Day: March 25, 2022

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.62718-31-4,1-Benzylpiperidine-4-carbonitrile,as a common compound, the synthetic route is as follows.

To a suspension of LiAlH4 (4.84 g, 0.128 mol) in dry Et2O (40ml) under an argon atmosphere at 00C was dropwise added a solution of l-benzyl-4-cyano-piperidine (18.3 g, 91.5 mmol) in dry Et2O (80 ml) and the mixture was stirred at room temperature for 24 h. The reaction mixture was treated carefully with H2O (10 ml) , 10% aqueous NaOH (10 ml) and H2O (30 ml) to give a mineral precipitate. The precipitate was filtered through a pad of kieselguhr, washed with Et2O and the filtrate evaporated in vacuo to leave the product as an oil (21.4 g, 82.3%) . EPO 1H-NMR (200 MHz, CDCl3): delta 7.37-7.22 (m, 5 H), 6.42 (br s, 1 H), 5.84 (br s, 1 H), 3.51 (s, 2 H), 2.94 (d, 2 H), 2.16-1.67 (m, 7 H), 62718-31-4

The synthetic route of 62718-31-4 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; BIO-MEDISINSK INNOVASJON AS; COCKBAIN, Julian; WO2007/7072; (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.53617-36-0,1-Methyl-4-(piperidin-4-yl)piperazine,as a common compound, the synthetic route is as follows.

7g) (R)-1-(8-methyl-imidazo[1.5-a]pyridin-6-ylmethyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylate A solution of 115 mg (0.18 mmol) (R)-1-carboxy-2-(8-methyl-imidazo[1,5-a]pyridin-6-yl)-ethyl 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylate, 70 mg (0.22 mmol) TBTU and 40 muL (0.29 mmol) triethylamine in 10 mL THF and 1 mL DMF was stirred for 1 h at RT. Then 50 mg (0.27 mmol) 1-methyl-4-piperidin-4-yl-piperazine were added and the reaction mixture was stirred overnight at RT. To complete the reaction another 70 mg TBTU and 50 mg 1-methyl-4-piperidin-4-yl-piperazine were added, the mixture was stirred for a further 65 h at RT and again combined with 70 mg TBTU, 50 mg 1-methyl-4-piperidin-4-yl-piperazine, 40 muL triethylamine and 1 mL DMF and stirred overnight at RT. 10 mL semisaturated NaHCO3 solution were added to the reaction mixture, it was extracted twice with 30 mL EtOAc and the combined organic phases were dried over Na2SO4. After the desiccant and solvent had been eliminated the residue was purified by HPLC. The fractions containing the product were combined and lyophilised. Yield: 49 mg (29percent of theory) ESI-MS: (M+H)+=657 retention time (HPLC): 2.0 min (method B), 53617-36-0

As the paragraph descriping shows that 53617-36-0 is playing an increasingly important role.

Reference：
Patent; Boehringer Ingelheim International GmbH; US2005/256099; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

32188-75-3, 5-Nitro-2-(piperidin-1-yl)benzonitrile is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 2; 2-(1-piperidinyl)-5-(amino)benzonitrile; The 2-(1-piperidinyl)-5-(nitro)benzonitrile (25 g, 108 mmol) was solubilized in methanol (400 ml). A spatula tip of Pd/C was added to the mixture and the crude was stirred for 16 hours under hydrogen atmosphere. The mixture was filtered on Celite, concentrated and the expected product was isolated by recrystallization in an equimolar volume of dichloromethane and cyclohexane. Yield: 87%

32188-75-3, As the paragraph descriping shows that 32188-75-3 is playing an increasingly important role.

Reference：
Patent; GENFIT; US2006/79696; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1187173-43-8, 2,7-Diazaspiro[4.5]decan-1-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2,7-Diazaspiro[4.5]decan-1 -one hydrogen chloride (430 mg, 2.255 mmol) was dissolved in dichloromethane (4 mL), and triethylamine (0.628 mL, 4.53 mmol) was added followed by 2-bromo-4-(trifluoromethyl)benzenesulfonyl chloride (804 mg, 2.484 mmol). After stirring for 20 h the reaction mixture was concentrated in vacuo. The resulting residue was redissolved in EtOAc, washed with aqueous 1 M HCI followed by washing by saturated aqueous Na2C03. The organic layer was passed through a hydrophobic frit, concentrated in vacuo and recrystallised from methanol to give 7-{[2-bromo-4-(trifluoromethyl)phenyl]sulfonyl}-2,7-diazaspiro[4.5]decan-1 -one (395 mg, 0.877 mmol, 38% yield). The mother liquor was concentrated in vacuo to give the following impure material: 7-{[2-bromo-4-(trifluoromethyl)phenyl]sulfonyl}- 2,7-diazaspiro[4.5]decan-1 -one (419 mg, 0.548 mmol, 57.7% purity by mass, 24% yield), a mixture of desired product and 2-bromo-4-(trifluoromethyl)benzenesulfonyl chloride (1 :1 by molar equivalence). 1 H NMR (400 MHz, DMSO-c/6) delta ppm 1.46 – 1 .63 (m, 3 H) 1.65 – 1.74 (m, 1 H) 1.87 – 1.99 (m, 2 H) 2.74 – 2.80 (m, 1 H) 2.83 (d, J=12.50 Hz, 1 H) 3.05 – 3.20 (m, 2 H) 3.43 (d, J=12.39 Hz, 1 H) 3.72 (d, J=1 1.40 Hz, 1 H) 7.74 (s, 1 H) 7.97 (dd, J=8.28, 1.21 Hz, 1 H) 8.18 (d, J=8.00 Hz, 1 H) 8.29 (d, J=1.15 Hz, 1 H). MS ES+ve m/z 441 (M+H)., 1187173-43-8

The synthetic route of 1187173-43-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CONVERGENCE PHARMACEUTICALS LIMITED; GLEAVE, Robert James; HACHISU, Shuji; PAGE, Lee William; BESWICK, Paul John; WO2011/141728; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

21168-72-9, 2-(4-(Aminomethyl)piperidin-1-yl)ethanol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The general synthesis of compound D-9 is illustrated in Scheme 4. The carboxylic acid group of intermediate D-1 is converted to ethyl ester. The reactionsof tert-butyl acetate substitution with K2C03 and tert-butyl eater hydrolysis with TFA are followed to afford acetic acid intermediate D-4. The intermediate D-4 is chlorinated with oxalyl chloride and DMF and coupled with 3-aminoisonicotinamide to afford the amide intermediate D-6. Subsequent cyclization with NaOtBu and hydrolysis with NaOH lead to intermediate D-8. This is followed by amide coupling reaction with HATU, which leads to amide compound D-9.

21168-72-9, The synthetic route of 21168-72-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; DONG-A SOCIO HOLDINGS CO., LTD.; KIM, Myeong-seop; PARK, Taesun; YOON, Taeyoung; YANG, Seung Min; KIM, Hae-Sun; KIM, Jun Gyu; (285 pag.)WO2016/68580; (2016); 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.1104083-27-3,tert-Butyl 3-hydroxy-3-methylpiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Into a 250-mL round-bottomed flask, was placed tert-butyl 3-hydroxy-3- methylpiperidine-l-carboxylate (3 g, 13.9 mmol, 1 eq.), DCM (60 mL), pyridine (2.2 g, 0.03 mmol, 2 eq.). This was followed by the addition of a solution of 4-nitrophenyl carbonochloridate (8.4 g, 0.04 mmol, 3 eq.) in DCM (30 mL) dropwise with stirring at 0 C. The resulting solution was stirred for 3 days at rt. The reaction was then quenched by the addition of water (50 mL). The resulting mixture was washed with H2O (1 x 50 mL). The mixture was dried over anhydrous sodium sulfate and concentrated. The residue was applied onto a silica gel column with ethyl acetate :petroleum ether (10:90). This resulted in 2.5 g (47.16%) of tert-butyl 3-methyl-3-[[(4-nitrophenoxy)carbonyl]oxy]piperidine-l-carboxylate as a colorless oil.

1104083-27-3, As the paragraph descriping shows that 1104083-27-3 is playing an increasingly important role.

Reference：
Patent; PRINCIPIA BIOPHARMA INC.; LOU, Yan; OWENS, Timothy Duncan; BRAMELD, Kenneth Albert; GOLDSTEIN, David Michael; (302 pag.)WO2019/99582; (2019); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

952681-82-2, 2-(1′-(tert-Butoxycarbonyl)spiro[chroman-2,4′-piperidine]-4-yl)acetic acid is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 5B Preparation of 5.10:[0252] To a solution of the carboxylic acid 5.7 (866 mg, 2.4 mmol) in acetonitrile (40 rnL) was added ./V,./V-diisopropylethylamine (2.6 rnL, 15 mmol) and glycine methyl ester hydrochloride (5.9) (480 mg, 3.8 mmol). The reaction mixture was cooled with ice-bath and TBTU (930 mg, 2.9 mmol) was added in small portions to the reaction mixture. The reaction mixture was stirred at room temperature overnight. The reaction mixture was concentrated and dissolved in ethyl acetate. The organic solution was washed with saturated aqueous sodium bicarbonate and dried over sodium sulfate. Evaporation of the solvent provided the crude product, which was chromato graphed using ethyl acetate/hexane (2:1) as eluent to yield the product 5.10. Yield:94%.1U NMR (400 MHz, CDCl3) delta 7.20 (m, IH), 7.12 (m, IH), 6.90 (m, 2H), 6.00 (brs, IH), 4.09 (d, 2H), 3.90 (m, IH), 3.78 (s+m, 4H), 3.48 (m, IH), 3.33 (m, IH), 3.03 (m, IH), 2.96 (dd, IH), 2.29 (dd, IH), 2.03 (m, IH), 2.83-2.57 (m, 4H), 1.48 (s+m, 10H)., 952681-82-2

As the paragraph descriping shows that 952681-82-2 is playing an increasingly important role.

Reference：
Patent; ADOLOR CORPORATION; WO2007/118151; (2007); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

71985-80-3, 1-Methylpiperidine-4-carboxylic acid hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

71985-80-3, N-Methylisonipecotic acid hydrochloride ( 0.5 g) was dissolved in dry SOC12 (1.5 mL). The mixture was then heated at 80 C for 2 hours under argon. Cooling and evaporation to dryness afforded a yellow solid which was used without further purification.

The synthetic route of 71985-80-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY; TAXIS PHARMACEUTICALS, INC.; LAVOIE, Edmond J.; PARHI, Ajit; PILCH, Daniel S.; ZHANG, Yongzheng; KAUL, Malvika; WO2014/74932; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

236406-22-7, 1-Boc-4-(Aminomethyl)-4-methylpiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a 0 oC solution of tert-butyl 4-(aminomethyl)-4-methylpiperidine-1- carboxylate (7.0 g, 30.66 mmol), NaHCO3 (3.86 g, 45.99 mmol) in ethanol (131 mL) and water (92 mL) was added benzyl chloroformate (4.4 mL, 30.66 mmol). The reaction mixture was stirred at room temperature for 2 hours and most of ethanol was removed under reduced pressure. The resulting mixture was extracted with Et2O (3 x 100 mL). Combined organic layers were washed with brine, dried over anhydrous MgSO4, filtrated and the volatiles were removed under reduced pressure. The resulting residue was purified on a silica gel pad (20 to 30% gradient of EtOAc/hexanes) to give tert-butyl 4-((benzyloxycarbonylamino)methyl)-4- methylpiperidine-1-carboxylate (9.78 g, 88% yield) as a yellowish oil.1H NMR (500 MHz, CDCl3) delta ppm 7.41- 7.29 (m, 5H), 5.17- 5.05 (m, 2H), 4.79 (br. s, 1H), 3.70- 3.58 (m, 2H), 3.22- 2.99 (m, 4H), 1.45 (s, 9H), 1.42- 1.35 (m, 2H), 1.31- 1.23 (m, 2H), 0.94 (s, 3H). MS (ES+) m/z 363 (M+1)., 236406-22-7

The synthetic route of 236406-22-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; RELAY THERAPEUTICS, INC.; D.E. SHAW RESEARCH, LLC; ALBRECHT, Brian K.; GIORDANETTO, Fabrizio; GREISMAN, Jack, Benjamin; MARAGAKIS, Paul; TAYLOR, Alexander M.; WALTERS, W. Patrick; (117 pag.)WO2018/57884; (2018); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

4801-58-5,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.

To a solution of 5,6-bis(4-chlorophenyl)pyrazine-2-carbonyl chloride, Inte. D (84 mg, 0.23 mmol) in DCM (1ml) was added slowly at room temperature a solution of hydroxypiperidine (93 mg, 0.91mmol) in pyridine (5 ml). After 40 minutes at room temperature, the solvent was removed in vacuo and the residue redissolved in diethyl ether. Extracted with 1M HC1 (aq) and K2CO3 (aq) and dried (MgSO4). The solvent was removed in vacuo to yield the subtitle compound (58 mg, 59%).JH NMR (399.964 MHz) 8 9.19 (s, 1H), 7.47-7.26 (m, 8H), 3.71-3.50 (m, 2H), 3.16-2.74 (m, 2H), 1.98-1.77 (m, 4H), 1.77-1.57 (m, 1H), 1.40-1.23 (m, 1H).13C NMR (100.58 MHz) 5 162.59,154.17, 151.20, 143.18,140.79,136.22, 136.17, 136.09,135.89, 131.42, 131.29, 129.08, 129.04, 57.87, 25.30, 23.27.MS m/z 428, 430, 432 (M+H)+.

As the paragraph descriping shows that 4801-58-5 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; WO2004/111033; (2004); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem