Month: August 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.957855-54-8,4-Amino-2-fluoro-N-(1-methylpiperidin-4-yl)benzamide,as a common compound, the synthetic route is as follows.

957855-54-8, General procedure: Dimethyl (4-aminobenzyl)phosphonate (1.1 equiv), X-phos (0.1equiv) and Cs2CO3 (3.0 equiv) in 1,4-dioxane, and Pd(AcO)2 (0.05equiv) were added to solutions of compounds 10a-h (1 equiv) undera nitrogen atmosphere. The mixture was purged with nitrogenfor 5 min and then heated at 90 C until the reactionwas complete.The mixture was diluted with ethyl acetate, and the organic layerwas washed with saline, dried over anhydrous Na2SO4, filtered andconcentrated. The residue was purified using column chromatographyto afford compounds 11a-h.

The synthetic route of 957855-54-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Chen, Yixuan; Cheng, Maosheng; Hao, Chenzhou; Wang, Ruifeng; Wu, Tianxiao; Yang, Bowen; Yu, Sijia; Zhao, Dongmei; Zhao, Xiangxin; European Journal of Medicinal Chemistry; vol. 188; (2020);,
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503614-91-3,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.503614-91-3,Ethyl 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate,as a common compound, the synthetic route is as follows.

Intermediate-E (35g, 0.0716 moles) is suspended in 30 % aq. ammonia solution. Mixture was heated to 80-90C in an autoclave. Aqueous ammonia develops in- build pressure ofl-2 kg. Progress of the reaction is monitored on TLC/HPLC. When reaction was completed in -l0 hrs, reaction mass is cooled to RT and diluted with water. Product is filter and washed with water, dried at 60-65 c to obtain crude apixaban 23-25 gm with HPLC purity 98.5%. This crude product contains acid impurity approx-1.0-l.5%. Crude apixaban is further dissolved in MDC and washed with 2.0-5.0% bicarbonate solution. MDC layer is then concentrated under reduced pressure and crystallize using mixture of solvents methanol water to obtain pure apixaban with l-IPLC purity >99% (yield 6 1%).

503614-91-3 Ethyl 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate 22240488, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; WANBURY LTD.; NITIN SHARADCHANDRA PRADHAN; SACHIN ULHAS SONAVANE; DAYAGHAN GHANGADHAR PATIL; UTTAM SAKHARAM PUJARI; RAVINDRA BHAUSAHEB PAGIRE; WO2015/111073; (2015); A3;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.29608-05-7,4-(Piperidin-1-ylmethyl)aniline,as a common compound, the synthetic route is as follows.

WORKING EXAMPLE 71 (Production of Compound 71) In THF (10 ml) was dissolved 3-(2-methylphenyl)cinnamic acid (0.48 g), and to the solution were added oxalyl chloride (0.35 ml) and a drop of DMF. The mixture was stirred at room temperature for 1 hour and concentrated under reduced pressure. The residue was dissolved in THF (20 ml), and to the solution were added 1-(4-aminobenzyl)piperidine (0.38 g) and triethylamine (0.34 ml) at room temperature. The reaction mixture was stirred at room temperature for 2 hours, and to the mixture was added water (50 ml). The mixture was extracted with ethyl acetate. The organic layer was washed with saturated sodium chloride solution, dried with anhydrous magnesium sulfate and concentrated under reduced pressure. The residue was washed with ethyl acetate-diisopropylether to give (E)-N-[4-(piperidinomethyl)phenyl]-3-(2-methyl-phenyl)-cinnamamide (Compound 71) (0.75 g) as pale yellow amorphous. Elemental Analysis for C28 H30 N2 O.0.5H2 O; Calcd: C, 80.16; H, 7.45; N, 6.68. Found: C, 80.15; H, 7.38; N, 6.64. 1 H NMR (200 MHz, CDCl3) delta: 1.45 (2H, m), 1.58 (4H, m), 2.27 (3H, s), 2.39 (2H, m), 3.47 (2H, s), 6.58 (1H, d, J=15.4 Hz), 7.24-7.35 (7H, m), 7.39-7.58 (6H, m), 7.80 (1H, d, J=15.6 Hz)., 29608-05-7

The synthetic route of 29608-05-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Takeda Chemical Industries, Ltd.; US6166006; (2000); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.741687-07-0,tert-Butyl 4-amino-4-ethylpiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.,741687-07-0

EXAMPLE 7: tert-hutyl 4-ethyl-4-(5-oxopyrrolo[4,3,2-de][2,6]naphthyridin- 4( l/f,3/f,5H)-yl)piperidine- 1 -carboxylate[0168] 1 -tert-QvXy 4-methyl 3-formyl- lH-pyrrolo[2,3-delta]pyridine- 1 ,4-dicarboxylate (211 mg, 0.692 mmol) was dissolved in MeOH (10 mL) and tert-hvXy 4-amino-4- ethylpiperidine-1 -carboxylate (158 mg, 0.692 mmol) were added followed by 2 drops of acetic acid. The solution was allowed to stir at room temperature for 2 h. Then sodium cyanoborohydride (44 mg, 0.692 mmol) was added over the course of 6 h at room temperature. The solution was quenched with water and extracted with ethyl acetate. The organics were dried over MgSO4 and concentrated in vacuo. Purification by silica gel chromatography (70% EtOAc/Hexanes) gave 127 mg of l-tert-buty 4-methyl 3-((l -(tert- butoxycarbonyl)-4-ethylpiperidin-4-ylamino)methyl)- lH-pyrrolo[2,3-delta]pyridine- 1 ,A- dicarboxylate. [M+H] found 417.[0169] 1 -tert-BvXy 4-methyl 3 -(( 1 -(tert-butoxycarbonyl)-4-ethylpiperidin-4- ylamino)methyl)-lH-pyrrolo[2,3-delta]pyridine-l,4-dicarboxylate (123 mg, 0.238 mmol) was stirred in MeOH (3 mL), IN NaOH (3 mL), and THF (2 mL) for 16 h. The mixture was concentrated in vacuo. Purification via basic prep HPLC 20% to 50% B in A gave 60 mg of 3-((l-(fert-butoxycarbonyl)-4-ethylpiperidin-4-ylamino)methyl)-lH-pyrrolo[2,3-6]pyridine-4-carboxylic acid. 1U NMR (400 MHz, CD3OD) delta 8.29 (d, IH, J= 4.8 Hz),7.68 (s, IH), 7.52 (d, IH, J= 5.1 Hz), 4.31 (s, 2H), 3.95-4.01 (m, IH), 2.03 (q, 2H, J= 7.6Hz), 1.92-1.94 (m, 4H), 1.47 (s, 9H), 1.46 (m, 2H), 1.07 (t, IH, J= 7.3 Hz). [M+H] found403.[0170] 3-((l-(tert-Butoxycarbonyl)-4-ethylpiperidin-4-ylamino)methyl)-l/-f-pyrrolo[2,3-6]pyridine-4-carboxylic acid (50 mg, 0.124 mmol), HATU (94 mg, 0.248 mmol), and A- dimethylaminopyridine (46 mg, 0.373 mmol) were stirred in DMF (3 mL) at room temperature for 1 h. The solution was concentrated in vacuo to give the title compound which was used without further purification.

741687-07-0 tert-Butyl 4-amino-4-ethylpiperidine-1-carboxylate 45095672, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; DONG, Qing; LAWSON, John, David; WALLACE, Michael, B.; KANOUNI, Toufike; WO2010/144486; (2010); A1;,
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74892-82-3, (2R,4R)-Ethyl 4-methylpiperidine-2-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

74892-82-3, 35kg of tetrahydrofuran,Add to the 50L reactor,2kg of N2-(3-methyl-8-quinolinesulfonyl)-NG-nitro-L-arginine was added.After warming up and refluxing,Cool down to -30 C,Keep 2 kg of phosphorus oxychloride at this temperature.Stir for 2 hours with heat.TLC test,The material points disappear,Then add 1.5 kg of ethyl (2R,4R)-4-methyl-2-piperidinecarboxylate at this temperature.Stir for 2 hours with heat.TLC detects the reaction completely,Layered with saturated brine,The organic phase is concentrated under reduced pressure to an oil.Add saturated NaHCO3 solution and 35 kg of dichloromethane,Layered,The organic phase is washed to neutral,Dry over anhydrous sodium sulfate,Distilling the solvent under reduced pressure,Obtaining a yellow oily product,The content is 81.5%,The yield was 72.6%.

74892-82-3 (2R,4R)-Ethyl 4-methylpiperidine-2-carboxylate 10313307, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; Tianjin Pharmaceutical Institute Pharmaceutical Co., Ltd.; Wang Yuewei; Xi Pengyan; Wang Yang; Jia Xianyong; Zhao Zhao; (7 pag.)CN109912570; (2019); A;,
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73889-19-7, tert-Butyl (1-benzylpiperidin-4-yl)carbamate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

73889-19-7, A solution of D6 (10G, 3. 4MMOL) in METHANOL (150M1) was hydrogenated at 50psi in a Parr hydrogenator using 10% Palladium on carbon catalyst (800mg) for 18h. Catalyst was filtered off and the filtrate concentrated under reduced pressure to afford the product as a white solid

The synthetic route of 73889-19-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXO GROUP LIMITED; WO2004/78749; (2004); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.149353-75-3,4-(1-(tert-Butoxycarbonyl)piperidin-4-yl)benzoic acid,as a common compound, the synthetic route is as follows.

1- (N-t-Butoxycarbonylamino)-2-aminobenzene (Method 17,3. 1 g, 14.7 mmol) was added to a stirred solution of 4- (l-t-butoxycarbonylpiperidin-4-yl) benzoic acid (4.1 g, 13.4 mmol) in DMF (50 ml) and the mixture stirred at ambient temperature for 10 minutes. 4- (4, 6- dimethoxy-1, 3,5-triazinyl-2-yl)-4-methylmorpholinium chloride (Method 18,4. 45 g, 16.1 mmol) was added and the mixture stirred at ambient temperature for 24 hours. The solvent was evaporated and the residue was dissolved in ethyl acetate (100 ml) and washed with water. The organics were dried over magnesium sulfate, filtered and evaporated. The resultant gum was purified by flash chromatography using 1% methanol/dichloromethane to give the title compound as a foam (5.44 g, 82%) ; NMR Spectrum : (DMSO-ds) 1.41 (s, 9H), 1.43 (s, 9H), 1.54 (m, 2H), 1.77 (m, 2H), 2.79 (m, 3H), 4. 08 (m, 2H), 7.15 (m, 2H), 7.40 (d, 2H), 7.52 (m, 2H), 7. 87 (d, 2H), 8.60 (br, 1H), 9.74 (br, 1H), Mass Spectrum: (M+E-Boc) 396.

149353-75-3, The synthetic route of 149353-75-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2003/87057; (2003); A1;,
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Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2971-79-1,Methyl piperidine-4-carboxylate,as a common compound, the synthetic route is as follows.,2971-79-1

To a stirred solution of methyl 4-piperidinecarboxylate (4.5 g, 30 mmol) in CH2Cl2(10 mL), propionyl chloride (3.5 mL, 40 mmol) and triethyl amine (5.6 mL, 37 mmol)were added slowly at 0 C. The reaction was continued at 0 C for 4 h. Then thereaction was quenched by adding water (10 mL), and extracted with CH2Cl2(2¡Á20 mL). The combined organic layer was washed with water, brine, dried overanhydrous Na2SO4 and filtered. After the solvent was removed under reducedpressure, methanol (20 mL) and aqueous NaOH (5.0 N, 20 mL) were added to theresidue. The resulted mixture was stirred at RT for 16 h. The methanol was removedunder reduced pressure, and pH of the solution was adjusted to 6-7 with 5 N aqueousHCl. The mixture was extracted with CH2Cl2 (3¡Á50 mL), and the combined organiclayer was washed with water, brine, dried over anhydrous Na2SO4 and filtered. Thesolvent was evaporated under vacuum, and the crude product was purified by silicagel column chromatography with PE/EtOAc (3:1) as eluent to afford 3 as a whitesolid (5.11 g, 88%), mp 86.5-87.8 C. 1H NMR (600MHz, CDCl3): delta 4.41 (d,J=13.3 Hz, 1H), 3.82 (d, J=13.6 Hz, 1H), 3.16-3.11 (m, 1H), 2.88-2.83 (m, 1H),2.60-2.56 (m, 1H), 2.39- 2.35 (m, 2H), 1.98-1.96 (m, 2H), 1.74-1.63 (q, J=7.4 Hz, 2H), 1.15 (t, J=7.4 Hz, 3H). (LC-MS, m/z): Calcd for C9H16NO3 ([M+H]+) 186.2, found:186.4.

As the paragraph descriping shows that 2971-79-1 is playing an increasingly important role.

Reference£º
Article; Jia, Limeng; Miao, Caihong; Dong, Fugui; Li, Wei; Wang, Min; Zheng, Qi-Huang; Xu, Zhidong; Bioorganic and Medicinal Chemistry Letters; vol. 29; 13; (2019); p. 1654 – 1659;,
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