Month: March 2022

89895-06-7, 1-(Piperidin-4-yl)ethanone hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,89895-06-7

Step 1: 4-acetyl-1-(benzyloxycarbonyl)piperidine To a stirred solution of 4-acetylpiperidine hydrochloride (22.6 g, 0.138 mol) in saturated aqueous Na2CO3 (100 mL), cooled to 5C, was added benzyl chloroformate (23.6 mL, 0.166 mol) dropwise over 10 – 15 min. The resulting suspension was stirred for 1/2 hour and was filtered. The solid was recrystallized from hexane (200 mL) and ethyl acetate (20 mL) producing 30.5 g of the title compound as a white solid. M.P. 87-89C.

The synthetic route of 89895-06-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK & CO., INC.; EP863757; (2003); 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.189333-49-1,3-Benzyl-3,9-diazaspiro[5.5]undecane,as a common compound, the synthetic route is as follows.

Example 8D (500 mg, 2.05 mmol) and Boc2O (450 mg, 2.06 mmol) in methanol mixture was added triethylamine (311 mg, 3.08 mmol) and the mixture was stirred at 20-30 deg.C for 16 hours. The reaction mixture was concentrated, and the residue was diluted with ethyl acetate (20 mL), and washed with water (15mL × 2) and brine (20 mL) was washed, and the organic layer was dried over anhydrous sodium sulfate, and concentrated. The crude intermediate was dissolved in ethanol (15mL) and acetic acid (2mL), followed by addition of palladium hydroxide / carbon (0.1 g). The mixture was reacted under hydrogen (50Psi) for 20 hours. The mixture was filtered, the filtrate was concentrated to give the acetate salt (320 mg, 1.26 mmol, 61.37% yield) of the title compound., 189333-49-1

Big data shows that 189333-49-1 is playing an increasingly important role.

Reference：
Patent; Nanjing Mingde New Drug Research and Development Co. Ltd.; Qilu Pharmaceutical Co., Ltd.; Ding, Zhaozhong; Zhang, Minghui; Chen, Shuhui; Liu, Xile; Zhu, Yidong; Fan, Chuanwen; Zhao, Baoping; Zhang, Long; Chen, Dong; Yang, Yingying; Zheng, Qingmei; Zheng, Shansong; Wan, Haiwen; Hu, Jinqing; (93 pag.)CN105330698; (2016); 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.122860-33-7,Benzyl 4-(hydroxymethyl)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Reaction Step 2 Synthesis of benzyl 4-formylpiperidine-1-carboxylate To a stirred solution of benzyl 4-(hydroxymethyl)piperidine-1-carboxylate (10.0 g, 40.2 mmol, 1.0 eq) in dichloromethane (150 ml), Dess-Martin periodinane (20.4 g, 48.2 mmol, 1.2 eq) was added at 0 C. and stirring was continued at room temperature for 12 h. After completion of the reaction (monitored by TLC, 30% ethyl acetate-hexane, Rf=0.45), the mixture was diluted with dichloromethane and washed with saturated sodium bicarbonate solution, followed by brine. The organic extract was dried over anhydrous sodium sulphate, filtered and concentrated under reduced pressure. The crude product was purified by column chromatography on silica gel (100-200 mesh), eluting with a 30-40% gradient of ethyl acetate in hexanes to obtain benzyl 4-formylpiperidine-1-carboxylate (6.2 g, 62.5%). LCMS Purity: 78.54% (ES+): m/z 248.27 (M+H+); tr=3.01 min., 122860-33-7

122860-33-7 Benzyl 4-(hydroxymethyl)piperidine-1-carboxylate 736490, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; INNOV17 LLC; Gaweco, Anderson; Tilley, Jefferson; Blinn, James; (68 pag.)US2016/24056; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

936130-82-4, Methyl 4-(piperidin-4-yl)benzoate hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

936130-82-4, A mixture of Compound 8BE (3 g, 11.73 mmol), CH2CI2 (30 ml_), triethyl amine(4.9 ml_, 35.19 mmol) and di-tert-butyl dicarbonate (3.83 g, 17.55 mmol) was stirred at room temperature for 3 hours. Diluted with CH2CI2 (100 ml_) and washed with water (100 ml_). The organic layer was dried over Na2SO4, filtered and concentrated. The residue was purified on silica gel eluting with 100% EtOAc to give the desired product 9BE (3.5 g, 93%).

The synthetic route of 936130-82-4 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SCHERING CORPORATION; WO2008/153858; (2008); 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.3612-20-2,1-Benzylpiperidin-4-one,as a common compound, the synthetic route is as follows.

To a solution of ammonium chloride (1.73 g, 32.3 mmol) in water (20 ml) is added a 30% ammonia solution (2 ml) followed by 1-benzyl-4-piperidone. After 20 minutes sodium cyanide (1.47 g, 30 mmol) is added portionwise over 15 minutes. After stirring for one hour, water (50 ml) is added and the products are extracted with DCM (3*50 ml), dried (MgSO4) filtered and concentrated in vacuo. Purification by chromatography on silica eluting with 50-100% EtOAc in iso-hexane affords 4-Aminomethyl-1-benzyl-piperidine-4-ylamine; [M+H]+ 216

3612-20-2, 3612-20-2 1-Benzylpiperidin-4-one 19220, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Vertex Pharmaceuticals Incorporated; Van Goor, Fredrick F.; Burton, William Lawrence; US2015/231142; (2015); 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.140645-24-5,(S)-3-(Aminomethyl)-1-N-Boc-piperidine,as a common compound, the synthetic route is as follows.

a) l,l-Dimethylethyl (3iS)-3-[({[(phenylmethyl)oxy]carbonyl}amino)methyl]-l- piperidinecarboxylateTo a solution of 1,1-dimethylethyl (3.S)-3-(aminomethyl)-l- piperidinecarboxylate (2.0 g, 9.33 mmol) in DCM (12 ml) at 0 0C were added triethylamine (1.7 ml, 12.1 mmol) followed by N-(benzyloxycarbonyloxy)succinimide (2.56 g, 10.3 mmol). After a few minutes the cooling bath was removed and the reaction was stirred at room temperature for 2h. The reaction was diluted with ethyl acetate and washed with water (2x), IN HCl, saturated aq. NaHCO3, brine, dried (Na2SO4) and concentrated. The product was purified on silica gel eluting with 10% ethyl acetate-DCM to give 3.48g of material containing a small amount of N-(benzyloxycarbonyloxy)succinimide which was used directly in next step. LC/MS (ES) m/e 349 (M+H)+.

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

Reference：
Patent; GLAXO GROUP LIMITED; WO2007/71936; (2007); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

406233-26-9,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.406233-26-9,4-(4,4-Dimethylpiperidin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

4.2 Acylsulfonamide (SZ2TA2) [ 0386 ] A solution of 15 (58 mg, 0.25 mmol), 18 (76 mg, 0.25 mmol), EDCI (60 mg, 0.314 mmol) and DMAP (8 mg, 0.065 mmol) in dichloromethane (10 mL) was stirred for 19 hours. Product (SZ2TA2) (42 mg, 32.5percent) was isolated after flash chromatography (DCM:MeOH = 24: 1). Rf = 0.6 (DCM: MeOH = 6: 1). 1H-NMR (400 MHz, DMSO- 6) delta: 7.85 (d, J = 8 Hz, 2H), 7.69 (d, J= 8.8 Hz, 2H), 7.44 (d, J= 8 Hz, 2H), 7.24-7.16 (m, 6H), 6.84 (d, J= 8.8 Hz, 2H), 3.80 (bs, 2H), 3.27-3.24 (m, 4H), 3.14 (s, 2H), 2.79 (bs, 4H), 2.33 (s, 3H), 1.35-1.32 (m, 2H), 0.91 (s, 6H) ppm. 13C-NMR (100 MHz, DMSC /6) delta: 166.9, 153.9, 139.9, 130.7, 129.9, 129.3, 129.0, 128.1, 126.8, 126.3, 113.5, 60.5, 58.5, 44.5, 41.7, 38.1, 32.6, 29.1, 28.3, 28.2 ppm. HRMS (ESI+) for [M+H]+; calculated: 520.2634, found: 520.2627 (error m/z = 1.3 ppm).

406233-26-9 4-(4,4-Dimethylpiperidin-1-yl)benzoic acid 11535980, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; UNIVERSITY OF SOUTH FLORIDA; MANETSCH, Roman; KULKARNI, Sameer Shamrao; IYAMU, Iredia David; WANG, Hong-Gang; DOI, Kenichiro; GUIDA, Wayne C.; SANTIAGO, Daniel N.; DUBOULAY, Courtney J.; WO2012/21486; (2012); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

61869-08-7, (3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1.0 g of oily paroxetine free base and 1.24 g of cholic acid were completely dissolved in a mixed solvent of purified water (5 mL) and methanol (30 mL) with stirring for 2 hours. The solution was allowed to stand at 0 C. for 48 hours, filtered, and dried under vacuum to yield 1.8 g of solid paroxetine cholate as a white powder., 61869-08-7

61869-08-7 (3S,4R)-3-((Benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine 44274603, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Lee, Sang Joon; Shin, Hee Jong; Ki, Min Hyo; Lee, Su Kyoung; Kim, Bok Young; Lee, Hong Woo; US2006/63747; (2006); 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.85908-96-9,N-Boc-2-Piperidone,as a common compound, the synthetic route is as follows.

[396] To a solution of tert-butyl 2-oxopiperidine-l-carboxylate (8.22 g, 41.3 mmol) in anhydrous THF (80 mL) was added LiHMDS (1.0 M in THF, 103 mL, 103 mmol) dropwise under nitrogen atmosphere at -78 C. The reaction mixture was stirred for 20 min and 3-bromoprop-l-ene (10.7 mL, 124 mmol) was added. The resulting mixture was stirred for 15 min, allowed to warm to rt, quenched with water (15 mL), and concentrated in vacuo. The residue was added water (30 mL) and extracted with EtOAc (50 mL x 3). The combined organic phases were washed with brine (50 mL), dried over anhydrous Na2SO i, concentrated in vacuo. The residue was purified by silica gel column chromatography (EtOAc/PE (v/v) = 1/50) to give the title compound as yellow oil (3.95 g, 35%). MS (ESI, pos. ion) m z: 224.2 [(M-C4H8)+H]+; NMR (600 MHz, CDCI3): delta (ppm) 5.72 (ddt, .7=16.5, 10.5, 7.0 Hz, 2H), 5.06 (d, J= 10.5 Hz, 2H), 5.03 (d, J= 16.5 Hz, 2H), 3.55 (t, J= 5.8 Hz, 2H), 2.46 (dd, J= 13.6, 7.0 Hz, 2H), 2.21 (dd, J= 13.6, 7.0 Hz, 2H), 1.75 (m, 4H), 1.48 (s, 9H).

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

Reference：
Patent; CALITOR SCIENCES, LLC; SUNSHINE LAKE PHARMA CO., LTD.; XI, Ning; LI, Minxiong; HU, Haiyang; WANG, Tingjin; WO2015/94803; (2015); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

189321-63-9, 1-Boc-4-Methylpiperidine-4-carboxylic acid is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A. Preparation of 4-methylpiperidine 4-carboxylic acid. 1-(tert-Butoxycarbonyl)-4-methylpiperidine-4-carboxylic acid (0.500 g, 2.06 mmol) was treated with 4 M HCl in dioxane (10 mL) for 2 hours at room temperature to afford the title compound (0.294 g, 100%) as the hydrochloride salt. MS (ES+) [M+H]+=144.0., 189321-63-9

As the paragraph descriping shows that 189321-63-9 is playing an increasingly important role.

Reference：
Patent; Burgoon, Hugh Alfred; Goodwin, Nicole Cathleen; Harrison, Bryce Alden; Healy, Jason Patrick; Liu, Ying; Mabon, Ross; Marinelli, Brett; Rawlins, David Brent; Rice, Dennis Stewart; Whitlock, Norris Andrew; US2009/264450; (2009); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem