Day: March 25, 2022

534595-51-2, 1-Boc-4-(isopropylamino)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 10; N-Isopropyl-N-piperidin-4-yl-3-trifluoromethylbenzenesulfonamide (19); [0258] NaB(OAc)3H (14 g, 66 mmol, Aldrich) was added to a mixture of compound 14 (10 g, 50 mmol, Aldrich), compound 15 (3 g, 52.5 mmol, Aldrich), molecular sieves (4A beads, 2Og, Aldrich) in DCE (200 ml) at 0 0C. The resulting mixture was stirred at room temperature for 24 hours. The reaction mixture was quenched with MeOH (2ml), filtered over celite, washed with water, 2N NaOH and concentrated under vacuum to afford crude compound 16 as a colorless oil. Compound 17 (12 g, 49 mmol, Aldrich) was added to a mixture of the above crude compound 16, TEA (10 ml) and DCM (10 ml) at room temperature. The resulting mixture was heated and stirred at 37 0C for 2 days. The reaction mixture was then cooled to room temperature, washed with water (10 ml), brine, concentrated and purified by column (silica gel, EtOAc/hexanes 3/7) to obtain compound 18 as a sticky oil (10 g, yield 45% in two steps), which was dissolved in 100 ml of 1,4-dioxane. HCl (10 ml, concentrated aq.) was added to the 1,4-dioxane solution at room temperature. The resulting mixture was stirred at room temperature for 48 hours, and concentrated under vacuum. The residue was washed with ethyl ether, and dried to obtain the title compound 19 as HCl-salt, which was suspended in EtOAc, and neutralized with IN NaOH aq, concentrated and dried under vacuum to give compound 19 as colorless oil (5 g, yield 65%).

534595-51-2, The synthetic route of 534595-51-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; EURO-CELTIQUE S.A.; SHIONOGI & CO., LTD.; WO2007/118854; (2007); 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: Chalcones analogs were synthesized by Claisen-Schmidt condensation reaction using appropriate equimolar amounts of substituted acetophenones and benzaldehydes in MeOH. NaOH was dissolved in the least amount of water and added dropwise (3mmol) (Scheme 1). Reactions were stirred overnight. All reactions were monitored by TLC using appropriate solvent or mixture of solvents. When the reaction was complete, the obtained precipitate was filtered, washed with cold methanol and dried under vacuum. The crude products were crystallized from different solvent systems based on their solubility or purified by column chromatography to give pure crystalline compounds., 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; Elkhalifa, Dana; Siddique, Abu Bakar; Qusa, Mohammed; Cyprian, Farhan S.; El Sayed, Khalid; Alali, Feras; Al Moustafa, Ala-Eddin; Khalil, Ashraf; European Journal of Medicinal Chemistry; vol. 187; (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.236406-22-7,1-Boc-4-(Aminomethyl)-4-methylpiperidine,as a common compound, the synthetic route is as follows.

Step 4. Synthesis of 4-benzyloxycarbonylaminomethyl-1-t-butoxycarbonyl-4-methylpiperidine To 6 ml of a tetrahydrofuran solution of 4-aminomethyl-1-t-butoxycarbonyl-4-methylpiperidine, obtained by Step 3, 1 ml of diisopropylehtylamine and 0.3 ml of benzyloxycarbonyl chloride were added successively, followed by stirring for 1 hour at the same temperature. The reaction mixture was diluted with ethyl acetate, washed successively with water and brine, and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and 324 mg of the crude title compound was obtained by purifying the resulting residue by silica gel column chromatography (eluding solvent: hexane/ethyl acetate=5/1~2/1)., 236406-22-7

236406-22-7 1-Boc-4-(Aminomethyl)-4-methylpiperidine 23282898, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Banyu Pharmaceutical Co Ltd; US6140333; (2000); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

39514-19-7, Ethyl 1-benzyl-3-oxopiperidine-4-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 3 Alternative synthesis of (3R,37?,4 ‘S)-l’-(6-amino-5-fluoropyrimidin-4-yl)-3-((3-chloro-5- (trifluoromethyl) phenyl)amino)-2-oxo- [ 1 ,3 ‘-bipiperidine] -4 ‘-carboxamide. [0101] In addition to the methods described in Example 2, (3R,3’R,4’S)- -(6-amino-5- fluoropyrimidin-4-yl)-3-((3-chloro-5-(trifluoromethyl) phenyl)amino)-2-oxo-[ 1 ,3 ‘-bipiperidine] – 4’-carboxamide (compound 1-1) was also synthesized according to Scheme 6. Scheme 6 3-1 3-2 [0102] 1-tert- utyl 4-ethyl 3-oxopiperidine-l,4-dicarboxylate 3-2. To a solution of 3-1 (5.0 kg, 19.1 mol, 1.0 equiv) in EtOH (50 L) under N2 was added (Boc)20 (4.2 kg, 19.1 mol, 1.0 equiv), Et3N (1.9 kg, 19.1 mol, 1.0 equiv) and 10percent Pd(OH)2/C (250 g, 10percentw/w). After evacuated and refilled with hydrogenation three times, the mixture was stirred under 1 atm of hydrogen at 50 °C for 15 hr. LC-MS indicated completely consumption of 3-1. After the mixture was cooled to ambient temperature, the catalyst was filtered through a layer of celite and washed with EtOH (2.5 L). The filtrate was concentrated in vacuo to afford crude 3-2 (5.2 kg) as an oil, which was used in next step without further purification.

39514-19-7, 39514-19-7 Ethyl 1-benzyl-3-oxopiperidine-4-carboxylate 419705, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; BIOGEN IDEC MA INC.; SUNESIS PHARMACEUTICALS, INC.; HOPKINS, Brian T.; CONLON, Patrick; CHAN, Timothy R.; JENKINS, Tracy J.; CAI, Xiongwei; HUMORA, Michael; SHI, Xianglin; MILLER, Ross A.; THOMPSON, Andrew; WO2013/185084; (2013); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

161975-39-9, tert-Butyl 4-(((methylsulfonyl)oxy)methyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-(cyanomethyl)piperidine-1-carboxylate tert-Butyl 4-{[(methylsulfonyl)oxy]methyl}piperidine-1-carboxylate (15.3 g) was dissolved in ethanol (80 mL), water (20 mL) and sodium cyanide (4.0 g, 80 mmol) were added, and stirring was conducted at 80 C. for 24 hours. Ethanol was distilled off, water and ethyl acetate were added, and then the resultant mixture was subject to Celite filtration, followed by extraction with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous sodium sulfate and concentrated under a reduced pressure, and the obtained residue was purified by using silica gel column chromatography (hexane:ethyl acetate=3:1?2:1) to give tert-butyl 4-(cyanomethyl)piperidine-1-carboxylate (6.87 g, 77%, 3 steps) as a white solid. 1H-NMR (CDCl3) delta: 1.21-1.31 (2H, m), 1.46 (9H, s), 1.78-1.86 (3H, m), 2.31 (2H, d, J=6.4 Hz), 2.64-2.78 (2H, m), 4.07-4.21 (2H, m)., 161975-39-9

The synthetic route of 161975-39-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; KOWA CO., LTD.; Morimoto, Toshiharu; Koshizawa, Tomoaki; Watanabe, Gen; Ohgiya, Tadaaki; Yamasaki, Nao; Inoue, Noriyuki; US2013/102621; (2013); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

19099-93-5, 1-Cbz-Piperidin-4-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

490 g of ammonium carbonate and 70 g of potassium cyanide were added to the reaction flask,700 mL of water and 700 mL of ethanol were added. Finally, 100 g of 1-benzyloxycarbonyl-4-piperidone was added, heated to 60 C, and reacted till the inorganic salt dissolves completely. After a period of time there will be a lot of crystals appear, reacted for 24 hours, and cooled to room temperature. The reaction solution was filtered off and the cake was washed with 1000 mL of water. The filter cake was then added to a 2000 mL mixture of ethanol and water (V ethanol: V = 4: 1), heated to 50C after slow cooling, followed by recrystallization to give 130 g of compound 5.

19099-93-5, The synthetic route of 19099-93-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Henan Normal University; Mao Longfei; Jia Shuhong; Li Wei; Wu Doucan; Dong Wenpei; Shen Jiaxuan; Jiang Tao; Xu Guiqing; Jiang Yuqin; (9 pag.)CN105017252; (2017); B;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.768-66-1,2,2,6,6-Tetramethylpiperidine,as a common compound, the synthetic route is as follows.,768-66-1

To a 1 liter four-necked round bottom flask equipped with a mechanical stirrer, a reflux condenser, a thermometer, a funnel and a septum are added 80 g of water, 20 g K2CO3 (99%; 0,1448 mol), 10 g 2,2,6,6-tetramethylpiperidine (99%; 7,079·10-2 mol) and 100 g toluene. Then, a solution of 15,34 g of peracetic acid (7,06·10-2 mol) in 80 g water is added slowly to the 1 liter flask while stirring vigorously (with a slightly exothermic reaction) and the flask is placed in a water bath at room temperature. After the addition is complete, the reaction medium is stirred at room temperature overnight and the organic phase becomes red due to the formation of 2,2,6,6-tetramethylpiperidine-1-oxide (TEMPO).

As the paragraph descriping shows that 768-66-1 is playing an increasingly important role.

Reference：
Patent; Detrembleur, Christophe; Gross, Thomas; Meyer, Rolf-Volker; US2003/236368; (2003); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

280774-03-0, (1-Isopropylpiperidin-4-yl)methanol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To the product from step 1 Example 139 (115 mg, 0.55 mmol) in DMSO (5 mL) was added (1-isopropanol-piperidin-4-yl)methanol (130 mg, 0.83 mmol) and 1M KtOBu (1.1 mL, 1.1 mmol). After overnight stirring at 100 C., the reaction was diluted with dichloromethane, washed with water/brine several times, dried over sodium sulfate, and concentrated. The product was purified by prep TLC plates to obtain 64 mg (35%); Mp 188-191 C.; MS m/z 329 (M+H).

280774-03-0, The synthetic route of 280774-03-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Cephalon, Inc.; US2008/27041; (2008); A1;,
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 l-chloro-4-nitrobenzene (23) (2.37 g, 15.0 mmol), alcohol 22 (1.94 g, 15.0 mmol), and DMSO (25 mL) was treated portionwise with NaH (60% in mineral oil, 660 mg, 16.5 mmol) at 40 0C. The mixture was stirred at 70 0C for 3 h, poured into water (15O mL), and extracted with Et2O (5 x 10O mL). The combined organic fractions were washed with water (250 mL) and brine (250 mL), dried (MgSQ4), and the solvent was removed in vacuo. The resulting solid was recrystallized from Et2O to give 24 (3.12 g, 83%) as yellow needles. 1H NMR (300 MHz, CDCl3): delta = 1.36-1.56 (m, 2 H, 3-Hax, 5-Hax), 1.75-1.91 (m, 3 H, 3-Heq, 4-H, 5-Heq), 1.98 (dt, J= 11.9, 1.9 Hz, 2 H, 2-Hax, 6-Hax), 2.30 (s, 3 H, NMe), 2.85-2.98 (m, 2 H, 2-Heq, 6-Heq), 3.90 (d, J= 5.8 Hz, 2 H, OCH2), 6.94 (me, 2 H, 2′-H, 6′-H), 8.19 Cm0, 2 H, 3′-H, 5′-H) ppm. – 13C NMR (50.3 MHz, CDCl3): 6 = 28.9 (C-3, C-5), 35.1 (C-4), 46.4 (NMe), 55.3 (C-2, C-6), 73.3 (OCH2), 114.3 (C-21, C-6′), 125.8 (C-3′, C-5′), 141.3 (C-41), 164.1 (C-I’) ppm. -MS (70 eV, EI): m/z (%) = 250 (79) [M]+, 249 (100) [M-H]+. – Ci3H]8N2O3 (250.29): calcd. C 62.38, H 7.25; found C 62.25, H 7.40., 20691-89-8

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

Reference：
Patent; SYNTARGA B.V.; GEORG-AUGUST-UNIVERSITAet GOeTTINGEN STIFTUNG OeFFENTLICHEN RECHTS (OHNE BEREICH HUMANMEDIZIN); WO2007/89149; (2007); 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.5810-56-0,4-Acetamidopiperidine,as a common compound, the synthetic route is as follows.

5810-56-0, Following the procedure of Example 74 using 5,5-Dioxo-2-(4-nitrobenzoxy-carbonylamino)dibenzothiophene (Example 24) and the appropriate amine the following compounds were prepared.

The synthetic route of 5810-56-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Block, Michael Howard; Donald, Craig Samuel; Brittain, David Robert; Foote, Kevin Michael; US2003/225097; (2003); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem