Day: November 23, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.21987-29-1,4,4-Difluoropiperidine,as a common compound, the synthetic route is as follows.

A mixture of Intermediate B (879 mg, 3.30 mmol), 4,4-difluoropiperidine (400 mg, 3.30 mmol), Pd2(dba)3 (302 mg, 0.330 mmol), xantphos (382 mg, 0.660 mmol) and KO’Bu (748 mg, 6.60 mmol) in toluene (10 ml) was bubbled with argon for 10 min. The mixture was then heated at 100¡ãC for overnight. The reaction was quenched with 60percent NaHC03 aqueous solution. The aqueous phase was extracted with DCM/IPA (20 ml x3, V/V = 3/1 ). The combined organic phase was dried over anhydrous MgS04. Filtered and concentrated. The residue was purified by silica gel chromatography (eluted with 2percent MeOH in DCM) to give the title compound as yellow solid (270 mg, 31 percent yield). LCMS (method B): [M+H]+ = 265, tR = 1.79 min.

21987-29-1, 21987-29-1 4,4-Difluoropiperidine 2758352, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; CHEN, Chao; DENG, Haibing; GUO, Haibing; HE, Feng; JIANG, Lei; LIANG, Fang; MI, Yuan; WAN, Huixin; XU, Yao-Chang; YU, Hongping; ZHANG, Ji Yue (Jeff); WO2013/38362; (2013); 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.24211-55-0,(S)-Piperidin-3-ol,as a common compound, the synthetic route is as follows.

4-Chloro-6-(6-(trifluoromethyl)pyridin-2-yl)-N-(2-(trifluoromethyl)pyridin-4-yl)-1,3,5-triazin-2-amine (43 mg, 0.10 mmol) prepared in step 4 of Example 1 was dissolved in 5 mL of tetrahydrofuran, and (S)-3-hydroxypiperidine (12 mg, 0.12 mmol) and sodium carbonate (16 mg, 0.15 mmol) were added. The mixture was heated under reflux for 16 h. The resultant solution was filtered, and the filtrate was purified by column chromatography to give the title compound. 1H NMR (500MHz, DMSO-d6): delta 10.70 (br, 1H), 8.55-8.66 (m, 3H), 8.26-8.33 (m, 1H), 8.08-8.11 (m, 1H), 7.85 -7.96 (m, 1H), 4.97-4.98 (m, 1H), 4.16-4.49 (m, 2H), 3.26-3.60 (m, 3H), 1.83-1.92 (m, 2H), 1.51-1.54 (m, 2H).ES: m/z 486.1 [M+H]+., 24211-55-0

24211-55-0 (S)-Piperidin-3-ol 6950221, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Nanjing Sanhome Pharmaceutical Co., Ltd.; WANG, Yong; ZHAO, Liwen; LIU, Xiaorong; ZHANG, Yan; HUANG, Dandan; JIANG, Chunhuan; SHI, Xinsheng; GU, Hongfeng; PANG, Silin; HAI, Wei; GE, Bingyang; (71 pag.)EP3489230; (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.1095010-47-1,1-tert-Butyl 3-methyl 5-hydroxypiperidine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

To a dichloromethane solution (25 mL) of 1-tert-butyl 3-methyl 5-hydroxypiperidine-1,3-dicarboxylate (1.30 g), Dess-Martin reagent (2.33 g) was added. After stirring for 3 hours at room temperature, Dess-Martin reagent (1.31 g) was further added to the reaction solution, and the mixture was stirred for further 2.5 hours. Then, saturated aqueous solution of sodium hydrogen carbonate (50 mL) and a 10% sodium thiosulfate aqueous solution (50 mL) were added sequentially to the mixture, and the organic layer was separated. The product was further extracted from the aqueous layer with dichloromethane (10 mL) four times. The obtained organic layer was dried with anhydrous sodium sulfate, filtered. The filtrate was concentrated under reduced pressure, the residue was purified with silica gel column chromatography (chloroform/methanol=100/0 to 98/2) to give 1-tert-butyl 3-methyl 5-oxopiperidine-1,3-dicarboxylate (1.14 g) as an oil. 1H NMR (300 MHz, CDCl3) delta 1.46 (s, 9H), 2.58-2.79 (m, 2H), 3.03-3.11 (m, 1H), 3.73 (s, 3H), 3.77-3.93 (m, 2H), 4.02 (s, 2H)

1095010-47-1, 1095010-47-1 1-tert-Butyl 3-methyl 5-hydroxypiperidine-1,3-dicarboxylate 45790959, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; SUMITOMO CHEMICAL COMPANY, LIMITED; SUMITOMO DAINIPPON PHARMA CO., LTD.; FUSANO, Akira; KOBAYASHI, Tomonori; SAITO, Yasuhiro; KANAI, Toshio; (55 pag.)US2016/221948; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

34622-39-4, (S)-2-Piperidinone-6-carboxylic acid is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 7-5: Preparation of (S)-N-(4-methoxybenzyl)-6-oxo-N-(4-(trimethylsilyl)but-2-en-1-yl)piperidine-2-carboxamide I5.1 and (S)-tert-butyl 2-((4-methoxybenzyl)(4-(trimethylsilyl)but-2-en-1-yl)carbamoyl)-6-oxopiperidine-1-carboxylate 15.2 [0199] [0200] To a solution of (S)-6-oxopiperidine-2-carboxylic acid (1.74 g, 12.15 mmol) in DMF (120 mL) were added N-(4-methoxybenzyl)-4-(trimethylsilyl)but-2-en-1-amine 14 (3.20 g, 12.2 mmol), EDC (2.79 g, 14.6 mmol) and HOBt (2.23 g, 14.6 mmol). After 2h stirring at room temperature EtO2 (300 mL) was added to the reaction and washed with sat. aq. NaCl solution (3 ¡Á 75 mL). The organic layer was dried over MgSO4 and the solvent was removed under reduced pressure and the crude compound I5.1 was used for the next step without further purification. MS (ESI): m/z (percent) = 389.29 [M + H]+, 777.25 [2M + H]+, 34622-39-4

As the paragraph descriping shows that 34622-39-4 is playing an increasingly important role.

Reference£º
Patent; Max-Planck-Gesellschaft zur Foerderung der Wissenschaften e.V.; The designation of the inventor has not yet been filed; EP2899192; (2015); 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.28697-07-6,N-Cbz-2-Piperidinecarboxylic acid,as a common compound, the synthetic route is as follows.

Example 27N-(3,5-Dichloroisonicotinoyl)-4-(2-piperidin-2-yl-3H-imidazo[4,5-b]pyridin-3-yl)-L- phenylalanine (Compound 11) To Intermediate 2 (3.41g) in DCM (40ml) is added 1-Cbz-2-piperidinecarboxylic acid (4.48g), HOBt (346mg) and EDC (4.88g). The reaction is stirred at room temperature for 3 days. The reaction is partitioned between DCM (40ml) and water (40ml) and the organic layer washed with 10% AcOH solution (40ml). The solvent is removed in vacuo and the residue dissolved in AcOH (12ml) and heated in a microwave at 1200C for 10 minutes. The mixture is evaporated to dryness in vacuo and partitioned between EtOAc (40ml) and saturated NaHCO3 (40ml), the organic layer is dried over Na2SO4, filtered, evaporated to dryness and the residue purified by chromatography on silica eluting with EtOAc/heptane. To a portion of the purified material (1.25g) in DCM (20ml) is added TFA (1.51 ml) at room temperature. The reaction is stirred at room temperature for 20 hours. The reaction is partitioned between DCM (50ml) and saturated NaHCO3 (50ml), dried over Na2SO4, filtered and the evaporated to dryness. To a portion of the obtained material (348mg) in DCM (4ml) is added DIPEA (138mul) followed by 2,6-dichloroisonicotinoyl chloride (169mg) in DCM (2ml). The reaction is stirred at room temperature for 1 hour. The reaction is partitioned between DCM (40ml) and water (40ml). The organic layer is dried over Na2SO4, filtered and evaporated to dryness in vacuo and the residue purified by chromatography on silica eluting with EtOAc/heptane. To the purified material (310mg) in EtOH (10ml) under N2(g) is added 10% Pd on carbon (50mg). The mixture is flushed with H2(g) and stirred at atmospheric pressure for 3 days. The mixture is filtered through a pad of celite, and the filtrate evaporated to dryness in vacuo. The crude material is dissolved in THF (4ml) and added slowly over 1 hour to a stirred solution of NaOH (2.0M, 5ml). Once addition is complete the reaction is stirred at room temperature for 1 hour, the reaction mixture acidified to acidic pH with HCI (6.0M), concentrated in vacuo and purified by preparative HPLC (Method C) to afford the title compound as a white solid (61 mg, 1%). LCMS (Method A) 539 [M+H] RT 1.72 mins. 1H NMR 300MHz (CDCI3) .81.10-1.41 (m, 2H), 1.43-1.60 (m, 2H), 1.70 (m, 2H), 1.88 (d, 1 H), 2.41 (m, 1 H), 3.00 (m, 2H), 3.39 (d, 1 H), 3.75 (d, 1 H), 4.77 (m, 1 H), 7.25 (m, 3H), 7.50 (d, 2H), 8.00 (d, 1 H), 8.09 (dd, 1 H), 8.40 (s, 2H), 28697-07-6

The synthetic route of 28697-07-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; UCB PHARMA, S.A.; WO2008/64823; (2008); 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.158407-04-6,tert-Butyl 4-(bromomethyl)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step B: tert-Butyl 4-{[(5-cyanopyridin-2-yl)sulfanyllmethyl|piperidine-l-carboxylate 6-Sulfanylpyridine-3-carbonitrile (220 mg, 1.6 mmol) was dissolved in DMF (10 mL) in a round bottom flask at room temperature, tert-butyl 4-(bromomethyl) piperidine-l-carboxylate (530 mg, 1.9 mmol) was added, followed by potassium carbonate (440 mg, 3.2 mmol). The resulting mixture was heated to 80 C and stirred over night. The reaction mixture was diluted with EtOAc, washed with water and brine, then dried over anhydrous sodium sulfate, filtered and concentrated. The resulting residue was purified by MPLC (eluent: 0->100% EtOAc/Hexane gradient) to provide tert-Butyl 4-{[(5-cyanopyridin-2-yl)sulfanyl]methyl}piperidine-l- carboxylate. NMR delta (ppm)(500 Hz, CDCh): 8.64 (d, J= 2.1 Hz, 1H), 7.64 (dd, J= 8.4, 2.2 Hz, 1H), 4.11 (m, 2 H), 3.17 (d, J= 6.8 Hz, 2H), 2.68 (m, 2 H), 1.84-1.80 (m, 2 H), 1.80-1.72 (m, 1 H), 1.55 (s, 9 H), 1.28-1.16 (m, 2 H). LC-MS (IE, m/z): 356 [M + 23]+.

158407-04-6, The synthetic route of 158407-04-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; WALSH, Shawn; PASTERNAK, Alexander; CATO, Brian; FINKE, Paul, E.; FRIE, Jessica; FU, Qinghong; KIM, Dooseop; PIO, Barbara; SHAHRIPOUR, Aurash; SHI, Zhi-Cai; TANG, Haifeng; WO2013/39802; (2013); 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.503614-92-4,1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid,as a common compound, the synthetic route is as follows.,503614-92-4

General procedure: A solution of 5,6-dihydro-3- (4-morpholinyl) -1- [4- (2-oxo-1-piperidinyl) phenyl]2 (1H) -pyridone and ethyl [(4-methoxyphenyl) hydrazino] chloroacetate,In the triethylamine for the acid binding agent under the conditions of condensation, and then by hydrochloric acid deprotection,The resulting intermediates,In the ethylene glycol under high temperature conditions with ammonia reaction in the preparation of an average of apixaban, the purity of 95.4%.In the 50L reactor,Add 2 kg of apixaban crude (purity 95. 4%) and 16L with 10% ammonia in ethylene glycol solution, heated to 90 C dissolved, then add 16L water cooling, stirring at 40 ~ 50 C for 2 hours , Cooling to 0 ~ 10 C. And then filtered to dryness to give 8 kg of a white solid, 90% yield, and an HPLC purity of 99. 97%.

503614-92-4 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid 22240440, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Zhongmei HuashitongBiotechnology Pharmaceutical Technology (Wuhan) Co.,Ltd; HU, MINGLONG; WU, HAOHAO; CUI, JIAN; QIAN, LINA; (13 pag.)CN106188036; (2016); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

4897-50-1, 4-Piperidinopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 1.; Preparation of 1-chlorocarbonyl-4-piperidinopiperidine base (IRT-4):; Dissolving 4-piperdinoperidine (100g) in benzene (1580ml) under stirring for 15 to 30 minutes at room temperature, adding a solution of triphosgene (150g) in benzene (660 ml) over a period of 1 to 3 hours at a temperature of 20¡ã- 25¡ãC. Filtering the solid, washing it with benzene and drying, then dissolve the dried solid in chloroform (5900 ml) by stirring at room temperature for about 30 minutes. Charging aqueous sodium bicarbonate solution (400 ml), stirring and separating chloroform layer, washing the chloroform layer with water (1800 ml), separating chloroform layer anddistilling off chloroform under vacuum at a temperature up to below 45¡ãC to obtain 1-chlorocorbonyl-4-piperidopiperidine base (60 g).

4897-50-1, The synthetic route of 4897-50-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SHILPA MEDICARE LIMITED; WO2006/16203; (2006); A1;,
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

(1) 2-Chloro-3-methyl-5-nitropyridine (6.02g) in N, N- dimethylformamide (35) at room temperature was added 2- (4-piperidinyl) -2-propanol (5.0 g) and potassium carbonate (9.65g), and stirred for 6 hours at 80 . After the reaction, it cooled to room temperature and, after addition of water, to give a yellow solid (9.09g) collected by the precipitated solid filtered.

22990-34-7, As the paragraph descriping shows that 22990-34-7 is playing an increasingly important role.

Reference£º
Patent; Mitsubishi Tanabe Pharma Corporation; Watanabe, Masayuki; Furukawa, Hiroyuki; Hamada, Maiko; Fuji, Naoto; Ushio, Hiroyuki; Takashima, Toru; (81 pag.)KR2015/2661; (2015); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

41373-39-1, (S)-Piperidin-2-ylmethanol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Into a 50-mL round-bottom flask, was placed a solution of 2-methylpyridine-4-carboxylic acid (548 mg, 4.00 mmol, 1.00 equiv), (2S)-piperidin-2-ylmethanol (460 mg, 3.99 mmol, 1.00 equiv), DIEA (1.29 g, 9.98 mmol, 2.50 equiv) and HATU (1.67 g, 4.39 mmol, 1.10 equiv) in dichloromethane (20 mL). The resulted solution was stirred for 30 min at room temperature. After concentration, the residue was dissolved with 200 mL of EA. Then it was washed with 3 x 20 mL of brine, dried over anhydrous sodium sulfate and concentrated under vacuum to give a residue. The crude was purified by silica gel column eluted with dichloromethane/methanol (10:1). This resulted in 426 mg (46percent, 97percent ee) of [(2S)-l-[(2-methylpyridin-4-yl)carbonyl]- piperidin-2-yl]methanol as yellow oil., 41373-39-1

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

Reference£º
Patent; GLOBAL BLOOD THERAPEUTICS, INC.; LI, Zhe; HARRIS, Jason, R.; DUFU, Kobina, N.; GENG, Xin; SINHA, Uma; (101 pag.)WO2016/160755; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem