Day: September 2, 2020

1892-22-4, 3-Aminopiperidin-2-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,1892-22-4

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.

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

387827-19-2, tert-Butyl 4-(3-aminophenyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Cooled at 0C, the solution of 4-(3-aminophenyl)piperidine-1-carboxylic acid tert-butyl ester in THF (6 mL) was slowly added Et3N (260 mul, 1.86 mmol) and propionyl chloride (59 mul, 0.68 mmol). The reaction mixture was stirred at room temperature for 3 hours. Dichloromethane was added and the reaction mixture was washed with brine. Dehydrated by Na2SO4. Filtered and concentrated to give a residue. The residue was purified by flash chromatography (silica gel, gradient from hexane to ethyl acetate). The desired product was obtained as a white solid (186 mg, 90% yield)., 387827-19-2

As the paragraph descriping shows that 387827-19-2 is playing an increasingly important role.

Reference£º
Patent; LABORATORIOS DEL DR. ESTEVE, S. A.; CUEVAS CORDOBES, FELIX; ALMANSA ROSALES, CARMEN; GARCIA LOPEZ, MONICA; (299 pag.)TW2016/27300; (2016); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

187834-88-4, 1-Boc-isonipecoticacidhydrazide is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

187834-88-4, To a solution of (R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxylic acid (Intermediate 10, 200 mg, 0.581 mmol) in DMF (3.8 mL) were added tert-butyl 4-(hydrazinecarbonyl)piperidine-1-carboxylate (212 mg, 0.871 mmol), DIPEA (0.304 mL, 1.74 mmol), HATU (331 mg, 0.871 mmol) at room temperature, The reaction mixture was stirred at room temperature for 18 hours and diluted with EtOAc. The mixture was washed with saturated aq. NH4Cl and brine, dried over Na2SO4, filtered and concentrate in vacuo. The residue was purified by column chromatography on SiO2 (EtOAc only to DCM_MeOH=20:1 to 10:1) to give the (R)-tert-butyl 4-(2-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidine-3-carbonyl)hydrazinecarbonyl)piperidine-1-carboxylate (265 mg, 80%) as a white solid. MS: 569.90 [MH+].

The synthetic route of 187834-88-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; HANDOK INC.; CMG Pharmaceutical Co., Ltd.; Kim, Moonsoo; Lee, Chaewoon; Lee, Gilnam; Yoon, Cheolhwan; Seo, Jeongbeob; Kim, Jay Hak; Lee, Minwoo; Jeong, Hankyul; Choi, Hyang; Jung, Myung Eun; Lee, Ki Nam; Kim, Hyun Jung; Kim, Hye Kyoung; Lee, Jae Il; Lee, MinWoo; Kim, Misoon; Choi, Soongyu; (124 pag.)US2016/168156; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

236406-39-6, 8-Boc-2,8-Diazaspiro[4.5]decane is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of intermediate I-i 3a (445 mg, 1 .25 mmol) in anhydrous DCM(50 mL) was added R-29a: tert-butyl 2,8-diazaspiro[4.5]decane-8-carboxylate(200 mg, 0.833 mmol), Cu(OAc)2 (181 mg, 1.0 mmol), DMAP (22 mg, 0.167 mmol), Et3N (337 mg, 3.332 mmol) and 4A MS (0.8 g), then the mixture was stirred at room temperature for 3 hrs under 02 atmosphere. After LC-MS showed the starting material was consumed completely, then added water,filtered, the mixture was extracted with DCM, the organic layer was washed with brine, dried over anhydrous Na2504, concentrated to give the crude compound which was purified by Prep-TLC ( PE/ EtOAc = 1 .5:1 ) to give the pure intermediate I-131a (60 mg, 13% yield) as a yellow solid. ESI-MS (Mi-i):551 calc. for C30H42N604: 550.3., 236406-39-6

As the paragraph descriping shows that 236406-39-6 is playing an increasingly important role.

Reference£º
Patent; FUNDACION PARA LA INVESTIGACION MEDICA APLICADA; CUADRADO TEJEDOR, Maria Del Mar; FRANCO FERNANDEZ, Rafael; GARCIA OSTA, Ana Maria; OYARZABAL SANTAMARINA, Julen; RABAL GRACIA, Maria Obdulia; WO2014/131855; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

25519-78-2, (4-Fluorophenyl)(piperidin-4-yl)methanone hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Production Example 395 [1-(6-Bromoquinazolin-4-yl)piperidin-4-yl]-(4-fluorophenyl)methanone 53 mg of the title compound was obtained as a colorless amorphous from 100 mg of 6-bromo-4-chloroquinazoline and 100 mg of (4-fluorophenyl)-piperidin-4-yl-methanonehydrochloride by the same reaction as in Production Example 391.1H-NMR(CDCl3) delta: 2.04-2.12(m, 4H), 3.30-3.38(m, 2H), 3.55-3.64(m, 1H), 4.33-4.40(m, 2H), 7.17-7.22(m, 2H), 7.78(d, J=8.6Hz, 1H), 7.81(dd, J=8.6, 2.0Hz, 1H), 8.01-8.06(m, 3H), 8.75(s, 1H)

25519-78-2, As the paragraph descriping shows that 25519-78-2 is playing an increasingly important role.

Reference£º
Patent; Eisai Co., Ltd.; EP1382603; (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.41373-39-1,(S)-Piperidin-2-ylmethanol,as a common compound, the synthetic route is as follows.

50 mg of 6-fluoro-4-oxo-7-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yloxy)-N-[(2S)(2S)-1,1,1-trifluorobutan-2-yl]-1-(2,4,6-trifluorophenyl)-1,4-dihydro-1,8-naphthyridine-3-carboxamide (86.0 mumol) were dissolved in DMF (980 mul). (2S)-Piperidin-2-ylmethanol (19.8 mg, 172 mumol) and N,N-diisopropylethylamine (52 mul, 300 mumol) were added and the mixture was stirred at RT for 2 h. 0.3 ml of 1 M hydrochloric acid and 1 ml of acetonitrile were then added to the reaction mixture, and the product was purified by preparative HPLC (acetonitrile/water with formic acid, C18 RP-HPLC). The product fractions were combined, concentrated and lyophilized from acetonitrile/water overnight. This gave 37.3 mg (77% of theory, 99% pure) of the title compound. LC-MS (Method 3): Rt=2.25 min; MS (ESIpos): m/z=561 [M+H]+ 1H-NMR (400 MHz, DMSO-d6) delta [ppm]: -0.149 (0.55), -0.008 (4.87), 0.008 (4.03), 0.146 (0.52), 0.948 (7.19), 0.967 (16.00), 0.985 (7.82), 1.344 (1.09), 1.376 (1.34), 1.471 (1.90), 1.530 (3.44), 1.549 (5.64), 1.577 (2.47), 1.606 (1.34), 1.624 (1.56), 1.631 (1.36), 1.641 (1.83), 1.649 (1.65), 1.659 (1.59), 1.666 (1.77), 1.684 (1.47), 1.703 (0.91), 1.723 (1.95), 1.740 (1.83), 1.832 (0.43), 1.851 (1.31), 1.861 (1.54), 1.869 (1.56), 1.879 (1.74), 1.886 (1.54), 1.896 (1.34), 1.905 (1.15), 1.914 (0.98), 2.367 (0.70), 2.519 (3.11), 2.524 (2.47), 2.711 (0.66), 2.925 (1.07), 2.955 (1.99), 2.988 (1.07), 3.479 (1.00), 3.495 (1.47), 3.506 (2.47), 3.520 (2.63), 3.536 (1.90), 3.559 (1.20), 3.574 (2.02), 3.588 (1.77), 3.616 (0.68), 3.855 (1.79), 3.888 (1.68), 4.288 (2.04), 4.662 (3.01), 4.676 (6.53), 4.689 (2.97), 4.737 (1.41), 4.758 (1.32), 7.531 (1.43), 7.535 (1.41), 7.550 (3.99), 7.555 (4.15), 7.573 (4.28), 7.578 (3.88), 7.597 (1.36), 8.001 (8.41), 8.036 (8.14), 8.869 (13.96), 10.274 (5.15), 10.298 (4.94)., 41373-39-1

As the paragraph descriping shows that 41373-39-1 is playing an increasingly important role.

Reference£º
Patent; Bayer Aktiengesellschaft; Bayer Pharma Aktiengesellschaft; TELLER, Henrik; VAKALOPOULOS, Alexandros; BOULTADAKIS ARAPINIS, Melissa; STRAUB, Alexander; TINEL, Hanna; BRECHMANN, Markus; WITTWER, Matthias Beat; KULLMANN, Maximilian Andreas; FREUDENBERGER, Till; MONDRITZKI, Thomas; MARQUARDT, Tobias; (165 pag.)US2019/263805; (2019); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

790667-49-1, (S)-tert-Butyl 2-methyl-4-oxopiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

790667-49-1, Combine 2-METHYL-4-OXO-PIPERIDINE-1-CARBOXYLIC acid tert-butyl ester isomer l (10.0 g, 46.89 mmol), absolute ethanol (200 mL), and sodium borohydride (2.66 g, 70.33 mmol) with stirring. After 2 hr. , concentrate the reaction mixture and then partition the residue between water (100 mL) and 1 : 1 hexane: ethyl acetate (100 mL). Separate the aqueous layer and wash with 1: 1 hexane: ethyl acetate (4X100 mL), combine the organic layers, wash with aqueous NACI solution, dry over sodium sulfate, filter and concentrate. Purify the residue by silica gel flash chromatography eluting with 7: 3 hexane : ethyl acetate to obtain the resolved trans isomer 1 (3.03 g, 30%) and cis isomer 1 (5.2 g, 52%). Trans isomer 1 :’H NMR (CDCl3) : 4.5 (m, 1H), 4.05 (m, 1H), 3.95 (M, 1H), 2.9 (M, 1H), 1.9 (m, 1H), 1.8 (m, 1H), 1.5 (m, 1H), 1.45 (s, 9H), 1.4 (m, 1H), 1.35 (m, 1H), 1.1 (d, 3H). cis isomer 1 :] H NMR (CDC13) : 4.25 (m, 1H), 4.15 (M, 1H), 3.8 (m, 1H), 3.25 (m, 1H), 1.8 (M, 1H), 1.65 (m, 3H), 1. 4 (s, 9H), 1.3 (d, 3H).

As the paragraph descriping shows that 790667-49-1 is playing an increasingly important role.

Reference£º
Patent; ELI LILLY AND COMPANY; WO2004/94380; (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.268550-48-7,tert-Butyl 1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate,as a common compound, the synthetic route is as follows.

A mixture of tert-butyl l-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate (1.83 g, 7.20 mmol), commercially available 4-bromofuran-2(5H)-one (1.41 g, 8.63 mmol), Xantphos (0.416 g, 0.720 mmol), water (0.389 mL, 21.6 mmol), and potassium carbonate (1.989 g, 14.39 mmol) in toluene (50 mL) was degassed with nitrogen followed by addition of palladium acetate (0.081 g, 0.36 mmol). The resulting mixture was heated at 65 C for 16 h. After filtration through CELITE, the filtrate was concentrated and the residue was purified on silica gel column using EtOAc /hexane as eluting solvents to give the title compound. LC/MS: (M+l)+: 337.18., 268550-48-7

The synthetic route of 268550-48-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; DING, Fa-Xiang; DONG, Shuzhi; FRIE, Jessica; GU, Xin; JIANG, Jinlong; PASTERNAK, Alexander; TANG, Haifeng; WU, Zhicai; YU, Yang; SUZUKI, Takao; WO2014/18764; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

71486-53-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.71486-53-8,Methyl 4-oxopiperidine-3-carboxylate hydrochloride,as a common compound, the synthetic route is as follows.

A mixture of 20 gm (103.3 mMol) methyl 4-oxo-3-piperidinecarboxylate hydrochloride and 75 mL saturated aqueous sodium bicarbonate in 150 mL dichloromethane was stirred vigorously at room temperature. A solution of 24.8 gm (113.6 mMol) di-tert-butyl dicarbonate in 100 mL dichloromethane was then added dropwise over three hours. After stirring at room temperature for about 16 hours, an additional 3.0 gm di-tert-butyl dicarbonate were added and stirring continued for an additional 2 hours. The reaction mixture was then diluted with water and extracted with 2 x 250 mL dichloromethane. The organic phases were combined, dried over magnesium sulfate, and concentrated under reduced pressure to provide 26.2 gm (99percent) of the desired compound as a yellow oil.

The synthetic route of 71486-53-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ELI LILLY AND COMPANY; EP1204659; (2003); B1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.896464-16-7,tert-Butyl 2,7-diazaspiro[3.5]nonane-7-carboxylate,as a common compound, the synthetic route is as follows.

Step A: tert-butyl 2-(5 -(methylsulfonyl)pyrazin-2-yl)-2,7-diazaspiro [3.5 lnonane-7-carboxvlate:A mixture of tert-butyl 2,7-diazaspiro[3.5]nonane-7-carboxylate (commercially available from numerous vendors, for example, AstaTech, Inc., catalog 52326; 75 mg, 0.33 mmol), 2-Chloro- 5-(methylsulfonyl)pyrazine (64 mg, 0.33 mmol), Pd2(dba)3 (15 mg, 0.0 17 mmol), X-Phos (24 mg, 0.050 mmol), K3P04 (140 mg, 0.66 mmol), and dioxane (1.7 mL) in a microwave tube was heated to 120 C under an atmosphere of nitrogen for 12 minutes. The reaction was diluted withEtOAc, washed with brine, dried over Na2504, and concentrated. The crude product was purified by silica gel chromatography to furnish the title compound. LCMS: m/z 383 (M+H), 896464-16-7

The synthetic route of 896464-16-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME CORP; TANG, Haifeng; PIO, Barbara; JIANG, Jinlong; PASTERNAK, Alexander; DONG, Shuzhi; FERGUSON, Ronald Dale, II; GUO, Zack Zhiqiang; CHOBANIAN, Harry; FRIE, Jessica; GUO, Yan; WU, Zhicai; YU, Yang; WANG, Ming; WO2015/17305; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem