157327-41-8 | Heterocyclic Building Blocks-piperidine

Some tips on 157327-41-8

As the paragraph descriping shows that 157327-41-8 is playing an increasingly important role.

157327-41-8, 1-Boc-3-[(Dimethylamino)methylene]-4-oxopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a 250 ml round bottom flask charged with anhydrous EtOH (50 ml) under nitrogen at 0 0C is added sodium hydride (60% in mineral oil, 2.4 g, 60 mmol, 4.0 eq.). The mixture is stirred at rt for10 min, and then 4-cyclobutyl-piperazine-l-carboxamidine from step 2 (about 15 mmol) is added, followed by the addition of terf-butyl-3-[(dimethylamino)methylene]-4-oxo-l-piperidinecarboxylate(3.81 g, 15 mmol, 1.0 eq.). The resulting mixture is stirred at 75 0C for 16 h. The solvent is evaporated under reduced pressure, and the residue is taken up in DCM (100 ml). The organics are washed with water and brine, dried (Na2SO4), and concentrated. The residue is purified through silica gel chromatography (EA / 4% TEA) to give the title compound as white solid. 1H NMR (300 MHz, CDCl3) delta 8.05 (IH, s), 4.41 (2H, s), 3.81 (4H, t), 3.67 (2H, t), 2.66-2.78 (3H, m), 2.36 (4H, t),1.62-2.10 (6H, m), 1.48 (9H, s)., 157327-41-8

As the paragraph descriping shows that 157327-41-8 is playing an increasingly important role.

Reference£º
Patent; NEUROGEN CORPORATION; WO2007/146122; (2007); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

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The synthetic route of 157327-41-8 has been constantly updated, and we look forward to future research findings.

157327-41-8, 1-Boc-3-[(Dimethylamino)methylene]-4-oxopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2,2-Dimethyl-1 -(2-(methylsulfonyl)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)- yl)propan-1-one[00138]To a solution of crude fe/f-butyl 3-((dimethylamino)methylene)-4-oxopiperidine- 1 -carboxylate (see Preparation 2) (10.70 g, 42.1 mmol) and methyl carbamimidothioate hemisulfate (14.05 g, 50.5 mmol, 1 .2 eq.) in DMSO (200 ml_) is added 4M HCI solution in dioxane (1 .1 ml_, 4.2 mmol, 0.1 eq.). The mixture is heated at 130 C overnight. After cooling down to room temperature EtOAc (330 ml_) and DEE (660 ml_) are added, and the organic layer is washed with water (1 L), brine (3 x, each 1 L), dried over Na2S04, and concentrated in vacuo. Purification by flash column chromatography (silica, gradient 100% heptane to 40% EtOAc/heptane) affords 4.6 g (35%, purity 90%) of theintermediate product fe/f-butyl 2-(methylthio)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5/-/)- carboxylate., 157327-41-8

The synthetic route of 157327-41-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERZ PHARMA GMBH & CO. KGAA; ABEL, Ulrich; KRUEGER, Bjoern; KUBAS, Holger; MEYER, Udo; ZEMRIBO, Ronalds; SMITS, Gints; WO2012/85167; (2012); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

Brief introduction of 157327-41-8

157327-41-8, 157327-41-8 1-Boc-3-[(Dimethylamino)methylene]-4-oxopiperidine 53395404, apiperidines compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.157327-41-8,1-Boc-3-[(Dimethylamino)methylene]-4-oxopiperidine,as a common compound, the synthetic route is as follows.

Example 21ferf-Butyl 2-((3-cyanophenyl)amino)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)- carboxylate[00164]fe/f-Butyl 3-((dimethylamino)methylene)-4-oxopiperidine-1 -carboxylate (1 .1 g, 4.33 mmol) is dissolved in abs. EtOH (20 mL), and 1 -(3-cyanophenyl)guanidine (0.46 g, 2.90 mmol) is added. The mixture is heated at 100 C for 16 h, then cooled and evaporated to dryness. Purification of the residue by flash column chromatography provides the title compound (0.62 g, 60%) as a yellow solid.1H NMR (CDCI3), deltaEta, 1 .49 (s, 9H), 2.85 (t, 2H), 3.73 (t, 2H), 4.51 (s, 2H), 7.24 – 7.41 (m, 3H), 7.62 – 7.66 (m, 1 H), 8.20 (s, 1 H), 8.24 (s, 1 H)LC/MS (M+H)+ = 352

157327-41-8, 157327-41-8 1-Boc-3-[(Dimethylamino)methylene]-4-oxopiperidine 53395404, apiperidines compound, is more and more widely used in various fields.

Brief introduction of 157327-41-8

157327-41-8 1-Boc-3-[(Dimethylamino)methylene]-4-oxopiperidine 53395404, apiperidines compound, is more and more widely used in various.

A mixture of 1-tert-butoxycarbonylpiperidine-4-one and N,N-dimethylformamide dimethylacetal was stirred for 6 hours heated to reflux to give 1-tert-butoxycarbonyl-3-[(dimethylamino)methylene]piperidine-4-one. A mixture of the obtained 1-tert-butoxycarbonyl-3-[(dimethylamino)methylene] piperidine-4-one, 2-hydrazinoethanol and MeOH was stirred for two hours heated to reflux to give a mixture of 2-(5-tert-butoxycarbonyl-4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridine-2-yl)ethanol and 2-(5-tert-butoxycarbonyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-1-yl)ethanol. A mixture of the obtained mixture, 4M HCl-EtOAc solution and EtOH was stirred for two hours at room temperature to give a mixture of 2-(4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridine-2-yl)ethanol dihydrochloride and 2-(4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c] pyridine-1-yl)ethanol dihydrochloride. ES-MS(+) : 168, 157327-41-8

157327-41-8 1-Boc-3-[(Dimethylamino)methylene]-4-oxopiperidine 53395404, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; Astellas Pharma Inc.; EP1806347; (2007); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

Some tips on 157327-41-8

157327-41-8, As the paragraph descriping shows that 157327-41-8 is playing an increasingly important role.

157327-41-8, 1-Boc-3-[(Dimethylamino)methylene]-4-oxopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

N-tert-butoxycarbonyl-4-piperidone (58, 5.8 g, 31.4 mmol) wasdissolved in N,N-dimethylformamide dimethyl acetal (45.0 mL),and the solution was heated under reflux for 1.5 h and concentrated.The residue was triturated with hexane, filtered, andwashed with hexane to give 59 as a yellow powder (5.1 g, 63.8%):mp 135e136 C; To a solution of 59 (5.0 g, 20.8 mmol) in EtOH(200.0 mL) were added guanidine carbonate (15.0 g, 84.0 mmol)and sodium acetate (13.7 g, 167.0 mmol), and the solution washeated under reflux for 48 h. The reaction mixturewas filtered, andthe insoluble material was extracted with CHCl3 and washed withwater. The organic layer was dried over anhydrous MgSO4 andevaporated. The resultant solid was triturated with 2-propanol,filtered, and washed with 2-propanol and Et2O to give a colorlesspowder. It was dissolved in TFA (50.0 mL) at 0 C, and the solutionwas stirred at room temperature for 1 h and concentrated. Theresidue was dissolved in 2-propanol and treated with concentrated HCl (4.0 mL). The precipitated solidwas filtered andwashed with 2-propanol and Et2O to give 60a (4.2 g, 81.6%) as a colorless powder: Mp 258e260 C; Compound 57g was obtained from 60a in thesame way as 57f.

157327-41-8, As the paragraph descriping shows that 157327-41-8 is playing an increasingly important role.

Reference£º
Article; Sun, Hao-Peng; Jia, Jian-Min; Jiang, Fen; Xu, Xiao-Li; Liu, Fang; Guo, Xiao-Ke; Cherfaoui, Bahidja; Huang, Hao-Ze; Pan, Yang; You, Qi-Dong; European Journal of Medicinal Chemistry; vol. 79; (2014); p. 399 – 412;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem