m, 1 H), 1.71 – 2.01 (m, 8 H), 2.87 (t, 2 H), 3.21 (t, J=6.4 Hz, 2 H), 3.49 – 3.60 (m, 4 H), 4.01 (br. s., 1 H), 6.67 (br. s., 1 H), 7.62 (d, J=6.0 Hz, 1 H); m/z (ES+APCl)+: 392 [M + H]+., 21987-29-1

As the paragraph descriping shows that 21987-29-1 is playing an increasingly important role.

Reference£º
Patent; MEDICAL RESEARCH COUNCIL TECHNOLOGY; MCIVER, Edward, Giles; SMILJANIC, Ela; HARDING, Denise, Jamilla; HOUGH, Joanne; WO2010/106333; (2010); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem