Tag: M.W:100-200

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 (80 mg, 0.420 mmol) was dissolved in dichloromethane (4 mL) and triethylamine (0.1 17 ml_, 0.839 mmol) before the addition of 2,4-dimethylbenzenesulfonyl chloride (94 mg, 0.462 mmol). After stirring for 20 h the reaction mixture was concentrated in vacuo and the resulting residue was purified by MDAP to give 7-[(2,4-dimethylphenyl)sulfonyl]-2,7- diazaspiro[4.5]decan-1 -one (64.4 mg, 0.190 mmol, 45% yield) as a white solid. 1 H NMR (500 MHz, DMSO-d6) delta ppm 7.71 (s, 1 H) 7.66 (d, J=8.0 Hz, 1 H) 7.26 (s, 1 H) 7.22 (d, J=8.1 Hz, 1 H) 3.59 (d, J=12.0 Hz, 1 H) 3.23 (d, J=1 1 .7 Hz, 1 H) 3.15 (m, 1 H) 3.09 (m, 1 H) 2.50 (s, 3 H) 2.48 (m, 2 H) 2.35 (s, 3 H) 1 .91 (t, J=6.9 Hz, 2 H) 1.69 (dt, J=12.8, 2.8 Hz, 1 H) 1.54 (m, 1 H) 1.48 (m, 2 H). MS ES+ve m/z 323 (M+H).

1187173-43-8, 1187173-43-8 2,7-Diazaspiro[4.5]decan-1-one hydrochloride 45074126, apiperidines compound, is more and more widely used in various fields.

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.1019351-46-2,Methyl 4-aminopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

200 g of tetrahydrofuran was placed in a 500 ml four-necked flask equipped with a stirring and a thermometer.12.5 g (0.05 mol) of (2S,5R)-5-benzyloxyaminopiperidine-2-carboxylic acid, 50 g of tri-n-butylamine,0.1 g of N,N-dimethylformamide, cooled at -10 C,A mixed solution of 23.8 g (0.08 mol) of solid phosgene and 80 g of tetrahydrofuran was added dropwise.The reaction was stirred at 10-20 C for 4 hours.Between 10 and 20 C, a mixed solution of 11.0 g (0.07 mol) of 1-methoxycarbonyl-4-aminopiperidine and 30 g of tetrahydrofuran was added.Stir the reaction between 15-20 C for 3 hours.The reaction liquid was poured into 300 g of ice water mixture and layered.The aqueous layer was extracted twice with dichloromethane, 50 g each time.The organic phases were combined and washed twice with saturated sodium chloride solution, 20 g each time.After the obtained organic phase recovers the solvent,18.2 g of (2S,5R)-N-(1-(methoxycarbonyl)piperidin-4-yl)-6-benzyloxy-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamide ,The liquid phase purity was 99.8%, and the yield was 93.3%., 1019351-46-2

The synthetic route of 1019351-46-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Xin Fa Pharmaceutical Co., Ltd.; Qi Yuxin; Li Xinfa; Wang Baolin; Xu Xin; Zhao Yinlong; Teng Yuqi; (9 pag.)CN109928970; (2019); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

20691-89-8, 1-Methyl-4-piperidinemethanol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 7-fluoro-6-methoxy-4-oxo-1,4-dihydro-3-quinolinecarbonitrile (1.5 g, 6.9 mmol) and (1-methylpiperidin-4-yl)-methanol (1.8 g, 13.7 mmol) (WO 200471212) and a 60% dispersion in mineral oil of sodium hydride (0.8 g, 34.4 mmol) is heated at 110 C. for 2 hours. The reaction mixture is quenched with methanol, concentrated, and azeotroped with toluene to give 2.25 g of a brown solid. A mixture of this solid and phosphorous oxychloride (15 mL, 159 mmol) is heated at reflux for 30 minutes then concentrated in vacuo. The residue is partitioned between aqueous sodium bicarbonate and methylene chloride. The organic layer is dried over sodium sulfate, filtered and concentrated on to silica gel. Purification by column chromatography eluting with a gradient of 1:9 methanol:methylene chloride to 0.05:1:5 triethylamine:methanol:methylene chloride provided 1.6 g of 4-chloro-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinoline-3-carbonitrile, mp 166-168 C. [0351] MS 346 (M+H)+ [0352] Analysis for C18H20ClN3O2-1 HCl+0.5 H2O [0353] Calcd: C, 54.72; H, 5.54; N 10.50. [0354] Found: C, 54.72; H, 6.07; N 10.05., 20691-89-8

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

Reference：
Patent; Wyeth Holdings Corporation; US2003/212276; (2003); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

5810-56-0, 4-Acetamidopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5810-56-0

Preparation 12 A mixture of 9.95 g. (0.07 mole) of 4-acetylaminopiperidine, 12.7 g. (0.095 mole) of alpha-phenylpropionaldehyde and a trace of p-toluenesulfonic acid in 150 ml. of toluene was refluxed under a Dean-Stark trap for about one and a quarter hours, during which time 1.1 ml. of water was collected. The solution was then taken to dryness in vacuo, the residual traces of water were azeotroped by distillation with ethanol, and the residue was dissolved in 200 ml. of ethanol and the mixture reduced with hydrogen over platinum oxide under an initial hydrogen pressure of 42 psig. When reduction was complete, the catalyst was removed by filtration, the filtrate was taken to dryness, and the residue was partitioned between toluene/ethyl acetate and water. The layers were separated, and the organic extracts were washed with dilute hydrochloric acid. The combined aqueous phase was rendered strongly basic with aqueous potassium hydroxide and extracted two times with toluene. The toluene extracts, on washing with brine, drying over anhydrous sodium sulphate and evaporation to dryness, afforded 16.3 g. of an oil which was crystallized from toluene/hexane to give 12.95 g. of 1-(2-phenylpropyl)-4-acetylaminopiperidine, m.p. 102-103 C.

5810-56-0 4-Acetamidopiperidine 1445156, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Sterling Drug Inc.; US4339576; (1982); A;; ; Patent; Sterling Drug Inc.; US4304911; (1981); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

138377-80-7, 3-Aminopiperidin-2-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 3-aminopiperidin-2-one hydrochloride (3.49 g) and triethylamine (6.20 mL) in THF (50 mL) was added di-tert-butyl bicarbonate (6.07 g) at room temperature. The reaction mixture was stirred at room temperature overnight, water was added, and the mixture was extracted with ethyl acetate. The organic layer was separated, washed with water, dried over magnesium sulfate, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate/hexane) to give the title compound (3.41 g) .XH NMR (300 MHz, DMSO-d6) delta 1.38 (9H, s) , 1.53-2.03 (4H, m) , 3.09 (2H, brs), 3.68-3.91 (1H, m) , 6.83 (1H, d, J = 8.1 Hz), 7.48 (1H, brs) ., 138377-80-7

The synthetic route of 138377-80-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; MATSUMOTO, Shigemitsu; ONO, Koji; TOMINARI, Yusuke; KATOH, Taisuke; MIWA, Kazuhiro; HASUOKA, Atsushi; IMAMURA, Shinichi; WO2013/18929; (2013); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

19365-08-3, 3-Hydroxypiperidin-2-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 3-hydroxypiperidin-2-one (3.0 g, 26.1 mmol) and 1H-imidazole (1.95 g, 28.7 mmol) in DMF (30 mL) was slowly added TBSCl (5.11 g, 33.9 mmol) at RT. The reaction mixture was degassed with nitrogen 3 times and stirred at RT for 16 hours. The resulting mixture was poured into ice-water (100 mL) and extracted with EA (3 x 50 mL). The combined organic layers were washed with brine (3 x 30 mL), dried over anhydrous Na2SO4 and filtered. The filtrate was concentrated under vacuum. The residue was purified by a silica gel column chromatography, eluting with 50% of EA in PE to afford the title compound: LCMS [M + 1]+: 230.

19365-08-3, The synthetic route of 19365-08-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DONG, Shuzhi; SCOTT, Jack, D.; TANG, Haiqun; ZHAO, Zhiqiang; YANG, Dexi; GU, Xin; JIANG, Jinlong; XIAO, Li; (209 pag.)WO2019/18186; (2019); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

5810-56-0, 4-Acetamidopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 12 A mixture of 0.042 mole of 2,6-dibromopyridine, 0.056 mole of anhydrous potassium carbonate and 0.052 mole of 4-acetamidopiperidine in 75 ml of sulfolane is heated to 150 C. with stirring for 20 hours, then the sulfolane is concentrated to 1/5th of its volume, the reaction mixture is poured in 100 ml of water and extracted with diethyl ether (4*150 ml). The organic phase is washed with water, dried over anhydrous sodium sulfate, concentrated to dryness and the residue is crystallized in 40 ml of ethyl acetate. The 4-acetamido-1-(6-bromo-2-pyridyl)piperidine is thus obtained; m.p. 158 to 160 C. Yield: 56% of the theoretical., 5810-56-0

As the paragraph descriping shows that 5810-56-0 is playing an increasingly important role.

Reference：
Patent; Sanofi; US4409228; (1983); 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.50607-30-2,Piperidine-2,4-dione,as a common compound, the synthetic route is as follows.,50607-30-2

[0239] 2,4-piperidinedione (1.0g, 8.84mmol) was dissolved in MeOH. NaBH4 (0.5g, 13.26mmol) was added at 0°C,stirred at 0°C for 30min, and the reaction mixture was then placed at room temperature and stirred for 1h. TLC (DCM/Me-OH) was employed to monitor the reaction. After the reaction completed, it was quenched by adding water and dried byspinning. Column chromatography afforded white solid powder 0.8g, yield 80.0percent.[0240] 1H NMR (400 MHz, DMSO-d6) delta 7.52-7.28 (s, 1H), 5.06-4.78 (d, J = 3.5 Hz, 1H), 4.03-3.78 (dp, J = 7.2,3.9,3.3Hz, 1H),3.28-3.14 (m, 1H),3.09-2.91 (dtt, J = 7.4, 5.2, 2.2 Hz, 1H), 2.42-2.25 (dd, J = 17.1,4.7 Hz, 1H), 2.13-1.93 (dd, J= 17.1, 6.1 Hz, 1H), 1.83-1.66 (ddt, J = 12.7, 7.9,3.6 Hz, 1H), 1.69-1.47 (dt, J = 13.2, 6.4 Hz, 1H).MS(ESI)m/z :[(M+1)+,117.1],

The synthetic route of 50607-30-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Shanghai Institute of Materia Medica, Chinese Academy of Sciences; Zhe Jiang Jutai Pharmaceutical Co., Ltd; YANG, Yushe; XUE, Tao; DING, Shi; GUO, Bin; EP2947085; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

14813-01-5, 1-Benzylpiperidin-3-ol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

14813-01-5, To a mixture of 0.50 g (2.62 mmol) of rac-2 and 1 ml of dry pyridine 0.57 ml (3.50 mmol) of butanoic anhydride was added at 0 C under nitrogen. The resulting mixture was stirred over night at room temperature. The reaction mixture was diluted with dichloromethane and then extracted with a saturated sodium carbonate solution (2 x 4 ml) and with 4 ml of a saturated sodium chloride solution. The organic phase was dried with sodium sulfate and then concentrated at reduced pressure to give 0.65 g (2.49 mmol) of rac-5 as a pale yellow oil (95% yield). 1H NMR (300 MHz,CDCl3, d ppm): 0.98 (t, 3H, J = 5.9 Hz); 1.43-1.45 (m, 1H); 1.63-1.90 (m, 3H); 2.31-2.40 (m, 4H); 2.46 (m, 2H), 2.67-2.83 (m,2H); 3.58-3.64 (m, 2H); 4.85-4.89 (m, 1H); 7.22-7.31 (m, 5H); TLC Rf = 0.60.

14813-01-5 1-Benzylpiperidin-3-ol 85773, apiperidines compound, is more and more widely used in various fields.

Reference：
Article; Tofani, Giorgio; Petri, Antonella; Piccolo, Oreste; Tetrahedron Asymmetry; vol. 26; 12-13; (2015); p. 638 – 643;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

63921-23-3, 1-Phenylpiperidin-4-amine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

This example illustrates the preparation of (1-benzyl-piperidin-4-yl)-carbamic acid 2-[7-(4-fluoro-phenoxy)-2,5-dioxo-1,2,3,5-tetrahydro-benzo[e][1,4]diazepin-4-yl]-3-methyl-butyl ester. Alcohol 63 was obtained according to steps a-e described in Example 21. Alcohol 63 (0.11 g, 0.3 mmol) in DCM (1 mL) was treated with p-nitrophenylchloroformate (0.12 g, 0.6 mmol.) and 4-methylmorpholine (0.12 g, 1.2 mmol) for 3 h at 0 C., then the reaction was quenched with sodium bicarbonate and extracted with EtOAc. The organic layer was washed with sodium bicarbonate and brine, dried and concentrated to yield 0.15 g carbonate 69, which was allowed to react with 4-amino-1-benylpiperidine to yield the title compound.

63921-23-3, As the paragraph descriping shows that 63921-23-3 is playing an increasingly important role.

Reference：
Patent; Amgen Inc.; US2006/199796; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem