Day: March 23, 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.,914988-10-6

To a solution of (±)-tert-butyl 3-cyano-4-oxo-piperidine-1-carboxylate (200 mg, 892 mumol, CAS 914988-10-6) in acetone (50 mL) was added potassium carbonate (370 mg, 2.68 mmol) and methyl iodide (380 mg, 2.68 mmol) in one portion. The reaction was stirred at 30 C for 12 hrs. On completion, 20 mL water was added to the solution. Then the solution was extracted with ethyl acetate (3 x 30 mL), washed with water (100 mL), dried over anhydrous sodium sulfate, and concentrated in vacuo to give the title compound. 1H NMR (400MHz, CDCl3) delta = 4.25 (s, 2H), 2.85 – 2.80 (m, 2H), 2.50 – 2.45 (m, 2H), 1.40 (s, 3H), 1.39 (s, 9H).

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1180112-41-7,tert-Butyl 1,7-diazaspiro[3.5]nonane-7-carboxylate,as a common compound, the synthetic route is as follows.,1180112-41-7

tert-Butyl 1,7-diazaspiro[3.5]nonane-7-carboxylate (1.5 g, crude) and 2,6-dichloro-4- ethylpyridine-3,5-dicarbonitrile (synthesis described in example 3 step 2, 1 g, 4.5 mmol) were dissolved in tetrahydrofuran (20 mL) and triethylamine (1.14 g, 11.25 mmol) was added at 0 C. The resultant mixture was stirred at ambient temperature for 2 hours and then diluted with ethyl acetate (60 mL). The mixture was washed with water (40 mL) and brine (40 mL), dried over anhydrous sodium sulfate and concentrated under reduced pressure to afford the title compound (2.1 g, crude) as a yellow oil which was used in the next step without further purification. LCMS m/z = 437.8 [M+Na]+.

1180112-41-7 tert-Butyl 1,7-diazaspiro[3.5]nonane-7-carboxylate 56962134, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; ADAMS, Nicholas David; BENOWITZ, Andrew B.; RUEDA BENEDE, Maria Lourdes; EVANS, Karen Anderson; FOSBENNER, David T.; KING, Bryan Wayne; LI, Mei; MILLER, William Henry; REIF, Alexander Joseph; ROMERIL, Stuart Paul; SCHMIDT, Stanley J.; WIGGALL, Kenneth; (1283 pag.)WO2017/216726; (2017); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

140645-24-5, (S)-3-(Aminomethyl)-1-N-Boc-piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(A) (S)-terf-butyl 3-((7-chloropyrido[4,3-ib]pyrazi n-5-ylami no)methyl)piperidi ne- 1 -carboxylate.[0123] A solution of (S)-teri-butyl 3-(aminomethyl)piperidine-1 -carboxylate (100 mg, 0.5 mmol), 5,7-dichloropyrido[4,3-?>]pyrazine (100 mg, 0.5 mmol) and DIPEA (77 mg, 0.6 mmol) in THF (5 ml_) was stirred at room temperature for 4 hours. The volatiles were removed under reduced pressure, and the residue was treated with ethyl acetate, with brine, and concentrated to give the crude title compound.

140645-24-5, As the paragraph descriping shows that 140645-24-5 is playing an increasingly important role.

Reference：
Patent; HUTCHISON MEDIPHARMA LIMITED; SU, Wei-Guo; DENG, Wei; JI, Jianguo; WO2012/167423; (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.10338-57-5,4-(Piperidin-1-yl)benzaldehyde,as a common compound, the synthetic route is as follows.

10338-57-5, General procedure: In a 100-mL round-bottom flask, ethyl 2-(7-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo- 2H-benzo[b][1,4]oxazin-4(3H)-yl)acetate (22) (1 g, 3.03 mmol, 1 equivalent) and triphenylphosphine (0.87 g, 3.33 mmol, 1.1 equivalent) were dissolved in ethanol (50 mL). After stirring at 25 C for 10-15 min, aromatic aldehyde (3.03 mmol, 1 equivalent) was added slowly along with stirring. The reaction mixture was allowed to stir for 24 h. The progress of the reaction was monitored by TLC (MeOH:CHCl3::1:19). On completion of the reaction, the solvent was evaporated under reduced pressure. The solid residue so obtained was purified by column chromatography (MeOH:CHCl3::1:49) to afford the desired benzoxazine-based arylidinyl succinimide derivative (23-36) in 64-80% isolated yield.

As the paragraph descriping shows that 10338-57-5 is playing an increasingly important role.

Reference：
Article; Sharma, Atul K.; Prasad, Suchita; Sharma, Sunil K.; Synthetic Communications; vol. 47; 20; (2017); p. 1854 – 1863;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.14813-01-5,1-Benzylpiperidin-3-ol,as a common compound, the synthetic route is as follows.

Step 3: To a solution of [3](1.00 g, 5.23 mmol) in benzene (90 mL),sodium (1 10 mg) was added. After refluxing for 2.5 h, a solution of methylbenzilate (1.27 g, 5.23 mmol) was added and the reaction refluxed overnight. The benzene was evaporated in vacuo and the residue purified by flash chromatography (eluted first with 20% EtOAc/Hexane, then 5%MeOH/CH2Cl2) to give [1O04] as transparent liquid (981 mg,46%).Analytical Data: [1004] ESIMS: 402[M++1]

14813-01-5, As the paragraph descriping shows that 14813-01-5 is playing an increasingly important role.

Reference：
Patent; SPHAERA PHARMA PVT. LTD.; DRUG DISCOVERY RESEARCH CENTRE; DUGAR, Sundeep; MAHAJAN, Dinesh; RAI, Santosh Kumar; RAO, Kanury; SINGH, Varshneya; WO2015/181837; (2015); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

85908-96-9, N-Boc-2-Piperidone is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,85908-96-9

General procedure: Based on the procedure by Bogle.1 To a solution of the amide 11 in THF at – 78 C was added dropwise a solution of lithium hexamethyldisilazide (1.0 M in THF, 2.1 eq) and the mixture stirred at – 78 C for 10 min. Benzylchloroformate (1.0 eq) was then added dropwise and the resulting mixture stirred at – 78 C for 1 h. The reaction was quenched at – 78 C with aq. NH4Cl (10 mL) and allowed to warm to room temperature. The aqueous layer was extracted with EtOAc (3 x 25 mL), the combined organic extracts washed with brine (10 mL), dried (Na2SO4) and concentrated in vacuo. The crude mixture was loaded onto a silica column and eluted with a PE/ethyl acetate mixture to yield the ester 12. NB. Deviations from this procedure are noted.

As the paragraph descriping shows that 85908-96-9 is playing an increasingly important role.

Reference：
Article; Moody, Catherine L.; Franckevi?ius, Vilius; Drouhin, Pauline; Klein, Johannes E.M.N.; Taylor, Richard J.K.; Tetrahedron Letters; vol. 53; 15; (2012); p. 1897 – 1899;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1211587-42-6, Benzyl 4-((chlorosulfonyl)methyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound 13 was prepared from sulfochloride 11 analogously to 12. Yield 11.6g (63%). White solid. Mp 75-76. [alpha]D=+5.3 ( 1.03, MeOH). MS (CI, m/z): 502 (MH+). Anal. Calcd for C26H35N3O5S: C, 62.25; H, 7.03; N, 8.38; S, 6.39. Found: C, 61.87; H, 7.09; N, 8.21; S, 6.48. 1H NMR (500MHz, CDCl3) delta 7.52-7.29 (m, 7H), 7.29-7.20 (m, 3H), 6.08-5.80 (m, 1H), 5.66-5.30 (m, 1H), 5.12 (s, 2H), 4.10 (s, 2H), 4.04-3.91 (m, 2H), 3.21-3.11 (m, 1H), 3.04-2.93 (m, 1H), 2.75 (s, 2H), 2.53-2.37 (m, 2H), 2.03-1.87 (m, 1H), 1.83-1.65 (m, 2H), 1.12 (d, J=6.0Hz, 3H), 1.12-1.04 (m, 2H), 1.04 (d, J=6.1Hz, 3H). 13C NMR (126MHz, cdcl3) delta 169.6, 155.1, 136.7, 136.6, 129.6, 128.9, 128.5, 128.0, 127.8, 127.4, 67.1, 59.0, 58.6, 43.6, 41.8, 39.4, 31.7, 31.5, 22.5, 22.3.

1211587-42-6, 1211587-42-6 Benzyl 4-((chlorosulfonyl)methyl)piperidine-1-carboxylate 50988934, apiperidines compound, is more and more widely used in various fields.

Reference：
Article; Grygorenko, Oleksandr O.; Zhersh, Sergey; Oliinyk, Bohdan V.; Shishkin, Oleg V.; Tolmachev, Andrey A.; Tetrahedron Asymmetry; vol. 25; 3; (2014); p. 229 – 237;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.220394-97-8,1-Boc-4-(Cbz-amino)piperidine,as a common compound, the synthetic route is as follows.

(Example 1b) Benzyl N-(piperidin-4-yl)carbamate A mixture of tert-butyl 4-{[(benzyloxy)carbonyl]amino}piperidine-1-carboxylate obtained in Example 1a (13.1 g, 39.2 mmol), a 5 N aqueous hydrochloric acid solution (40 ml, 200 mmol) and methanol (40 ml) was stirred at room temperature for 23 hours. A 5 N aqueous sodium hydroxide solution (40 ml) was added to the reaction mixture under ice-cooling. Water and the solvent were distilled off from the reaction mixture while the mixture was azeotropically distilled with ethanol. Ethanol was added to the residue, the insoluble matter was removed by filtration, and the filtrate was concentrated to give the title compound (9.10 g, yield 99.1%). 1H-NMR (400 MHz, CDCl3) delta ppm; 1.31-1.42 (2H, m), 1.92-2.04 (2H, br), 2.70 (2H, d, J=12 Hz), 3.10 (2H, d, J=12 Hz), 3.56-3.68 (1H, br), 4.72-4.81 (1H, br), 5.09 (2H, s), 7.26-7.40 (5H, m).

220394-97-8, As the paragraph descriping shows that 220394-97-8 is playing an increasingly important role.

Reference：
Patent; Eisai R&D Management Co., Ltd.; YOSHIDA Ichiro; OKABE Tadashi; MATSUMOTO Yasunobu; WATANABE Nobuhisa; OHASHI Yoshiaki; ONIZAWA Yuji; HARADA Hitoshi; EP2757103; (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.1062580-52-2,(3R,4R)-1-Benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride,as a common compound, the synthetic route is as follows.

To the reaction flask was added 200g (3R,4R)-N-(phenylmethyl)-3-methylamino-4-methylpiperidine hydrochloride, 210g 2,4-dichloro-7H-pyrrolo[2,3-D]pyrimidine (compound II), 160g of potassium carbonate, 1000mL of water and a 500 mL of ethanol, stirring while reflux, TLC monitored the reaction. After completion of the reaction, cooled to below 30 deg. C, 2000mL of ethyl acetate was added, with stirring, suction filtered, the filter cake was washed with 200 mL of ethyl acetate, the aqueous layer was extracted with ethyl acetate 1000mL and then the combined organic phase was dried over anhydrous sodium sulfate, suction filtered, evaporated to dryness to obtain 295g crude oil, the crude was added 300mL ethyl acetate and 900mL hexane, dissolved clear, cooled to -10 deg. C overnight incubation, solid precipitation, filtration, drying, 280g white solid product compound IV.

1062580-52-2, As the paragraph descriping shows that 1062580-52-2 is playing an increasingly important role.

Reference：
Patent; Nantong Changyou Pharmaceutical Science and Technology Co., Ltd.; Li, Zebiao; Liu, Jie; Pan, Jing; Zhang, Lei; Yan, Jun; Lu, Lianling; (10 pag.)CN105732641; (2016); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

32559-18-5, Methyl piperidine-2-carboxylate hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(a) N-Methylpiperidine-2-carboxamide.; To methyl pipecolinate hydrochloride (5.0 g, 28 mmol, Aldrich) was added methylamine (20 mL, 40 wt. % solution in H2O, Aldrich). The mixture was stirred at 25 C. for 18 h and then evaporated under reduced pressure. The residue was dried in vacuo to give the crude title compound, which was used in the next step without additional purification., 32559-18-5

The synthetic route of 32559-18-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Bo, Yunxin Y.; Chakrabarti, Partha P.; Chen, Ning; Liao, Hongyu; Norman, Mark H.; Stec, Markian; Tamayo, Nuria; Wang, Xianghong; US2006/183745; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem