Day: October 15, 2020

138007-24-6, tert-Butyl piperidine-4-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

tert-Butyl piperidine-4-carboxylate (2.84 g, 15.33 mmol) and 2-(1-oxo-1,3- dihydroisobenzofuran-5-yl)acetaldehyde(4.05 g, 22.99 mmol) were dissolved in DCE (120m1) then sodium triacetoxyborohydride (9.75 g, 46.0 mmol) was added and and the mixtue was stirred for 16 hrs. The reaction mixture was poured into aqueous NaHCO3 solution and extractedwith DCM. The organic layer was separated and dried over Na2504, filtered and concentrated. The crude residue was chromatographed through a 330g ISCO Redi-sep column and eluted with 5percent (NHOH: MeOH 1:9) in 95percent DCM to yield tert-butyl 1-(2-(1-oxo-1,3- dihydroisobenzofuran-5-yl)ethyl)piperidine-4-carboxylate. LC-MS (IE, m/z): 346 [M + 1]¡À; lHNMR (500 MHz, CDC13) oe ppm 7.859 (d, J= 7.9 Hz, 1H), 7.394 (d, J= 8.0 Hz, 1H), 7.352 (s,1H), 5.311 (s, 2H), 2.965 (b, 4H), 2.641 (b, 2H), 2.234 (b, 1H), 2.139 (b, 2H), 1.925(d, J 9.5 Hz, 2H), 1 .788( t, J 11.5 Hz, 2H,) 1.447 (s, 9H)., 138007-24-6

138007-24-6 tert-Butyl piperidine-4-carboxylate 1512676, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; TANG, Haifeng; FRIE, Jessica; FERGUSON, Ronald Dale; GUO, Zhiqiang; SHI, Zhi-Cai; CATO, Brian; FU, Qinghong; WO2015/65866; (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.160357-94-8,1-Acetyl-4-aminopiperidine,as a common compound, the synthetic route is as follows.

Example 102 N-(1-acetyl-piperidin-4-y)-4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-3-methoxy-benzamide (I-102) A mixture of 0.045 g (0.1 mmole) of 4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-3-methoxybenzoic acid (I-22), 0.042 g (0.110 mmole) of 1-[bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium-3-oxide hexafluorophosphate, 0.052 ml (0.300 mmole) of ethyldiisopropyl amine and 1.0 mL of dimethylformamide was stirred for 5 minutes and then 0.017 g (0.12 mmole) of 1-(4-Amino-piperidin-1-yl)-ethanone was added. The mixture was stirred for 3 hours, then diluted with 10 mL of water plus 2 mL of saturated aqueous sodium bicarbonate and then extracted 3 times with 10 mL of ethyl acetate. The combined extracts were washed with brine, dried over anhydrous magnesium sulfate, filtered and concentrated under reduced pressure. The residue was purified by reverse phase silica gel chromatography, eluding with water-acetonitrile (gradient, 0:100-80:20) to give 0.05 g of N-(1-acetyl-piperidin-4-yl)-4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-3-methoxy-benzamide (I-102) as a white solid., 160357-94-8

160357-94-8 1-Acetyl-4-aminopiperidine 4962477, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Cai, Jianping; Chen, Shaoqing; Chu, Xin-Jie; Luk, Kin-Chun; Mischke, Steven Gregory; Sun, Hongmao; Wovkulich, Peter Michael; US2009/318408; (2009); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

5570-78-5, 1-Isopropylpiperidin-4-ol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5570-78-5, To a solution of l-(l-methylethyl)piperidin-4-ol (103 mg, 0.724 mmol) in THF (3 ml) under an atmosphere of nitrogen was added KO1Bu (136 mg, 1.21 mmol). The mixture was stirred for 15 min at room temperature before 2-chloro-6-methyl-5,6,7,8-tetrahydro-l,6- naphthyridine-3-carbonitrile (100 mg, 0.483 mmol) was added. The resulting mixture was heated to 90 0C by microwave irradiation and stirred for 15 min. After cooling to RT, the reaction mixture was quenched by pouring onto saturated aqueous NaHCO3 , extracted with EtOAc (3 x 20 ml), dried (Na2SO4), filtered and concentrated at reduced pressure. The residue was purified by FCC (SiO2, eluting with 95:5 chloroform / MeOH) to give the title compound (36 mg, 24 %) as yellow oil. LCMS data: Calculated MH+ (315); Found 94 % (MH+) m/z 315, Rt = 4.78 min.1H NMR (400 MHz, MeOD) delta ppm 7.73 (1 H, s), 5.29 – 5.36 (1 H, m), 3.55 (2 H, s), 2.93 – 3.07 (5 H, m), 2.78 – 2.84 (4 H, m), 2.48 (3 H, s), 2.10 – 2.20 (2 H, m), 1.95 – 2.04 (2 H, m), 1.20 (6 H, d, J=6.6 Hz).

As the paragraph descriping shows that 5570-78-5 is playing an increasingly important role.

Reference£º
Patent; EVOTEC NEUROSCIENCES GMBH; WO2009/121812; (2009); 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.7149-42-0,(1-Methylpiperidin-4-yl)methanamine,as a common compound, the synthetic route is as follows.

7149-42-0, (Z)-4-(((l -Acetyl-6-(methoxycarbonyl)-5-methyl-2-oxoindolin-3-ylidene) (phenyl)methyl)ami no)benzoic acid, trifluoroacetate adduct (Intermediate E) (75 mg,0.128 mmol) and HATU (73.2 mg, 0.192 mmol) in DMF (2 mL) were stirred at rt for 10 mm.Then Hunig?s base (179 p1, 1.02 mmol) and (1-methylpiperidin-4-yl)methanamine (32.9 mg,0.257 mmol) in DMF (0.2 mL) were added. The mixture was stirred at rt for 16 h. Piperidine(127 p1, 1.28 mmol) was added. The mixture was stirred at RT for 4 h and the reaction mixture was partitioned between DCM (25 mL) and saturated aqueous NaHCO3 solution (10 mL). The organic layer was washed with brine (10 mL) and the solvent was evaporated under reduced pressure. The crude product was purified by preparative HPLC (Method A, 20-50% MeCN in water) to afford the title compound (Z)-methyl 5-methyl-3-(((4-(((1 -methyl piperidin-4-yl)methyl)carbamoyl) phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate, formate as a light yellow solid (19 mg, 25%); Rt 1.55 mm (Method 1); mlz 539 (M+H) (ES); 1H NMR O: 1.11-1.28 (2H, overlapping m), 1.53 (1H, m), 1.60-1.73 (2H, overlapping m), 2.13 (3H, 5), 2.15-2.24 (2H, overlapping m), 2.34 (3H, 5), 2.89-3.00 (2H, overlapping m), 3.09 (2H, t), 3.75 (3H, 5), 5.61 (1H, 5), 6.87 (2H, m), 7.36 (1H, 5), 7.52 (2H, m), 7.58-7.69 (5H, overlapping m),8.17 (1H, 5), 8.36 (1H, t), 10.88 (1H, 5), 12.23 (1H, 5).

7149-42-0 (1-Methylpiperidin-4-yl)methanamine 81574, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; RESPIVERT LIMITED; WALTERS, Iain; BIRCH, Louise; COLLINGWOOD, Stephen, Paul; STEVENSON, Christopher, Scott; (110 pag.)WO2017/153748; (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.14691-88-4,4-Amino-2,2,6,6-tetramethylpiperidine 1-Oxyl,as a common compound, the synthetic route is as follows.

To a solution of 3,5-t-butyl-4-hydroxyl benzoic acid (2.50 g, 10 mmol), 4-amino-TEMPO (1.55 g, 9.1 mmol) and DMAP (0.5 g, 4 mmol) in CH2Cl2 (50 mL) At 0-5¡ã C., DCC (2.30 g, 1 mmol) in dichloromethane (50 mL) was added dropwise. After addition is complete, the mixture was stirred at room temperature overnight. The reaction mixture was filtered and the filtrate was washed with 1N HCl (20 mL) and dried over MgSO4. After MgSO4 was filtered off, the solvent was removed in vacuum to give a solid The solid was purified by column chromatography (silica gel, EtOAc/Hexane). The product is an orange solid (1.3 g). The yield was 35percent.

14691-88-4, As the paragraph descriping shows that 14691-88-4 is playing an increasingly important role.

Reference£º
Patent; Patil, Ghanshyam; Mousa, Shaker A.; US2008/200405; (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.883984-95-0,Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate,as a common compound, the synthetic route is as follows.

INTERMEDIATE 16 r-(Methoxymethvnspirorpiperidine-4.4′-pyrido[2.3-(iiri.31oxazinl-2riy)-one Step A. Benzyl 7′-chloro-l’-(‘methoxymethyl)-2′-oxo-r,2′-dihvdro-lH-spiro[piperidme-4,4’- pyridor2.3-lithium bis(trimethylsilyl)amide (2.86 niL of IM solution, 2.86 mmol) followed by chloromethyl methyl ether (0.094 mL, 1.01 mmol). After 0.5 h, the reaction was diluted with EtOAc, extracted with water (3x) and brine, dried over MgSO4, filtered, and concentrated under reduced pressure. The crude product was purified by silica gel chromatography, eluting with a gradient of 0 to 20% ethyl acetate : dichloromethane to give the title compound (0.21 g). MS 432.1 (M + 1)., 883984-95-0

883984-95-0 Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate 59165781, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK & CO., INC.; WO2006/44504; (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.153749-89-4,tert-Butyl 2-cyanopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Example 9.1; 2-(2H-Tetrazol-5-yl)-piperidine-1-carboxylic acid tert-butyl ester; 2-Cyano-piperidine-1-carboxylic acid tert-butyl ester (2.1 g, 10 mmol) was mixed with sodium azide (0.715 g, 11 mmol) and ammonium chloride (0.588 g, 11 mmol) in N,N-dimethylformamide (7.5 mL). The reaction mixture was heated at 100 C. for overnight. The reaction mixture was cooled to room temperature and diluted with water. The product was extracted using ethyl acetate. The organic phase was dried over anhydrous sodium sulfate, filtered and concentrated in vacuo. The crude yellow oil gave a white solid after trituration with ethyl acetate, as the title product (1.23 g, 48.6%).1H NMR (300 MHz, CDCl3): delta 5.63 (br, 1H), 4.02 (m, 1H), 2.76 (td, 1H), 2.43 (m, 1H), 1.96 (m, 2H), 1.8 (m, 2H), 1.55 (m, 2H), 1.49 (s, 9H)., 153749-89-4

As the paragraph descriping shows that 153749-89-4 is playing an increasingly important role.

Reference£º
Patent; AstraZeneca AB; NPS PHARMACEUTICALS, INC.; US2007/259916; (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.203662-51-5,4-Allyl-1-Boc-4-hydroxypiperidine,as a common compound, the synthetic route is as follows.

4.i) 4-Hydroxy-4-oxiranylmethyl-piperidine-1-carboxylic acid tert-butyl esterA solution of 4-allyl-4-hydroxy-piperidine-1-carboxylic acid tert-butyl ester (3.1 g, 12.8 mmol, prepared according to J. Comb. Chem. 2002, 4, 125) in DCM and 0.3 M phosphate buffer (pH 8, 150 mL) was treated with mCPBA (3.5 g, 1.1 eq, 70%) and the mixture vigorously stirred at rt overnight. Further 3.5 g of mCPBA were added. After a total of 24 h, the phases were separated, the org. phase dried over MgSO4 and concentrated. CC (hex/EA 2:1 to 1:1 to EA) gave the desired intermediate as colourless oil (0.88 g, 26%).1H NMR (CDCl3) delta: 3.90-3.70 (m, 2H), 3.30-3.10 (m, 3H), 2.83 (dd, J=4.1, 4.9 Hz, 1H), 2.51 (dd, J=2.7, 4.9 Hz, 1H), 1.89 (dd, J=3.8, 14.5 Hz, 1H), 1.80-1.40 (m, 4H), 1.47 (s, 9H)., 203662-51-5

As the paragraph descriping shows that 203662-51-5 is playing an increasingly important role.

Reference£º
Patent; Actelion Pharmaceuticals Ltd; US2011/39823; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

32018-96-5, 1-Benzyl-4-methylpiperidin-3-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The TiCl4(0.2g, 1mmol), NEt3(0.15g, 1 . 5mmol) suspended 200 ml in toluene, then add 1-benzyl-4-methyl-3-ketone piperidine (20.3g, 100mmol), temperature control 35 C methylamine solution is added to the reaction solution (9.32g, 120mmol) reaction 4 hours, adding NaBH (OAC) 3 (0.32g, 1 . 5mmol), glacial acetic acid 2 ml, temperature control 35 C reaction, thin layer monitoring after the reaction is complete. Adding saturated salt water washing, anhydrous sodium sulfate for drying the organic phase, the organic phase concentrated, with residues 35% hydrochloric acid ethanol re-crystallization, to obtain (3R, 4R)-cis-1-benzyl-4-methyl-3-methylamino-piperidine dihydrochloride 17.2g, yield 85.0%, optical purity 99.0% (HPLC method)., 32018-96-5

32018-96-5 1-Benzyl-4-methylpiperidin-3-one 12084828, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Shandong Elohim Pharmaceutical Group Co., Ltd.; Liu, Xiaofeng; Sun, Yuanlong; Yang, Linlin; (12 pag.)CN105884781; (2016); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

79099-07-3,79099-07-3, 1-Boc-4-Piperidone is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

was carried out for 12 h at room temperature.The reaction of the starting material V was completed by TLC (dichloromethane:methanol = 10:1).Spin dry methanol,Adjust pH=9 with saturated NaOH solution,Extracted with dichloromethane (10.00 ml x 3),Dry over anhydrous sodium sulfate, filter,The solvent was evaporated to give a pale yellow oil (yield: 1.00 g).

As the paragraph descriping shows that 79099-07-3 is playing an increasingly important role.

Reference£º
Patent; China Pharmaceutical University; Xu Yungen; Ji Dezhong; Zhang Jingjing; Zhu Qihua; Liang Tingting; Bai Ying; Wang Zhibin; (31 pag.)CN109734700; (2019); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem