Month: March 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13754-38-6,1-Benzoylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: To a mixture of 1-benzoylpiperazine (1.0 eq) and potassium carbonate (2.0 eq) in dimethylformamide was added dropwise a solution of the corresponding substituted 9-bromo-9H-fluorene (1.0 eq) in dimethylformamide (The synthesis of 9-bromo-9H-fluorene derivatives is reported in supporting information). After stirring for 24 h at room temperature, solvent was removed and the crude residue was dissolved in diethyl ether, washed with brine, dried over magnesium sulfate,filtered and concentrated under vacuum. The residue was purified by flash chromatography as indicated in each case to afford the title compound. Reagents: 1-Benzoylpiperazine (0.23 mmol, 44 mg), potassium carbonate (0.46 mmol, 64 mg) and 3-(benzyloxy)-9-bromo-9H-fluorene (0.23 mmol, 81 mg). The crude product was purified by flash chromatography (gradient, 100% petroleum ether to 100% ethyl acetate in 15 min) to afford a yellow oil (54.3 mg, 50%). TLC Rf: 0.40 (petroleum ether/ethyl acetate 80/20). IR (cm-1): 697, 710, 770, 1001, 1017, 1186, 1257, 1278, 1427, 1448, 1488, 1578, 1628, 2851, 2920. HPLC: method 2, rt = 3.65 min, purity 98%. 1H NMR (300 MHz, CDCl3) delta (ppm): 2.45 (bs, 2H); 2.86 (bs, 2H); 3.38 (bs, 2H); 3.83 (bs, 2H); 4.86 (s, 1H); 5.18 (s, 2H); 6.97 (dd, J = 2.4 Hz, 8.1 Hz, 1H); 7.34 (td, J = 2.1 Hz, 7.8 Hz, 2H); 7.37-7.48 (m, 9H); 7.51 (s, 1H); 7.53 (t, J = 8.4 Hz, 2H); 7.65 (t, J = 8.1 Hz, 2H). 13C NMR (75 MHz, CDCl3) delta (ppm): 42.9 (CH2); 48.6 (2 * CH2); 49.5 (CH2); 69.4 (CH2); 70.4 (CH2); 106.3 (CH); 113.8 (CH); 119.8 (CH); 125.9 (CH); 126.6 (CH); 127.1 (2 * CH); 127.4 (CH); 127.6 (2 * CH); 128.1 (CH); 128.3 (CH); 128.4 (2 * CH); 128.7 (2 * CH); 129.6 (CH); 135.7 (C); 135.9 (C); 137.0 (C); 140.9 (C); 142.6 (C); 144.4 (C); 159.5 (C); 170.3 (C). MS (DCI/CH4) m/z: 461.22 [M+H+]. HRMS (DCI/CH4): for C31H29N2O2 [M+H+]: calcd: 461.2229; found: 461.2235., 13754-38-6

As the paragraph descriping shows that 13754-38-6 is playing an increasingly important role.

Reference£º
Article; Chollet, Aurelien; Mori, Giorgia; Menendez, Christophe; Rodriguez, Frederic; Fabing, Isabelle; Pasca, Maria Rosalia; Madacki, Jan; Kordulakova, Jana; Constant, Patricia; Quemard, Annaik; Bernardes-Genisson, Vania; Lherbet, Christian; Baltas, Michel; European Journal of Medicinal Chemistry; vol. 101; (2015); p. 218 – 235;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13484-40-7, 1-(2-Methoxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A15. 1-(5-Bromo-pyridine-2-sulfonyl)-4-(2-methoxy-ethyl)-piperazine; 809 mg of 1-(2-methoxyethyl)-piperazine are dissolved in 9.0 ml of dichloromethane and 9.0 ml of an aqueous K2CO3 solution (strength 4.0 M). Subsequently, the reaction mixture is cooled in an ice bath and a solution of 1.20 g of 5-bromo-pyridine-2-sulfonyl chloride (compound B8) in 2.0 ml of dichloromethane is added dropwise. Thereafter, the reaction mixture is allowed to warm up to room temperature during which time the two-phase system is vigorously stirred for 1 hour. For workup, the organic layer is separated and the aqueous layer is extracted once with 10 ml of dichloromethane. The combined organic layers are dried, using Na2SO4, filtered with suction and evaporated to dryness to yield 1.70 g of the title compound as yellow oil, which crystallizes at room temperature. M. p. 940C. ESI- MS: 364.3/366.1 (MH+). TLC: Rf = 0.40 (dichloromethane/ethanol 20:1 parts by volume)., 13484-40-7

13484-40-7 1-(2-Methoxyethyl)piperazine 2734638, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ALTANA Pharma AG; WO2007/39578; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In THF (30 ml) were added N-(2-hydroxyethyl)piperazine (500 mg, 3.84 mmol), a solution of formaldehyde (3117 mg, 38.41 mmol) and sodium cyanoborohydride (1207 mg, 19.20 mmol). The mixture was heated up to 50¡ã C. overnight under stirring. After cooling some water was added and the mixture was extracted with DCM (3.x.). The organic layers were dried over MgSO4 and evaporated. The residue was purified over a silica plug with DCM/MeOH 9:1 as eluant to afford an oil (370 mg, Y=67percent). 1H NMR (DMSO-d6) delta 4.45 (t, J=5.3 Hz, 1H), 3.51-3.45 (m, 2H), 3.02-2.84 (m, 4H), 2.71-2.64 (m, 2H), 2.61 (s, 3H), 2.58-2.53 (m, 2H), 2.47-2.43 (m, 2H).

103-76-4, 103-76-4 N-(2-Hydroxyethyl)piperazine 7677, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ARES TRADING S.A.; US2008/51397; (2008); 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.169448-87-7,(R)-tert-Butyl 2-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of tert-butyl (2f?)-2-(hydroxymethyl)piperazine-1-carboxy.ate (0.479 g) and triethylamine (0.618 ml_) in THF (6 ml_) was added dropwise a solution of 6-bromo-1-oxo- 1 ,2-dihydroisoquinoline-4-sulfonyl chloride (Example 46a, 0.715 g) in THF (10 ml_). The reaction was stirred at room temperature for 20 min. The resulting solution was concentrated under reduced pressure before adding water and extracting into ethyl acetate. The combined organics were dried (MgSO4), filtered and evaporated under reduced pressure. Trituration with ethyl acetate gave the subtitle compound (0.855 g). MS: APCI(-ve) 500 / 504 (M-H)” 1H NMR delta (CDCI3) 8.34 (d, 1 H), 8.30 (d, 1 H), 8.05 (s, 1 H), 7.73 (dd, 1 H), 4.32 – 4.18 (m, 1H), 4.00 (d, 1 H), 3.88 (d, 1 H), 3.72 (d, 1 H), 3.63 (d, 2H), 3.10 – 2.96 (m, 1 H), 2.84 (td, 2H), 1.44 (s, 9H)

169448-87-7, The synthetic route of 169448-87-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; BROUGH, Stephen, John; LUKER, Timothy, Jon; ROBERTS, Bryan, Glyn; ST-GALLAY, Stephen, Anthony; WO2010/39079; (2010); 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.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Description 146(S)-tert-butyl 3-methylpiperazine-1-carboxylate (1)146)NHBocTo a solution of (S)-2-methylpiperazine (500 mg) in DCM (5 mL) was added Et3N (1010 mg) and(Boc)20 (1198 mg) in DCM (3 mL) dropwise. The mixture was stirred at 0C for 2 hours. DCM(10 mL), water (5 mL) and 30% NaHSO4 (10 mL) aqueous solution were added to the reactionmixture. The resulted mixture was stirred for 10 mm, and to the aqueous layer was added saturatedNa2CO3 solution until pH = 8, extracted with isopropyl alcohol: chlorofonn1: 3 (5 x20 mL). The combined organic layer was washed with brine (5 mL), dried over Na2SO4, filtered and concentrated to afford the title compound (562 mg) as pale yellow oil, MS (ESI): C10H20N202 requires 200; found 201 [M+H]., 74879-18-8

The synthetic route of 74879-18-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXOSMITHKLINE (CHINA) R&D COMPANY LIMITED; DENG, Jing; LEI, Hui; MA, Xin; LIN, Xichen; WO2015/180612; (2015); 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.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.

To a stirred solution of IV (0.100 g, 0.30 mmol), VI (0.095 g, 0.46 mmol) in DMF (2 mL) wasadded HATU (0.230 g, 0.61 mmol) and DIPEA (0.16 mL, 0.9 mmol) and reaction mixture was allowed tostir at RT for 16 h. Reaction mixture was diluted with water and extracted with ethyl acetate (10 mL x 3).Brine washing was given to the organic layer and dried over Na2SO4. Combined organic layer wasconcentrated under vacuum and purified by using reverse phase HPLC to obtain 3 (0.017 g, 11%).LCMS: 525 [M+1]+1HNMR (400 MHz,CD3OD) delta 8.3 (s, 1H), 8.0 (s, 1H), 7.9 (t, 2H), 7.8 (d, 1H), 7.7 (d, 2H),7.6 (m, 2H), 7.5(m, 2H), 7.4 (d, 2H), 7.1 (t, 1H), 3.6 (s, 2H), 2.8 (s, 4H), 2.6 (s, 4H), 2.5 (s, 3H), 2.4 (s, 3H), 70261-82-4

70261-82-4 4-(4-Methylpiperazin-1-ylmethyl)phenylamine 3153996, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Ramachandran, Sreekanth A.; Jadhavar, Pradeep S.; Miglani, Sandeep K.; Singh, Manvendra P.; Kalane, Deepak P.; Agarwal, Anil K.; Sathe, Balaji D.; Mukherjee, Kakoli; Gupta, Ashu; Haldar, Srijan; Raja, Mohd; Singh, Siddhartha; Pham, Son M.; Chakravarty, Sarvajit; Quinn, Kevin; Belmar, Sebastian; Alfaro, Ivan E.; Higgs, Christopher; Bernales, Sebastian; Herrera, Francisco J.; Rai, Roopa; Bioorganic and Medicinal Chemistry Letters; vol. 27; 10; (2017); p. 2153 – 2160;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of fe/f-butyl (2S)-2-methylpiperazine-1 -carboxylate (22.2 g, 1 1 1 mmol), 2,4- dichloropyrimidine (15.0 g, 101 mmol), and triethylamine (30 mL) in dichloromethane (200 mL) was stirred at 30 C for 15 hours, whereupon it was washed sequentially with water (150 mL) and with saturated aqueous sodium chloride solution (100 mL), dried over magnesium sulfate, filtered, and concentrated in vacuo. Chromatography on silica gel (Gradient: 20% to 50% EtOAc in petroleum ether) afforded C36 as a white solid. Yield: 25.0 g, 79.9 mmol, 79%.

169447-70-5, The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PFIZER INC.; ASPNES, Gary Erik; BAGLEY, Scott W.; CONN, Edward L.; CURTO, John M.; EDMONDS, David James; FLANAGAN, Mark E.; FUTATSUGI, Kentaro; GRIFFITH, David A.; HUARD, Kim; LIMBERAKIS, Chris; MATHIOWETZ, Alan M.; PIOTROWSKI, David W.; RUGGERI, Roger B.; (149 pag.)WO2019/239371; (2019); A1;,
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

Weigh between methoxybenzoate 7.6g (0.05mol) was dissolved in 20ml of dry tetrahydrofuran was slowly added CDI8.9g (0.055mol), at room temperature for 4hAfter the reaction solution through a dropping funnel was added dropwise to a solution of constant piperazine dihydrochloride 20g (0.125mol), anhydrous piperazine 10g (0.125mol), 60ml of an aqueous solution of sodium chloride, 14g, and reacted for 5 hours at room temperature .After completion of the reaction by suction, the filtrate evaporated to remove THF, 10ml ethyl acetate again, NaOH saturated solution was adjusted to pH = 10, and the combined organic phase was extracted 3 times with ethyl acetate. The organic phase was dried over anhydrous sodium sulfate overnight, pumping filtered, spin dry ethyl acetate, the resulting white crystals is 1- (3-methoxybenzoyl) piperazine crude product 6.5g, 59% yield.

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

Reference£º
Patent; Xi’an Jiaotong University; Zhang, Jie; Lu, Wen; Dong, Jinyun; Pan, Xiaoyan; He, Langchong; Zhang, Tao; Wang, Sicen; Shen, Xiuxiu; (16 pag.)CN104262238; (2016); B;,
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.

A solution of l-bromo-4-(trifluoromethyl)benzene (1.0 g, 4.44 mmol, 1.00 equiv), pyridin-4-ylboronic acid (820 mg, 6.67 mmol, 1.50 equiv), PCy3 (156 mg, 0.56 mmol, 0.14 equiv), Pd2(dba)3 (220 mg, 0.24 mmol, 0.06 equiv), and K3P04 (2.5 g, 11.79 mmol, 3.00 equiv) in 1,4-dioxane (10 mL) was placed in a 20-mL sealed tube under inert atmosphere stirred overnight at 100C in an oil bath, and then concentrated under vacuum. Purification via silica gel column (ethylacetate/petroleum ether (1:20)) yielded 1.2 g (crude) of 4-(4- (trifluoromethyl)phenyl)pyridine as a yellow solid., 30459-17-7

The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIOENERGENIX; MCCALL, John, M.; MCKEARN, John; ROMERO, Donnal, L.; CLAIR, Michael; WO2011/28947; (2011); A2;,
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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Compound P42: 5-(Morpholin-4-yl)-2-nitroaniline To the flask 2-amino-3-nitro-6-chloropyridine (1.50 g, 8.47 mmol), potassium carbonate (1.30 g, 9.32 mmol) and morpholine (10.5 ml, 119 mmol) were added. The reaction was carried out under argon flow at 130¡ãC overnight. The progress of the reaction was monitored by TLC (system: heptane/ethyl acetate, 1 /1 ). The mixture was cooled to room temperature and poured into the ice-water. A precipitated yellow solid was filtered and dried. 1.789 g of the title product were obtained (yield 94.2percent). Compound P48: 5-[(3R,5S)-3,5-dimethylpiperazin-1 -yl]-2-nitroaniline; The compound was obtained by the method analogous to that described for Compound P42. Starting from 5-chloro-2-nitroaniline (0.800 g, 4.64 mmol), potassium carbonate (0.705 g, 5.10 mmol) and cis-2,6-dimethylpiperazine (1.620 g, 13.9 mmol) in 5 ml of DMF, 1.144 g of the title product in the form of a yellow solid were obtained (yield 98.6percent). MS-ESI: (m/z) calculated for C12H19N4O2 [ + H]+: 251.15, found 251.1.

21655-48-1, 21655-48-1 cis-2,6-Dimethylpiperazine 6950261, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CELON PHARMA S.A.; ZDZALIK, Daria; LIPNER, Joanna; WIECZOREK, Maciej; DZWONEK, Karolina; YAMANI, Abdellah; DUBIEL, Krzysztof; LAMPARSKA-PRZYBYSZ, Monika; GRYGIELEWICZ, Paulina; STANCZAK, Aleksandra; WO2014/141015; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics