Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.140645-24-5,(S)-3-(Aminomethyl)-1-N-Boc-piperidine,as a common compound, the synthetic route is as follows.

4 (0.30 g, 0.92 mmol) was dissolved in 20 mL of ethanol,(S) -1-Boc-3-aminomethylpiperidine (0.26 g, 1.20 mmol) and DIPEA (0.18 mL, 1.01 mmol)Reflux reaction 48h,Ethyl acetate dissolved, suction filter,Purification by column chromatography [P: E = 1: 1 (V: V)] gave 0.24 g of a pale yellow solid in 51.8% yield., 140645-24-5

The synthetic route of 140645-24-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; China Pharmaceutical University; Lai Yisheng; Zhang Yingyi; Xiao Jianhu; Jin Shuanglong; Li Yuezhen; Zhang Yihua; (31 pag.)CN107043366; (2017); 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.109384-19-2,tert-Butyl 4-hydroxypiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

To the stirred solution of tert- butyl 4-hydroxypiperidine-l-carboxylate (26 g, 130 mmol) in /V, N- dimethyl form amide (100 mL) under nitrogen atmosphere at 0C, sodium hydride (6 g, 149 mmol) was added in portions and reaction mixture was stirred at 0 C for 20 min. 4-fluorobenzonitrile (15 g, 124 mmol) was dissolved in 20 mL of /V,/V-dimethyl form amide and added drop wise at 0 C. The reaction mixture was heated to 25 C and stirred for 16 h, then cooled to 0 C and quenched by adding water (100 mL) drop wise. The product was extracted twice by ethyl acetate (200 mL). The combined ethyl acetate layer was washed with ice cold water (300 mL), dried over anhydrous sodium sulphate and concentrated under reduced pressure to obtain a crude product. The crude product was purified by flash column chromatography using 40% ethyl acetate in hexane as an eluent to obtain tert- butyl 4-(4- cyanophenoxy)piperidine-l-carboxylate (37.2 g, 123 mmol, 99 % yield).

109384-19-2, As the paragraph descriping shows that 109384-19-2 is playing an increasingly important role.

Reference：
Patent; PI INDUSTRIES LTD.; BHUJADE, Paras Raybhan; NAIK, Maruti N; PAWAR, Rajesh; TRIVEDI, Pooja; DENGALE, Rohit Arvind; KULKARNI, Shantanu Ganesh; TEMBHARE, Nitin Ramesh; AUTKAR, Santosh Shridhar; GARG, Ruchi; VENKATESHA, Hagalavadi M; KLAUSENER, Alexander G.M.; (172 pag.)WO2020/70610; (2020); 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.138022-04-5,tert-Butyl methyl(piperidin-4-ylmethyl)carbamate,as a common compound, the synthetic route is as follows.,138022-04-5

Stage (i): tert-Butyl methyl((1-(pyrimidin-4-yl)piperidin-4-yl)methyl)carbamatetert-Butyl methyl(piperidin-4-ylmethyl)carbamate (1.4 mmol, 1.0 eq) and 4-chloropyridine (4.2 mmol, 3.0 eq) were dissolved in 2-propanol (5 ml) and DIPEA (7.0 mmol. 5.0 eq) and refluxed for 16 hours. After monitoring by TLC, the reaction solution was diluted with ethyl acetate and sat. sodium hydrogen carbonate solution and the phases were separated. The aqueous phase was washed with ethyl acetate. The combined organic phases were dried over magnesium sulfate, concentrated under reduced pressure and purified by column chromatography (silica gel, ethyl acetate:ethanol 10:1+ammonia solution). Yield: 51%

138022-04-5 tert-Butyl methyl(piperidin-4-ylmethyl)carbamate 23004743, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; GRUENENTHAL GmbH; US2012/71461; (2012); 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.140645-24-5,(S)-3-(Aminomethyl)-1-N-Boc-piperidine,as a common compound, the synthetic route is as follows.

Compound 10a was prepared from compound 8 in 85% yield as a colorless solid, using a similar approach to that described for 9a. 1H NMR (DMSO-d6) delta 1.16-1.85 (5H, m), 1.32 (9H, s), 2.31-2.78 (2H, m), 2.58 (3H, s), 3.15-3.29 (2H, m), 3.60-3.94 (2H, m), 3.80 (3H, s), 6.78 (1H, t, J = 2.1 Hz), 7.54 (1H, t, J = 2.1 Hz), 7.59-7.67 (1H, m), 7.71-7.76 (1H, m), 7.92 (1H, d, J = 3.7 Hz), 9.44 (1H, s); MS (ESI) m/z 514 [M+H]+.

140645-24-5, As the paragraph descriping shows that 140645-24-5 is playing an increasingly important role.

Reference：
Article; Kunikawa, Shigeki; Tanaka, Akira; Mukoyoshi, Koichiro; Nagashima, Shinya; Tominaga, Hiroaki; Chida, Noboru; Tasaki, Mamoru; Shirai, Fumiyuki; Bioorganic and Medicinal Chemistry; vol. 23; 13; (2015); p. 3269 – 3277;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

180307-56-6, tert-Butyl 4-vinylpiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1-M ethyl-3-nitro-1-nitrosoguanidine (3.00 g, 20.4 mmol) was added in small portions with agitation to a mixture of 5M aqueous NaOH solution (14 ml) and ether (70 ml), cooled to 0 C. The yellow ether layer was decanted into a flask precooled in an ice bath and containing a few KOH pellets for drying. To a solution of olefin 20 (0.20 g, 0.95 mmol) in ether (5 ml) cooled to 0 C. was added Pd(OAc)2 (0.006 g, 0.03 mmol), followed by the ethereal CH2N2 solution in portions (prepared as described above), and the reaction mixture was stirred at rt for 5 hr. It was quenched with AcOH and diluted with saturated aqueous NaHCO3 solution. The product was extracted with CH2Cl2 and the organic layer was dried over Na2SO4. Purification by flash chromatography (CH2Cl2) provided 0.16 g of 21 as a clear liquid.

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

Reference：
Patent; Schering Corporation; US2007/10513; (2007); 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.149554-03-0,tert-Butyl 2-(4-oxopiperidin-1-yl)acetate,as a common compound, the synthetic route is as follows.

A mixture of 45 (2.1 g, 10 mmol), BOC-piperidone (3.4 g, 17 [MMOL)] and KOH (0.28 g, 5 [MMOL)] in CH30H (150 ml) was [REFLUXED] for eight days. The reaction mixture was then concentrated in vacuo, partitioned between water (50 [ML)] and [CH2CI2] (100 [ML),] and acidified with [ACOH.] The organic layer was isolated and concentrated to provide crude 46.

149554-03-0, The synthetic route of 149554-03-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SCHERING CORPORATION; WO2004/831; (2003); 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.61995-20-8,Benzyl 3-oxopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.,61995-20-8

To a solution of Compound 1 (5.0 g, 21.5 mmol) and ethyl 2-diazoacetate (3.2 g, 28.1 mmol) in THF (100 mL) was added BF3-Et2O (2.7 mL, 21.5 mmol) at -78 C. under N2. The reaction mixture was stirred at -78 C. for 1.5 h, then warmed to 28 C. slowly and stirred for 1.5 h. The resulting mixture was quenched with NaHCO3 (sat.) and extracted with EA (300 mL). The organic layer was dried over Na2SO4 and concentrated in vacuo to give a crude product, which was purified by flash column chromatography to give a mixture of Compound 2 and 3 (3.4 g, 50%). LCMS: 320.0 [M+1]. To a suspension of NaH (338 mg, 8.5 mmol) in THF (30 mL) was added a solution of a mixture of Compound 3 and Compound 3?(2.7 g, 8.5 mmol) in THF (30 mL) at 0 C. under N2, and stirred at rt for 0.5 h. A solution of Select F (2.7 g, 8.5 mmol) in DMF (15 mL) was added dropwise. The reaction mixture was stirred at r.t. for 3 h. The resulting mixture was quenched with NH4Cl and extracted with EA (200 mL). The organic layer was washed with brine, dried over Na2SO4 and concentrated in vacuo to give the crude product, which was purified by flash column chromatography to give Compound 4 (1.0 g, 35%) and Compound 4? (0.9 g, 32%). Compound 4: 1H NMR (400 MHz, CDCl3) delta=7.28-7.39 (m, 5H), 5.18 (s, 2H), 4.40-4.68 (m, 1H), 4.11-4.39 (m, 3H), 3.45-3.63 (m, 1H), 3.21-3.38 (m, 1H), 1.85-2.45 (m, 4H), 1.26-1.30 (m, 3H). Compound 4?: 1H NMR (400 MHz, CDCl3) delta=7.28-7.40 (m, 5H), 5.14-5.18 (m, 2H), 4.24-4.47 (m, 4H), 3.88-4.00 (m, 1H), 3.09-3.25 (m, 1H), 2.85-2.91 (m, 2H), 1.92-1.95 (m, 2H), 1.27-1.35 (m, 3H).

61995-20-8 Benzyl 3-oxopiperidine-1-carboxylate 1514169, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Hartman, George D.; US2015/197493; (2015); 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.236406-22-7,1-Boc-4-(Aminomethyl)-4-methylpiperidine,as a common compound, the synthetic route is as follows.

HATU (294 mg, 0.8 mmol) was added to the mixture of 6-methyl-7-oxo-6,7-dihydro- 1 H- pyrrolo[2,3-c]pyridine-4-carboxylic acid (Intermediate C) (135 mg, 0.7 mmol), tert-butyl 4- (aminomefhyl)-4-methylpiperidine-l-carboxylate (160 mg, 0.7 mmol), and diisopropylethylamine (181 mg, 1.4 mmol) in DMF (3 mL). After addition, the reaction mixture was stirred at room temperature for 2 h, at which time LCMS indicated that the reaction had gone to completion. The mixture was quenched by addition of water (5 mL) and extracted with ethyl acetate (2 x 10 mL). The combined organic extracts were washed with brine, dried over sodium sulfate and concentrated under reduced pressure to give the crude title compound (275 mg, 94% yield) as light brown oil. This crude material was used directly in the next step. LCMS M/Z (M+H) 402.9.

236406-22-7, As the paragraph descriping shows that 236406-22-7 is playing an increasingly important role.

Reference：
Patent; GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS, INC.; ALBRECHT, Brian, K.; BELLON, Steven, F.; BURDICK, Daniel, J.; COTE, Alexandre; CRAWFORD, Terry; DAKIN, Les, A.; HSIAO-WEI TSUI, Vickie; HEWITT, Michael, Charles; LEBLANC, Yves; MAGNUSON, Steven, R.; NASVESCHUK, Christopher, G.; ROMERO, F., Anthony; TANG, Yong; TAYLOR, Alexander, M.; WANG, Shumei; (251 pag.)WO2016/77375; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

78190-11-1, 1-[(Benzyloxy)carbonyl]-3-piperidinecarboxylic acid is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1: To the corresponding Cbz-protected product from general procedure G, step D (323 mg, 0.441 mmol), N-cbz-piperidin-3-ylcarboxylic acid (370 mg, 1.405 mmol), and TBTU (450 mg, 1.400 mmol) in THF (15 ml) is added at room temperature N-ethyldiisopropylamine (0.3 ml, 1.718 mmol) and the mixture is stirred at room temperature overnight and then heated to reflux for 8 h. Sat. aq. sodium bicarbonate (40 ml) is added, the mixture stirred for 15 min., and then extracted with ether (3 x 70 ml). The combined org. layers are dried over sodium sulfate, concentrated in vacuo, and the residue purified by flash chromatography (silica, dichloromethane/MeOH 20:1) to give a mixture of the 2 diastereoisomeric bis-Cbz-protected intermediates. Flash chromatography (silica, ethyl acetate/MeOH 100:0 – 50:1) afforded the 2 diastereoisomers (23 % and 16 %). ESI-MS: (M+H)+ = 942. Step 2: The 2-Cbz-protected diastereoisomers are submitted separately to hydrogenation in MeOH (20 ml) at 50 psi in the presence of Pd/C (10 %) at 50 C for 2 h. The catalyst is removed by filtration and the filtrate is concentrated in vacuo to give the product (41 % and 35 %). ESI-MS: (M+H)+ = 674

78190-11-1, As the paragraph descriping shows that 78190-11-1 is playing an increasingly important role.

Reference：
Patent; NOVO NORDISK A/S; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; WO2004/48345; (2004); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

122860-33-7, Benzyl 4-(hydroxymethyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Reaction step 2: Synthesis of benzyl 4-formylpiperidine-1-carboxylate To a stirred solution of benzyl 4-(hydroxymethyl)piperidine-1-carboxylate (10.0 g, 40.2 mmol, 1.0 eq) in dichloromethane (150 ml), Dess-Martin periodinane (20.4 g, 48.2 mmol, 1.2 eq) was added at at 0 C. and stirring was continued at room temperature for 12 h. After completion of the reaction (monitored by TLC, 30% ethyl acetate-hexane, Rf=0.45), the mixture was diluted with dichloromethane and washed with saturated sodium bicarbonate solution, followed by brine. The organic extract was dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure. The crude product was purified by column chromatography on silica gel (100-200 mesh), eluting with a 30-40% gradient of ethyl acetate in hexanes to obtain benzyl 4-formylpiperidine-1-carboxylate (6.2 g, 62.5%). LCMS Purity: 78.54% (ES+): m/z 248.27 (M+H+); tr=3.01 min.

122860-33-7, The synthetic route of 122860-33-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; INNOV17 LLC; Gaweco, Anderson; Tilley, Jefferson; Blinn, James; US2015/252022; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem