Day: September 30, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.79099-07-3,1-Boc-4-Piperidone,as a common compound, the synthetic route is as follows.

79099-07-3, Cvclopropylmethyl-{l-[2-(lH-indazol-4-yl)-4-morpholin-4-yl-thienor3,2- d1pyrimidin-6-ylmethyl1-piperidin-4-yl}-(2-methoxy-ethyl)-amine (108).Prepared via [l-(2-Chloro-4-mophiholin-4-yl-thieno[3,2-d]pyrimidin-6- ylmethyl)-piperidin-4-yl]-cyclopropylmethyl-(2-methoxy-ethyl)-amine, prepared from cyclopropylmethyl-(2-methoxy-ethyl)-piperidin-4-yl-amine. Amine preparation: l-BOC-4-piperidone (500mg) and 2-methoxyethylamine(218muL) were stirred in MeOH at room temperature. After 16 h, sodium borohydride was added (190mg) carefully. After a further 3 h, the reaction mixture was diluted with DCM, washed with water, dried (MgSO4) and the solvent removed in vacuo to yield 4-(2-methoxy-ethylamino)-piperidine-l-carboxylic acid tert-butyl ester (560mg).A mixture of 4-(2-methoxy-ethylamino)-piperidine-l-carboxylic acid tert- butyl ester (525mg), cyclopropylmethyl bromide (218muL) and potassium carbonate (340mg) was heated to reflux in MeCN for 16 h. After cooling the reaction mixture was diluted with chloroform, washed with brine, dried (MgSO4) and the solvent removed in vacuo to yield 4-[cyclopropylmethyl-(2-methoxy-ethyl)-amino]- piperidine-1-carboxylic acid tert-butyl ester (475mg). Removal of the BOC group with HCl yielded the desired compound, which was isolated as the hydrochloride salt.1H NMR (400MHz, CDCl3): -0.01-0.01 (2H, m), 0.40-0.48 (2H, m), 1.45-1.60 (3H, m), 1.62-1.70 (2H, m), 1.97-2.04 (2H, m), 2.33 (2H, d), 2.52-2.61 (IH, m), 2.67 (2H, t), 2.92-3.00 (2H, m), 3.25 (3H, s), 3.34 (2H, t), 3.71 (2H, s), 3.82 (4H, t), 4.00 (4H, t), 7.22 (IH, s), 7.49 (IH, t), 7.48 (IH, d), 8.28 (IH, d), 8.90 (IH, s), 10.00 (IH, br); MS (ESf) 562 (MH+).; 111 { l-[2-(lH-Indazol-4-ylV4-morpholin-4-yl-thienor3,2-d”|pyrimidin-6-ylmethyl1- piperidin-4-vU-(2-methoxy-ethyl)-(2,2,2-trifluoro-ethyl)-amine. Via [l-(2-Chloro-4-mophiholin-4-yl-thieno[3,2-d]pyrimidin-6-ylmethyl)-piperidin-4- yl]-(2-methoxy-ethyl)-(2,2,2-trifluoro-ethyl)-amine, prepared from (2-methoxy- ethyl)-piperidin-4-yl-(2,2,2-trifluoro-ethyl)-amine.Amine preparation: l-BOC-4-piperidinone (2.0Og) and 2-methoxyethylamine (872muL) were stirred together in MeOH (2OmL) at room temperature overnight. Sodium borohydride (760mg) was then added portionwise and the reaction mixture was allowed to stir further at ambient temperature. After 16 h, the solvent was removed in vacuo, the residue was diluted with DCM, washed with brine, dried (MgSO4) and the solvent removed in vacuo. The residue was purified using flash chromatography to yield 4-(2-methoxy-ethylamino)-piperidine-l-carboxylic acid tert-butyl ester as a colourless oil (1.69g).To a solution of 4-(2-methoxy-ethylamino)-piperidine-l-carboxylic acid tert- butyl ester (500mg) in DCM (5mL) and triethylamine (540muL) was added trifluoroacetic anhydride (548muL). The reaction mixture was stirred at room temperature overnight, diluted with DCM, washed with brine, dried (MgSO4) and the solvent removed in vacuo. The residue was purified using flash chromatography to yield 4-[(2-methoxy-ethyl)-(2,2,2-trifluoro-acetyl)-amino]-piperidine- 1 -carboxylic acid tert-huy ester as an oil (685mg).To a solution of 4-[(2-methoxy-ethyl)-(2,2,2-trifiuoro-acetyl)-amino]- piperidine-1 -carboxylic acid tert-butyl ester (685mg) in dry THF (7mL) was added borane-methyl sulfide complex (405uL) at O0C under inert atmosphere. The reaction mixture was refluxed for 3 h, and then stirred at room temperature overnight, quenched with MeOH, diluted with DCM, washed with brine, dried (MgSO4) and the solvent removed in vacuo. The residue was purified using flash chromatography to yield 4-[(2-methoxy-ethyl)-(2,2,2-trifluoro-ethyl)-amino]-piperidine-l -carboxylic acid tert-huy ester as an oil (635mg). Treatment of this compound with HCl in DCM/MeOH furnished the desired amine, isolated as the hydrochloride salt. EPO 1H NMR (400MHz, CDCl3) 1.55-1.64 (2H, m), 1.76-1.82 (2H, m), 2.12-2.18 (2H, m), 2.58-2.62 (IH, m), 2.86 (2H, t, J=6.3Hz), 3.03-3.08 (2H, m), 3.20 (2H, q, J=9.4Hz), 3.33 (3H, s), 3.45 (2H, t, J=6.4Hz), 3.84 (2H, s), 4.00 (4H, t, J=5.1Hz), 7.22 (IH, s), 7.49 (IH, t, J=7.2Hz), 7.48 (IH, d, J=8.3Hz), 8.28 (IH, d, J=7.1Hz), 8.90 (IH, s), 10.00 (IH, br); MS (ESI+) 590 (MH+).

As the paragraph descriping shows that 79099-07-3 is playing an increasingly important role.

Reference£º
Patent; PIRAMED LIMITED; WO2006/46031; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

2971-79-1, Methyl piperidine-4-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2971-79-1, General procedure: A solution of 56 (1.50 g, 7.16 mmol), the appropriate secondary amine (8.59 mmol, 1.20 equiv) and diisopropylethylamine (1.50 mL, 8.59 mmol) in n-butanol (15 mL)was heated in a microwave reactor using variable wattage to 140 C for 1 h. The mixture was concentrated and purified by flash column chromatography on silica, eluting with 9:1 dichloromethane/methanol, to give gave 58-63.

The synthetic route of 2971-79-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Caldwell, John J.; Veillard, Nicolas; Collins, Ian; Tetrahedron; vol. 68; 47; (2012); p. 9713 – 9728,16;; ; Article; Caldwell, John J.; Veillard, Nicolas; Collins, Ian; Tetrahedron; vol. 68; 47; (2012); p. 9713 – 9728;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

163271-08-7, tert-Butyl (4-methylpiperidin-4-yl)carbamate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 6-chloro-3-(2,3-dichlorophenyl)pyrazine-2-carbonitrile (50 mg, 176 mupiiotaomicron, 1 equiv) and ter/-butyl(4-methylpiperidin-4-yl)carbamate (56.5 mg, 264 mupiiotaomicron, 1.5 equiv) in dioxane (1 mL) and DIPEA (1 mL) was warmed to 120 C and stirred for 2 hours. The mixture was then concentrated under reduced pressure to give ter/-butyl(l-(6-cyano-5-(2,3- dichlorophenyl)pyrazin-2-yl)-4-methylpiperidin-4-yl)carbamate (80 mg, crude) as a yellow oil which was used directly in the next step without further purification. LC-MS (ESI): m/z: [M + H] calculated for C22H25C12N502: 462.14; found 462.0., 163271-08-7

The synthetic route of 163271-08-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; REVOLUTION MEDICINES, INC.; JOGALEKAR, Ash; WON, Walter; KOLTUN, Elena S.; GILL, Adrian; MELLEM, Kevin; AAY, Naing; BUCKL, Andreas; SEMKO, Christopher; KISS, Gert; (496 pag.)WO2018/13597; (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.123495-48-7,(S)-Ethyl piperidine-2-carboxylate hydrochloride,as a common compound, the synthetic route is as follows.

Example 27 (S)-1-(3-(10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-propyl)-2-piperidinecarboxylic acid hydrochloride Crude (S)-(-)-2-piperidinecarboxylic acid (19.5 g, prepared as described in example 26) was suspended in ethanol (250 ml), and thionyl chloride (40 ml, 0.46 mol) was added dropwise. After addition was complete, the suspension was heated at reflux temperature for 2 h. The mixture was filtered hot, and the filtrate was cooled to room temperature. Filtration and evaporation in vacuo afforded an oil, which was crystallized by rubbing. Ethanol (10 ml) was added, followed by slow addition of diethyl ether (150 ml). The precipitated solid was filtered off, washed with diethyl ether and dried by suction to give 13.8 g (35% calculated from 2-piperidinecarboxylic acid) (S)-(-)-2-piperidinecarboxylic acid ethyl ester hydrochloride. [alpha]25D=-10.7 (c=4.5% in water) Gas Chromatography (run as described in example 26) of N-acetyl derivative: Rt=47.2 minutes. Enantiomeric excess=96% 5-(3-Bromo-1-propylidene)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene (2.7 g, 8.6 mmol, prepared as described in WO 9518793), potassium carbonate (7.14 g, 52 mmol), potassium iodide (1.4 g,8.6 mmol), and (S)-(-)-2-piperidinecarboxylic acid ethyl ester hydrochloride (3.3 g, 17 mmol) were mixed in methyl ethyl ketone (50 ml) and heated at reflux temperature for 3 days. After cooling to room temperature, ethyl acetate (100 ml) was added and the mixture was washed with water (2*100 ml), dried. (MgSO4) and evaporated in vacuo. The residue was purified by column chromatography on silica gel (600 ml), using a mixture of ethyl acetate and heptane (1:4) as eluent. This afforded 2.3 g (69%) of (S)-1-(3-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-propyl)-2-piperidinecarboxylicacid ethyl ester as an oil. TLC: Rf=0.22 (SiO2: ethyl acetate/heptane=1:4), 123495-48-7

As the paragraph descriping shows that 123495-48-7 is playing an increasingly important role.

Reference£º
Patent; Novo Nordisk A/S; US6239148; (2001); B1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1029413-55-5,tert-Butyl 4-(4-amino-1H-pyrazol-1-yl)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

[0554j A mixture of 2-chloro-4-methoxypyrimidine (970 mg, 6.7 mmol), tert-butyl 4-(4- amino-1H-pyrazol-1-yl)piperidine-1-carboxylate (1.8 g, 6.77 mmol), S-phos (548 mg, 1.35 mmol), Pd2(dba)3 (577 mg, 0.63 mmol) and NaOtBu (1.9 g, 20.2 mmol) in 1,4-dioxane (18 mL) was stirred at 115 C for 2 h under nitrogen. After dilution with EtOAc (200 mL), the mixture was washed with water and brine. The organic phase was concentrated and the residue was purified by silica gel colunm (petroleum ether: EtOAc , 4:1 to 2:1) to give the compound ten?butyl 4-(4-((4-methoxypyrimidin-2-yl)amino)- 1H-pyrazol- 1 -yl)piperidine- 1 -carboxylate (1.15 g, yield: 48%) as a gray solid. ESI-MS (M+H): 375.2.

1029413-55-5, As the paragraph descriping shows that 1029413-55-5 is playing an increasingly important role.

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

40064-34-4, Piperidine-4,4-diol hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

PREPARATION 62 N-t-Butoxycarbonyl-4-piperidone A solution of di-t-butyl dicarbonate (56.8 g, 0.26 mole) in acetonitrile (100 ml) was added dropwise to a stirred, ice-cooled suspension of 4-piperidone hydrochloride monohydrate (40.0 g, 0.26 mole) in triethylamine (26.3 g, 0.26 mole) and acetonitrile (300 ml). After a further 5 days the reaction mixture was filtered and the filtrate evaporated under reduced pressure to give an off-white solid (69 g) which was purified by chromatography on silica gel, using hexane:ether (1:1) as eluant, to provide the title compound (37.5 g) as a white solid, m.p. 74-75 C. Rf 0.60 (SS 17). Found: C,60.36; H,8.78; N,6.88. C10 H17 NO3 requires C,60.28; H,8.60; N,7.03%., 40064-34-4

As the paragraph descriping shows that 40064-34-4 is playing an increasingly important role.

Reference£º
Patent; Pfizer Inc.; US5917034; (1999); 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.79099-07-3,1-Boc-4-Piperidone,as a common compound, the synthetic route is as follows.

EXAMPLE 10; N-Isopropyl-N-piperidin-4-yl-3-trifluoromethylbenzenesulfonamide (19); [0258] NaB(OAc)3H (14 g, 66 mmol, Aldrich) was added to a mixture of compound 14 (10 g, 50 mmol, Aldrich), compound 15 (3 g, 52.5 mmol, Aldrich), molecular sieves (4A beads, 2Og, Aldrich) in DCE (200 ml) at 0 0C. The resulting mixture was stirred at room temperature for 24 hours. The reaction mixture was quenched with MeOH (2ml), filtered over celite, washed with water, 2N NaOH and concentrated under vacuum to afford crude compound 16 as a colorless oil. Compound 17 (12 g, 49 mmol, Aldrich) was added to a mixture of the above crude compound 16, TEA (10 ml) and DCM (10 ml) at room temperature. The resulting mixture was heated and stirred at 37 0C for 2 days. The reaction mixture was then cooled to room temperature, washed with water (10 ml), brine, concentrated and purified by column (silica gel, EtOAc/hexanes 3/7) to obtain compound 18 as a sticky oil (10 g, yield 45% in two steps), which was dissolved in 100 ml of 1,4-dioxane. HCl (10 ml, concentrated aq.) was added to the 1,4-dioxane solution at room temperature. The resulting mixture was stirred at room temperature for 48 hours, and concentrated under vacuum. The residue was washed with ethyl ether, and dried to obtain the title compound 19 as HCl-salt, which was suspended in EtOAc, and neutralized with IN NaOH aq, concentrated and dried under vacuum to give compound 19 as colorless oil (5 g, yield 65%)., 79099-07-3

The synthetic route of 79099-07-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; EURO-CELTIQUE S.A.; SHIONOGI & CO., LTD.; WO2007/118854; (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.123855-51-6,tert-Butyl 4-(hydroxymethyl)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

156 6-(4-Imidazol- 1 – ylmethyl-piperidin- 1 -ylmethyl)-2-( 1 H-indazol-4- yl)-4- mophiholin-4-yl-thieno[3,2-dlpyrimidine.Via 2-chloro-6-(4-imidazol- 1 -ylmethyl-piperidin- 1 -ylmethyl)-4-morpholin-4- yl-thieno[3,2-d]pyrimidine, prepared from 4-imidazol-l-ylmethyl-piperidine.Amine preparation: To a solution of 4-hydroxymethyl-piperidine-l- carboxylic acid tert-butyl ester (250mg), in dry THF (15mL), was added carbon tetrabromide (769mg), and triphenyl phosphine (609mg). The reaction mixture was stirred at room temperature for 24 h, and then the solvents were evaporated in vacuo to give a residue which was purified by flash chromatography to give 4- bromomethyl-piperidine-1-carboxylic acid tert-butyl ester (279mg), as a colourless oil. To a solution of 4-bromomethyl-piperidine-l-carboxylic acid tert-butyl ester (240mg), in dry DMF (5.OmL), was added imidazole (129mg). The reaction mixture was heated in a sealed reaction vial at 1000C for 24 h, then cooled and the contents evaporated onto flash silica for purification. Treatment of this compound with HCl in DCM/MeOH yielded the desired amine, isolated as the hydrochloride salt. 1H NMR (400 MHz, 123855-51-6, 123855-51-6 tert-Butyl 4-(hydroxymethyl)piperidine-1-carboxylate 2764081, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; PIRAMED LIMITED; WO2006/46031; (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.19733-56-3,4-(Piperidin-3-yl)aniline,as a common compound, the synthetic route is as follows.

To a mixture of 4-(piperidin-3-yl) aniline (Compound 16) (0.5 g) in acetone (5 mL), succinic acid (0.36 g) was charged at reflux temperature. The reaction mass was stirred at reflux temperature for 30 minute. The reaction mass was cooled to 20-25C and stirred further for 3 h. The solid obtained was filtered, washed with acetone (3 mL) and dried under vacuum at 50-55C to afford the titled compound (Yield: 0.63 g; HPLC Purity: >95.0% ).

19733-56-3, As the paragraph descriping shows that 19733-56-3 is playing an increasingly important role.

Reference£º
Patent; TEVA PHARMACEUTICALS USA, INC.; TEVA PHARMACEUTICALS INTERNATIIONAL GMBH; LUTHRA, Parven, Kumar; VASOYA, Sanjay, Lakhabhai; PATIL, Bhatu, Tumba; TANEJA, Amit, Kumar; SRIVASTAV, Naveen, Chandra; SINGH, Rinku; (63 pag.)WO2019/36441; (2019); 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.79098-85-4,3-(Piperidin-4-yl)indolin-2-one hydrochloride,as a common compound, the synthetic route is as follows.,79098-85-4

EXAMPLE 179 4-(2-Oxo-2,3-dihydroindol-3-yl)-1-(3-phenoxypropyl)piperidine STR215 From a mixture of 4-[2-oxo-2,3-dihydroindol-3-yl)piperidine hydrochloride (198 mg, 0.73 mmol), 3-phenoxy-propyl chloride (476 mg, 2.22 mmol) and K2 CO3 (138 mg) in toluene (15 mL) was obtained 170 mg (70%) of the title compound as a yellow oil, 1 H NMR (CDCl3): 1.42-1.50 (m, 2H), 1.79-2.03 (m, 6H), 2.10-2.15 (m, 1H), 2.47-2.52 (m, 2H), 2.90-3.04 (m, 2H), 3.408 (d, 1H, J=3.5), 7.001 (t, 1H, J=7.5), 7.022 (t, 1H, J=7.5), 7.23-7.29 (m, 3H), 7.909 (s, 1H). The hydrochloride mp 182-3 C.

The synthetic route of 79098-85-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Warner-Lambert Company; Cocensys, Incorporated; US6124323; (2000); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem