Day: September 14, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.256411-39-9,1-Boc-4-(Cyanomethyl)piperidine,as a common compound, the synthetic route is as follows.

256411-39-9, t-BuOK (3 g, 26.7 mmol) was added portionwisely to a solution of tert-butyl 4-(cyanomethyl)piperidine-1-carboxylate (1 g, 4.46 mmol) in DMF (40 mL) at 510 C. After addition, the mixture was stirred for 30 min. A solution of ethyl formate (2 g, 26.7 mmol) in DMF (10 mL) was added dropwise. Then the mixture was allowed to warm to RT and stirred at 35 C. for 12 h (overnight). 10 mL of water was added to quench the reaction. The solvent was removed under reduced pressure. 100 mL of water was added and extracted with EA (20 mL¡Á2). The combined organic phases were dried over Na2SO4, filtered and concentrated to give 1 g (90%) of desired product as a yellow solid. 1H NMR (400 MHz, CDCl3-d1) delta 8.88 (br s, 1H), 4.16-4.08 (m, 2H), 2.84-2.64 (m, 2H), 1.81-1.62 (m, 2H), 1.57-1.38 (m, 2H), 1.46 (s, 9H), 1.31-1.23 (m, 1H). MS (ESI) m/e [M+23]+ 275.1

The synthetic route of 256411-39-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Wang, Zhiwei; Guo, Yunhang; US2015/5277; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

143900-44-1, (S)-tert-Butyl 3-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred mixture of 3-iodo-lH-pyrazolo[3,4-d]pyrimidin-4-amine (5.9 g, 22.6 mmol, 1.00 equiv), (S)-tert-butyl 3-hydroxypiperidine-l -carboxylate (lOg, 50 mmol, 2.2 equiv) and triphenylphosphine (1 1.8g, 45 mmol, 2.0 equiv) in tetrahydrofuran (300 mL) at 10 C was added a solution of diisopropyl azodicarboxylate in tetrahydrofuran (30 mL) dropwise in 30 min. The resulting mixture was stirred at room temperature for 12 h and then concentrated under vacuum. The residue was purified on a silica gel column eluted with dichloromethane/methanol (100/1) to give 3g of (R)-tert-butyl 3-(4-amino-3-iodo-lH- pyrazolo[3,4-d]pyrimidin-l-yl)piperidine-l-carboxylate as a yellow solid.

143900-44-1, 143900-44-1 (S)-tert-Butyl 3-hydroxypiperidine-1-carboxylate 1514399, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; PRINCIPIA BIOPHARMA INC.; OWENS, Tim; VERNER, Erik; WO2014/39899; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1312412-87-5, tert-Butyl 3-bromo-2,4-dioxopiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step iv: tert-butyl 2-amino-4-oxo-6,7-dihvdrothiazolo[5,4-clpyridine-5(4H)-carboxylate To a 50 mL round bottom flask, were added tert-butyl 3-bromo-2,4-dioxopiperidine-l- carboxylate (1 g, 0.0034 mol), thiourea (0.287 g, 0.0038 mol), sodium bicarbonate (0.317 g, 0.0038 mol) and ethanol (15 mL). The reaction mixture was stirred at 80 C for 2.5 h. The volatiles were evaporated under reduced pressure to get residue. The residue was partitioned between ethyl acetate and water. The organic layer was separated, washed with brine and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure to obtain the title compound [0.7 g, 76 %]. NMR (300 MHz, CDsOD): delta 4.05 (t, 2H), 2.83 (t, 2H), 1.52 (s, 9H)., 1312412-87-5

The synthetic route of 1312412-87-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AURIGENE DISCOVERY TECHNOLOGIES LIMITED; KOTRABASAIAH UJJINAMATADA, Ravi; HOSAHALLI, Subramanya; BEJUGAM, Mallesham; WO2015/101928; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

184637-48-7, tert-Butyl 3-aminopiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 93; 1 ,1-Dimethylethyl ri-(2-amino-6-chloro-4-pyrimidinyl)-3-piperidinyllcarbamate; 2-Amino-4,6-dichloropyrimidine (3.33 g, 20.30 mmol) was added to a stirring mixture of 3- Lambda/-Boc-aminopiperidine (4.28 g, 21.4 mmol) and K2CO3 (2.95 g, 21.4 mmol) in ethanol (50 ml_). The reaction was refluxed for 1 hour. HPLC indicated complete conversion. Water (50 ml.) was slowly added to the hot mixture, which was then allowed to cool to room temperature with stirring. The precipitated product was collected by filtration and washed with 1 :1 ethanohwater (50 ml.) and dried to afford the title compound (5.98 g) as a white powder. LC-MS (ES) m/z = 328 [M+H]+.

184637-48-7, 184637-48-7 tert-Butyl 3-aminopiperidine-1-carboxylate 545809, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXOSMITHKLINE LLC; AXTEN, Jeffrey, Michael; BLACKLEDGE, Charles, William; BRADY, Gerald, Patrick; FENG, Yanhoug, G.; GRANT, Seth, W.; MEDINA, Jesus, Rahul; MILLER, William, H.; ROMERIL, Stuart, P.; WO2010/59658; (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.3202-33-3,4-Phenoxypiperidine,as a common compound, the synthetic route is as follows.

To a solution of 4-phenoxypiperidine (500 mg, 2.82 mmol) in DMF (6 mL) was added K2CO3 (0.78 g, 5.64 mmol) and 2-bromoethanol (0.39 g, 3.1 mmol). The reaction mixture was heated to 50C and stirred at that temperature for 3 h. TLC showed most of the product. The reaction was poured into water and extracted with DCM (3 x 40 mL). The combined organics were washed with saturated aqueous NaCl (2 x 20 mL). The combined organics were dried over anhydrous Na2SO4, filtered and concentrated in vacuo. The resulting oil was purified by flash column chromatography with a gradient elution of DCM (95%) and MeOH (5%) to DCM (85%) and MeOH (15%) to provide 2-(4- phenoxypiperidin-1-yl)ethanol (260 mg, 1.17 mmol) as a yellow solid.

3202-33-3, 3202-33-3 4-Phenoxypiperidine 18878, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; SUNOVION PHARMACEUTICALS INC.; HEFFERNAN, Michele L.R.; HARDY, Larry Wendell; BROWN, Scott P.; HERMAN, Lee W.; (180 pag.)WO2018/26371; (2018); 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.184637-48-7,tert-Butyl 3-aminopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Example 10: Intermediate 10.1 : 3-Amino-l,l-bis-[3-(3-methoxy-phenyl)-propyl]-piperidinium chloride hydrochloride Piperidin-3-yl-carbamic acid tert-butyl ester (110 mg, 0.55 mmol) and l-(3-Bromo-propyl)-3-methoxy- benzene (320 mg, 1.4 mmol), potassium carbonate (100 mg, 0.72 mmol) and sodium iodide (150 mg, 1 mmol) are dissolved in acetonitril (2 ml) and stirred at reflux overnight and purified by preparative HPLC-MS (MeOH/H20 + 0.1percent TFA). The residue is dissolved in dichloromethane (1 ml) and TFA (1 ml), stirred at room temperature for 1 h and concentrated in vacuo. The residue is dissolved in acetonitril, 1M HCI (1 ml) is added and evaporated. LC (method L): tR = 1.02 min; Mass spectrum (ESI+): m/z = 397 [M]+.

184637-48-7, The synthetic route of 184637-48-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; WIEDENMAYER, Dieter; HAMPRECHT, Dieter; HECKEL, Armin; WO2015/18754; (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.203662-51-5,4-Allyl-1-Boc-4-hydroxypiperidine,as a common compound, the synthetic route is as follows.

203662-51-5, tert-butyl (3RS)-3-hydroxy-1-oxa-8-azaspiro[4.5ldecane-8-carboxylate tert-butyl 4-allyl-4-hydroxypiperidine-1-carboxylate (1153 g, 4.8 mol) was dissolved in tert-butanol (10 L) and water (4 L). To the solution sodium periodate (1124 g, 5.3 mol, 1.1 eq) was added and the mixture was stirred at 50 0C for 30 minutes. At 50 0C a solution of Na2S2O5 (1007 g, 5.3 mol, 1.1 eq) in water (4.2 L) was added dropwise over 4 hours to the solution. After addition the reaction mixture was stirred for 7 hours at 50 0C and another 48 hours at RT. The mixture was transferred to an extraction vessel and the organic layer was separated from the aqueous layer. The aqueous layer was extracted (3x) with ethyl acetate. The organic layers were combined and washed with a saturated solution of Na2S2O3 (3x) to give a colorless solution. The solution was washed with brine and evaporated to give crude product (987 g, 80percent). The crude product was purified by flash chromatography (10-80percent EtOAc/Heptane) to give the title compound (287 g, 35percent). m/z 158 (MH+ minus Boc).

The synthetic route of 203662-51-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PFIZER INC.; LONG, Scott Allen; MEYERS, Marvin Jay; PELC, Matthew James; SCHWEITZER, Barbara Ann; THORARENSEN, Atli; WANG, Lijuan Jane; WO2010/58318; (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.161609-84-3,Benzyl 4-cyanopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

(3) The above-mentioned compound (1.42 g) was dissolved in N-methyl-2-pyrrolidone (60 mL), and sodium azide (1.13 g) and triethylamine hydrochloride (1.24 g) were added thereto. The mixture was stirred at 150C for 6 hr. 1 mol/L Hydrochloric acid was added to the reaction mixture to adjust its pH to 1, and the mixture was extracted with ethyl acetate. 10% Aqueous sodium hydroxide solution was added to the extract, and the mixture was washed with diethyl ether. The aqueous layer was adjusted to pH 1 with concentrated hydrochloric acid, and the mixture was extracted with ethyl acetate. The extract was dried and concentrated under reduced pressure. Trifluoroacetic acid (6 mL), tert-butanol (0.900 g) and concentrated sulfuric acid (0.16 mL) were added to the residue, and the mixture was stirred at room temperature for 3 days. Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The extract was washed successively with 2.5 mol/L aqueous sodium hydroxide solution and brine, dried, and concentrated under reduced pressure. The residue was purified by HPLC to give 1-benzyloxycarbonyl-4-(2-tert-butyl-2H-tetrazol-5-yl)piperidine (140 mg) as a white solid.

161609-84-3, 161609-84-3 Benzyl 4-cyanopiperidine-1-carboxylate 22028286, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; WELFIDE CORPORATION; EP1308439; (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.52763-21-0,Ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride,as a common compound, the synthetic route is as follows.

Preparation 29: Ethyl 1-benzyl-3-oxo-4-(prop-2-en-1-yl)piperidine-4-carboxylate (P29)A mixture of potassium ferf-butoxide (3.77 g, 33. 58 mmol) in THF (100 m L) was stirred at RT for 0.5 h. The resulting milky solution was cooled to 0 C, and then Ethyl l-benzyl-3-oxopiperidine-4-carboxylate hydrochloride (5 g, 16.79 mmol) was added portion wise keeping the internal temperature below 5 C. The mixture was then warmed to RT and further stirred for 1 h, resulting in a yellow solution. After cooling to 0 C, allyl bromide (1.6 mL, 18.47 mmol) was added dropwise. The reaction mixture was warmed to RT and stirred overnight. The reaction solution was cooled to 0 C, and 50 m L of saturated N H4CI solution was added. After extraction and phase separation, the aqueous phase was extracted twice with 100 mL of EA. The combined organic phases were washed with 100 m L of saturated NaCI solution and dried; the solvent was evaporated under reduced pressure and the obtained crude material was purified by FC on silica gel (eluent: Cy to Cy/AcOEt 80/20) to give ethyl l-benzyl-3-oxo-4-(prop-2-en- l-yl)piperidine-4-carboxylate (p29, 4.23 g, y= 84%) as a yellow oil.MS (ES) (m/z): 302.23 [M+H]+., 52763-21-0

52763-21-0 Ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride 2723880, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; SHIRE INTERNATIONAL GMBH; SEMERARO, Teresa; TARSI, Luca; MICHELI, Fabrizio; LUKER, Tim; CREMONESI, Susanna; (122 pag.)WO2016/42451; (2016); 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.299428-04-9,2-(1-Benzylpiperidin-4-yl)-2-propanol,as a common compound, the synthetic route is as follows.

The benzyl protecting group was removed with palladium, 10 wt. % on activated carbon and placing the reaction vessel under hydrogen (g) overnight. Upon completion, the reaction mixture was filtered through Celite. The filtrate was concentrated to produce 2-(piperidin-4-yl)propan-2-ol., 299428-04-9

As the paragraph descriping shows that 299428-04-9 is playing an increasingly important role.

Reference£º
Patent; Hu, Essa; Kunz, Roxanne; Nixey, Tom; Hitchcock, Stephen; US2009/62291; (2009); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem