Day: March 18, 2022

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.914988-10-6,tert-Butyl 3-cyano-4-oxopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of (±)-tert-butyl 3-cyano-4-oxo-piperidine-1-carboxylate (3.00 g, 13.3 mmol, CAS 914988-10-6) in acetone (25 mL) was added potassium carbonate (3.70 g, 26.7 mmol) and iodoethane (4.17 g, 26.7 mmol). The mixture was stirred at 25 C for 16 hrs. On completion, the reaction mixture was concentrated in vacuo to give a residue. The residue was diluted with ice water (20 mL) and extracted with dichloromethane (3 × 20 mL). The combined organic layers were washed with brine (60 mL), dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure to give the title compound, which was used in the next step directly without further purification. 1H NMR (400MHz, CDCl3) delta = 3.84 – 3.71 (m, 3H), 3.57 (t, J = 5.7 Hz, 1H), 2.79 – 2.72 (m, 1H), 2.60 – 2.50 (m, 1H), 2.36 (br. s., 1H), 2.07 – 1.99 (m, 1H), 1.53 (s, 9H), 1.12 (t, J = 7.5 Hz, 3H)., 914988-10-6

914988-10-6 tert-Butyl 3-cyano-4-oxopiperidine-1-carboxylate 42609283, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; RAZE THERAPEUTICS, INC.; MAINOLFI, Nello; MOYER, Mikel P.; (208 pag.)WO2017/156177; (2017); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

6258-28-2, 2-(2,6-Dioxopiperidin-4-yl)acetic acid is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,6258-28-2

Example 14 4-{2-[4-(2-tert-Butylphenyl)piperazin-1-yl]-2-oxoethyl}piperidine-2,6-dione A mixture of 1-(2-tert-butylphenyl)piperazine dihydrochloride obtained in Reference Example 1 (500 mg), (2,6-dioxopiperidin-4-yl)acetic acid (311 mg), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (403 mg), 1-hydroxy-1H-benzotriazole monohydrate (322 mg), triethylamine (0.627 mL), and N,N-dimethylformamide (5 mL) was stirred at room temperature for over-night. Water was added to the reaction solution, and the mixture was extracted with ethyl acetate. The ethyl acetate layer was washed with saturated brine, and dried over anhydrous magnesium sulfate. The solvent was evaporated under reduced pressure, and the residue was subjected to purification by high performance liquid chromatography [Column: Gilson, Ltd. High throughput purification system, YMC Combiprep ODS-A, S-5 mum, 50 mm*20 mm; Gradient cycle: H2O (contains 0.1% CF3COOH)-acetonitrile (contains 0.1% CF3COOH), 90:10 (0 min)-90:10 (1 min)-10:90 (4.2 min)-10:90 (5.4 min)-90:10 (5.5 min)-90:10 (5.6 min); Flow rate: 25 mL/min; detection wavelength: UV 220 nm] to give the title compound (47 mg, 13%) as a white solid. 1H NMR (300 MHz, DMSO-d6) delta 1.41 (s, 9H), 2.35-2.74 (m, 12H), 3.20-3.31 (m, 1H), 3.85-3.98 (m, 1H), 4.40-4.50 (m, 1H), 7.13-7.21 (m, 2H), 7.30-7.34 (m, 2H), 10.72 (br, 1H).

6258-28-2 2-(2,6-Dioxopiperidin-4-yl)acetic acid 234331, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Kasai, Shizuo; McGee, JR., Kevin Francis; US2012/71489; (2012); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

914988-10-6,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.914988-10-6,tert-Butyl 3-cyano-4-oxopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

[0127] Step b: N,N-diisopropylethylamine (8 mL, 46.0 mmol) was added to a mixture of (2,6- diethylphenyl)hydrazine hydrochloride (8 g, 39.9 mmol), tert-butyl 3-cyano-4-oxopiperidine-1- carboxylate (5 g, 22.3 mmol) and EtOH (60 mL) in a 250 mL round bottom flask under magnetic stirring. The resulting mixture was stirred under reflux for 3 h. Glacial acetic acid (12 mL, 208 mmol) was added and the mixture was stirred under reflux for another 2 h. The solvent was removed under reduced pressure and the residue was dissolved in EtOAc and washed with NaOH solution (2N), brine, and dried over MgSO4. The solvent was removed under reduced pressure and the residue was purified by silica gel flash chromatography (5 to 55% EtOAc in hexanes) to give tert-butyl 3-amino-2-(2,6-diethylphenyl)-6,7-dihydro-2H-pyrazolo[4,3- c]pyridine-5(4H)-carboxylate . MS: (ES) m/z calculated for C21H31 N4O2 [M + H]+ 371.2, found 371.2. Caution: Diazonium formation could be potentially dangerous, please handle with care and wear proper personal protection equipment.

914988-10-6 tert-Butyl 3-cyano-4-oxopiperidine-1-carboxylate 42609283, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; CHEMOCENTRYX, INC.; FAN, Pingchen; LANGE, Christopher W.; LUI, Rebecca M.; MALATHONG, Viengkham; MALI, Venkat Reddy; PUNNA, Sreenivas; SINGH, Rajinder; TANAKA, Hiroko; ZENG, Yibin; ZHANG, Penglie; (284 pag.)WO2018/222598; (2018); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

142851-03-4, Ethyl N-Boc-piperidine-4-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 41Atert-Butyl 4-(hydrazinylcarbonyl)piperidine-1-carboxylate; 10.0 g (38.9 mmol) of 1-tert-butyl 4-ethyl piperidine-1,4-dicarboxylate were initially charged in 35 ml of ethanol, and 3.8 ml (3.90 g, 78 mmol) of hydrazine hydrate were added with stirring. The mixture was stirred at reflux for 9 h. The reaction mixture was cooled to RT, 1.9 ml (39 mmol) of hydrazine hydrate were added and the reaction solution was stirred at reflux for another 24 h. The solvent was concentrated, ethanol (50 ml) was added and the mixture was concentrated again. Diethyl ether (150 ml) was added, and the mixture was stirred in an ultrasonic bath for 5 min. The product was filtered off and dried. This gave 9.20 g (97% of theory) of the product.LCMS (Method 6): Rt=0.95 min. (m/z=244 (M+H)+)1H-NMR (400 MHz, DMSO-d6): delta=8.99 (s, 1H), 4.17 (br, 2H), 3.95 (br d, 2H), 2.71 (br, 2H), 2.23 (m, 1H), 1.60 (m, 2H), 1.40 (m, 11H).

142851-03-4, As the paragraph descriping shows that 142851-03-4 is playing an increasingly important role.

Reference：
Patent; BAYER SCHERING PHARMA AKTIENGESELLESCHAFT; US2011/144131; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

10338-57-5, 4-(Piperidin-1-yl)benzaldehyde is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The synthesis of compounds 5, 14-23 and 26-31 follows a multi-component procedure described by Groebke et al.1 N-Cyclohexyl-2-(4-morpholinophenyl)imidazo[1,2-a]pyridin-3- amine 17: 0.30 g (3.1 mmol) 2-aminopyridine and 0.60 g (3.1 mmol) 4-morpholinobenzaldehyde were stirred with glacial acetic acid and 35 mL anhydrous MeOH, then 0.35 g (3.1 mmol) cyclohexyl isocyanide was added. After 18 h the reaction mixture was quenched with 5 mL 2N HCl to destroy the residual isocyanide. MeOH was removed under reduced pressure and 50 mL saturated NaHCO3 solution was added. The product was extracted with EtOAc (3 x 40 mL) and the solvent was removed under reduced pressure. The purification was completed by recrystallization from EtOAc/MeOH yielding 0.50 g (42.2%) yellow solid.

10338-57-5, The synthetic route of 10338-57-5 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Hieke, Martina; Roedl, Carmen B.; Wisniewska, Joanna M.; La Buscato, Estel.; Stark, Holger; Schubert-Zsilavecz, Manfred; Steinhilber, Dieter; Hofmann, Bettina; Proschak, Ewgenij; Bioorganic and Medicinal Chemistry Letters; vol. 22; 5; (2012); p. 1969 – 1975;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.61995-20-8,Benzyl 3-oxopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.,61995-20-8

Part A. Preparation of N-(benzyloxycarbonyl)-2-phenylmethyl-3-piperidone. A stirring solution of N-(benzyloxycarbonyl)-3-piperidone (1000 mg, 4.25 mmol) and pyrrolidine (454 mg, 6.38 mmol, Aldrich) in dry toluene (10 mL) in a round bottom flask fitted with a Dean-Stark trap was refluxed for 4 h. The reaction was conc. in vacuo to a orange oil. The oil was dissolved in dry acetonitrile (10 mL) and then benzyl bromide (800 mg, 4.68 mmol, Aldrich) was added. The reaction was heated to reflux for 16 h and then cooled to room temperature. The reaction was quenched by the addition of 1M HCl (50 mL) and then extracted with EtOAc (4*40 mL). The organic layers were combined, washed with brine, dried over Na2SO4, and conc. in vacuo to an oil. The oil was purified by flash chromatography (SiO2, 7-20% EtOAc in hexanes) to yield 86 mg of the product as a white solid. MS (ESI) 324 (M+H).

61995-20-8 Benzyl 3-oxopiperidine-1-carboxylate 1514169, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Ko, Soo S.; DeLucca, George V.; Duncia, John V.; Santella, III, Joseph B.; Wacker, Dean A.; US6331545; (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.10338-57-5,4-(Piperidin-1-yl)benzaldehyde,as a common compound, the synthetic route is as follows.

General procedure: A mixture of the appropriate aromatic aldehydes 2b-d (12 mmol) and compound 1 (10 mmol, 2.15 g) dissolved in ethanol (50 ml) was added slowly to an aqueous solution of sodium hydroxide (12.8 mmol) in water (10 ml). The reaction mixture was stirred at 20-25 C for 4 h. The mixture was filtrated and the solid was washed with cold water. The product was crystallized from ethanol to give 3b-d., 10338-57-5

10338-57-5 4-(Piperidin-1-yl)benzaldehyde 291354, apiperidines compound, is more and more widely used in various fields.

Reference：
Article; Abdel-Wahab, Bakr F.; Abdel-Latif, Ehab; Mohamed, Hanan A.; Awad, Ghada E.A.; European Journal of Medicinal Chemistry; vol. 52; (2012); p. 263 – 268;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.534595-51-2,1-Boc-4-(isopropylamino)piperidine,as a common compound, the synthetic route is as follows.

To a solution of tert-butyl 4-(isopropyIamino)piperidine-carboxylate (0.25 g) (prepared using similar chemistry described in Step 1 , Example 1) in CH2Cl2 (10 ml) were added 3- trifluoromethylsulfinylchloride (1.4 mL; 0.8 M in THF solution) [J. Org. Chem. USSR (Engl. Transl.) 13: 2086-2087 (1977)], N,N-dimethyIamnopyridine (2 grains), diisopropylethylamine (0.71 mL). The resulting reaction mixture was stirred at room temperature two hours, and then diluted with ether (50 mL), washed with IN HCl (50 mL) and then 50 ml 5 % KOH. The organic phase was washed with water, dried over Na2SOi, filtered and concentrated. The residue obtained was purified by silica gel chromatography using ethyl acetate/hexane (1 :3) to afford the titled compound as a white solid (110 mg). 1H NMR (CDCl3): 7.94 (s, IH), 7.87 (d, J=7.8 Hz5 IH), 7.76 (d, J=8.0 Hz, IH), 7.66 (t, J=7.8 Hz, IH), 4.2 (b, 2H)5 3.57 (qint, J=4.6 Hz5 IH)5 3.23 (m, IH), 2.74 (b5 IH), 2.60 (b, IH), 2.15 (m5 IH)5 1.95 (m5 IH)5 1.75 (m, 1 H), 1.48 (s, 9H), 1.43 (d, J=5.6 HZ5 3H)5 1.15 (b5 3H). MS: m/e 435 (M-H )+., 534595-51-2

The synthetic route of 534595-51-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK & CO., INC.; WO2007/75524; (2007); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

109384-19-2, tert-Butyl 4-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-Fluorobenzonitrile (3. 0G) was dissolved in THF (50ML) and then N-tert-butoxy-carbonyl- 4-piperidinol (4.98g) was added. Potassium HEXAMETHYIDISILAZIDE (20% wt solution in THF, 24.62g) was then added dropwise and the reaction stirred at rt for 2h. The reaction mixture was then evaporated to a minimum, redissolved in EtOAc (100 ml) and washed with aqueous 1N HCI (2X100 ML), saturated sodium bicarbonate solution (2X100 ML) and brine (100 ML). The organic layer was dried (MGS04) and then purified by chromatography [silica gel, step gradient 0-60% EtOAc/Hexane]. Fractions containing the required product were evaporated to give the title compound (D21) as a clear oil which crystallised on standing (6.83 g).’H NMR 8 (CDCI3) : 7.59 (2H, d, J=7. 50HZ), 6.95 (2H, d, J=7. 50HZ), 4.44 (1H, m), 3.70 (2H, m), 3.38 (2H, m), 1.91 (2H, m), 1.77 (2H, m), 1.47 (9H, s).

109384-19-2, As the paragraph descriping shows that 109384-19-2 is playing an increasingly important role.

Reference：
Patent; GLAXO GROUP LIMITED; WO2004/37788; (2004); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

86542-94-1, 1-(Piperidin-4-yl)propan-1-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

86542-94-1, General procedure: HOBt*H2O (969 mg, 7.17 mmol), EDCI*HCl(1.37 g, 7.17 mmol), 2,2,6,6-tetramethylpiperidin-4-amine (2.49 mL,3.00 mmol) and Et3N (3.31 mL, 13.9 mmol) were added to a solution of 2-(benzo[d][1,3]dioxol-5-ylamino)-2-oxoacetic acid (1.00 g, 4.78 mmol) in DMF(23.9 mL) at 0 C. The reaction mixture was heated to room temperature and stirred for 20 h. Subsequently, the reaction mixture was concentrated under reduced pressure. Saturated aqueous NaHCO3 was added to the residue, andthe mixture was extracted with CHCl3 (150 mL 3), then washed with brineand dried over MgSO4. Concentration under reduced pressure followed by column chromatography (MeOH/CHCl3, 1/10) provided the title compound 5 (1.46 g, 88% yield) as white powder.

86542-94-1 1-(Piperidin-4-yl)propan-1-one 18620952, apiperidines compound, is more and more widely used in various fields.

Reference：
Article; Mizuguchi, Takaaki; Harada, Shigeyoshi; Miura, Tomoyuki; Ohashi, Nami; Narumi, Tetsuo; Mori, Hiromi; Irahara, Yu; Yamada, Yuko; Nomura, Wataru; Matsushita, Shuzo; Yoshimura, Kazuhisa; Tamamura, Hirokazu; Bioorganic and Medicinal Chemistry Letters; vol. 26; 2; (2016); p. 397 – 400;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem