Simple exploration of 548769-02-4

The synthetic route of 548769-02-4 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.548769-02-4,1-(Piperidin-4-yl)pyrrolidin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

548769-02-4, EXAMPLE 23; 1-(1-{2-[4-(Benzothiazol-2-yloxy)-phenoxy]-ethyl}-piperidin-4-yl)-pyrrolidin-2-one; A suspension of 2- [4- (2-BROMO-ETHOXY)-PHENOXY]-BENZOTHIAZOLE (EXAMPLE 9; 200 mg, 0.57 mmol), 1-piperindin-4-yl-pryyolidin-2-one hydrochloride (117 mg, 0.57 MMOL), and SILICYCLEE dimethylamine resin (800 mg, 1. 14 mmol) in CH3CN was heated to 70 C for 18 h. The reaction mixture was filtered, and the collected resin was rinsed with CH3CN. The combined filtrates were concentrated under reduced pressure yielding a crude solid, which was purified on SI02 (10 G ; 0-100% 10% [2 M NH3 in CH3OH] in CH2CI2/CH2CI2) to provide a tacky off-white solid (142 mg, 63% yield). MS (ESI) : mass calculated for C24H27N3O3S, 337.18 ; m/z found, 348. 5 [M+H}+. 1H NMR (400 MHz, CECI3) : 7.85 (dd, J= 8.0, 0.5, 1H), 7.75 (dd, J= 8.0, 0.8, 1H), 7.41 (dt, J=7 3,1. 5, 1H), 7.34-7. 22 (m, 3H), 7.02-6. 92 (m, 2H), 4.15 (br d, J = 48.8, 2H), 3.80-3. 65 (m, 1H), 3.40 (t, J=7. 0, 1H), 3.30-3. 10 (BRS, 1H), 3.15, (q, J= 7.2, 1H), 2.96 (brs, 1H), 2.42, (t, J=7. 9,2H), 2.10-1. 99 (m, 1H), 1.81-1. 70 (m, 1H) 1.68-1. 52 (m, 4H), 1.50 (d, J=6. 5,3H)

The synthetic route of 548769-02-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2005/12296; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

New learning discoveries about 1496-40-8

The synthetic route of 1496-40-8 has been constantly updated, and we look forward to future research findings.

1496-40-8, 2-(Piperidin-1-yl)-5-(trifluoromethyl)aniline is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Isonicotinoyl chloride hydrochloride (6.48 g, 36.4 mmol, commercially available product) and triethylamine (5.57 ml, 54.6 mmol) were sequentially added at 0C to a dichloromethane (10 ml) solution of 2-(1-piperidinyl)-5-(trifluoromethyl)aniline (4.45 g, 18.2 mmol) obtained as described in Referential Example 1-2B. The mixture was stirred for half an hour. Water was added to the mixture, and the resulting mixture was extracted three times with ethyl acetate. The obtained organic layer was washed with a saturated sodium chloride solution, dried over anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (200 g, hexane/ethyl acetate = 1/1) and recrystallization. Thus, N-[2-(1-piperidinyl)-5-(trifluoromethyl) phenyl]isonicotinamide (SRPIN-1, GIF-0340) (5.49 g, 86.3%) was yielded as a colorless solid., 1496-40-8

The synthetic route of 1496-40-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; HAGIWARA, Masatoshi; EP1712242; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Some tips on 214834-18-1

214834-18-1 tert-Butyl 4-carbamothioylpiperidine-1-carboxylate 2735648, apiperidines compound, is more and more widely used in various fields.

214834-18-1, tert-Butyl 4-carbamothioylpiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 1: Preparation of E-3-{4-[4-(3,4-ethylendioxphenyl)-thiazol-2-yl]-piperidin-1-yl}-1-(3,4-methylendioxyphenyl)-3-prop-1-ene (Compound I) [Show Image] A. Preparation of intermediate (7) [Show Image] To a solution of tert-butyl 4-(aminocarbonothioyl)piperidine-1-carboxylate (5) (1 eq.) in DMF (5 vol eq.) a solution of bromoketone (6) (1.05 eq.) in DMF (10 vol eq.) is added drop wise at 0C. The mixture is left to stir overnight gradually warming to room temperature. Triethylamine (2.2 eq.) is added portionwise to the resulting solution at room temperature, and then stirred for further 30 minutes. The reaction mixture is poured into water and extracted 3 times with ethyl acetate. The organic layers are combined, washed with waterand brine, dried overnight over MgSO4, and concentrated in vacuo. The desired product is obtained as a pale orange oily residue, collected and dried in a vacuum oven. Yield 68%., 214834-18-1

214834-18-1 tert-Butyl 4-carbamothioylpiperidine-1-carboxylate 2735648, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Oridis Biomed Forschungs- und Entwicklungs GmbH; EP1832585; (2007); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

New learning discoveries about 930785-40-3

930785-40-3 tert-Butyl 1-oxa-4,9-diazaspiro[5.5]undecane-9-carboxylate 53302318, apiperidines compound, is more and more widely used in various fields.

930785-40-3,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.930785-40-3,tert-Butyl 1-oxa-4,9-diazaspiro[5.5]undecane-9-carboxylate,as a common compound, the synthetic route is as follows.

Example 40; Methyl (3-{2-[9-(4-{[6-amino-2-(2-methoxyethoxy)-8-oxo-7,8-dihydro-9H-purin-9-yl]methyl}benzyl)-1-oxa-4,9-diazaspiro[5.5]undec-4-yl]ethoxy}phenyl)acetate; [Show Image] Step (i); tert-Butyl 4-{2-[3-(2-methoxy-2-oxoethyl)phenoxy]ethyl}-1-oxa-4,9-diazaspiro[5.5]undecane-9-carboxylate; [Show Image] tert-Butyl 1-oxa-4,9-diazaspiro[5.5]undecane-9-carboxylate (769mg, 3mmol) and potassium carbonate (622mg, 4.5mmol) were suspended in dimethylformamide (15ml) and thereto was added at room temperature methyl [3-(2-bromoethoxy)phenyl]acetate (1.09g, 4mmol), followed by stirring at 85C for 15 hours. After being cooled, thereto was added water and the mixture was extracted with ethyl acetate. The organic layer was washed with water and saturated brine and dried over sodium sulfate. After removal of the solvent by distillation, the residue was purified by silica gel column chromatography to give the object compound 565mg as a colorless oil. Yield 42% 1H NMR (CDCl3) delta7.27-7.23 (1H, m), 6.93-6.78 (3H, m), 4.13-4.06 (2H, m), 3.90-3.65 (4H, br), 3.71 (3H, s), 3.61 (2H, s), 3.22-3.15 (2H, br), 2.73 (2H, br), 2.54 (2H, brs), 2.37 (2H, brs), 2.00-1.91 (2H, br), 1.51-1.41 (2H, br), 1.46 (9H, s).

930785-40-3 tert-Butyl 1-oxa-4,9-diazaspiro[5.5]undecane-9-carboxylate 53302318, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Dainippon Sumitomo Pharma Co., Ltd.; AstraZeneca AB; EP1939202; (2008); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Simple exploration of 268550-48-7

As the paragraph descriping shows that 268550-48-7 is playing an increasingly important role.

268550-48-7, tert-Butyl 1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The mixture of tert-butyl l-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate (1.83 g, 7.20 mmol), commercially available 4-bromofuran-2(5H)-one (1.41 g, 8.63 mmol), xantphos (0.416 g, 0.720 mmol), water (0.389 mL, 21.6 mmol) , and potassium carbonate (1.989 g, 14.39 mmol) in toluene (50 mL) was degassed with nitrogen followed by addition of palladium acetate (0.081 g, 0.36 mmol). The resulting mixture was heated at 65 C for 16 h. After filtration through celite, the filtrate was concentrated and the residue was purified on silica gel column using EtOAc /hexane as eluting solvents to give the title compound. LC/MS: (M+l)+: 337.18., 268550-48-7

As the paragraph descriping shows that 268550-48-7 is playing an increasingly important role.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; DING, Fa-Xiang; DONG, Shuzhi; FRIE, Jessica; GU, Xin; JIANG, Jinlong; PASTERNAK, Alexander; TANG, Haifeng; WU, Zhicai; YU, Yang; SUZUKI, Takao; WO2014/15495; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

New learning discoveries about 91419-48-6

91419-48-6 tert-Butyl 4-carbamoylpiperidine-1-carboxylate 2735646, apiperidines compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.91419-48-6,tert-Butyl 4-carbamoylpiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

91419-48-6, 2) Second Step: Synthesis of the t-butyl ester of 4-cyanopiperidine-1-carboxylic acid 2.05 g (9 mmol) of the t-butyl ester of 4-carbamoylpiperidine-1-carboxylic acid as obtained in the first step above were introduced into a Schlenck tube in the presence of 1.7 ml of DIEA (1-1 eq.). The medium was flushed under argon, and 18 ml of anhydrous THF were then added. The reaction medium was then cooled to a temperature of 0 C. and 1.38 ml of trifluoroacetic anhydride (1.1 eq.) were added dropwise. The medium then became totally clear. If the reaction is not complete after 1 hour, a further 0.5 equivalent of DIEA and then of trifluoroacetic anhydride are added. The reaction was monitored by TLC, staining with ninhydrin. At the end of the reaction, the organic phase was washed successively with aqueous solutions of 5% NaHCO3, 0.1N KHSO4 and saturated NaCl solution. The expected product was not visible under UV light. In the event of appearance of a UV-visible compound, a purification by flash chromatography in a gradient of eluent ranging from cyclohexane up to a 9/1 cyclohexane/ethyl acetate mixture may be performed. 1.1 g of a very pale yellow liquid that solidified after a few hours were obtained.1H NMR: (CDCl3): 3.63 (m, 2H), 3.36 (m, 2H), 2.8 (m, 1H), 1.84 (m, 4H), 1.45 (s, 9H).MS m/z: 211 (M++1)

91419-48-6 tert-Butyl 4-carbamoylpiperidine-1-carboxylate 2735646, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Institut Pasteur De Lille; Centre National De La Recherche Scientifique; Universite De Lille 2, Universite Du Droit Et De La Sante; Institut National De La Sante Et De La Recherche Medicale (Inserm); US2011/136823; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Simple exploration of 71233-25-5

The synthetic route of 71233-25-5 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.71233-25-5,1-tert-Butyl 4-ethyl 3-oxopiperidine-1,4-dicarboxylate,as a common compound, the synthetic route is as follows.,71233-25-5

G. 5-Amino-3,6-dihydro-2H-pyridine-1,4-dicarboxylic acid 1-tert-butyl ester 4-ethyl ester (35a2) To a solution of 34a2 (24 g, 88.5 mmol) was added ammonium in EtOH (88 mL, 180 mmol, 2M). The reaction mixture was heated to 60 C for 3 h. The solvent was evaporated under reduced pressure to afford a yellow solid (23 g, 91.5percent). MS (ES+): m/z=271 (M+1)

The synthetic route of 71233-25-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Hurley, Timothy Brian; Lee, Kwangho; Peukert, Stefan; Wattanasin, Sompong; US2009/325948; (2009); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

New learning discoveries about 154775-43-6

The synthetic route of 154775-43-6 has been constantly updated, and we look forward to future research findings.

154775-43-6, 3-(1-(tert-Butoxycarbonyl)piperidin-4-yl)propanoic acid is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,154775-43-6

Step A Iodomethane (556 muL, 8.93 mmol) was added dropwise to a cooled (0 C.) mixture of commercially available 3-[1-(tert-butoxycarbonyl)piperidin-4-yl]propanoic acid (2.09 g, 8.12 mmol) and K2CO3 (2.81 g, 20.3 mmol) in 20 mL of DMF. The reaction mixture was permitted to warm to rt and stir overnight. The reaction mixture was diluted with ether and washed four times with water, then once with brine. The ethereal layer was dried over anhydrous MgSO4, filtered, and concentrated. Purification by MPLC (silica, 40% ethyl acetate/hexanes) provided tert-butyl 4-(3-methoxy-3-oxopropyl)piperidine-1-carboxylate:

The synthetic route of 154775-43-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Goble, Stephen D.; Mills, Sander G.; Yang, Lihu; Pasternak, Alexander; US2007/238723; (2007); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Downstream synthetic route of 84163-13-3

84163-13-3 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride 11334359, apiperidines compound, is more and more widely used in various fields.

84163-13-3, 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

84163-13-3, 10g of reactant 6-fluoro-3-(4-piperidinyl)-1,2-benzoisoxazole hydrochloride and 10.4g of reactant 1-[4-(3-chloropropoxyl)-3-inethoxyphenyl]ethyl ketone were placed in a 250ml reaction flask, and a solution prepared with 17.9g potassium carbonate and 120ml water was added thereto. The reaction mixture was heated to 80-90 C and stirred for 1.5 hours, then naturally cooled to room temperature under stirring and filtered. The filter cake was washed twice with water, and then washed twice with methanol, and dried in vacuum at 50 C to obtain 15.1g crude iloperidone. The yield was 91.0%. The crude product was decolored by active carbon, then recrystallized with toluene to obtain iloperidone. The purity was 99.5% (determined by HPLC), and the melting point was 118~120C.

84163-13-3 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride 11334359, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Zhejiang Huahai Pharmaceutical Co., Ltd.; EP2479176; (2012); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Brief introduction of 167757-45-1

The synthetic route of 167757-45-1 has been constantly updated, and we look forward to future research findings.

167757-45-1, Benzyl 4-(aminocarbonyl)tetrahydro-1(2H)-pyridinecarboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of compound VI-A-43 (13.8 g), P2S5 (15.4 g) and anhydrous NaHCO3 (17.9 g) in ethylene glycol dimethyl ether (207 muL) was stirred at 60 C. overnight. After cooling to room temperature, the solution was filtered and concentrated to about of original volume, then poured into ice/water. The precipitated light yellow solid was collected by filtration and dried to give 13.5 g of intermediate X-B-43., 167757-45-1

The synthetic route of 167757-45-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Kalypsys, Inc.; US2005/234046; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem