Category: 109384-19-2

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.

A solution of N-Boc-4-hydroxypiperidine (600 mg, 3.0 mmol) in HCl/Et20 (2.0 M, 10 mL) was stirred at room temperature for 2 hours. The reaction mixture was concentrated and the residue obtained washed with Et20 and dried to give the title product (370 mg, 90percent) as white solid which was used without purification.

109384-19-2, 109384-19-2 tert-Butyl 4-hydroxypiperidine-1-carboxylate 643502, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; CTXT PTY LIMITED; BERGMAN, Ylva Elisabet; CAMERINO, Michelle Ang; STUPPLE, Paul Anthony; (81 pag.)WO2017/153520; (2017); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

109384-19-2, tert-Butyl 4-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 82A tert-butyl 4-(4-amino-1H-pyrazol-1-yl)piperidine-1-carboxylate The title compound was prepared as described in Example 41A substituting tert-butyl 4-hydroxypiperidine-1-carboxylate for 1-methylpiperidin-4-ol., 109384-19-2

The synthetic route of 109384-19-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Abbott Laboratories; US2010/317680; (2010); 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.109384-19-2,tert-Butyl 4-hydroxypiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Fluorobenzonitrile (3. 0G) was dissolved in THF (50ML) and then N-tert-butoxy-carbonyl- 4-piperidinol (4.98g) was added. Potassium hexamethyldisilazide (20% wt solution in THF, 24.62g) was then added dropwise and the reaction stirred at rt for 2h. The reaction mixture was then evaporated to a minimum, redissolved in EtOAc (100 ML) and washed with aqueous 1N HCI (2X100 ML), saturated sodium bicarbonate solution (2X100M1) and brine (100 ML). The organic layer was dried (MGS04) and then purified by chromatography [silica gel, step gradient 0-60% EtOAc/Hexane]. Fractions containing the required product were evaporated to give the title compound (D29) as a clear oil which crystallised on standing (6. 83G).1 H NMR delta (CDCI3) : 7.59 (2H, d, J=7. 50HZ), 6.95 (2H, d, J=7. 50HZ), 4.44 (1 H, m), 3.70 (2H, m), 3.38 (2H, m), 1.91 (2H, m), 1.77 (2H, m), 1.47 (9H, s)., 109384-19-2

109384-19-2 tert-Butyl 4-hydroxypiperidine-1-carboxylate 643502, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; GLAXO GROUP LIMITED; WO2004/37800; (2004); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

109384-19-2, tert-Butyl 4-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Tert-butyl-4-hydroxypiperidine-1-carboxylate (4.5 g, 22.4 mmol)4-hydroxybenzonitrile (2.7 g, 22.7 mmol)And triphenylphosphine(8.8 g, 33.5 mmol) was dissolved in tetrahydrofuran (80 mL)Cooled to 0 C,Diethyl azodicarboxylate (5.8 g, 33.3 mmol) was added.25 C for 4 hours,LC-MS detection reaction is completed,Concentrated, ethyl acetate (150 mL) and water (50 mL) were added,The aqueous phase was extracted with ethyl acetate (50 mL)Combined organic phase,The residue was purified by silica gel column chromatography (petroleum ether: ethyl acetate = 10: 1) to give the product (4.6 g, 67.6% yield).

109384-19-2, The synthetic route of 109384-19-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Shandong Xuanzhu Pharmaceutical Technology Co., Ltd.; Wu Yongqian; Qi Qu; Li Lin; (54 pag.)CN107226807; (2017); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

109384-19-2, tert-Butyl 4-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-Fluorobenzonitrile (3. 0G) was dissolved in THF (50ML) and then N-tert-butoxy-carbonyl- 4-piperidinol (4.98g) was added. Potassium HEXAMETHYIDISILAZIDE (20% wt solution in THF, 24.62g) was then added dropwise and the reaction stirred at rt for 2h. The reaction mixture was then evaporated to a minimum, redissolved in EtOAc (100 ml) and washed with aqueous 1N HCI (2X100 ML), saturated sodium bicarbonate solution (2X100 ML) and brine (100 ML). The organic layer was dried (MGS04) and then purified by chromatography [silica gel, step gradient 0-60% EtOAc/Hexane]. Fractions containing the required product were evaporated to give the title compound (D21) as a clear oil which crystallised on standing (6.83 g).’H NMR 8 (CDCI3) : 7.59 (2H, d, J=7. 50HZ), 6.95 (2H, d, J=7. 50HZ), 4.44 (1H, m), 3.70 (2H, m), 3.38 (2H, m), 1.91 (2H, m), 1.77 (2H, m), 1.47 (9H, s).

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

Reference：
Patent; GLAXO GROUP LIMITED; WO2004/37788; (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.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

109384-19-2, tert-Butyl 4-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation Example 1 (4-(4-(trifluoromethoxy)phenoxy)piperidine (I-6a) P-trifluoromethoxy phenol (32.7 g, 184 mmol), N-Boc-4-hydroxy piperidine (37 g, 184 mmol) and triphenylphosphine (48.3 g, 184 mmol) were dissolved in dry THF (500 mL), DIAD (37.2 g, 184 mmol) was added dropwise while cooling in ice-bath, followed by stirring overnight at room termperature. THF were spun out, residuals were extracted by petroleum ether, extracting solution was concentrated to give 71.2 g light yellow oily matter, crude product yield was more than 100%, directly put into the next reaction step. The crude products obtained from the previous step (66.5 g, 184 mmol) were dissolved in TFA (500 mL), stirring at room temperature. After 3 h, TFA were spun out, add water to residuals, use NaOH solution to adjust pH to above pH 10, extract by ethyl acetate, extracting solution was concentrated followed by column chromatography to give 35.3 g white solid, yield was 73%. ESI-LR: 262.1 [M+1]+.

109384-19-2, 109384-19-2 tert-Butyl 4-hydroxypiperidine-1-carboxylate 643502, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Wang, Tiancai; Xin, Ting; Fan, Houxing; Chen, Yilang; US2013/143864; (2013); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

109384-19-2, tert-Butyl 4-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of tert-butyl 4-hydroxypiperidine- 1 -carboxylate (5 g, 24.84 mmol, 1.00 equiv) and HC1 (saturated solution in 30 mL of 1 ,4-dioxane) was stirred for 2 h at room temperature. The resulting mixture was concentrated under vacuum to afford the title compound (3.4 g, 99percent) as an off- white solid.

109384-19-2, The synthetic route of 109384-19-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; GENENTECH, INC.; CHEN, Huifen; CHU, Yanyan; DO, Steven; ESTRADA, Anthony; HU, Baihua; KOLESNIKOV, Aleksandr; LIN, Xingyu; LYSSIKATOS, Joseph P.; SHORE, Daniel; VERMA, Vishal; WANG, Lan; WU, Guosheng; YUEN, Po-wai; WO2015/52264; (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.109384-19-2,tert-Butyl 4-hydroxypiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

The compound 4-hydroxypiperidine-1-carboxylic acid tert-butyl ester (485 mg, 2.41 mmol) and DMAP (29.4 mg,0.241 mmol) was dissolved in DCM (15 mL), and Et3N (0.67 mL, 4.82 mmol) and MsCl (0.223 mL, 2.879 mmol) were slowly added to the reaction mixture at 0 C.After the reaction mixture was stirred at room temperature for 5 hours, an aqueous solution of NaHCO3 (25 mL, 1 M) was added.The mixture was extracted with DCM (50 mL×2). The combined organic phases were washed with brine (25 mL).Dry over anhydrous Na 2 SO 4 and concentrate under reduced pressure.The crude product obtained was used directly in the next step without further purification.The compound 4-iodo-1H-pyrazole (467.5 mg, 2.41 mmol) was dissolved in dry DMF (8 mL) then EtOAc.NaH (60%, 193 mg, 4.82 mmol) was added portionwise to the reaction mixture. Raise the reaction to room temperature,After stirring the reaction for 2 hours at room temperature, a solution of the above crude product in DMF (4 mL) was added to the mixture.After the reaction mixture was stirred at 100 C for 12 hours, the reaction was quenched by the addition of aqueous NH4Cl (20 mL).The mixture was extracted with EtOAc (40 mL×2). The combined organic phases were washed with brine (25 mL).Dry over anhydrous Na 2 SO 4 and concentrate under reduced pressure.The residue was chromatographed on silica gel (EtOAc/EtOAc)Purification to give the title compound as a yellow solid(620 mg, 68%)., 109384-19-2

109384-19-2 tert-Butyl 4-hydroxypiperidine-1-carboxylate 643502, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Guangdong Dongyangguang Pharmaceutical Co., Ltd.; Jiatuo Sciences Corporation; Xi Ning; Li Xiaobo; Zhou Shiqing; (62 pag.)CN103833753; (2017); B;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem