Heterocyclic Building Blocks-piperidine

21987-29-1, 4,4-Difluoropiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In a 100 mL flask was placed 4-[5-(2-tert-butyl-4-pyridyl)-3-thienyl]-3-chloro-benzoic acid (150 mg, 0.40 mmol, 1 eq.) in DMF (10 mL), followed by addition of DIPEA (0.37 mL, 1.61 mmol, 5 eq.) and HATU (307 mg, 0.80 mmol, 2 equiv), and the resulting mixture was stirred for 5 min at RT and 3,3-difluoropiperidine (196 mg, 1.61 mmol, 4 eq.) were added and the mixture stirred at RT under nitrogen atmosphere overnight. The progress of the reaction was monitored by TLC and LCMS. After completion of reaction, the mixture was diluted with water (100 mL) and extracted with EtOAc (2*100 mL), washed with water (4*100 mL) then dried over anhydrous sodium sulfate and the combined organic layer was concentrated under reduced pressure to give a viscous compound, which was purified by reverse phase HPLC process to afford [4-[5-(2-tert-butyl-4-pyridyl)-3-thienyl]-3-chloro-phenyl]-(4,4-difluoro-1-piperidyl) methanone (50 mg) as an off-white solid, the free base. 1H NMR (400 MHz, Methanol-d4) delta (ppm): 8.49 (d, J=5.2 Hz, 1H), 7.91 (s, 1H), 7.78 (s, 1H), 7.71-7.61 (m, 3H), 7.52 (d, J=5.2 Hz, 1H), 7.47 (d, J=7.9 Hz, 1H), 3.87 (t, 2H), 3.62 (t, 2H), 2.08 (t, 4H), 1.42 (s, 9H). LCMS: (M+1) 475.2.

21987-29-1, 21987-29-1 4,4-Difluoropiperidine 2758352, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Medivation Technologies LLC; Pujala, Brahmam; Jangir, Ramniwas; Guguloth, Rambabu; Shinde, Bharat Uttam; Rai, Roopa; Pham, Son Minh; Bernales, Sebastian; Lindquist, Jeffrey; Guha, Mausumee; Kallem, Satyanarayana; Bhatt, Bhawana; Bhagwat, Vikas Ramdas; (162 pag.)US2018/51013; (2018); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

336191-17-4, tert-Butyl 2,8-diazaspiro[4.5]decane-2-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,336191-17-4

Step A: teri-Butyl 8-(2-chlorofuro[3,2-i/]pyrimidin-4-yl)-2,8-diazaspiro[4.5]decane-2- carboxylateA mixture of teri-butyl 2,8-diazaspiro[4.5]decane-2-carboxylate (0.83 g, 3.4 mmol, Alfa Aesar), 2,4-dichlorofuro[3,2-i/]pyrimidine (0.65 g, 3.4 mmol, ArkPharm) and TEA (0.96 mL, 6.9 mmol) in 1,4-dioxane (35 mL) was stirred at about 25 C for about 12 h. Water (4 mL) and EtOAc (25 mL) were added and the layers were separated. The organic layer was concentrated under reduced pressure to give teri-butyl 8-(2-chlorofuro[3,2-i/]pyrimidin-4-yl)-2,8-diazaspiro[4.5]decane-2- carboxylate (1.25 g, 55%): LC/MS (Table 2, Method f) Rt = 2.12 min; MS m/z: 393 (M+H)+.

336191-17-4 tert-Butyl 2,8-diazaspiro[4.5]decane-2-carboxylate 34178604, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; ABBOTT LABORATORIES; CALDERWOOD, David, J.; WILSON, Noel, S.; COX, Philip; HOEMANN, Michael, Z.; CLAPHAM, Bruce; MULLEN, Kelly, D.; VASUDEVAN, Anil; VILLAMIL, Clara I; LI, Bin; SOMAL, Gagandeep; WO2012/48222; (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.3040-44-6,1-(2-Hydroxyethyl)piperidine,as a common compound, the synthetic route is as follows.

A mixture of 20 mg of 2-(4-bromophenyl)-l,3-benzoxazole-5-carbonitrile (INTERMEDIATE 7), 17 mg of 2-piperidin-l-ylethanol, and 8 mg of sodium hydride (60% dispersion in oil) in 1 mL of toluene was purged and flushed with argon. Tris(dibenzylideneacetone) dipalladium (3 mg) and racemic BINAP (3 mg) were added and the mixture was heated to 800C and stirred overnight at this temperature. The reaction mixture was cooled and added directly to a 1000-muM thin-layer chromatography plate, eluting with 4% isopropanol in CH2Cl2 to provide 3.4 mg (15%) of the title compound. Mass spectrum (ESI)348.3 (M+l). 1H NMR (500 MHz, CDCl3): delta 8.18 (d, J=8.5 Hz, 2H), 8.02 (s, IH), 7.63 (m, 2H), 7.05 (d,J=9 Hz, 2H), 4.26 (t, J=6 Hz, 2H), 3.48 (d, J=3Hz, IH), 2.88 (br t, J=5.5 Hz, 2H), 2.61 (m, 3H), 1.68 (m, 5H), 1.49 (m, IH)., 3040-44-6

As the paragraph descriping shows that 3040-44-6 is playing an increasingly important role.

Reference£º
Patent; MERCK & CO., INC.; WO2007/70173; (2007); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1201935-36-5, 1-(1-Methylpiperidin-4-yl)-1H-pyrazol-4-amine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0483j To a solution of N-(2-(2-chloropyrimidin-4-yl)-6,7,8 ,9-tetrahydro-5H- benzo [7] annulen-5 -yl)-3 -isopropoxyazetidine- 1 -carboxamide (130 mg, 0.32 mmol) in 1,4- dioxane (5 mL) were added 1-ethyl-1H-pyrazol-4-amine (36 mg, 0.32 mmol), Pd2(dba)3 (29 mg, 0.032 mmol), S-Phos (26 mg, 0.064 mmol) and Cs2CO3 (312 mg, 0.96 mmol). The mixture was stirred at 100 C for 2 h. After diluted with water (50 mL), the mixture was extracted with EtOAc (60 mL x 2). The combined organic layers were dried (Na2SO4), filtered and concentrated. The crude product was purified by prep-HPLC (CH3CN/H20 with 0.05% NH4OH as mobile phase) to give N-(2-(2-(( 1-ethyl-i H-pyrazol-4-yl)amino)pyrimidin-4-yl)-6,7,8 ,9-tetrahydro-5H- benzo[7]annulen-5-yl)-3-isopropoxyazetidine-1-carboxamide as a yellow solid (129 mg, yield:73%). [0499j Synthesis of 3 -(tert-butoxy)-N-(2-(2-(( 1 -(1 -methylpiperidin-4-yl)- 1H-pyrazol-4- yl)amino)pyrimidin-4-yl)-6,7, 8 ,9-tetrahydro-5H-benzo [7] annulen-5 -yl)azetidine- 1 -carboxamide was similar to that of Example 161. The residue was purified by prep-TLC (DCM/MeOH=10/1) to give 3-Qert-butoxy)-N-(2-(2-((1 -(1 -methylpiperidin-4-yl)- 1H-pyrazol-4-yl)amino)pyrimidin- 4-yl)-6,7, 8 ,9-tetrahydro-5H-benzo [7]annulen-5 -yl)azetidine- 1 -carboxamide (33 mg, yield: 41%) as a yellow solid. ESI-MS (M+H) : 573.3. ?H NMR (400 MHz, CD3OD) 5: 8.26 (d, J = 5.2 Hz, 1H), 7.97 (s, 1H), 7.53 (d, J = 7.6 Hz, 1H), 7.77 (s, 1H), 7.57 (s, 1H), 7.26 (d, J = 8.0 Hz, 1H),7.07 (d, J = 5.2 Hz, 1H), 4.94 (d, J = 10.0 Hz, 1H), 4.52-4.46 (m, 1H), 4.15-4.00 (m, 3H), 3.77-3.69 (m, 2H), 2.94-2.79 (m, 4H), 2.23 (s, 3H), 2.17-2.11 (m, 2H), 2.06-1.85 (m, 7H), 1.82-1.72 (m, 1H), 1.61-1.52(m, 1H), 1.30-1.24(m, 1H), 1.11 (s,9H).

1201935-36-5, The synthetic route of 1201935-36-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIOGEN IDEC MA INC.; SUNESIS PHARMACEUTICALS, INC.; HOPKINS, Brian, T.; MA, Bin; CHAN, Timothy, Raymond; SUN, Lihong; ZHANG, Lei; KUMARAVEL, Gnanasambandam; LYSSIKATOS, Joseph, P.; KOCH, Kevin; MIAO, Hua; WO2015/89337; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

216854-23-8, (S)-tert-Butyl piperidin-3-ylcarbamate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A microwave vial containing 4-iodo-5-nitro-2,3-dihydrofuro[2,3-b]pyridine (2.05 g, 7.02 mmol), tert-butyl (3S)-piperidin-3-ylcarbamate (Combi-Blocks, 1.489 g, 7.435 mmol), DIPEA (1.836 g, 14.20 mmol) and EtOH (12.0 mL) was heated under microwave irradiation at 100 C. for 2 h. The reaction was then concentrated under reduced pressure. The resulting residue was purified by flash chromatography on silica gel (0-100% EtOAc in hexanes) to give the sub-title compound as a yellow solid (2.46 g, 96%). LCMS calc. for C17H25N4O5 (M+H)+: m/z=365.2. found 365.1, 216854-23-8

As the paragraph descriping shows that 216854-23-8 is playing an increasingly important role.

Reference£º
Patent; INCYTE CORPORATION; Li, Yun-Long; Burns, David M.; Feng, Hao; Xue, Chu-Biao; Wang, Anlai; Pan, Jun; US2014/200216; (2014); 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.120014-07-5,2-((1-Benzylpiperidin-4-yl)methylene)-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one,as a common compound, the synthetic route is as follows.

Preparation of l-Benzyl-4-[(5, 6-dimethoxy-l-indanon)-2-v? methylpiperidine hydrochloride (Donepezil Hydrochloride) l-Benzyl-4-[5, 6-dimethoxy-l-indanon)-2-ylidenyl] methyl piperidine was taken in tetrahydrofuran (200ml) followed by addition of palladium-carbon (Ig). The mixture was hydrogenated at 20-30 0C under 1,5 atmospheric pressure for 8 hours, monitored by HPLC analysis and analysis shows ~ 38.5% of debenzylated impurity in the reaction mass.

120014-07-5, 120014-07-5 2-((1-Benzylpiperidin-4-yl)methylene)-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one 10762160, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; IND-SWIFT LABORATORIES LIMITED; WO2007/108011; (2007); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

138007-24-6, tert-Butyl piperidine-4-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 22: tert-Butyl l-(2-(2,4-dioxo-3,4-dihvdrobenzo[g1pteridin-10(2H)-vI)ethyl)piperidine-4- carboxylate; Step 1 Preparation of tert-butyl l-(cvanomethyl)piperidine-4-carboxylate; [0111] To a solution of tert-butyl piperidine-4-carboxylate (750 mg, 4.05 mmol) in anhydrous DCM (15 mL), is added 2-chloroacetonitrile (333 muL, 5.26 mmol) and potassium carbonate (1.7 g, 12.15 mmol). The reaction mixture is stirred at room temperature for 18 h. The reaction mixture is diluted with water (100 mL) and the aqueous layer is extracted with DCM (100 mL). The organic layer is dried over Na2SO4, filtered, and concentrated under reduced pressure. The residue is dry loaded on silica gel and purified by Biotage flash column chromatography using a gradient from 0 to 10percent MeOH in DCM as eluent. Desired product (463 mg) is isolated (yield: 51 percent). percent). 1H NMR (400 MHz, CDCl3) delta 1.44 (s, 9H), 1.73 (m, 2H), 1.93 (m, 2H), 2.19 (m, 1H), 2.35 (m, 2H), 2.79 (m, 2H), 3.5 l (s, 2H)., 138007-24-6

138007-24-6 tert-Butyl piperidine-4-carboxylate 1512676, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; BIORELIX, INC.; COISH, Philip, D.G.; WICKENS, Philp; AVOLA, Stephanie; BABOULAS, Nick; BELLO, Angelica; BERMAN, Judd; KAUR, Harpreet; MOON, David; PHAM, Vinh; ROUGHTON, Andrew; WILSON, Jeffrey; ARISTOFF, Paul, Adrian; BLOUNT, Kenneth, F.; DIXON, Brian, R.; MYUNG, Jayhyuk; OSTERMAN, David; BELLIOTTI, Thomas, R.; CHRUSCIEL, Robert, A.; EVANS, Bruce, R.; LEIBY, Jeffrey, A.; SCHOSTAREZ, Heinrich, J.; UNDERWOOD, Dennis; NAVIA, Manuel; SCIAVOLINO, Frank; WO2011/8247; (2011); 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.4138-26-5,Piperidine-3-carboxamide,as a common compound, the synthetic route is as follows.,4138-26-5

General procedure: During the purification and characterization of amidase from Cupriavidus sp. KNK-J915, an enzyme assay was performed with (R,S)-BNPD as a substrate. The standard reaction mixture (0.2 mL) contained 100 mM potassium phosphate buffer (pH 7.0), 45.8 mM BNPD, and an appropriate amount of the enzyme. After the reaction was performed at 30C for 0.5-1 h, the amount of BNPA was determined using HPLC. One unit of the enzyme was defined as the amount catalyzing the formation of 1 mol of BNPA per minute under the aforementioned condition. Protein content was determined by the Bradford method [11] with BSA as a standard using a kit from Bio-Rad Laboratories Ltd. (Tokyo, Japan).

The synthetic route of 4138-26-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Nojiri, Masutoshi; Taoka, Naoaki; Yasohara, Yoshihiko; Journal of Molecular Catalysis B: Enzymatic; vol. 109; (2014); p. 136 – 142;,
Piperidine – Wikipedia
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142643-29-6, 3-(Boc-aminomethyl)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

64a) {1-[2-(3-Chloro-6-methoxy-quinolin-4-yl)-2-hydroxy-ethyl]-piperidin-3-ylmethyl}-carbamic acid tert-butyl ester (enantiomer1)Epoxide (56f) (900 mg), 3-(N-Boc-aminomethyl)piperidine (819ing) i potassium carbonate (555 mg) and lithium perchlorate (405mg) were suspended in DMF (9 ml) and heated in the microwave for35 minutes at 130C. The mixture was concentrated, the residuedissolved in ethyl acetate and washed with water and brine. Theorganic layer was dried over magnesium sulfate, filtered andevaporated. The residue was purified by flash chromatography(silica gel, dichloromethane/methanol 97:3) to give the desiredproduct (1.6 g).MS (El): m/z: 450 [M+H]+, 142643-29-6

The synthetic route of 142643-29-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MORPHOCHEM AKTIENGESELLSCHAFT FUeR KOMBINATORISCHE CHEMIE; WO2006/21448; (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.91419-52-2,1-Boc-4-Cyanopiperidine,as a common compound, the synthetic route is as follows.,91419-52-2

To a mixture of 4-cyano-piperidine-1-carboxylic acid tert-butyl ester (6.3 g, 30 mmol), K2C03 (4.2 g, 30 mmol) in H20 (50 mL) and EtOH (30 mL) was added hydroxylamine hydrogenchloride (4.17 g, 60 mmol). The mixture was heated under reflux overnight, cooled to room temperature and ethanol was removed in vacuo. The residue was extracted with EtOAc (300 mL). The organic layer was washed successively with H20 and brine. After drying (Na2 SO4), the solvent was removed to afford the desired product

91419-52-2 1-Boc-4-Cyanopiperidine 1514443, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; CYMABAY THERAPEUTICS; MCWHERTER, Charles A.; (176 pag.)WO2018/26890; (2018); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem