Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.561314-57-6,2,8-Diazaspiro[4.5]decan-3-one,as a common compound, the synthetic route is as follows.,561314-57-6

To a solution of ethyl 5-oxo-2-azabicyclo[2.2.2]octane-2-carboxylate (6.70 g, 34 mmol)and 2,8-diazaspiro[4.5]decan-3-onel (5.24 g, 34 mmol) in DMF (30 mL) was addedHOAc (2.9 mL, 51 mmol) under nitgogen, the reaction mixture was stirred at rt for 20mi Na(OAc)3BH (21.60 g,102 mmol) was added and the reaction was stirred at45 0Cfor 3 d. Then the reaction mixture was warmed to 60 0C and stirred for another 24 h.The solvent was removed in vacuo and the residue was dissolved in water (20 mL)and basified with sat.NaHCO3. The aqueous layer was concentrated to dryness andthe resulting white solid was diluted with DCM (100 mL). The suspension was stirred atrt for 30 mm, filtered and the filter cake was washed with DCM (4 x 25 mL). Theorganic layers were combined and the solvent was removed in vacuo. The residuewas purified by preparative reversed phase HPLC (Instrument: Gilson, Column:Xbridge 21 .2*250 mm C18, 10 um; Mobile Phase: A: water (10 mMol/L NH4HCO3) B:CAN); Flow rate(ml/min): 25.00) to give the two racemic isomers of ethyl 5-(3-oxo-2,8-diazaspi ro[4. 5]dec-8-yl)-2-azabicyclo[2 .2.2]octane-2-carboxylate. Which were furtherpurified by chiral SFC (Column: OJ-H, 4.6*250mm; Co-solvent: MeOH(0.1% NH4OH);column temperature: 40;C02 flow rate: 2.55) to give ethyl 5-(3-oxo-2,8-diazaspi ro[4. 5]dec-8-yl)-2-azabicyclo[2 .2.2]octane-2-carboxylate, Example 3-1 Isomer1 (0.78 g, 6.9%) as a colourless solid, ethyl 5-(3-oxo-2,8-diazaspiro[4.5]dec-8-yl)-2-azabicyclo[2.2.2]octane-2-carboxylate, Example 3-1 Isomer 2 (1.20 g, 10.5%) as acolourless solid, ethyl 5-(3-oxo-2, 8-diazaspi ro[4. 5]dec-8-yl)-2-azabicyclo[2 .2 .2]octane-2-carboxylate, Example 3-1 Isomer 3 (0.45 g, 3.9%) as a colourless solid and ethyl 5-(3-oxo-2, 8-diazaspiro[4. 5]dec-8-yl)-2-azabicyclo[2 .2.2]octane-2-carboxylate, Exam pie3-1 isomer 4 (1.30 g, 11.4%) as a colourless solid.

The synthetic route of 561314-57-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; HEPTARES THERAPEUTICS LIMITED; CONGREVE, Miles Stuart; BROWN, Giles Albert; TEHAN, Benjamin Gerald; PICKWORTH, Mark; CANSFIELD, Julie Elaine; (105 pag.)WO2015/140559; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

106-52-5, 1-Methylpiperidin-4-ol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of N-methyl piperidinol (0.22 g, 1.96 mmol) and sodium hydroxide (79 mg, 1.96 mmol) in benzene (10 mL) was heated to reflux for 2 hours with stirring under nitrogen atmosphere and then cooled to 25 C. followed by the addition of compound 133 (0.25 g, 0.65 mmol) at same temperature. The mixture was heated to reflux for 6 hours, concentrated under vacuum and diluted with water (10 mL). The precipitated solid was filtered and purified by column chromatography (5-10% MeOH-CHCl3) to afford the title compound E26 as a pale yellow solid (0.16 g, 53%). HPLC: Hichrom RPB (250*4.6 mm) 5 microns [solvent A=0.01 M KH2PO4 (pH 7.0); solvent B=CH3CN], Gradient elution program: T/% B=0/60, 10/60, 25/80, 40/80, 45/60, 50/60; 270 nm, Rt 35.21 min, 98.09% purity; MS (CI): m/z 461 (M+H, 50), 364 (100).

106-52-5, As the paragraph descriping shows that 106-52-5 is playing an increasingly important role.

Reference£º
Patent; Timmer, Richard T.; Alexander, Christopher W.; Pillarisetti, Sivaram; Saxena, Uday; Yeleswarapu, Koteswar Rao; Pal, Manojit; Reddy, Jangalgar Tirupathy; Krishna Reddy, Velagala Venkata Rama Murali; Sridevi, Bhatlapenumarthy Sesha; Kumar, Potlapally Rajender; Reddy, Gaddam Om; US2004/209881; (2004); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.7149-42-0,(1-Methylpiperidin-4-yl)methanamine,as a common compound, the synthetic route is as follows.

General procedure: Exam le: Synthesis of final product 1A mixture of (1-methyl-4-piperidinyl)methanamine (101 mg, 0.78 mmol) and Intermediate 1-42 (100 mg, 0.26 mmol) in DMA (5 mL) was heated at 100 C for 8 h. The solvents were removed in vacuo and the residue was purified by column chromatography (DCM/7N NH3 in MeOH 100:0 to 98:2). The product obtained was triturated from Et20 to afford Final Product 1 (32 mg) as a white solid., 7149-42-0

The synthetic route of 7149-42-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS (CNIO); MCNEENEY, Stephen, Phillip; PASTOR FERNANDEZ, Joaquin; MARTINEZ GONZALES, Sonia; MARTIN HERNANDO, Jose Ignacio; RODRIGUEZ HERGUETA, Antonio; RICO FERREIRA, Maria del Rosario; BLANCO APARICIO, Carmen; WO2013/4984; (2013); A1;,
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Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.111153-74-3,1-Phenylpiperidine-4-carbaldehyde,as a common compound, the synthetic route is as follows.

Step E 4-[2-{1-(Triphenylmethyl)-4-imidazolyl}ethenyl]-1-phenylpiperidine The product from Step D is dissolved in THF and cooled to -78 C. under nitrogen. A solution of LDA in THF is added dropwise. The reaction was stirred at -78 C. for 1 h, then a solution of 4-formyl-1-phenylpiperidine from Step A is added, and the reaction warmed to room temperature overnight. The reaction is quenched with ammonium chloride solution, and extracted with ethyl acetate. The title compound is obtained after chromatography on silica gel.

111153-74-3, 111153-74-3 1-Phenylpiperidine-4-carbaldehyde 13842992, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Merck & Co., Inc.; US5891889; (1999); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.159635-49-1,tert-Butyl 4-methylenepiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Synthesis of tert-butyl 1,1-dichloro-2-oxo-7-azaspiro[3.5]nonane-7-carboxylate; Dry DME (8.0 L) and tert-butyl 4-methylenepiperidine-1-carboxylate (800 g, 4.06 mol) were charged to a reactor. Zinc-copper couple (800 g; CAS No.53801-63-1, Alfa-Aesar) was charged to the reactor, and the mixture was warmed to 34¡ã C. Trichloroacetyl chloride (1448 g, 8.0 mol, 888 mL) was added dropwise under a nitrogen atmosphere to the stirred suspension in the following manner: 80 mL of trichloroacetyl chloride was added. After 10 min, an exotherm elevated the reaction temperature to 39¡ã C. Dropwise addition of the remaining trichloroacetyl chloride was resumed immediately at a rate to maintain a temperature between 40-44¡ã C. using a 25¡ã C. jacket. After the addition was complete, the reaction was stirred at 40¡ã C. for 15 min. Cyclohexane (10 L) was added to the mixture. The mixture was filtered through a pad of celite, washing with cyclohexane (2 L). The filtrate was concentrated to approximately 3 L and then was diluted with MTBE (3 L) and cyclohexane (2 L) and filtered through a pad of magnesol (1 kg), washing with 1:1 cyclohexane/MTBE (3 L). The filtrate was washed with saturated potassium bicarbonate (3 L) and brine (2 L). The organic layer was filtered through a pad of silica gel (300 g) with a pad of magnesol (200 g) on top. The filtrated was concentrated to yield the title compound as an orange solid (1123 g, 91percent). 1H NMR (400 MHz, CDCl3) delta ppm 4.05-4.13 (m, 2H), 3.08 (s, 2H), 2.80-2.88 (m, 2H), 1.88-1.97 (m, 2H), 1.71-1.78 (m, 2H), 1.46 (s, 9H). m/z 252, 254 (MH+ minus t-Bu)., 159635-49-1

159635-49-1 tert-Butyl 4-methylenepiperidine-1-carboxylate 2756808, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Pfizer Inc.; US2010/113465; (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.7462-86-4,Methyl piperidine-4-carboxylate hydrochloride,as a common compound, the synthetic route is as follows.

7462-86-4, EXAMPLE II The purpose of this example is to demonstrate one method for the preparation of a piperidinyl intermediate of Formula III. To a stirred, room temperature, mixture of isonipecotic acid methyl ester hydrochloride (5.00 g, 2.78*10-2 mole), potassium carbonate (7.70 g, 5.57*10-2 mole), and DMF (100 ml) was added 1-(2-bromoethyl)-4-methoxybenzene (5.99 g, 2.78*10-2 mole). The reaction was then immersed in an oil bath which had been preheated to ca. 90 C. The reaction was heated at ca. 90 C. for ca. 17 hours and was then poured into a separatory funnel containing water and a 2:1 mixture of ethyl acetate:toluene. The two phases were mixed and the aqueous layer was separated. The organic layer was washed two times with H20 and once with saturated aqueous NaCl before being dried over anhydrous Na2 SO4. The drying agent was removed by filtration and the filtrate was evaporated at reduced pressure leaving an oil. Purification by flash chromatography (ethyl acetate) and crystallization from cyclohexane gave 1-[2-(4-methoxyphenyl)ethyl]-4-piperidinecarboxylic acid, methyl ester as a colorless solid: 3.98 g (52%), m.p. 66-68 C. Analysis Calculated for C16 H23 NO3: C, 69.29; H, 8.36, N, 5.05. Found: C, 69.50; H, 8.40; N, 4.94.

As the paragraph descriping shows that 7462-86-4 is playing an increasingly important role.

Reference£º
Patent; Merrell Dow Pharmaceuticals Inc.; US4908372; (1990); A;,
Piperidine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.3970-68-1,4-Methylpiperidin-4-ol,as a common compound, the synthetic route is as follows.

To a solution of (S) -1-phenylethyl 2 -bromo- 2-phenylacetate (0.464 g, 1.45 mmol) in THF (8 mL) was added triethylamine (0.61 mL, 4.35 mmol), followed by tetrabutylammonium iodide (0.215 g, 0.58 mmol) . The reaction mixture was stirred at room temperature for 5 minutes and then a solution of 4- methyl-4-hydroxypiperidine (0.251 g, 2.18 mmol) in THF (2 mL) was added. The mixture was stirred for 1 hour at room temperature and then it was heated at 55-60 0C (oil bath temperature) for 4 hours. The cooled reaction mixture was then diluted with ethyl acetate (30 mL) , washed (H2O x2 , brine), dried (MgSO4), filtered and concentrated. The residue was purified by silica gel chromatography (0-60% ethyl acetate-hexane) to provide first the (S, R) -isomer of the title compound (0.306 g, 60%) as a white solid and then the corresponding (S, S)- isomer (0.120 g, 23%), also as a white solid. (S, R)- isomer: 1H NMR (CD3OD) 5 7.51-7.45 (m, 2H), 7.41-7.25 (m, 8H), 5.85 (q, ,7=6.6 Hz, IH) , 4.05 (s, IH), 2.56-2.45 (m, 2H), 2,41-2.29 (m, 2H), 1.71-1.49 (m, 4H) , 1.38 (d, J=6.6 Hz, 3H), 1.18 (s, 3H) . LCMS: Anal. Calcd. for C22H27NO3: 353; found: 354 (M+H) + . (S, S) -isomer : 1H NMR (CD3OD) 6 7.41-7.30 (m, 5H) , 7.20-7.14 (m, 3H), 7.06-7.0096 (m, 2H), 5.85 (q, J=6,6 Hz, IH), 4.06 (s, IH), 2.70-2.60 (m, IH), 2.51 (dt, J=6.6 , 3.3 Hz, IH), 2.44-2.31 (ra, 2H), 1.75-1.65 (m, IH) , 1.65-1.54 (m, 3H), 1.50 (d, <;J=6.8 Hz, 3H), 1.20 (s, 3H) . LCMS: Anal. Calcd. for C22H27NO3: 353; found: 354 (M+H)+. 3970-68-1, As the paragraph descriping shows that 3970-68-1 is playing an increasingly important role.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; LAVOIE, Rico; BENDER, John A.; BACHAND, Carol; RUEDIGER, Edward H.; KADOW, John F.; WO2010/120621; (2010); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

37656-48-7, 4-(4-Fluorophenyl)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 5 was synthesized from 4-fluoro-4-phenylpiperidine using the reaction scheme detailed in the synthesis of Intermediate 4. A mixture of methyl and dimethyl compounds were synthesized.

37656-48-7, 37656-48-7 4-(4-Fluorophenyl)piperidine 2759136, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK & CO. INC.; WO2004/82682; (2004); 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.3202-33-3,4-Phenoxypiperidine,as a common compound, the synthetic route is as follows.

To a solution of 4-phenoxypiperidine (500 mg, 2.82 mmol) in DMF (6 mL) was added K2CO3 (0.78 g, 5.64 mmol) and 2-bromoethanol (0.39 g, 3.1 mmol). The reaction mixture was heated to 50C and stirred at that temperature for 3 h. TLC showed most of the product. The reaction was poured into water and extracted with DCM (3 x 40 mL). The combined organics were washed with saturated aqueous NaCl (2 x 20 mL). The combined organics were dried over anhydrous Na2SO4, filtered and concentrated in vacuo. The resulting oil was purified by flash column chromatography with a gradient elution of DCM (95%) and MeOH (5%) to DCM (85%) and MeOH (15%) to provide 2-(4- phenoxypiperidin-1-yl)ethanol (260 mg, 1.17 mmol) as a yellow solid.

3202-33-3, 3202-33-3 4-Phenoxypiperidine 18878, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; SUNOVION PHARMACEUTICALS INC.; HEFFERNAN, Michele L.R.; HARDY, Larry Wendell; BROWN, Scott P.; HERMAN, Lee W.; (180 pag.)WO2018/26371; (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.1892-22-4,3-Aminopiperidin-2-one,as a common compound, the synthetic route is as follows.

To a solution of 0.1 g of 6-chloro-2-(3,5-dimethyl-1H-pyrazol-1-yl)-N-(3-(trifluoromethyl) phenyl) pyrimidin-4-amine [0735] in acetonitrile was added 3-amino-2-piperidone [0562] (0.062 g, 0.543 mmol) and N,N-diisopropyl ethylamine. The reaction mixture was heated at 180 C. under microwave for 5 h. The reaction mixture was concentrated under reduced pressure to afford crude product which was purified by column chromatography using 40% ethyl acetate in pet ether to afford 0.038 g of 3-((2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)amino) piperidin-2-one [0744], Compound 189 as a white solid. MS(M+1)+=446.2. 1H NMR (400 MHz, DMSO-d6) delta 9.52 (s, 1H), 8.55 (s, 1H), 7.69-7.66 (m, 2H), 7.47 (t, J=8.0 Hz, 2H), 7.23 (d, J=7.7 Hz, 1H), 6.05 (s, 1H), 5.82 (s, 1H), 4.43 (s, 1H), 3.17 (bs, 2H), 2.52 (s, 3H), 2.18 (s, 3H), 2.15-2.10 (m, 1H), 1.89-1.64 (m, 3H).

1892-22-4, The synthetic route of 1892-22-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Cadent Therapeutics, Inc.; Jefson, Martin R.; Keaney, Gregg F.; Larsen, Janus Schreiber; Lowe, III, John A.; McCall, John M.; (110 pag.)US2017/355708; (2017); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem