Day: March 17, 2022

25137-01-3, (R)-Ethyl piperidine-3-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Chlorobenzenesulfonyl chloride (0.25 mL, 1.8 mmol) was added to a solution of (R)-(+)-nipecotic acid ethyl ester (available from Aldrich Chemical Company; Inc., Milwaukee, Wisc.; 250 mg, 1.6 mmol) and triethylamine (0.5 mL, 3.6 mmol) in dichloromethane (5 mL) under argon. An additional portion of dichloromethane (10 mL) was added and the solution was stirred for five days at room temperature. The reaction mixture was washed with water and the water layer was back-extracted with dichloromethane. The combined organic layers were washed with 80% saturated brine, dried (magnesium sulfate), filtered and evaporated to give (3R)-1-(2-chloro-benzenesulfonyl)-piperidine-3-carboxylic acid ethyl ester (561 mg) as a colorless viscous oil, which was used directly in the next step. NMR indicated the presence of the desired product along with a small amount of dichloromethane.

25137-01-3, 25137-01-3 (R)-Ethyl piperidine-3-carboxylate 185582, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Gillespie, Paul; Goodnow, Robert Alan; Kowalczyk, Agnieszka; So, Sung-Sau; Zhang, Qiang; US2006/199816; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

885279-92-5, 1-Boc-1,8-diaza-spiro[4.5]decane is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 142: 1,1,1,3,3,3-Hexafluoropropan-2-yl 1-((1-acetyl-1,2,3,4-tetrahydroquinolin-8- yl)methyl)-1,8-diazaspiro[4.5]decane-8-carboxylate Step 1: Preparation of 1-tert-butyl 8-(1,1,1,3,3,3-hexafluoropropan-2-yl) 1,8- diazaspiro[4.5]decane-1,8-dicarboxylat A flask was charged with triphosgene (2.46 g, 8.29 mmol, 0.50 equiv), DCM (100 mL) and HFIP (4.21 g, 24.9 mmol, 1.50 equiv). DIEA (6.45 g, 49.7 mmol, 3.00 equiv) was added dropwise at 0 ^C. The reaction mixture was stirred for 2 h at 0 ^C. tert-Butyl 1,8- diazaspiro[4.5]decane-1-carboxylate (4.01 g, 16.6 mmol, 1.00 equiv) was added, and the reaction was stirred for 3 h at 0 ^C before quenching with H2O (50 mL). The mixture was extracted with DCM (3 x 50 mL) and the organic layers were combined, washed with H2O (3 x 100 mL), dried over anhydrous Na2SO4, filtered, and concentrated. The residue was purified on a silica gel column (1:2 EtOAc/petroleum ether) to provide 4.34 g (60% yield) of 1-tert-butyl 8-(1,1,1,3,3,3- hexafluoropropan-2-yl) 1,8-diazaspiro[4.5]decane-1,8-dicarboxylate as a white solid. LCMS (ESI, m/z): 435 [M+H]+.

885279-92-5, As the paragraph descriping shows that 885279-92-5 is playing an increasingly important role.

Reference：
Patent; ABIDE THERAPEUTICS, INC.; BUZARD, Daniel J.; SHAGHAFI, Michael B.; CISAR, Justin S.; GRICE, Cheryl A.; JONES, Todd K.; WEBER, Olivia D.; (277 pag.)WO2017/197192; (2017); 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.4801-58-5,Piperidin-1-ol,as a common compound, the synthetic route is as follows.

General procedure: To a 25-mL flask equipped with a magnetic stirrer, in which the air was replaced by N2, was added CuBr (0.05 mmol), toluene (1.0 mL), aldehyde (1.0 mmol), alkyne (1.5 mmol), and hydroxylamine (1.5 mmol). The mixture was stirred at 70C. After the completion of the reaction (monitored by TLC), the reaction solution was submitted to flash chromatographic separation on silica gel using petroleum ether/ethyl acetate as an eluent to give the corresponding product.

4801-58-5, 4801-58-5 Piperidin-1-ol 20935, apiperidines compound, is more and more widely used in various fields.

Reference：
Article; Guo, Na; Ji, Jian-Xin; Tetrahedron Letters; vol. 53; 36; (2012); p. 4797 – 4801;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

4629-80-5, 1,3-Dimethylpiperidin-4-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 14 6-chloro-3-(1,3-dimethyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-indole Beginning with 0.97 gm (6.4 mMol) 6-chloro-1H-indole and 1.6 gm (13.0 mMol) 1,3-dimethyl-4-piperidone, 1.05 gm (63%) of the title compound were recovered as a crystalline solid. m.p.=170-172 C. MS(FD): m/e=260 (M+) EA: Calculated for: C15 H17 N2 Cl: Theory: C, 69.09; H, 6.57; N, 10.74. Found: C, 69.39; H, 6.40; N, 10.97., 4629-80-5

Big data shows that 4629-80-5 is playing an increasingly important role.

Reference：
Patent; Eli Lilly and Company; US5846982; (1998); 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.1187173-43-8,2,7-Diazaspiro[4.5]decan-1-one hydrochloride,as a common compound, the synthetic route is as follows.

Preparation 44: tert-butyl 1-oxo-2,7-diazaspiro[4,5]decane-7-carboxylate (P44)2,7-diazaspiro[4.5]decan-l-one hydrochloride (600 mg, 3.15 mmol), was dissolved in 30 m L of DCM. To this solution, TEA (1.98 mL, 14.18 mmol) and Boc20 (895 mg, 4.10 mmol) were added and the reaction mixture was stirred at RT for 4 hrs. Water was added and the two layers were separated; the organic layer was washed with NH4CI, dried and evaporated to obtain ferf-butyl l-oxo-2,7- diazaspiro[4.5]decane-7-carboxylate (p44, 830 mg, y= quant.), colourless oil.MS (ES) (m/z): 255.2 [M+H]+.

1187173-43-8, As the paragraph descriping shows that 1187173-43-8 is playing an increasingly important role.

Reference：
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.297172-16-8,(4-Methylpiperidin-4-yl)methanol,as a common compound, the synthetic route is as follows.

69B. tert-Butyl 3-(4-((4-(hydroxymethyl)-4-methylpiperidin-1-yl)methyl)-3-methylphenoxy)azetidine-1-carboxylate To a solution of 69A (3.00 g, 10.3 mmol) in DCM (50 mL) was added (4-methylpiperidin-4-yl)methanol (2.56 g, 15.5 mmol) followed by DIPEA (3.60 mL, 20.6 mmol). The reaction mixture was stirred at RT for 20 min and then sodium triacetoxyborohydride (6.55 g, 30.9 mmol) was added. The mixture was stirred at RT overnight and then washed with a saturated aqueous solution of Na2CO3. The aqueous layer was extracted several times with DCM. The organic layers were filtered through a phase separator and then evaporated. There was obtained 3.1 g (74%) of the product as an oil. 1H NMR (500 MHz, CDCl3): delta 0.95 (s, 3H), 1.33 (m, 2H), 1.45 (s, 9H), 1.51 (m, 2H), 2.26 (m, 2H), 2.30 (s, 3H), 2.51 (m, 2H), 3.38 (s, 2H), 3.39 (s, 2H), 3.99 (m, 2H), 4.27 (m, 2H), 4.84 (m, 1H), 6.48 (dd, 1H), 6.56 (d, 1H), 7.16 (d, 1H), MS (APCI+) m/z 405 [M+H]+.

297172-16-8, As the paragraph descriping shows that 297172-16-8 is playing an increasingly important role.

Reference：
Patent; AstraZeneca AB; US2012/10189; (2012); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

3612-20-2, 1-Benzylpiperidin-4-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step A 1-benzyl-4-(methylamino)piperidine A solution of 1 mol of N-benzylpiperid-4-one in 2200 cm3 of isopropanol is cooled to 18 C. A freshly prepared solution of 3 mol of methylamine in 300 cm3 of methanol is added to the first solution. The mixture is left at that temperature for one hour. 1.66 mol of sodium hydroxide in the form of pellets are added. 1.37 mol of sodium borohydride are added at a constant temperature of 18 C. The mixture is allowed to return to room temperature and then the reagents are left in contact for 12 hours. The solvents are evaporated, and the residue is taken up in ether and then washed with water. Drying and evaporation yield an oil which is the desired compound. Yield: 78%., 3612-20-2

3612-20-2 1-Benzylpiperidin-4-one 19220, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Adir et Compagnie; US5298503; (1994); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

35856-62-3, Piperidine-1-sulfonyl chloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 25 Piperidine-1-sulfonic acid (6-propyl-pyridin-2-yl)-amide A solution of 6-propyl-pyridin-2-ylamine (0.2 g) and piperidine-1-sulfonyl chloride (0.296 g, Bull. Soc. Chim. Fr.; 1936, 2143) in pyridine (7 mL) was heated to reflux for 15 h. After concentration of the reaction mixture in vacuo the residue was taken up in EtOAc, which was then washed with 1N aqueous HCl, saturated brine, dried over sodium sulphate and concentrated in vacuo. The residue was applied to a silica gel column with EtOAc/toluene (9:1 to 1:1) as eluent. Combination of the purified fractions and concentration in vacuo gave the desired piperidine-1-sulfonic acid (6-propyl-pyridin-2-yl)-amide (0.133 g) as a colorless amorphous solid. MS (ESI-): 282.0 ([M-H]-)., 35856-62-3

The synthetic route of 35856-62-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Amrein, Kurt; Hunziker, Daniel; Kuhn, Bernd; Mayweg, Alexander; Neidhart, Werner; US2006/74237; (2006); 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.142851-03-4,Ethyl N-Boc-piperidine-4-carboxylate,as a common compound, the synthetic route is as follows.

To 1-tert-butyl 4-ethyl piperidine-1, 4-dicarboxylate (4.96 g, 19.3 ?tmol) in methanol (20 mL) was added hydrazine hydrate (5 mL) and the mixture was heated to reflux for 3 days . The mixture was concentrated to dryness to give tert- butyl 4- (hydrazinocarbonyl)piperidine-l-carboxylate as a white crystalline solid (4.2 g, 90%) : 1H NMR (400 MHz, DMSO-d6) delta1.39 (s, 9H), 1.39-1.42 (m, 2H), 1.55-1.64 (m, 2H), 2.18-2.27 (in, IH), 2.63-2.76 (m, 2H), 3.89-3.97 (m, 2H), 9.03 (br, IH); m/z (APCI pos) 144.1 (100%) [M+H-Boc] .

142851-03-4, The synthetic route of 142851-03-4 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; WO2008/11130; (2008); 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.25137-01-3,(R)-Ethyl piperidine-3-carboxylate,as a common compound, the synthetic route is as follows.

Step B. Ethyl (3R)-1-{[2-tert-butyl-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-benzimidazol-5-yl]sulfonyl}piperidine-3-carboxylateA suspension of 2-tert-butyl-1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-benzimidazole-5-sulfonyl chloride (300 mg, 0.80 mmol) in DCE (5 mL) was slowly added to a solution of ethyl (3R)-piperidine-3-carboxylate (140 mg, 0.88 mmol) and DIPEA (1.4 mL, 8.0 mmol) in DCE (25 mL). The reaction mixture was stirred overnight at ambient temperature and the solvent was concentrated. The product was purified by MPLC on silica gel using 60-90% EtOAc/Heptane to provide the title compound as white solid. Yield: 265 mg (66%); 1H NMR (400 MHz, CDCl3) delta 1.26 (t, J=7.13 Hz, 3H), 1.33 (td, J=12.55, 4.00 Hz, 1H), 1.50-1.57 (m, 3H), 1.59 (s, 9H), 1.62-1.71 (m, 2H), 1.72-1.84 (m, 1H), 1.90-2.02 (m, 1H), 2.22-2.38 (m, 2H), 2.44 (t, J=11.03 Hz, 1H), 2.57-2.69 (m, 1H), 3.28-3.41 (m, 2H), 3.70 (d, J=11.33 Hz, 1H), 3.91 (dd, J=11.43, 3.81 Hz, 1H), 4.01 (dd, J=11.23, 2.83 Hz, 2H), 4.13 (q, J=7.16 Hz, 2H), 4.25 (d, J=7.42 Hz, 2H), 7.43 (d, J=8.59 Hz, 1H), 7.64 (dd, J=8.40, 1.76 Hz, 1H), 8.18 (d, J=1.17 Hz, 1H); MS (ESI) (M+H)+=492.0.

25137-01-3, As the paragraph descriping shows that 25137-01-3 is playing an increasingly important role.

Reference：
Patent; Brown, William; Liu, Ziping; Page, Daniel; Qadoumi, Zena; Srivastava, Sanjay; Tremblay, Maxime; Walpole, Christopher; Wei, Zhong-yong; Yang, Hua; US2011/86853; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem