Month: November 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.479630-08-5,1-Boc-4-(2-Ethoxycarbonyl-acetyl)piperidine,as a common compound, the synthetic route is as follows.

Tert-butyl 4-(3-ethoxy-3-oxopropanoyl)piperidine-l -carboxylate (818 mg, 2.27 mmol), 4-methyl-lH- pyrazolo[3,4-b]pyridin-3-amine (224 mg, 1.51 mmol) and potassium phosphate (642 mg, 3.02 mmol) were suspended in l-methoxy-2-propanol (8 ml) in a 20 ml microwave vial. The vial was capped and the mixture was heated in a microwave to 180C for 15 min. The reaction mixture was diluted with water and neutralized (pH 6) by the addition of IN HC1. The resulting solid was filtrated, washed with ethyl acetate and water and dried under vacuo. The solid was stirred in a mixture of water, ammonia and acetonitrile. The solid was filtered off and the filtrate was purified by preparative HPLC (Method 2A) to yield the title compound (40 mg, 7% of theory). LC-MS (Method 3B): Rt = 1.75 min, MS (ESIPos): m/z = 384 [M+H]+

479630-08-5, As the paragraph descriping shows that 479630-08-5 is playing an increasingly important role.

Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; HASSFELD, Jorma; KINZEL, Tom; KOeBBERLING, Johannes; CANCHO-GRANDE, Yolanda; BEYER, Kristin; ROeHRIG, Susanne; KOeLLNBERGER, Maria; SPERZEL, Michael; BURKHARDT, Nils; SCHLEMMER, Karl-Heinz; STEGMANN, Christian; SCHUHMACHER, Joachim; WERNER, Matthias; ELLERMANN, Manuel; WO2015/67549; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

144913-66-6, Methyl 4-hydroxypiperidine-2-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a cold (5 C.) solution of methyl 4-hydroxypiperidine-2-carboxylate, 13a, (5.17 g, 32.48 mmol) and triethylamine (6.00 mL, 43.05 mmol) in CH2Cl2 (135 mL) was added dropwise benzyl chloroformate (6.20 mL, 43.43 mmol) over 10 min. The resulting solution was stirred at 5 C. for 1 hour and then allowed to warm to room temperature. The reaction mixture was diluted with water and the layers were separated. The aqueous was re-extracted with CH2Cl2 and the combined organics were dried over MgSO4, filtered and evaporated to dryness. The crude was passed through a plug of silica gel, eluting with 30-80% EtOAc/Hexanes to afford the desired product, 13b.

144913-66-6, 144913-66-6 Methyl 4-hydroxypiperidine-2-carboxylate 10103419, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; VERTEX PHARMACEUTICALS INCORPORATED; US2012/171245; (2012); 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.309956-78-3,(R)-tert-Butyl piperidin-3-ylcarbamate,as a common compound, the synthetic route is as follows.

2) A mixture of 13.8 g (50 mmol) of 6-chloro-1- (2-isocyaninyl) -3-methylpyrimidine-2,4- (1H, 3H) -dione(R) -3-tert-butyloxycarbonylaminopiperidine (11.0 g, 55 mmol)Potassium carbonate 17.3 g (125 mmol) was mixed in DMF at 65 C,After the reaction,add water,Then extracted with dichloromethane,concentrate,N-hexane washing,(R) -tert-butyl-1- (3- (2-isocyaninyl) -1-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidine- Yl) piperidin-3-ylcarbamate (21.6 g)The yield was 98.2%Purity 99.20%., 309956-78-3

The synthetic route of 309956-78-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Qingdao Chenda Biological Technology Co., Ltd.; Chen, Linghao; (8 pag.)CN105837557; (2016); 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.614730-97-1,1-Boc-4-Fluoro-4-(hydroxymethyl)piperidine,as a common compound, the synthetic route is as follows.

614730-97-1, To a mixture of tert-butyl 4-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (30 g, 129 mmol, prepared as described in the synthesis of AMI04) and NaH (3.09 g, 129 mmol) in THF (500 mL) was added iodomethane (41.9 g, 295 mmol) at room temperature, and then the mixture was stirred at 25 C for 12 h, The reaction mixture was diluted with water and extracted with EtOAc. The combined organic phases were washed with water and brine. The organic fraction was dried over Na2SO4, filtered, and concentrated under vacuum. The residue was purified on a silica gel column eluted with petroleum ether/EtOAc=2:1 to give 4- fluoro-4-(methoxymethyl)piperidine-1-carboxylate (25 g, 101 mmol, 79% yield).

614730-97-1 1-Boc-4-Fluoro-4-(hydroxymethyl)piperidine 22248400, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; ABBVIE S.A.R.L; GALAPAGOS NV; AKKARI, Rhalid; ALVEY, Luke Jonathan; BOCK, Xavier Marie; BROWN, Brian S.; CLAES, Pieter Isabelle Roger; COWART, Marlon D.; DE LEMOS, Elsa; DESROY, Nicolas; DUTHION, Beranger; GFESSER, Gregory A.; GOSMINI, Romain Luc Marie; HOUSSEMAN, Christopher Gaetan; JANSEN, Koen Karel; JI, Jianguo; KYM, Philip R.; LEFRANCOIS, Jean-Michel; MAMMOLITI, Oscar; MENET, Christel Jeanne Marie; MERAYO, Nuria Merayo; NEWSOME, Gregory John Robert; PALISSE, Adeline Marie Elise; PATEL, Sachin V.; PIZZONERO, Mathieu Rafael; SHRESTHA, Anurupa; SWIFT, Elizabeth C.; VAN DER PLAS, Steven Emiel; WANG, Xueqing; DE BLIECK, Ann; (1004 pag.)WO2017/60874; (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.216854-23-8,(S)-tert-Butyl piperidin-3-ylcarbamate,as a common compound, the synthetic route is as follows.

216854-23-8, To a solution of l-chloro-7-methoxyisoquinoline-6-carbonitrile (218 mg) in DIPEA (4.0 mL) was added compound 1 (300 mg). The mixture was stirred at 120 C for 8 h. The title compound 2 was obtained as a yellow solid (170 mg, yield 45%) after standard work up procedure.

As the paragraph descriping shows that 216854-23-8 is playing an increasingly important role.

Reference£º
Patent; SYNBLIA THERAPEUTICS, INC.; XIE, Yinong; BABISS, Lee, E.; (89 pag.)WO2019/89422; (2019); 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.50585-89-2,Methyl piperidine-3-carboxylate,as a common compound, the synthetic route is as follows.

Compound 4 (200 mg, 0.56 mmol), methyl 3-piperidinecarboxylate (80.2 mg, 0.56 mmol), triethylamine (0.25 mL, 1.68 mmol) and potassium iodide (11 mg, 0.067 mmol) were suspended in acetonitrile (10 mL) in a 15 mL tube. The mixture was stirred at room temperature for 4 h. The reaction was followed by TLC (DCM:MeOH = 100:1, Rf = 0.4). The solvent was steamed out from the mixture upon the completion of the reaction. The crude product was purified by flash chromatography (DCM:MeOH = 90:1) to yield compound 5e in the form of a yellow solid (167 mg, 71%). 1H NMR (600 MHz, Chloroform-d) delta = 8.60 (ddd, J = 1.9, 4.3, 8.9, 1H), 8.30 (s, 1H), 7.93 (dd, J = 1.8, 8.3, 1H), 7.83 (d, J = 8.2, 1H), 7.54 (dd, J = 3.0, 6.2, 1H), 7.45 (td, J = 4.3, 6.1, 7.4, 1H), 3.68 – 3.61 (m, 5H), 2.90 (d, J = 11.4, 1H), 2.60 (d, J = 11.3, 1H), 2.28 (d, J = 10.6, 1H), 2.13 (t, J = 11.1, 2H), 1.91 (d, J = 12.9, 1H), 1.76 – 1.70 (m, 1H), 1.59 (d, J = 12.1, 1H), 1.48 (d, J = 13.7, 1H). 13C NMR (151 MHz, Chloroform-d) delta = 181.70 (d, J = 2.7), 178.08, 174.49, 161.92, 160.26, 157.93, 145.59, 144.06, 142.42 (d, J = 2.4), 135.97, 130.74, 127.36, 124.79 (d, J = 23.9), 123.38, 119.68 (d, J = 7.5), 112.02 (d, J = 24.4), 62.44, 55.28, 53.73, 51.68, 29.60, 26.69, 24.41. HPLC tR = 1.989 min, purity 96.76%. HR-MS (ESI): calcd. for C23H20FN3NaO4 [M+Na]+: 444.1336, found: 444.1336.

50585-89-2, As the paragraph descriping shows that 50585-89-2 is playing an increasingly important role.

Reference£º
Article; Cui, Menghan; Kuang, Chunxiang; Li, Yuanyuan; Liu, Wei; Wang, Rong; Yang, Qing; Zhang, Shengnan; Bioorganic and medicinal chemistry letters; (2020);,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.214834-18-1,tert-Butyl 4-carbamothioylpiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

55 mg (1.5 mmol) of 4-thiocarbamoyl-piperidine-1-tert-butyl carboxylate is added to a suspension of 57 mg (0.15 mmol) of 8-(2-bromo-acetyl)-4-oxo-4,5-dihydro-3H-pyrrolo[2,3-c]quinoline-1-ethyl carboxylate in 3 mL of ethanol. The mixture is stirred at 90 C. for 3 hours then the mixture is cooled to room temperature. Triethylamine (2 mmol) is added, then the solvent is evaporated and the product is purified by chromatography on silica (chloroform/methanol/triethylamine 8/2/1). After drying, 11 mg (17%) of 4-oxo-8-(2-piperidin-4-yl-thiazol-4-yl)-4,5-dihydro-3H-pyrrolo[2,3-c]quinoline-1-ethyl carboxylate is obtained in the form of a beige solid.LCMS (IE, m/z): (M+1) 423.241H-NMR: deltaH ppm 400 MHz, DMSO11.76 (1H, bs, NH), 9.76 (1H, d, CHarom), 8.00 (1H, s, CHarom), 7.95 (1H, dd, CHarom), 7.74 (1H, s, CHarom), 7.44 (1H, d, CHarom), 4.35 (2H, q, CH2), 3.35-3.30 (1H, m, CHpiper), 3.16-3.10 (2H, m, 2¡ÁCHpiper), 2.80-2.72 (2H, m, 2¡ÁCHpiper), 2.13-2.06 (2H, m, 2¡ÁCHpiper), 1.77-1.68 (2H, m, 2¡ÁCHpiper), 1.36 (3H, t, CH3).

214834-18-1, The synthetic route of 214834-18-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Pierre Fabre Medicament; US2009/42876; (2009); 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.

General procedure: In a typical experiment Pd(OAc)2 (2.81 mg, 0.0125 mmol), triphenylphosphine (6.55 mg, 0.025 mmol) or Xantphos (7.23 mg, 0.0125 mmol), iodoalkene (1-5) or iodo(hetero)arene (6-11) substrates (0.5 mmol), and 3-aminolactams (3-amino-azepan-2-one (a), 3-amino-piperidin-2-one (b), 3-amino-pyrrolidin-2-one (c)) (0.55 mmol) and triethylamine (0.25 mL) were dissolved in DMF (5 mL) under argon in a 100 mL three-necked flask equipped with reflux condenser connected to a balloon filled with argon. The atmosphere was changed to carbon monoxide. The reaction was conducted for the given reaction time upon stirring at 50 C and analyzed by Gc and GC-MS. The cooled reaction mixture was then distilled to dryness under reduced pressure. The residue was dissolved in chloroform (15 mL) and washed twice with water (15 mL). The organic phase was dried over Na2SO4, filtered and evaporated under reduced pressure to a solid material. All compounds (except 10a, 10b) were subjected to column chromatography (Silicagel 60 (Sigma), 0.063-0.200 mm) or Aluminum oxide (Sigma), activated, neutral, Brockmann activity I), CHCl3/MeOH or CHCl3/EtOH eluent mixtures (the exact ratios are specified in Characterization (3.4) for each compound). In the case of 10a and 10b chloroform (10 mL) was added to the residue and the insoluble material (product) was filtered and dried.

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

Reference£º
Article; Kollar, Laszlo; Takacs, Attila; Tetrahedron; vol. 74; 42; (2018); p. 6116 – 6128;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

22990-34-7, 2-(4-Piperidyl)-2-propanol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

22990-34-7, Step A: cis-4-(2-(4-(2-Hydroxypropan-2-yl)piperidin-l-yl)-5- nitropyridin-4-ylamino)-N-isopropylcyclohexanecarboxamide. A suspension of cis-4- (2-chloro-5-nitropyridin-4-ylamino)-N-isopropylcyclohexanecarboxamide (0.200 g, 0.587 mmol) and 2-(piperidin-4-yl)propan-2-ol (0.420 g, 2.93 mmol) in 2-propanol (2.003 mL) was microwave irradiated for 1 hour at 150C. The reaction mixture was concentrated in vacuo, and the residual material was purified via silica gel chromatography eluting with isocratic 90: 10:1 DCM:MeOH:NH4OH, to provide cis-4-(2-(4-(2-hydroxypropan-2- yl)piperidin- 1 -yl)-5 -nitropyridin-4-ylamino)-N-isopropylcyclohexanecarboxamide as a yellow solid (0.263 g, 100 % yield). MS m/z = 448.2 [M+H], calc 447.57 for

The synthetic route of 22990-34-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AMGEN INC.; BODE, Christiane, M.; CHENG, Alan, C.; CHOQUETTE, Deborah; LEWIS, Richard, T.; POTASHMAN, Michele, H.; ROMERO, Karina; STELLWAGEN, John, C.; WHITTINGTON, Douglas, A.; WO2012/18668; (2012); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

29976-53-2, N-Carbethoxy-4-piperidone is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

23 mL (311 mmol) of trifluoroacetic acid is added after 5 minutes to a solution of 20 g (156 mmol) of 3-amino-2-chloropyridine and 26 mL (171 mmol) of 4-oxo-1-piperidine ethyl carboxylate in 250 mL of isopropyl acetate. The reaction mixture is stirred for 30 minutes at room temperature and then 40 g (19 mmol) of sodium triacetoxyborohydride is added. The reaction mixture is stirred for 2 hours at room temperature and then 23 mL of a 10% solution of sodium hydroxide is added to pH8-9 and the mixture is heated to 50 C. After cooling, the reaction mixture is decanted and then extracted with ethyl acetate. The organic phases are combined, and dried over sodium sulphate. The solvents are evaporated and the residue is purified by silica gel chromatography eluted with a heptane/ethyl acetate 60/40 mixture. 43.2 g (98%) of 4-(2-chloro-pyridin-3-ylamino)-piperidine-1-ethyl carboxylate is obtained in the form of a colourless oil.

29976-53-2, The synthetic route of 29976-53-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GALDERMA RESEARCH & DEVELOPMENT; Fournier, Jean-Francois; Clary, Laurence; Thoreau, Etienne; (164 pag.)US2018/50992; (2018); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem