Day: October 20, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.333986-70-2,Methyl 4-(piperidin-4-ylmethyl)benzoate hydrochloride,as a common compound, the synthetic route is as follows.

Example of General Method C:Preparation of 4-{l-[(S)-4-(2,3-Dihydro-benzo[l,4]dioxin-2-yl)-benzyl]-piperidin-4- ylmethylj-benzoic acid methyl esterA solution of A (100 mg, 0.42 mmol), 4-piperidin-4-ylmethyl-benzoic acid methyl ester hydrochloride (146 mg, 0.54 mmol), sodium cyanoborohydride (52 mg, 0.83 mmol), and TEA (0.08 mL, 0.54 mmol) in THF (5 mL) is treated with 2 drops of acetic acid, and stirred at room temperature for 16 h. The mixture is concentrated, and the residue is purified by flash chromatography eluting with a gradient of 0-10% MeOH in DCM to give the title compound.

333986-70-2, As the paragraph descriping shows that 333986-70-2 is playing an increasingly important role.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; ABEYWARDANE, Asitha; BURKE, Michael J.; KIRRANE, Thomas Martin, Jr.; NETHERTON, Matthew Russell; PADYANA, Anil Kumar; SMITH KEENAN, Lana Louise; TAKAHASHI, Hidenori; TURNER, Michael Robert; ZHANG, Qiang; ZHANG, Qing; WO2012/125598; (2012); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

54012-73-6,54012-73-6, Piperidin-3-amine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The steps will be a 3 – amino piperidine (50.1g) soluble in the 2L of in DMF, by adding 1, 2 – diphenyl vinylidene carbonate (119.1g), triethylamine (1L), for ice water bath stirring to the reaction is complete (about 30min) after, adding ethyl acetate, the combined organic layer, dried with anhydrous sodium sulfate, to remove the organic solvent. The resulting product is dissolved in the 1L trifluoroacetic in, as for 20 C stirring for 2 hours, concentrated in vacuo, to remove the surplus trifluoro acetic acid, to obtain a product of formula Chinese (148.5g, yield 92.3%)

The synthetic route of 54012-73-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Borui Bio-pharmaceutical (Suzhou) Co., Ltd.; Yuan Jiandong; (12 pag.)CN103450201; (2017); B;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

157327-41-8, 1-Boc-3-[(Dimethylamino)methylene]-4-oxopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a 250 ml round bottom flask charged with anhydrous EtOH (50 ml) under nitrogen at 0 0C is added sodium hydride (60% in mineral oil, 2.4 g, 60 mmol, 4.0 eq.). The mixture is stirred at rt for10 min, and then 4-cyclobutyl-piperazine-l-carboxamidine from step 2 (about 15 mmol) is added, followed by the addition of terf-butyl-3-[(dimethylamino)methylene]-4-oxo-l-piperidinecarboxylate(3.81 g, 15 mmol, 1.0 eq.). The resulting mixture is stirred at 75 0C for 16 h. The solvent is evaporated under reduced pressure, and the residue is taken up in DCM (100 ml). The organics are washed with water and brine, dried (Na2SO4), and concentrated. The residue is purified through silica gel chromatography (EA / 4% TEA) to give the title compound as white solid. 1H NMR (300 MHz, CDCl3) delta 8.05 (IH, s), 4.41 (2H, s), 3.81 (4H, t), 3.67 (2H, t), 2.66-2.78 (3H, m), 2.36 (4H, t),1.62-2.10 (6H, m), 1.48 (9H, s)., 157327-41-8

As the paragraph descriping shows that 157327-41-8 is playing an increasingly important role.

Reference£º
Patent; NEUROGEN CORPORATION; WO2007/146122; (2007); 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.103816-19-9,[1,4′-Bipiperidine]-1′-carbonyl chloride,as a common compound, the synthetic route is as follows.

To a stirred solution of fulvestrant (0.2 g) in chloroform (6 ml) and water (1 ml), sodium hydroxide (0.132 g) and tetra-n-butylammonium bromide (0.128 g) was added at room temperature and vigorously stirred at room temperature for 30 min. 4-Piperidinopiperidine-l -carbonyl chloride (0.097 g) was added to the reaction mixture and stirred at room temperature for 16 h. The reaction was monitored by TLC and LCMS. After completion of reaction, the reaction mixture was evaporated under vacuum to obtain crude material. The crude material was purified by preparative HPLC using mobile phase A) 5 mmol ammonium bicarbonate + 0.1% N in water and B) acetonitrile. Product fraction was lyophilized to afford (7R,8R,9S, l3S, l4S, l7S)-l7-hydroxy-l3- methyl-7-(9-((4,4,5,5,5-pentafluoropentyl)sulfmyl)nonyl)-7,8,9, 11, 12, 13, 14, 15, 16, l7-decahydro- 6//-cyclopenta|a|phenanthren-3-yl [l,4′-bipiperidine]-r-carboxylate (0.019 g, 7.20%) as a white solid. (0376) -NMR (400 MHz, DMSO): d 7.272 (d, 1H), 6.821 (d, 1H), 6.781 (s, 1H), 4.559 (s, 1H), 4.131 (s, 1H), 4.047 (s, 1H), 3.558 (m, 2H), 3.501-3.486 (m, 5H), 2.961 (s, 2H), 2.892-2.623 (m, 10H), 2.446-2.279 (m, 12H), 1.996-1.885 (m, 4H), 1.835-1.746 (m, 5H), 1.771-1.514 (m, 4H), 1.734- 1.601 (m, 8H), 1.525-1.262 (m, 24H), 0.901 (dd, 2H) and 0.684 (s, 3H).

103816-19-9, 103816-19-9 [1,4′-Bipiperidine]-1′-carbonyl chloride 9813375, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; KASHIV BIOSCIENCES, LLC; PUROHIT, Parva Yogeshchandra; BRAHMKSHATRIYA, Pathik Subhashchandra; GOSWAMI, Vishalgiri Gunvantgiri; (107 pag.)WO2019/224790; (2019); 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.3970-68-1,4-Methylpiperidin-4-ol,as a common compound, the synthetic route is as follows.,3970-68-1

Compound 13-6 (0.250g, 0.5mmol), 4- hydroxypiperidine (0.125g, 1.1mmol) was dissolved in 1,2-dichloroethane (12ml), the protection purged with nitrogen, stirred 30min, was added NaBH (OAc 3(1.151g, 5.4mmol), reacted at room temperature overnight. TLC showed the reaction of the starting material was completed, and saturated sodium bicarbonate solution and DCM (50ml / 40ml) were added, and the aqueous phase was extracted with DCM (50ml ¡Á 2). The phase was dried over anhydrous sodium sulfate, concentrated, and then purified by thin layer chromatography to yield 0.090 g of pure product, yield: 32%.

The synthetic route of 3970-68-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Suzhou Yuanzhi Pharmaceutical Technology Co., Ltd.; Chen Li; Zhao Jian; (48 pag.)CN109896991; (2019); 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.4897-50-1,4-Piperidinopiperidine,as a common compound, the synthetic route is as follows.

Example 61; 7-(l,4′-bipiperidin-r-ylV5-chloro-l-(2,6-difluorophenylV3,4-dihvdropyrimido[4.5- ^pyrimidin-2(‘l.H)-one )To a solution of 5-chloro- 1 -(2,6-difluorophenyl)-7-(methylsulfinyl)-3 ,A- dihydropyrimido[4,5-d]pvrimidin-2(lH)-one (200 mg, 0.56 mmol) in DCM (10 mL) were added 1 ,4’-bipiperidine (270 mg, 1.61 mmol) and AzetaN-diisopropylethylamine (0.3 mL, 1.7 mmol). The resultant solution was stirred at room temperature over night. The result mixture was concentrated. CombiFlash chromatography (mobile phase DCM/DCM[90]+MeOH[7]+NuH4OH[3]) provided the title compound as a white solid (298 mg, 83 percent). LC-MS m/z 463 (M + H)+.

4897-50-1, As the paragraph descriping shows that 4897-50-1 is playing an increasingly important role.

Reference£º
Patent; GLAXO GROUP LIMITED; WO2006/104917; (2006); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

896464-16-7,896464-16-7, tert-Butyl 2,7-diazaspiro[3.5]nonane-7-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Add to tert-butyl 2,7-azaspiro[3,5]nonane-7-carboxylate (226 mg, 1.0 mmol) at room temperature4-trifluoromethoxyacetophenone (204 mg, 1.0 mmol) andTetraisopropyl titanate (568 mg, 2.0 mmol) was reacted at 80 C overnight.After cooling to room temperature, sodium cyanoborohydride (188 mg, 3.0 mmol) was added to the mixture, and the mixture was reacted at 40 C for 2 hours.Work-up: extraction with water and extraction with dichloromethane (20 mL x 3).The organic layer was combined, dried over anhydrous magnesium sulfate and evaporated(Ethyl acetate: petroleum ether = 1 : 2) gave pale yellow oil (150 mg).

The synthetic route of 896464-16-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Chinese Academy Of Medical Sciences Pharmaceutical Bio-technology Institute; Liu Mingliang; Wang Apeng; Lv Kai; Tao Zeyu; Ma Chao; Han Bing; Ma Xican; Wang Aoyu; Xu Shijie; (23 pag.)CN110204546; (2019); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

5984-56-5,5984-56-5, Piperidine-4-carboxylic acid hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of piperidine-4-carboxylic acid hydrochloride (500 mg, 2.26 mmol) and triethylamine (2.29 g, 22.6 mmol) in 1,2-dichloroethane (50 mL) was added methyl2-(chlorosulfonyl)acetate (1.17 g, 6.78 mmol) at 0 C under nitrogen atmosphere. After stirred at 0 C for 4 hours, the mixture was poured into water (40 mL) and extracted with dichloromethane (50 mL) for three times. The combined organic layers were washed with brine (100 mL) twice, dried over Na2SO4(), filtered and concentrated under reduced pressure to give a residue, which was purified by silica gel columnchromatography (petroleum ether: ethyl acetate = 9 : ito 3 : 1) to give the title compound (475 mg, 65 % yield) as yellow solids. ?H NIVII{ (400 1VIHz, CDC13) 3.92 (s, 2H), 3.79 (s, 3H), 3.75 – 3.70 (m, 2H), 3.04 – 2.98 (m, 2H), 2.39 – 2.32 (m, 1H), 1.98 -1.92 (m, 2H), 1.81 – 1.71 (m, 2H), 1.44 (s, 9H).

The synthetic route of 5984-56-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JANSSEN PHARMACEUTICA NV; JOHNSON & JOHNSON (CHINA) INVESTMENT LTD.; WAN, Zhao-Kui; JIANG, Yimin; DAI, Xuedong; LIU, Qian; CHEUNG, Wing Shun; DENG, Gang; FU, Liqiang; (547 pag.)WO2019/1420; (2019); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

479630-08-5,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.479630-08-5,1-Boc-4-(2-Ethoxycarbonyl-acetyl)piperidine,as a common compound, the synthetic route is as follows.

The intermediate 12h was obtained as describe below: piperidine-1,4-dicarboxylic acid mono-tert-butyl ester (150 g, 0.655 mol) in anhydrous acetonitrile (800 ml), 1,1′-carbonyldiimidazole was added in small portions (132 g, 0.851 mol) under vigorous stirring. The resulting mixture was stirred for 30 min at ambient temperature. Then powder of mixture of anhydrous MgCl2 (62g, 0.655 mol) and methyl potassium malonate (102g, 0.655 mol) was added in portions. The resulted slurry was heated at reflux for 2 h. The reaction mixture was cooled down, diluted with mixture of ice-cold water and dichloromethane and neutralized by citric acid. The separated organic layer was washed with 5% aqueous solution of potassium carbonate, dried over sodium sulfate and concentrated under reduced pressure. Further flash-chromatography using ethyl acetate/ hexane (1/1) gave 151 g (81%) of intermediate 31. 4-(6-Hydroxy-2-methyl-pyrimidin-4-yl)-piperidine-1-carboxylic acid tert-butyl ester (32) [0223] Acetamidine hydrochloride (29 g, 0.3 mol) was added to the solution of sodium ethylate (0.3 mol) in anhydrous ethanol (400 ml). The mixture was stirred at ambient temperature for 10 min, and compound 31 (0.3 mol) in ethanol was added. The resulting mixture was heated at reflux for 5 h (TLC control). The reaction mixture was concentrated under reduced pressure, the remains was dissolved in water and acidified with 1N HCl to pH 5.0 and extracted with ethyl acetate (2×200 ml). The combined extracts were dried over sodium sulfate and concentrated in vacuo. The residue was purified by flash-chromatography on silica gel (eluent: n-hexane/ethyl acetate – 1/1). As a result, compound 32 (50 g, 33%) was obtained. 4-(6-Chloro-2-methyl-pyrimidin-4-yl)-piperidine-1-carboxylic acid tert-butyl ester (12h) [0224] Intermediate 32 (50 g, 0.170 mol) and N,N-dimethylaniline (166 g, 1.365 mol) was dissolved in anhydrous toluene (1000 ml) and POCl3 (52 g, 0.34 mol) was added dropwise. The reaction mixture was heated at reflux for 3 h; then cooled down to ambient temperature and allowed to stay overnight. To this end, the mixture was poured into water; organic layer was separated, washed with 1N HCl and water. The crude product was concentrated under reduced pressure and purified with flash chromatography on silica gel (eluent: n-hexane/ethyl acetate 4/1) to provide 12h (34.3 g , 65%).

As the paragraph descriping shows that 479630-08-5 is playing an increasingly important role.

Reference£º
Patent; Asinex Limited; KAZULKIN, Denis Nikolaevich; KOCHUBEY, Valeriy Sergeevich; EP2719696; (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.203662-51-5,4-Allyl-1-Boc-4-hydroxypiperidine,as a common compound, the synthetic route is as follows.

Example 271 4-(2,3-Epoxypropan-1-yl)-1-(tert-butoxycarbonyl)piperidin-4-ol To a solution of 4.115 g of 4-allyl-1-(tert-butoxycarbonyl)piperidin-4-ol in dichloromethane (100 ml) were added 7.07 g of 3-chloroperbenzoic acid and 2.87 g of sodium hydrogencarbonate and the resulting mixture was heated under reflux for 24 hours. To the reaction mixture were added ethyl acetate and an aqueous solution of sodium metabisulfite and the resulting mixture was stirred for 1 hour. The organic layer was dried over anhydrous magnesium sulfate, filtered and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (eluted with dichloromethane/ethyl acetate) to thereby give 1.43 g of the title compound as a colorless solid. 1H-NMR(CDCl3) delta ppm: 1.45(s, 9H), 1.40-1.56(m, 5H), 1.88(dd, J=3, 14 Hz, 1H), 2.00(br.s, 1H), 2.50(dd, J=3, 6 Hz, 1H), 2.82(t, J=3 Hz, 1H), 3.14-3.27(m, 3H), 3.91(br.s, 2H), 203662-51-5

203662-51-5 4-Allyl-1-Boc-4-hydroxypiperidine 21955339, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Eisai Co., Ltd.; US6518423; (2003); B1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem