Category: 21168-72-9

21168-72-9, 2-(4-(Aminomethyl)piperidin-1-yl)ethanol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

12 g of 2- (4- (aminomethyl) piperidin-1-yl) ethanol was added to150 ml of N, N-dimethylformamide,Add 18g bromoethane, then add 15g of potassium carbonate,Heated to reflux for 2 hours,Water and ethyl acetate were added, the mixture was extracted and separated, and the organic phase was collected, dried and concentrated. The residue was separated on a silica gel column to obtain 9 g2- (4 – ((ethylamino) methyl) piperidin-1-yl) ethanol., 21168-72-9

As the paragraph descriping shows that 21168-72-9 is playing an increasingly important role.

Reference：
Patent; Hunan Huateng Pharmaceutical Co., Ltd.; Bu Gonggaofamingren; (5 pag.)CN104557672; (2016); 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.21168-72-9,2-(4-(Aminomethyl)piperidin-1-yl)ethanol,as a common compound, the synthetic route is as follows.

(Z)-4-(((1 -Acetyl-6-(methoxycarbonyl)-5-methyl-2-oxoindolin-3-ylidene) (phenyl)methyl)ami no)benzoic acid, trifluoroacetate adduct (Intermediate E) (75 mg,0.128 mmol), and HATU (73 mg, 0.192 mmol) in DMF (2 mL) were stirred at rt for 10 mm thenHunig?s base (179 p1, 1.03 mmol) and 2-(4-(aminomethyl)piperidin-1-yl)ethanol (73.1 mg,0.462 mmol) were added. The mixture was stirred at rt for 3 h and piperidine (127 p1, 1.28mmol) was added. The mixture was stirred at rtfor 18 h. The reaction mixture was partitioned between DCM (25 mL) and saturated aqueous NaHCO3 solution (10 mL). The organic layer was washed with brine (10 mL) and the solvent was evaporated under reduced pressure. The crude product was loaded onto a column of SCX (2 g) in 5% AcOH in MeOH (10 mL). The column was washed with MeOH (10 mL) and the filtrte was discarded. Then the product waseluted with 1% ammonia in MeOH (25 mL). The solvent was evaporated under reduced pressure and the product was purified by flash column chromatography (Si02, 12 g, 0-30% MeOH in DCM, gradient el ution) to afford (Z)-methyl 3-(((4-(((1 -(2-hydroxyethyl)piperidin-4- yl)methyl)carbamoyl)phenyl)am ino)(phenyl) methylene)-5-methyl-2-oxoindoline-6-carboxylate as a light yellow solid (63 mg, 63%); Rt 1.56 mm (Method 1); mlz 569 (M+H) (ES); 1H NMRO: 1.05-1.19 (2H, overlapping m), 1.47 (1H, m), 1.58 (2H, m), 1.81-1.94 (2H, overlapping m), 2.13 (3H, s), 2.28-2.40 (2H, overlapping m), 2.82 (2H, m), 3.07 (2H, t), 3.46 (2H, m), 3.75 (3H, s), 4.34 (1H, s), 5.61 (1H, s), 6.86 (2H, m), 7.36 (1H, s), 7.52 (2H, m), 7.57-7.70 (5H, m), 8.32 (1H, t), 10.88 (1H, s), 12.23 (1H, s).

21168-72-9, 21168-72-9 2-(4-(Aminomethyl)piperidin-1-yl)ethanol 7330476, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; RESPIVERT LIMITED; WALTERS, Iain; BIRCH, Louise; COLLINGWOOD, Stephen, Paul; STEVENSON, Christopher, Scott; (110 pag.)WO2017/153748; (2017); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

21168-72-9, 2-(4-(Aminomethyl)piperidin-1-yl)ethanol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The general synthesis of compound D-9 is illustrated in Scheme 4. The carboxylic acid group of intermediate D-1 is converted to ethyl ester. The reactionsof tert-butyl acetate substitution with K2C03 and tert-butyl eater hydrolysis with TFA are followed to afford acetic acid intermediate D-4. The intermediate D-4 is chlorinated with oxalyl chloride and DMF and coupled with 3-aminoisonicotinamide to afford the amide intermediate D-6. Subsequent cyclization with NaOtBu and hydrolysis with NaOH lead to intermediate D-8. This is followed by amide coupling reaction with HATU, which leads to amide compound D-9.

21168-72-9, The synthetic route of 21168-72-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; DONG-A SOCIO HOLDINGS CO., LTD.; KIM, Myeong-seop; PARK, Taesun; YOON, Taeyoung; YANG, Seung Min; KIM, Hae-Sun; KIM, Jun Gyu; (285 pag.)WO2016/68580; (2016); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

21168-72-9, 2-(4-(Aminomethyl)piperidin-1-yl)ethanol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To the solution of compound 2-(4-(aminomethyl)piperidin-1-yl)ethanol (150 mg, 0.95 mmol) and compound 6-chloro-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazine (200 mg, 0.64 mmol) in 3 mL DMSO was added DIEA (0.3 mL, 1.37 mmol) and 10 mg CsF, the solvent was stirred for 5 h at 120 C., Then the mixture was purified by HPLC to afford the compound 2-(4-(((3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-yl)amino)methyl)cyclohexyl)ethanol (34 mg, 8.2%) as a brown solid. (0522) 1H-NMR (CDCl3/400 MHz): delta 8.61 (s, 1H), 8.20-8.25 (m, 1H), 7.95-8.05 (m, 2H), 7.66 (t, J=4.4 Hz, 1H), 7.21-7.28 (m, 1H), 3.80-3.90 (m, 2H), 3.62-3.75 (m, 2H), 3.37 (d, J=6.4 Hz, 2H), 3.21 (t, J=5.2 Hz, 2H), 2.91-3.09 (m, 2H), 2.10 (d, J=14.0 Hz, 2H), 1.51-1.69 (m, 2H). MS (ES+, m/z): (M+H)+: 435.5.

21168-72-9, 21168-72-9 2-(4-(Aminomethyl)piperidin-1-yl)ethanol 7330476, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Tolero Pharmaceuticals, Inc.; Xu, Yong; Brenning, Benjamin Gary; Kultgen, Steven G.; Liu, Xiaohui; Saunders, Michael; Ho, Koc-Kan; (119 pag.)US9416132; (2016); B2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

21168-72-9, 2-(4-(Aminomethyl)piperidin-1-yl)ethanol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To 2-(4-Aminomethyl-piperidin-l-yl)-ethanol (0.5 mmol) in tetrahydrofuran (2 mL) at room temperature are added cyclohexylmethylaldehyde (0.6 mmol)) and anhydrous magnesium sulfate (60 mg). After stirring for 1.5h at room temperature, sodium borohydride (0.5 mmol) is added and the mixture is then stirred for a further 2h. Water (3 mL) is added to the mixture and stirring resumed for 10 min. Additional water is added (1 mL) and the mixture is extracted with dichloromethane (10 mL x 3). After being dried over anhydrous magnesium sulfate the solvent is removed under reduced pressure to give the crude product. This material is used in subsequent steps without requiring further purification. [00349] The amine obtained in the previous step (0.26mmol) is added to a solution of 5-chloro-l- methyl-3-tert-Butyl-l,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one (0.13mmol) in t- BuOH (0.5 mL). The reaction is heated in a sealed tube to 1000C for 24h. On complete reaction (monitored by LCMS), the mixture is allowed to cool to room temperature and the solvent is removed under reduced pressure. The final compound is then isolated by preparative HPLC.[00350] Preparative HPLC: Waters XBridge Prep C18 5mum ODB 19mm ID x 100mm L. The method uses MeCN/H2O 35-60% gradients. H2O contains 0.1% Trifluoroacetic acid (TFA).., 21168-72-9

As the paragraph descriping shows that 21168-72-9 is playing an increasingly important role.

Reference：
Patent; Galapagos NV; WO2009/71707; (2009); 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.21168-72-9,2-(4-(Aminomethyl)piperidin-1-yl)ethanol,as a common compound, the synthetic route is as follows.

[00351 ] To the solution of compound 2-(4-(aminomethyl)piperidin-1 – yl)ethanol (150 mg, 0.95 mmol) and compound 6-chloro-3-(3- (trifluoromethoxy)phenyl)imidazo[1 ,2-b]pyridazine (200 mg, 0.64 mmol) in 3 ml_ DMSO was added DIEA (0.3 ml_, 1 .37 mmol) and 10 mg CsF, the solvent was stirred for 5 h at 120 C, Then the mixture was purified by HPLC to afford the compound 2-(4-(((3-(3-(trifluoromethoxy)phenyl)imidazo[1 ,2-b]pyridazin-6- yl)amino)methyl)cyclohexyl)ethanol (34 mg, 8.2 %) as a brown solid. [00352] 1 H-NMR (CDCI3/400 MHz): delta 8.61 (s, 1 H), 8.20 – 8.25 (m, 1 H), 7.95 – 8.05 (m, 2 H), 7.66 (t, J = 4.4 Hz, 1 H), 7.21 – 7.28 (m, 1 H), 3.80 – 3.90 (m, 2 H), 3.62 – 3.75 (m, 2 H), 3.37 (d, J = 6.4 Hz, 2 H), 3.21 (t, J = 5.2 Hz, 2 H), 2.91 – 3.09 (m, 2 H), 2.10 (d, J = 14.0 Hz, 2 H), 1 .51 – 1 .69 (m, 2 H). MS (ES+, m/z): (M+H)+: 435.5.

21168-72-9, The synthetic route of 21168-72-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TOLERO PHARMACEUTICALS, INC.; XU, Yong; BRENNING, Benjamin, Gary; KULTGEN, Steven, G.; LIU, Xiaohui; SAUNDERS, Michael; HO, Koc-Kan; WO2013/13188; (2013); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem