Heterocyclic Building Blocks-piperidine

39945-51-2, Benzyl 3-(hydroxymethyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

39945-51-2, Example 70A Benzyl 3-[(vinyloxy)methyl]piperidine-1-carboxylate At RT, 23 ml (241 mmol) of ethyl vinyl ether were added to 321 mg (0.65 mmol) of chloro(triphenylphosphine)gold(I) and 108 mg of silver(I) acetate. After 10 min of stirring, 6.00 g (24.07 mmol) of benzyl 3-(hydroxymethyl)piperidine-1-carboxylate were added. The mixture was stirred at 50 C. for 5 h. This was followed by concentration under reduced pressure. The crude product was purified by chromatography on silica gel (mobile phase: cyclohexane/ethyl acetate gradient 100:0-100:1-20:1-10:1). This gave 4.40 g of product (66% of theory). LC-MS[Method 1]: Rt=1.15 min; MS (ESI+): m/z=276 (M+H)+

39945-51-2 Benzyl 3-(hydroxymethyl)piperidine-1-carboxylate 2776577, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Bayer Pharma Aktiengesellschaft; BECKER-PELSTER, Eva Maria; BUCHGRABER, Philipp; BUCHMUeLLER, Anja; ENGEL, Karen; GNOTH, Mark Jean; HIMMEL, Herbert; KAST, Raimund; KELDENICH, Joerg; KLAR, Juergen; KNORR, Andreas; LANG, Dieter; LINDNER, Niels; SCHMECK, Carsten; SCHOHE-LOOP, Rudolf; TINEL, Hanna; TRUeBEL, Hubert; WUNDER, Frank; (97 pag.)US2016/318866; (2016); A1;,
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614731-04-3, 1-Boc-4-fluoro-4-piperidinecarboxylic Acid is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

614731-04-3, To a solution of 1- (tert-butoxycarbonyl) -4-fluoropiperidine-4-carboxylic acid (5.00 g, 20.20 mmol) in tetrahydrofuran (100 mL) was added a solution of borane tetrahydrofuran complex (30.3 mL, 30.30 mmol, 1.0 M solution in tetrahydrofuran) . The reaction mixture was refluxed for 16 hours, and then another 24 mL of borane tetrahydrofuran complex was added and continued to reflux for another 16 hours. After cooling to ambient temperature the reaction mixture poured onto ice-cold water (50 mL) and saturated ammonium chloride (100 mL) , and extracted with ethyl acetate (3 x 100 mL) , dried over anhydrous sodium sulfate and filtered. The filtrate was concentrated to afford the title compound (4.60 g, 98) . Which was used in the next step without further purification: MS (ES+) m/z 234.1 (M +1) .

614731-04-3 1-Boc-4-fluoro-4-piperidinecarboxylic Acid 21050397, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; GENENTECH, INC.; XENON PHARMACEUTICALS INC.; ANDREZ, Jean-Christophe; BICHLER, Paul Robert; CHEN, Chien-An; CHOWDHURY, Sultan; DECKER, Shannon Marie; DEHNHARDT, Christoph Martin; FOCKEN, Thilo; GRIMWOOD, Michael Edward; HEMEON, Ivan William; JIA, Qi; LI, Jun; LIU, Zhiguo; ORTWINE, Daniel F.; SAFINA, Brian; SUTHERLIN, Daniel; SHENG, Tao; SUN, Shaoyi; WHITE, Andrew D.; WILSON, Michael Scott; ZENOVA, Alla Yurevna; ZHU, Jiuxiang; WO2015/78374; (2015); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.32018-96-5,1-Benzyl-4-methylpiperidin-3-one,as a common compound, the synthetic route is as follows.

To a stirred solution of 1-benzyl-4-methyl-piperidin-3-one (2.3 grams, 11.5 mmol), prepared by the methods of lorio, M.A. and Damia, G., Tetrahedron, 26, 5519 (1970) and Grieco et aL, Journal of the American Chemical Society, 107. 1768 (1985), (modified using 5% methanol as a co-solvent), both references are incorporated by reference in their entirety, dissolved in 23 mL of 2 M methylamine in tetrahydrofuran was added 1.4 mL (23 mmol) of acetic acid and the resulting mixture stirred in a sealed tube for 16 hours at room temperature. Triacetoxy sodium borohydride (4.9 grams, 23 mmol) was added and the new mixture stirred at room temperature in a sealed tube for 24 h, at which time, the reaction was quenched upon addition of 1 N sodium hydroxide (50 mL). The reaction mixture was then extracted 3 x 80 ml_ with ether, the combined ether layers dried over sodium sulfate (Na2SO4) and concentrated to dryness in vacuo affording 1.7 grams (69%) of the title compound as a white solid. LRMS: 219.1 (M+1 )., 32018-96-5

32018-96-5 1-Benzyl-4-methylpiperidin-3-one 12084828, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; PFIZER PRODUCTS INC.; WO2008/29237; (2008); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.98977-34-5,1-tert-Butyl 3-ethyl 4-oxopiperidine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.,98977-34-5

1 -(1 , 1 -Dimethylethyl) 3-ethyl 4-oxo-1 ,3-piperidinedicarboxylate (Intermediate 1 , 380.48 g, 1.40 moles) was dissolved in toluene (2.97 Kg). The solution was stirred for 10 mins and then cooled to -7 0C and then treated with N,N-diisopropylethylamine (271.56 g, 2.10 mol) while maintaining the reaction below -7 0C. After stirring the reaction mixture for approximately 10 minutes, trifluoromethanesulfonic anhydride (436.29 g, 1.55 mol) was added while maintaining the temperature below 5 0C. The reaction mixture was stirred at 1 0C for 31 minutes. The product was used in the next step without purification (see preparation of Intermediate 3); HPLC: Rt= 2.69 min (HPLC instrument Agilent 1 100 Series analysis performed on a Agilent Zorbax SB C18 (50×3.0 mm, 1.8um), mobile phase: water:acetonitrile:TFA (0.05%), gradient from 0 to 95% in 2.5 min, hold for 0.2 min, then re-equilibrate; T=60; flow= 1.5 mL/min)

The synthetic route of 98977-34-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXO GROUP LIMITED; WO2009/109608; (2009); A1;,
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4897-50-1, 4-Piperidinopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 3 PREPARATION OF 4-PIPERIDINOPIPERIDINE CARBAMOYL CHLORIDE 150 g of 4-piperidinopiperidine was dissolved in 10.5 L of dichloromethane and the solution was cooled to about 0¡ã C. A solution of triphosgene (94.8 g of triphosgene in 1.2 L of dichloromethane) was added slowly to the solution at about 5¡ã C. over a period of 45 minutes under a nitrogen atmosphere with simultaneous stirring. The resultant reaction mixture was stirred at 27¡ã C. for 12 hours. The reaction mixture was filtered and then the filtrate was washed with 1.2 L of 7percent sodium bicarbonate solution. The organic layer was separated and concentrated completely at about 40¡ã C. under a vacuum of 580 mm Hg to afford title compound. Purity: 97.2percent by GC.

4897-50-1, 4897-50-1 4-Piperidinopiperidine 78607, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Palle, Venkata Raghavendra Acharyulu; Nariyam, Sekhar Munaswamy; Matti, Lankeshwararao; Vinjamuri, Raghupati Rama Subrahmanyam; US2007/208050; (2007); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2971-79-1,Methyl piperidine-4-carboxylate,as a common compound, the synthetic route is as follows.

Methyl 1-(4-methoxybenzyl)piperidine-4-carboxylate; 4-Methoxybenzyl chloride (1.10 g, 6.98 mmol) was added dropwise to a solution of isonipecotic acid methyl ester (1.00 g, 6.98 mmol) and triethylamine (1.40 g, 14 mmol) in THF (30 ml), and stirring was carried out for 72 h at 60 C. 5% sodium hydrogen carbonate solution (50 ml) was then added to the reaction mixture, and extraction with ethyl acetate (3¡Á50 ml) was carried out. The combined organic phases were dried over sodium sulfate and concentrated in vacuo. The residue was purified by flash chromatography with cyclohexane/ethyl acetate (2:1).Yield: 1.23 g (67%) of methyl 1-(4-methoxybenzyl)piperidine-4-carboxylate1H-NMR (DMSO-d6): 1.53 (dq, 2H); 1.77 (dd, 2H); 1.93 (dt, 2H); 2.28 (tt, 1H); 2.71 (td, 2H); 3.35 (s, 2H); 3.58 (s, 3H); 3.72 (s, 3H); 6.86 (d, 2H); 7.17 (d, 2H)., 2971-79-1

The synthetic route of 2971-79-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Gruenenthal GmbH; US2008/312231; (2008); A1;,
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896464-16-7, tert-Butyl 2,7-diazaspiro[3.5]nonane-7-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In a microwave vessel, a mixture of tert-butyl 2,7-diazaspiro[3 .5 ]nonane-7-carboxylate (85 mg, 0.38 mmol), DIEA (44 jiL, 0.25 mmol), and 4-(6-fluoropyridin-3-yl)-6-(i-methyl-1H- pyrazol-4-yl)pyrazolo[i,5-a]pyridine-3-carbonitrile (Intermediate P6; 40 mg, 0.13 mmol) in DMSO (1 mL) was subjected to microwave irradiation at 125 C for 2 h. After cooling to ambient temperature, the reaction mixture was directly purified by reverse-phase preparative HPLC (10 to 80% acetonitrile/water) to give the title compound (12 mg, 18% yield). MS (apci) m/z = 525.2 (M+H)., 896464-16-7

896464-16-7 tert-Butyl 2,7-diazaspiro[3.5]nonane-7-carboxylate 24820512, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; ARRAY BIOPHARMA, INC.; ANDREWS, Steven W.; BLAKE, James F.; CHICARELLI, Mark J.; GOLOS, Adam; HAAS, Julia; JIANG, Yutong; KOLAKOWSKI, Gabrielle R.; (594 pag.)WO2017/11776; (2017); 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.892493-65-1,tert-Butyl piperidine-4-carboxylate hydrochloride,as a common compound, the synthetic route is as follows.

892493-65-1, A solution of ethyl 6-chloro-5-cyano-2-methyhiicotinate (6.00 g, 26.7 mmol), tert-butyl piperidine-4-carboxylate hydrochloride (6.51, 29.4 mmol) and DBPEA (23.3 mL, 134 mmol) in DMA (50 mL) were heated to 80 ¡ãC for 2 h. After cooling to r.t, the reaction mixture was diluted with EtOAc (300 mL), washed with saturated NH4Cl (4 x 50 mL), brine (50 mL), dried (MgSO4), passed through silica gel and concentrated. Flash chromatography produced ethyl 6-(4-(tert-butoxycarbonyl)piperidm-l-yl)-5-cyano-2-memylnicotinate as a solid. Yield: 8.85 g (89 percent). EPO 1H NMR (400 MHz, CDCl): delta 1HNMR (400 MHz, CDCl5): delta 1.37 (3H, t, J= 7.1 Hz), 1.45 (9H, s), 1.75-1.84 (2H, m), 1.99-2.03 (2H, m), 2.49-2.57 (IH, m), 2.72 (3H, s), 3.24-3.31 (2H, m), 4.31 (2H, q, J= 7.1 Hz), 4.55-4.60 (2H, m), 8.34 (IH, s). MS m/z: 374 (M+l).

892493-65-1 tert-Butyl piperidine-4-carboxylate hydrochloride 42614227, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; WO2007/8140; (2007); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.333986-70-2,Methyl 4-(piperidin-4-ylmethyl)benzoate hydrochloride,as a common compound, the synthetic route is as follows.

Example of General Method C:Preparation of 4-{l-[(S)-4-(2,3-Dihydro-benzo[l,4]dioxin-2-yl)-benzyl]-piperidin-4- ylmethylj-benzoic acid methyl esterA solution of A (100 mg, 0.42 mmol), 4-piperidin-4-ylmethyl-benzoic acid methyl ester hydrochloride (146 mg, 0.54 mmol), sodium cyanoborohydride (52 mg, 0.83 mmol), and TEA (0.08 mL, 0.54 mmol) in THF (5 mL) is treated with 2 drops of acetic acid, and stirred at room temperature for 16 h. The mixture is concentrated, and the residue is purified by flash chromatography eluting with a gradient of 0-10% MeOH in DCM to give the title compound.

333986-70-2, As the paragraph descriping shows that 333986-70-2 is playing an increasingly important role.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; ABEYWARDANE, Asitha; BURKE, Michael J.; KIRRANE, Thomas Martin, Jr.; NETHERTON, Matthew Russell; PADYANA, Anil Kumar; SMITH KEENAN, Lana Louise; TAKAHASHI, Hidenori; TURNER, Michael Robert; ZHANG, Qiang; ZHANG, Qing; WO2012/125598; (2012); A1;,
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Piperidine | C5H11N – PubChem

54012-73-6,54012-73-6, Piperidin-3-amine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The steps will be a 3 – amino piperidine (50.1g) soluble in the 2L of in DMF, by adding 1, 2 – diphenyl vinylidene carbonate (119.1g), triethylamine (1L), for ice water bath stirring to the reaction is complete (about 30min) after, adding ethyl acetate, the combined organic layer, dried with anhydrous sodium sulfate, to remove the organic solvent. The resulting product is dissolved in the 1L trifluoroacetic in, as for 20 C stirring for 2 hours, concentrated in vacuo, to remove the surplus trifluoro acetic acid, to obtain a product of formula Chinese (148.5g, yield 92.3%)

The synthetic route of 54012-73-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Borui Bio-pharmaceutical (Suzhou) Co., Ltd.; Yuan Jiandong; (12 pag.)CN103450201; (2017); B;,
Piperidine – Wikipedia
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