Day: March 17, 2022

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.

Step 2:Oxalyl chloride (9.4 g; 74 mmol) is dissolved in DCM (55 ml) and cooled to -78C. DMSO (7.5ml; 106 mmol) is added dropwise and the mixture is stirred for 15 min at -78C. In a separateflask, 4a3 (13 g; 53 mmol) is dissolved in DCM (55 ml) and added dropwise to the first flask viacannula. Once the addition is finished, the mixture is stirred at -55C for 15 min. The reactionmixture is cooled to -78C and a solution of triethylamine (22 ml; 158 mmol) in DCM (28 ml) isadded dropwise to the reation mixture via cannula. The mixture is stirred for 1 hat -78C then15 min at ooc and 30 min at RT. The reaction is neutralized with 11 ml of AcOH and dilutedwith 100 ml of DCM and 100 ml of water. The layers are separated and the aqueous layer isextracted with DCM (2 x 100 ml). The combined organic layers are washed with brine, driedover MgS04, filtered and concentrated. Purification by Combiflash (120 g column, 0-50%EtOAc/Hex) gives 4a4., 122860-33-7

As the paragraph descriping shows that 122860-33-7 is playing an increasingly important role.

Reference：
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; THIBEAULT, Carl; RANCOURT, Jean; BEAULIEU, Pierre L.; DECOR, Anne; GRAND-MAITRE, Chantal; KUHN, Cyrille; VILLEMURE, Elisia; LEBLANC, Melissa; LACOSTE, Jean-Eric; MOREAU, Benoit; JOLICOEUR, Eric; SURPRENANT, Simon; HUCKE, Oliver; WO2014/70976; (2014); 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: 1-(4-(1H-imidazol-1-yl)phenyl)ethan-1-one (1) (0.316 g, 0.0017 mol) and appropriate 4-substitutedbenzaldehydes (2a-2o) derivatives (0.0017 mol) in methanol were stirred for 10 h in the presence ofpotassium hydroxide. The precipitated product was washed with water, dried, and recrystallizedfrom ethanol., 10338-57-5

10338-57-5 4-(Piperidin-1-yl)benzaldehyde 291354, apiperidines compound, is more and more widely used in various fields.

Reference：
Article; Osmaniye, Derya; Avu?o Glu, Bet l Kaya; Sa gl?k, Beg m Nurpelin; Levent, Serkan; Acar evik, Ulviye; Atl?, Zlem; Zkay, Yusuf; Kaplanc?kl?, Zafer As?m; Molecules; vol. 23; 4; (2018);,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1062580-52-2,(3R,4R)-1-Benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride,as a common compound, the synthetic route is as follows.

(3R,4R)-N,4-dimethyl-1-(phenylmethyl)-3-piperidinamine hydrochloride 234g (0.79 mol), 3000 ml of purified water was added to a 5 L reaction flask.177 g (1.61 mol) of potassium carbonate was added thereto with stirring, and then 150 g (0.79 mol) of 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine was added thereto, and the mixture was heated to 98-102 C to stir the reaction.After reacting for 10 h, the temperature was lowered to 20-25 C, stirred for 4 h, filtered, and washed with 750 ml of purified water.Drying at 60-65 C to give an off-white solid ((3R,4R)-1-benzyl-4-methyl-piperidin-3-yl)-methyl-(2-Chloro-7H-pyrido[2,3-d]pyrimidin-4-yl)amine 276.1 g, yield 93.6%., 1062580-52-2

1062580-52-2 (3R,4R)-1-Benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride 45790119, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Hunan Tiandi Hengyi Pharmaceutical Co., Ltd.; Wang Hengxin; Zeng Weiqiang; Cheng Xueqing; (6 pag.)CN108640923; (2018); 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.53617-36-0,1-Methyl-4-(piperidin-4-yl)piperazine,as a common compound, the synthetic route is as follows.

6m) (R)-1-(8-methyl-2,3-dihydro-1,4-benzodioxin-6-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylate A solution of 80 mg (0.16 mmol) (R)-1-carboxy-2-(8-methyl-2,3-dihydro-1,4-benzodioxin-6-yl)-ethyl 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylate, 51 mg (0.16 mmol) TBTU, 42 muL (0.30 mmol) triethylamine and 29 mg (0.16 mmol) 1-methyl-4-piperidin-4-yl-piperazine in 1 mL DMF was stirred overnight at RT. The reaction mixture was purified by HPLC, the fractions containing the product were combined and lyophilised. Yield: 60 mg (57percent of theory) ESI-MS: (M+H)+=675 retention time (HPLC): 5.0 min (method A), 53617-36-0

The synthetic route of 53617-36-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Boehringer Ingelheim International GmbH; US2005/256099; (2005); 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.141943-04-6,1-Benzylpiperidine-3-carboxylic acid,as a common compound, the synthetic route is as follows.

Triethylamine (0.38 ml, 2.73 mmol) and diphenylphosphoryl azide (0.692 g, 2.52 mmol) were added to a solution of 1-benzyl-3-piperidinecarboxylic acid (0.501 g, 2.28 mmol) in toluene (10 ml), and the resulting mixture was stirred for 2 hours with heating under reflux. The solvent was distilled off under reduced pressure and a solution of the resulting residue in tert-butanol (10 ml) was stirred for 4 hours with heating under reflux. The solvent was distilled off under reduced pressure and a 1N-aqueous sodium hydroxide solution was added to the residue, followed by extraction with ethyl acetate (three times). The extract solution was dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure and the residue was purified by a silica gel chromatography (eluent: hexane/ethyl acetate = 5/1) to obtain tert-butyl 1-benzyl-3-piperidinylcarbamate (0.475 g, 72%).

141943-04-6, The synthetic route of 141943-04-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Sumitomo Pharmaceuticals Company, Limited; EP1403255; (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.10315-06-7,Methyl 1-benzylpiperidine-4-carboxylate,as a common compound, the synthetic route is as follows.

B. Synthesis of l-benzylpiperidine-4-carboxylic acid hydrochloride; [0096] Methyl l-benzylpiperidine-4-carboxylate (11.6 g, 50 mmol) was refluxed with 6N HCl (140ml) overnight. The reaction mixture was concentrated to remove water. The residue compound (l-benzylpiperidine-4-carboxylic acid hydrochloride, 12 g) was obtained by heating and drying under vacuum in the oven.

10315-06-7, 10315-06-7 Methyl 1-benzylpiperidine-4-carboxylate 11436222, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; NEUROMED PHARMACEUTICALS LTD.; WO2008/31227; (2008); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

72551-53-2, Ethyl 1-benzylpiperidine-3-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

72551-53-2, A mixture of 2,3-pyridinediamine (321 mg, 2.95 mmol), ethyl l-benzyl-3- piperidinecarboxylate (CAS: 72551-53-2; 850 mg, 2.98 mmol) and polyphosphoric acid (5 mL) was stirred at 180 C for 16 h. Then the mixture was cooled to rt. Water was added and the mixture was stirred at 50 C until it became homogeneous. This mixture was then cooled to room temperature and aqueous NaOH (3N) was added until pH = 8 was reached. Then EtOAc was added and the organic layer was separated, dried over Na2S04, filtered and the filtrate was evaporated in vacuo. The resultant oil was purified by flash column chromatography (silica; 7M solution of ammonia in MeOH in EtOAc 0/100 to 10/90). The desired fractions were concentrated in vacuo to yield intermediate 29 as yellow oil (430 mg, 50% yield).

As the paragraph descriping shows that 72551-53-2 is playing an increasingly important role.

Reference：
Patent; JANSSEN PHARMACEUTICA NV; BARTOLOME-NEBREDA, Jose, Manuel; TRABANCO-SUAREZ, Andres, Avelino; MARTINEZ VITURRO, Carlos, Manuel; TRESADERN, Gary, John; ALCAZAR-VACA, Manuel, Jesus; (126 pag.)WO2018/109198; (2018); 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 (80 mg, 0.420 mmol) was dissolved in dichloromethane (4 ml_). Then, triethylamine (0.1 17 ml_, 0.839 mmol) was added followed by 4-[(trifluoromethyl)oxy]benzenesulfonyl chloride (0.078 ml_, 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-({4-[(trifluoromethyl)oxy]- phenyl}sulfonyl)-2,7-diazaspiro[4.5]decan-1 -one (93 mg, 0.241 mmol, 57% yield) as a white solid. 1 H NMR (400 MHz, DMSO-d6) delta ppm 1.34 – 1 .47 (m, 2 H) 1.51 – 1 .64 (m, 1 H) 1.66 – 1.73 (m, 1 H) 1.90 – 1 .99 (m, 1 H) 2.00 – 2.08 (m, 1 H) 2.18 – 2.26 (m, 2 H) 3.19 (t, J=6.91 Hz, 2 H) 3.30 (s, 1 H) 3.62 (d, J=1 1 .35 Hz, 1 H) 7.64 (dd, J=8.85, 0.90 Hz, 2 H) 7.76 (s, 1 H) 7.86 – 7.90 (m, 2 H). MS ES+ve m/z 379 (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.180307-56-6,tert-Butyl 4-vinylpiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

To the mixture of Zn (4.64 g, 70.99 mmol) in dioxane (50 mL) under N 2 atmosphere was added tert-butyl 4-vinylpiperidine-1-carboxylate (5.0 g, 23.66 mmol) at 20C. Then CCl 3COCl (6.45 g, 35.49 mmol) was added at 20C. The mixture was stirred at 20C for 12 hours. To the reaction mixture was added aq. NaHCO 3 (50 mL) at 0C. Then the mixture was extracted with EA (50 mL5) and the combine organic phase was dried over anhydrous Na 2SO 4 and concentrated. The residue was purified by column chromatography (SiO 2, PE/EA = 50/1 to 20/1). Tert-butyl 4- (2, 2-dichloro-3-oxocyclobutyl) piperidine-1-carboxylate (3.0 g) was obtained. 1H NMR (400 MHz, CDCl 3) delta ppm: 4.05 -4.21 (m, 2 H) 3.04 -3.27 (m, 2 H) 2.77 (br, 2 H) 2.60 (q, J = 10.4 Hz, 1H) 2.03 -2.10 (m, 1H) 1.84 -1.97 (m, 1H) 1.52 -1.63 (m, 1H) 1.46 (s, 9 H) 1.16 -1.41 (m, 3 H)., 180307-56-6

As the paragraph descriping shows that 180307-56-6 is playing an increasingly important role.

Reference：
Patent; BEIGENE, LTD.; GUO, Yunhang; XUE, Hai; WANG, Zhiwei; SUN, Hanzi; (493 pag.)WO2019/210828; (2019); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

4629-78-1, 3-Methylpiperidin-4-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

methyl 6-r(1-methylethyl)sulfonyll-3-r(3-methyl-4-oxo-1-piperidinyl)methyll-2-r3- (trifluoromethyl)phenyll-4-quinolinecarboxylateA suspension of methyl 3-methyl-6-[(1-methylethyl)sulfonyl]-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxylate (1.25 g, 2.77 mmol), V-bromosuccinimide (0.641 g, 3.60 mmol), and benzoyl peroxide (0.067 g, 0.277 mmol) in carbon tetrachloride (27 ml) was heated to 100C for 19 h. The mixture was cooled to room temperature, and the solvent was removed under reduced pressure. The residue was suspended in acetonitrile (20 mL), and 3-methyl-piperidin-4-one hydrochloride (0.497 g, 3.32 mmol) and A/, V-diisopropylethylamine (1.209 mL, 6.92 mmol) were added. The mixture was stirred at room temperature for 22 h. The solvent was removed under reduced pressure, and the residue was diluted with 10% Na2C03. The aqueous mixture was extracted with ethyl acetate (2 x 25 mL). The combined organic extracts were dried over Na2S04, filtered, and concentrated in vacuo. The crude residue was loaded onto florisil and purified using silica gel chromatography (ISCO, 12 g silica, 5-40% ethyl acetate/hexanes, 12 g silica) to afford methyl 6-[(1-methylethyl)sulfonyl]-3-[(3-methyl-4-oxo-1-piperidinyl)methyl]-2-[3- (trifluoromethyl)phenyl]-4-quinolinecarboxylate (1.24 g, 76% yield). 1H NMR (400 MHz, DMSO- d6) 58.35 – 8.41 (m, 2H), 8.22 (dd, J = 2.01 , 8.81 Hz, 1 H), 8.03 (s, 1 H), 7.93 (t, J = 8.94 Hz, 2H), 7.75 – 7.82 (m, 1 H), 4.08 (s, 3H), 3.82 (s, 2H), 3.65 (quin, J = 6.74 Hz, 1 H), 2.87 (dd, J = 5.04, 10.07 Hz, 2H), 2.22 – 2.47 (m, 3H), 2.06 (d, J = 13.60 Hz, 1 H), 1.92 – 2.01 (m, 1 H), 1.23 (s, 3H), 1.21 (s, 3H), 0.77 (d, J = 6.55 Hz, 3H); MS (m/z) 563.1 (M+H+)., 4629-78-1

The synthetic route of 4629-78-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXOSMITHKLINE LLC; BROOKS, Carl, A.; CHEUNG, Mui; EIDAM, Hilary, S.; FOX, Ryan, M.; HILFIKER, Mark, A.; MANAS, Eric, S.; YE, Guosen; WO2011/119701; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem