Month: April 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of 2-methylpiperazine (2.2 g) in tetrahydrofuran (15 ml) was added di-tert-butyl dicarbonate (4.0 g) slowly under ice-cooling, and the mixture was stirred at room temperature for 3.5 hours. Then the reaction mixture was diluted with ethyl acetate (20 ml), washed successively with water and brine, and dried over magnesium sulfate. The solvent was evaporated to give the title compound as a colorless oil. The obtained compound was used for the next step without further purification. [00318] 1H-NMR (300 MHz, CDCl3) delta 1.04 (d, J=5 Hz, 3H), 1.45 (s, 9H), 2.40 (br, 1H), 2.65-2.86 (m, 4H), 2.88-3.08 (m, 1H), 3.75-4.15(m, 2H)., 109-07-9

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Fujisawa Pharmaceutical Co., Ltd.; US6825200; (2004); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.208167-83-3,tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,208167-83-3

Into a 50-mL sealed tube, was placed tert-butyl 4-(2-chloroethyl)piperazine-1-carboxylate (300 mg, 1.21 mmol, 1.00 equiv), methylamine (in ethanol) (10 mL), and NaI (100 mg). The resulting solution was stirred for 12 h at 70 C. in an oil bath. The resulting mixture was concentrated under vacuum. The resulting solution was diluted with 3 mL of water and adjusted to pH 7-8 with sodium bicarbonate (5%). The resulting solution was extracted with 2¡Á5 mL of dichloromethane and the organic layers combined. The resulting mixture was washed with 1¡Á3 mL of water and 1¡Á3 mL of brine. The resulting mixture was concentrated under vacuum. This resulted in 180 mg (crude) of tert-butyl 4-(2-(methylamino)ethyl)piperazine-1-carboxylate as brown oil.

The synthetic route of 208167-83-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Ardelyx, Inc.; Lewis, Jason G.; Jacobs, Jeffrey W.; Reich, Nicholas; Leadbetter, Michael R.; Bell, Noah; Chang, Han-Ting; Chen, Tao; Navre, Marc; Charmot, Dominique; Carreras, Christopher; Labonte, Eric; (323 pag.)US9301951; (2016); B2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

142-64-3, Piperazine Dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 5.1.5 Preparation of 1-(2-fluorobenzoyl)piperazine (5) A solution of 2-fluorobenzoic acid (7.00 g, 0.05 mol) and CDI (8.90 g, 0.055 mol) was stirred in dry THF (30 mL) at room temperature for 30 min. In a separate round bottom flask add piperazine (10.76 g, 125 mmol) and piperazine dihydrochloride (20.0 g, 125 mmol) in 60 mL of water. Stir the reaction mixture for 5 min and add 14.0 g of NaCl. Add this brine solution to the round bottom flask containing acyl imidazole. Stir the reaction mixture for 5 hour. The mixture was filtered and the filtrate distilled by rotary evaporation to remove THF. The aqueous layer was washed with ethyl acetate (3 * 10 mL) to remove diacylated product. The PH of the aqueous layer was adjusted to about 9 using saturated solution of NaOH and washed with ethyl acetate (4 * 30 mL). The aqueous layer was discarded. The organic layer was washed with water (4 * 25 mL), dried over anhydrous Na2SO4 and concentrated by rotary evaporation and purified by flash chromatography to afford 1-(2-fluorobenzoyl)piperazine as colourless solid (4.90 g, 48%). The other intermediates 1-(2-chlorobenzoyl)piperazine (6) and 1-[3-(trifluoromethyl)benzoyl]piperazine (7) were prepared by using the general procedure described above., 142-64-3

142-64-3 Piperazine Dihydrochloride 8893, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Dong, Jinyun; Lu, Wen; Pan, Xiaoyan; Su, Ping; Shi, Yaling; Wang, Jinfeng; Zhang, Jie; Bioorganic and Medicinal Chemistry; vol. 22; 24; (2014); p. 6876 – 6884;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

General procedure: A mixture of aryl bromide (1.0 mmol), 4-methylpiperazin-2-one (for compounds 15-17)/morpholin-3-one (for compounds 18-20) (2.0 mmol), N,N0-dimethylethylene diamine (0.1 mmol), K2CO3 (2.0 mmol) and CuI (0.05 mmol) in anhydrous toluene was heated to reflux with stirring for 6 h. Then the reaction mixture was cooled to room temperature, poured into water, stirred vigorously and extracted thrice with ethyl acetate, dried over anhydrous Na2SO4, concentrated under reduced pressure and purified by flash chromatography to afford compounds 14a-f in 54-68% yields. 6.1.16 4-Methyl-1-(4-vinylphenyl)piperazin-2-one (14a) A mixture of 1-bromo-4-vinylbenzene 9 (1.0 g, 5.46 mmol), 4-methylpiperazin-2-one (1.24 g, 10.93 mmol), N,N’-dimethylethylene diamine (0.04 g, 0.54 mmol), K2CO3 (1.51 g, 10.93 mmol) and CuI (0.05 g, 0.27 mmol) in anhydrous toluene was heated to reflux and the reaction was continued as described in general procedure IV to afford 14a (0.7 g) in 60% yield. 1H NMR (400 MHz, CDCl3): delta 7.39-7.48 (m, 2H), 7.24-7.27 (m, 2H), 6.70 (dd, J = 17.6, 10.9 Hz, 1H), 5.73 (dt, J = 17.6, 0.9 Hz, 1H), 5.26 (dt, J = 10.9, 0.9 Hz, 1H), 3.65-3.75 (m, 2H), 3.28 (s, 2H), 2.75-2.83 (m, 2H), 2.41 (s, 3H); LC-MS: 217 (M++1)., 34770-60-0

As the paragraph descriping shows that 34770-60-0 is playing an increasingly important role.

Reference£º
Article; Rakesh; Bruhn, David; Maddox, Marcus; Lee, Robin B.; Yang, Lei; Lee, Richard E.; Madhura, Dora B.; Trivedi, Ashit; Meibohm, Bernd; Scherman, Michael S.; Gilliland, Janet C.; Gruppo, Veronica; McNeil, Michael R.; Lenaerts, Anne J.; Bioorganic and medicinal chemistry; vol. 20; 20; (2012); p. 6063 – 6072,10;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1284243-44-2, tert-Butyl 4-(4-fluorophenyl)-3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 2: 1-(4-fluorophenyl)piperazin-2-one To the solution of tert-butyl 4-(4-fluorophenyl)-3-oxopiperazine-1-carboxylate (2 g, 6.80 mmol) in dichloromethane (5 ml) was added slowly hydrogenchloride in 1,4-dioxane (16.99 ml, 68.0 mmol) at 0 C. and reaction was stirred for 3 h at 25 C. After completion of the reaction, the solvent was evaporated under reduced pressure to obtained salt was triturated with diethyl ether (2*10 ml) decanted it and dried to give 1-(4-fluorophenyl)piperazin-2-one hydrochloride (1.2 g, 5.20 mmol, 77%) 1H NMR (400 MHz, DMSO-d6) delta 9.90 (bs, 1H, D2O exchangeable), 7.38-7.34 (m, 4H), 3.85-3.72 (m, 4H), 3.55-3.50 (m, 2H). MS: m/z 195 (M+1)., 1284243-44-2

The synthetic route of 1284243-44-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; LUPIN LIMITED; Jana, Gourhari; Kurhade, Sanjay Pralhad; Jagdale, Arun Rangnath; Kukreja, Gagan; Sinha, Neelima; Palle, Venkata P.; Kamboj, Rajender Kumar; US2015/152118; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 2; In a reaction vessel, a mixture of 1 l-piperazinyldibenzo[b,fj[l,4]-thiazepine ( 10 Kg), 2- (2-chloroethoxy)ethanol (6.33 kg), sodium carbonate (21.55 kg), 1 kg tetrabutyl ammonium bromide and 0.2 kg sodium iodide was heated in 30 liters of water to about 100 0C. The reaction mixture was maintained at about 100 to 1050C for about 5 hours. EPO Starting l l-piperazinyldibenzo[b,f][l,4]-thiazepine was about 0.3 % by HPLC. Maintained for another 2 hours till the l l-piperazinyldibenzo[b,f][l,4]-thiazepme was about less than 0.08 % by HPLC analysis. The reaction mass was cooled to about 30 0C and aqueous layer extracted with methylenedichloride(100 liters). The organic layer was washed with water and concentrated under reduced pressure. The oily residue was so obtained was suspended in 100 litres of ethanol ( commercial) and 4.1 kg fumaric acid was added. The mixture was stirred for about 4 hours and cooled to about 1O0C. The precipitated quetiapine hemi-fumarate salt was filtered and dried to give 12Kg ( yield 80 % & purity 99.8% by HPLC analysis), 5747-48-8

Big data shows that 5747-48-8 is playing an increasingly important role.

Reference£º
Patent; IPCA LABORATORIES LIMITED; WO2006/77602; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

EXAMPLE 46 5-(3,4-Dimethoxybenzylamino)-2-(2-furyl)-8-[4-(4-trifluoromethylphenyl)piperazin-1-ylmethyl][1,2,4]triazolo[1,5-c]pyrimidine (Compound 46) The subject compound (quantitative) was obtained as a pale brown oily matter from 5-(3,4-dimethoxybenzylamino)-8-formyl-2-(2-furyl)[1,2,4]triazolo[1,5-c]pyrimidine and 1-(4-trifluoromethylphenyl)piperazine in a manner similar to that in Example 1. 1H NMR (CDCl3, delta, ppm): 2.75 (t, J=5.0 Hz, 4H), 3.31 (t, J=5.0 Hz, 4H), 3.88 (s, 3H), 3.88 (s, 3H), 3.90 (s, 2H), 4.76 (d, J=5.6 Hz, 2H), 6.44 (t, J=5.6 Hz, 1H), 6.57 (dd, J=1.7, 3.3 Hz, 1H), 6.85 (d, J=8.0 Hz, 1H), 6.90 (d, J=8.9 Hz, 2H), 6.95 (s, 1H), 6.96 (d, J=8.0 Hz, 1H), 7.22 (d, J=3.3 Hz, 1H), 7.45 (d, J=8.9 Hz, 2H), 7.60 (d, J=1.7 Hz, 1H), 7.96 (s, 1H)

30459-17-7, As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference£º
Patent; Uesaka, Noriaki; Imma, Hironori; Kashima, Hajime; Kurokawa, Masako; Nonaka, Hiromi; Kanda, Tomoyuki; Kuwana, Yoshihisa; Toki, Shinichiro; Shimada, Junichi; US2004/110826; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step D: tert-butyl (3S)-4-[2-(3-cyano-4-fluoro-2-methylphenyl)-2-hydroxyethyl]-3-(hydroxymethyl)piperazine~1~carboxylate: 6-Fluoro-2-methyl-3-(oxiran-2-yl)benzonitrile (12.0g, 67.7 mmol) and (S)-4-N-BOC-2-hydroxymethylpiperazine (22.0 g. 102 mmol) were suspendedin ethanol (100 mL) then heated in a microwave apparatus for 30 minutes at 150 C. Thereaction mixture was cooled and evaporated dryness. The residue was purified by MPLC chromatography through a 330g Redi-sep column eluting with 5%MeOH/95% EtOAc solventsystem to yield the title compound. LC-MS: M+ 1 = 394., 314741-40-7

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; WO2013/28474; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution [OF TERT-BUTYL 3-OXOPIPERAZINE-1-CARBOXYLATE] (0.500 mg, 2. [50] mmol) in 10 mL of DMF at [0 C] was added NaH as a 60% dispersion in mineral oil (2.62 mmol), and the reaction was stirred for 45 minutes. [4-BROMO-1-BUTENE] was added (0.280 mL, 2.75 mmol) dropwise as a solution in 1 mL of THF. The solution was stirred overnight, allowing it to warm to room temperature. The reaction was partitioned between EtOAc and saturated [NAHC03] solution. The organic phase was washed with brine, dried [(NA2S04),] filtered, and concentrated in vacuo to give the titled compound. Proton NMR for the product was consistent with the titled compound. ESI+MS : 255.1 [[M+H]] [+.], 76003-29-7

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference£º
Patent; MERCK & CO., INC.; WO2004/14851; (2004); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

At 0C under nitrogen, 366mg of commercially available 2-chloropyridine-4-carbonyl chloride dissolved in 2ml of dichloromethane were added dropwise to a solution of 530mg of commercially available 4-(1 -piperazinyl)-2-trifluoromethylbenzonitrile in 5ml ofdichloromethane and 630mg of Et3N. The reaction mixture was stirred overnight at room temperature, poured over a stirred mixture of 100ml EtOAc and 40ml of water. The aqueous layer was extracted with EtOAc. The combined organic layers were washed with brine, dried over MgS04, filtered, concentrated under vacuum and purified by column chromatography on silica gel to isolate 620mg of 4-{4-[(2-chloropyridin-4-yl)carbonyl]piperazin-1 -yl}-2- (trifluoromethyl)benzonitrile. 99mg of this material were then added to a degased mixture of 85mg of commercially available 1 -(4-trifluoromethylphenyl)piperazine, 6mg of Pd(OAc)2, 23mg of RuPhos, 163mg of Cs2C03, and 1 .5ml of ie/f-Butanol then, heated to 85 C overnight. The reaction mixture was then poured at room temperature over a stirred mixture of 50ml of EtOAc and 10ml of water. The aqueous layer was extracted with 10ml EtOAc. The combined organic layers were washed with brine, dried over MgS04, filtered, concentrated under vacuum and purified by column chromatography to isolate 60mg of compound No. 32 in Table 2., 30459-17-7

30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS TIERGESUNDHEIT AG; GAUVRY, Noelle; PAUTRAT, Francois; WO2015/71417; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics