Month: March 2022

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.769944-71-0,3-(4-Bromophenyl)piperidin-2-one,as a common compound, the synthetic route is as follows.

769944-71-0, Weighing the compound 4 (0.75 g, 2 . 96 mmol) dissolved in 15 mlTHF (tetrahydrofuran) after lowering the temperature to 0 C, adding borane tetrahydrofuran complex (6.65 ml, 1.0 M in THF, 6 . 65 mmol, CAS: 14044 – 65 – 6) stir at room temperature overnight, after adding several drops of dilute hydrochloric acid quenching reaction reflux 1.5 h, turns on lathe does solvent evaporation, adding an amount of the sodium hydroxide solution, dichloromethane is used for extraction (25 ml * 3), combined with the organic phase, washed with saturated sodium chloride (25 ml * 2), drying, filtering, concentrating add 25 ml water and 25 ml hydrochloric acid in 110 C reflow 3 h, the reaction is finished adding proper amount of sodium hydrate to ph 7, dichloromethane is used for extraction (30 ml * 3), combined with the organic phase, washed with saturated sodium chloride (30 ml * 2) concentrated under reduced pressure to obtain yellow solid that the target compound 5 (0.64 g, yield 90%).

As the paragraph descriping shows that 769944-71-0 is playing an increasingly important role.

Reference：
Patent; Southeast University; Cai Jin; Wang Yingying; Ji Min; Ning Yao; Wei Qing; Zhan Mengmeng; Liu Wenjing; (9 pag.)CN108409638; (2018); A;,
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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.140645-24-5,(S)-3-(Aminomethyl)-1-N-Boc-piperidine,as a common compound, the synthetic route is as follows.

Step 3. Preparation of tert-butvl (3SV3-(r6-(4-chlorophenvn-2-(2-methoxyphenvl)-4-oxoquinazolin-3(4H)-vl1methvl)piperidine-1-carboxylate; O[260] tert-Butyl (3S)-3-(aminomethyl)piperidine-1-carboxylate (1.00 g, 4.67 mmol) in toluene(20 mL) was added to 6-(4-chlorophenyl)-2-(2-methoxyphenyl)-4H-3,1-benzoxazin-4-one (1.31 g,3.59 mmol) (step 2) and the mixture was stirred at reflux for 15 h. Ethanediol (20 mL) and NaOH67(288 mg, 7.2 mmol) were added, and the resulting mixture was stirred at 150C for for 15 h. Thecrude was diluted with DCM and water. The aq mixture was extracted with DCM (50 mL x 2) andthe organic solvent was removed under reduced pressure. The crude was then purified by silicagel flash chromatography with 10 to 50% ethyl acetate in hexanes. 1H NMR (300 MHz, DMSO-d6)6 8.41 (d, 1 H), 8.18 (dd, 1 H), 7.85 (d, 2 H), 7.76 (d, 1 H), 7.54-7.61 (m, 3 H), 7.47-7.51 (m, 1 H),7.21 (dd, 1 H), 7.14 (t, 1 H), 4.00-4.20 (br, 1 H), 3.80 (s, 3 H), 3.56-3.70 (br, 1 H), 2.52-2.68 (br, 2H), 2.21-2.38 (br, 1 H), 1.11-1.72 (br, 15 H); ES-MS m/z 560.1 (MhT); HPLC RT (min) 4.50., 140645-24-5

The synthetic route of 140645-24-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; BAYER PHARMACEUTICALS CORPORATION; WO2006/12577; (2006); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.122860-33-7,Benzyl 4-(hydroxymethyl)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

26c. Phenylmethyl 4-formylpiperidinecarboxylate To a stirred solution of oxalyl chloride (2M solution in dichloromethane, 10.9 mL, 21.9 mmol) was added DMSO (3.1 mL, 3.4 g, 43.8 mmol) in dichloromethane (6 mL) over a period of 15 minutes. The product of Example 26b (4.4 g, 17.5 mmol) in dichloromethane (7 mL) was then added at -78 C. over a period of 15 minutes. The resultant solution was stirred at -78 C. for 1 hour and then triethylamine (12.2 mL, 8.86 g, 87.5 mmol) was added, dropwise, over a period of 15minutes. The mixture was further stirred at -78 C. for 30 min and then at 0 C. for 15 min. The reaction mixture was quenched with water and extracted with dichloromethane. The combined organic phase was washed with 1% HCl, water, dried over sodium sulfate, filtered and evaporated to give the title compound (4.4 g, 100%) which was used in the next step without purification. 1H NMR (300 MHz, CDCl3) delta9.65 (s, 1H), 7.28-7.38 (m, 5H), 5.12 (s, 2H), 4.04 (br d, J=13.1 Hz, 2H), 2.97-3.06 (m, 2H), 2.38-2.45 (m, 1H), 1.88-1.92 (m,2H), 1.52-1.64 (m, 2H). 13C NMR (75 MHz, CDCl3) delta202.7, 155.2, 136.7, 128.5, 128.6, 127.9, 67.2, 47.8, 43.0, 25.1. LRMS (APIMS) m/z 248 (MH+)., 122860-33-7

122860-33-7 Benzyl 4-(hydroxymethyl)piperidine-1-carboxylate 736490, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Fang, Xinqin; Garvey, David S.; Gaston, Ricky D.; Lin, Chia-En; Ranatunga, Ramani R.; Richardson, Stewart K.; Wang, Tiansheng; Wang, Weiheng; Wey, Shiow-Jyi; US2003/203915; (2003); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1187173-43-8, 2,7-Diazaspiro[4.5]decan-1-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2,7-Diazaspiro[4.5]decan-1 -one hydrogen chloride (100 mg, 0.524 mmol) was dissolved in dichloromethane (10 mL) and triethylamine (0.219 mL, 1 .573 mmol), and 2,5-bis(trifluoromethyl)benzenesulfonyl chloride (197 mg, 0.629 mmol) was added. After stirring for 17 h the reaction mixture was concentrated in vacuo and the resulting residue was purified by MDAP to give 7-{[2,5-bis(trifluoromethyl)phenyl]- sulfonyl}-2,7-diazaspiro[4.5]decan-1 -one (96 mg, 0.221 mmol, 42% yield) as a white solid. 1 H NMR (400 MHz, DMSO-d6) delta ppm 1 .46 – 1 .63 (m, 3 H) 1.66 – 1 .75 (m, 1 H) 1 .85 – 2.03 (m, 2 H) 2.72 – 2.78 (m, 1 H) 2.80 (d, J=12.28 Hz, 1 H) 3.1 1 – 3.19 (m, 2 H) 3.47 (d, J=12.28 Hz, 1 H) 3.71 (d, J=1 1 .78 Hz, 1 H) 7.75 (s, 1 H) 8.24 (s, 1 H) 8.26 – 8.33 (m, 2 H). MS ES+ve m/z 431 (M+H)., 1187173-43-8

The synthetic route of 1187173-43-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CONVERGENCE PHARMACEUTICALS LIMITED; GLEAVE, Robert James; HACHISU, Shuji; PAGE, Lee William; BESWICK, Paul John; WO2011/141728; (2011); 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.20691-89-8,1-Methyl-4-piperidinemethanol,as a common compound, the synthetic route is as follows.

To Example 60 (0. 78 g, 6 mmol) was added thionyl chloride (10 mL) and the mixture was heated to reflux for about 2 hours. The mixture was cooled and concentrated to dryness. The residue was washed with acetone, suspended in saturated aqueous sodium carbonate and extracted with dichloromethane. The combined organic extracts were dried (Na2SO4), filtered and concentrated under vacuum to provide the desired product. MS (ESI) : m/z 148 (M+H) +.

20691-89-8, The synthetic route of 20691-89-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ABBOTT LABORATORIES; MAKOTO, Aoyama; WO2005/95387; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

10338-57-5, 4-(Piperidin-1-yl)benzaldehyde is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a mixture of NaH (146mg, 6.08mmol) in THF (2mL) was added a solution of intermediate 11 (500mg, 1.52mmol) in THF (4mL) at 0C, and the mixture was stirred for 40min under argon. And a solution of corresponding substituted benzaldehydes (2-1b-m, 1.52mmol) in THF (1mL) was added dropwise. Then the mixture was stirred for another 4-7h under argon. After the reaction was completed, the mixture was quenched with 3mol/L HCl and basified with saturated aqueous solution of Na2CO3. Then the mixture was extracted with ethyl acetate (15mL×3) and the combined organic phases were washed with brine, dried over anhydrous Na2SO4, filtered and concentrated under reduced pressure to provide crude product, the crude product was purified on silica chromatography to afford corresponding target compounds 12b-m.

10338-57-5, As the paragraph descriping shows that 10338-57-5 is playing an increasingly important role.

Reference：
Article; Cao, Zhongcheng; Deng, Yong; Li, Wei; Shi, Yichun; Song, Qing; Yang, Xia; Zhang, Li; Bioorganic Chemistry; vol. 97; (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.162166-99-6,1-Boc-3-Methanesulfonyloxymethyl-piperidine,as a common compound, the synthetic route is as follows.

tert-butyl 3-(methylsulfonyloxymethyl)piperidin-1-carboxylate (0.41 g, 1.4 mmol) obtained in Step B was dissolvedin 7 mL of DMF. Sodium cyanide (0.075 g, 1.54 mmol) was added thereto, and the mixture was stirred at 60Cfor 16 hours. The reaction solution was concentrated under reduced pressure, diluted with water, and extracted withEtOAc. The organic layer was separated and dried with MgSO4 to obtain the title compound (0.29 g, 93 %).1H-NMR (CDCl3) delta 3.90 (1H, m), 3.82 (1H, m), 2.92 (2H, m), 2.30 (2H, m), 1.92 (2H, m), 1.68 (1H, m), 1.49 (1H, m),1.46 (9H, s), 1.35 (1H, m), 162166-99-6

As the paragraph descriping shows that 162166-99-6 is playing an increasingly important role.

Reference：
Patent; LG Chem, Ltd.; KIM, Young Kwan; PARK, Sang Yun; JOO, Hyun Woo; CHOI, Eun Sil; PAEK, Seung Yup; KANG, Seung Wan; KIM, Byung Gyu; LEE, Chang Seok; KIM, Sung Wook; LEE, Sang Dae; (369 pag.)EP3239143; (2017); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.690261-64-4,2-(Piperidin-4-yl)pyrimidine hydrochloride,as a common compound, the synthetic route is as follows.

A solution of EDC.HCI (ALFA-AESAR, 340 mg, 1.77 mmol), TEA (ALFA-AESAR, 0.25 mL, 1 .77 mmol), HOBt (ALDRICH, 240 mg, 1 .77 mmol), Intermediate 30 (295.3 mg, 1.48 mmol) and 4,4,4-trifluorobutyric acid (ALFA-AESAR, 252 mg, 1.77 mmol) in DMF (15 mL) was stirred at rt overnight. The mixture was then washed with NaHCC>3 saturated solution and EtOAc was added, the two phases were separated and the aqueous one was further extracted with EtOAc. The collected organic layer was dried(anh) Na2SC>4, filtered and evaporated. The crude so obtained was purified by flash chromatography (Si SNAP 50, CyHex EtOAc from 1/1 to 0/10, then DCM/MeOH 8/2) to give title compound (141 mg, 33%) as a white solid. 1H NMR (500 MHz, DMSO-de) delta ppm: 8.75 (d, J = 4.9 Hz, 2H), 7.35 (t, J = 4.9 Hz, 1 H), 4.44 (d, J = 13.2 Hz, 1 H), 3.94 (d, J = 13.7 Hz, 1 H), 3.22-3.13 (m, 1 H), 3.13-3.05 (m, 1 H), 2.82-2.72 (m, 1 H), 2.70-2.57 (m, 2H), 2.57-2.45 (m, 2H), 2.02-1.90 (m, 1 H), 1.79-1.67 (m, 1 H),1.65-1.51 (m, 1 H). [ES+ MS] m/z 288 (MH+)., 690261-64-4

690261-64-4 2-(Piperidin-4-yl)pyrimidine hydrochloride 56965759, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; BIOVERSYS AG; PORRAS DE FRANCISCO, Esther; REMUINAN-BLANCO, Modesto Jesus; BOUROTTE, Marilyne; DEPREZ, Benoit; WILLAND, Nicolas; (89 pag.)WO2019/34701; (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.10315-06-7,Methyl 1-benzylpiperidine-4-carboxylate,as a common compound, the synthetic route is as follows.

1.5 (1-Benzylpiperidin-4-yl)-N-methoxy-N-methylcarboxamide A solution of 4.17 g (42.8 mmol) of N,O-dimethylhydroxylamine hydrochloride in 195 mL of THF is cooled to -20 C., and 6.51 g (28 mmol) of methyl (1-benzylpiperidin-4-yl)carboxylate are added. Next, 85 mL of a 1M solution of isopropylmagnesium bromide in THF are added over 20 minutes while keeping the temperature in the region of 5 C. The mixture is stirred at -10 C. for 20 minutes. The reaction medium is hydrolyzed with 40 mL of 20% ammonium chloride solution and then extracted with ethyl acetate. The combined organic phases are washed with water and with brine, and then dried over anhydrous sodium sulfate and evaporated under reduced pressure. 6.9 g of an oily product are obtained.1H NMR (DMSO-d6, 250 MHz) delta ppm: 1.5-1.75 (m, 4H); 1.9-2.05 (m, 2H); 2.55-2.7 (m, 1H); 2.8-2.9 (m, 2H); 3.09 (s, 3H); 3.46 (s, 2H); 3.67 (s, 3H); 7.2-7.4 (m, 5H).

10315-06-7, As the paragraph descriping shows that 10315-06-7 is playing an increasingly important role.

Reference：
Patent; SANOFI-AVENTIS; US2009/124624; (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.154307-84-3,(2S,5S)-5-Hydroxypiperidine-2-carboxylic acid hydrochloride,as a common compound, the synthetic route is as follows.

Step 2 To a solution of (2S,5S)-5-hydroxypiperidine-2-carboxylic acid, HCl (0.603 g, 3.32 mmol) in 1,4-dioxane (4 mL) and water (16 mL) was added potassium carbonate (1.835 g, 13.28 mmol) followed by (9H-fluoren-9-yl)methyl carbonochloridate (0.859 g, 3.32 mmol) at 0 C. The mixture was stirred at RT for 18 hrs and then treated with water (10 ml). The resulting mixture was extracted with diethyl ether (2*15 ml). The aqueous phase was acidified with aq. HCl (1M) to pH 2-3, and extracted with DCM (3*20 ml). The combined organic layers were dried over MgSO4 and concentrated to give the crude product (2S,5S)-1-(((9H-fluoren-9-yl)methoxy)carbonyl)-5-hydroxypiperidine-2-carboxylic acid (800 mg, 65.6% yield) as a white solid. 1H NMR (500 MHz, methanol-d4) d 7.86-7.78 (m, 2H), 7.69-7.57 (m, 2H), 7.48-7.37 (m, 2H), 7.37-7.20 (m, 2H), 4.81-4.77 (m, 1H), 4.59-4.36 (m, 2H), 4.32-4.20 (m, 1H), 4.18-4.08 (m, 1H), 3.75-3.64 (m, 2H), 3.58-3.43 (m, 1H), 2.01-1.89 (m, 1H), 1.81-1.57 (m, 1H), 1.30-1.17 (m, 1H). ESI-MS(+) m/z=368.2 (M+Na), 154307-84-3

The synthetic route of 154307-84-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Bristol-Myers Squibb Company; Miller, Michael Matthew; Mapelli, Claudio; Allen, Martin Patrick; Bowsher, Michael S.; Boy, Kenneth M.; Gillis, Eric P.; Langley, David R.; Mull, Eric; Poirier, Maude A.; Sanghvi, Nishith; Sun, Li-Qiang; Tenney, Daniel J.; Yeung, Kap-Sun; Zhu, Juliang; Reid, Patrick C.; Scola, Paul Michael; (892 pag.)US9308236; (2016); B2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem