Month: July 2021

1030377-21-9, (S)-1-Boc-2-(Hydroxymethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,1030377-21-9

A suspension of 1-fluoro-4-nitrobenzene (1.305 g, 9.25 mmol), (S)-tert-butyl 2-(hydroxymethyl)piperazine-1-carboxylate (2.00 g, 9.25 mmol) and potassium carbonate (1.917 g, 13.87 mmol) in anhydrous DMF (10 mL) was heated to 50 C under a nitrogen atmosphere overnight. The reaction mixture was allowed to cool to room temperature, diluted with water (70 mL) and stirred at roomtemperature for 15 minutes. The precipitated solid was isolated by filtration, washed with water (50 mL), sucked dry and freeze-dried overnight to give the title compound as an orange solid (2.13 g, 68%) . ?H NMR (300 MHz, CDC13) 3 8.11 (dt, 2H), 6.78 (dt, 2H), 4.25 (br s, 1H), 3.85-4.04 (m, 2H), 3.61-3.80 (m, 3H), 3.25-3.43 (m, 2H), 3.18(ddd, 1H), 1.49 (s, 9H). LCMS (Method C): RT = 1.39 mm, m/z = 338 [M+H].

As the paragraph descriping shows that 1030377-21-9 is playing an increasingly important role.

Reference：
Patent; ALMAC DISCOVERY LIMITED; HARRISON, Timothy; TREVITT, Graham; HEWITT, Peter Robin; O’DOWD, Colin Roderick; BURKAMP, Frank; WILKINSON, Andrew John; SHEPHERD, Steven D.; MIEL, Hugues; WO2015/92431; (2015); A1;,
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

General procedure: Synthesis of new compounds 1-4 and 7-9 was performed bynucleophilic substitution (alkylation of amines) following theprocedure previously reported with certain modifications [43].Briefly, the corresponding ferrocene haloalkane (1.0 mmol), thesubstituted amine (1.0 mmol) and K2CO3 or NaH (2.0 mmol) weredissolved in THF (20 mL). The reaction was stirred at room temperatureuntil TLC (CH2Cl2/methanol or hexane/ethyl acetate)proved that the reaction did not go (about 48 h). THF was removedand the residue was diluted in CH2Cl2. The organic phase waswashed with water, dried over anhydrous Na2SO4, filtered, andevaporated. The residue obtained was purified either by automatedflash chromatography, eluting in gradient with CH2Cl2/methanol, orby precipitation with cold diethyl ether. Compounds 5 and 6 werepreviously characterized and evaluated as antibacterial agents [48].So, the general procedure for their synthesis was followed asdescribed by Damljanovic et al. with slight modifications [48]. Amixture of i3 (1.0 mmol), the corresponding amine (1.5 mmol) andMontmorillonite K10 (100 mg) was irradiated by microwave (50W,1.5 min). TLC was used to follow the reaction. The crude wasextracted with CH2Cl2 and evaporated on the rotary evaporator. Theresidue obtained was purified by automated flash chromatography,eluting in gradient with hexane/ethyl acetate. The final compoundwas precipitated with cold diethyl ether in order to obtain an orangepowder.

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

Reference：
Article; Paucar, Rocio; Martin-Escolano, Ruben; Moreno-Viguri, Elsa; Cirauqui, Nuria; Rodrigues, Carlos Rangel; Marin, Clotilde; Sanchez-Moreno, Manuel; Perez-Silanes, Silvia; Ravera, Mauro; Gabano, Elisabetta; European Journal of Medicinal Chemistry; vol. 163; (2019); p. 569 – 582;,
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.1403898-64-5,(2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Tert-butyl (2R,5R)-5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate (770 mg, 3.34 mmol), 181 tert-butylchlorodimethylsilane (756 mg, 5.02 mmol), 132 triethylamine (677 mg, 6.69 mmol) and 182 N,N-dimethylpyridin-4-amine (41 mg, 0.33 mmol) were dissolved in 63 DCM (6 ml) and the mixture was stirred at room temperature for 2 hours. The reaction was quenched with saturated 152 aqueous NH4Cl and extracted with DCM (3×30 ml). The organic phase was washed with brine and dried. The solvent was removed under reduced pressure and the crude product was purified by flash chromatography on a silica gel, eluting from 0-30% (57 EtOAc in 148 petroleum ether). The fractions containing the desired product were evaporated to dryness to afford 183 tert-butyl (2R,5R)-5-(((tert-butyldimethylsilyl)oxy)methyl)-2-methylpiperazine-1-carboxylate (1.04 g, 90%) as a colourless oil. 1H NMR (Chloroform-d, 400 MHz) 0.08 (6H, d), 0.91 (9H, s), 1.30 (3H, d), 1.47 (9H, s), 2.56 (1H, dd), 2.96-3.05 (1H, m), 3.10 (1H, dd), 3.30 (1H, dd), 3.55 (1H, dd), 3.68-3.82 (2H, m), 4.15-4.25 (1H, m), (1 exchangeable proton not seen). m/z (ES+), [M+H]+=345., 1403898-64-5

The synthetic route of 1403898-64-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; Kettle, Jason Grant; Bagal, Sharanjeet; Robb, Graeme Richard; Smith, James Michael; Goldberg, Frederick Woolf; Cassar, Doyle Joseph; Feron, James Lyman; US2019/177338; (2019); 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.17766-28-8,1-Cyclohexylpiperazine,as a common compound, the synthetic route is as follows.

Dissolving Intermediate 5 in DMSO, then adding triethylamine and 1-cyclohexyl piperazine into the solution at temperature about 50-70 C. Adding MTBE and MeOH solution. Isolation and washing of the wet cake with MTBE and MeOH followed by filtering provided Intermediate 6 as a solid

17766-28-8, The synthetic route of 17766-28-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; VM Oncology LLC; Wu, Jay Jie-Qiang; US2015/218132; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of the product of EXAMPLE 5E (300 mg, 1.4 mmol), 2-methoxy-4-(4- methylpiperazin-l -yl)aniline (338 mg, 1 .53 mmol) and triethylamine (421 mg, 4.1 7 mmol) in 1 ,4-dioxane (30 mL) was stirred at 105C under nitrogen for 12 hours. The solvent was removed under vacuum and the residue was washed with sodium bicarbonate solution and ethanol. The crude product was recrystallized from l ;4-dioxane to give the title compound. ‘ H NMR (DMSO-t?) 6 ppm 12.66 (s, 1H), 1 1.35 (s, 1H), 8.31 (d, 7 = 9.0 Hz, 1H), 8.25 (s, 1H), 6.68 (d, J = 1.2 Hz, 1H), 6.54 (dd, J = 1.2, 9.0 Hz, 1 H), 3.89 (s, 3H), 3.21 -3.10 (m, 4H), 2.50-2.44 (m, 4H), 2.25 (s, 3H)., 122833-04-9

122833-04-9 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline 20136253, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ABBOTT LABORATORIES; VASUDEVAN, Anil; PENNING, Thomas, Dale; CHEN, Huanming; LIANG, Bo; WANG, Shaohui; ZHAO, Zhongqiang; CHAI, Dikun; YANG, Leifu; GAO, Yingxiang; WO2012/97479; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: (1) Reaction. To a half-dram vial, in which reagent amine or its hydrochloride (0.050 mmol)was pre-weighed, were added 0.65 mL of a 0.1 M solution of 1-acryloyl-N,N-dimethylindoline-2-carboxamide (rac)-3 in 3.75% dry Et3Neanhydrous THF and 0.25 mL of 3.75% dry Et3N/dry dimethylacetamide and the resulting mixture was shaken at 60 C for 16 h. After cooling to room temperature, the reaction mixture was loaded onto an Oasis MCX cartridge (1 g/6 mL) preconditioned 8 mL of MeOH. The solid-phase matrix was washed with 10 mL of MeOH and then eluted with 5 mL of 1 M ammonia/MeOH. The elute was concentrated to dryness by vacuum centrifuge, providing crude product. In case it is needed, the crude material was purified with preparative LS/MS to give the desired product as salt-free form or formic acid salt dependent on the purification condition. (2) HPLC/LCeMS method. (i) Analytical condition: equipment, Waters 2795; column: Waters XTerra C18, 5 mm, 4.6 50 mm; column temperature, 40 C; detector, photodiodearray (210e400 nm); flow, 1.0 mL/min; solvent (a) as acidic condition, A: 0.1% HCO2H; B: MeOH, gradient, solvent (b) as basic condition, A: 0.1% aqueous ammonia; B: MeOH, gradient; MS condition (ionization method), ESI (positive). (ii) Preparativeconditions: equipment, Waters prep LC/MS system; column, Waters XTerra C18, 5 mm, 20 50 mm; column temperature, ambient temperature; flow, 20.0 mL/min; solvent (a) as acidic condition, A: 0.1% HCO2H; B: MeOH, gradient, solvent (b) as basic condition, A: 0.1% aqueous ammonia; B: MeOH, gradient., 21043-40-3

The synthetic route of 21043-40-3 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Hayashi, Shigeo; Ohashi, Katsuyo; Nakata, Eriko; Emoto, Chie; European Journal of Medicinal Chemistry; vol. 55; (2012); p. 228 – 242;,
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.393781-71-0,1-Boc-2-Ethylpiperazine,as a common compound, the synthetic route is as follows.

Example 55A tert-butyl (2R)-4-[(6-{[5-(difluoromethyl)pyridin-2-yl]oxy}quinolin-2-yl)carbonyl]-2-ethylpiperazine-1-carboxylate The product from Example 14A (300 mg, 0.95 mmol) was subjected to the conditions described in Example 14B, substituting (R)-tert-butyl 2-ethylpiperazine-1-carboxylate for tert-butyl piperazine-1-carboxylate to give the titled compound (470 mg, 97%)., 393781-71-0

As the paragraph descriping shows that 393781-71-0 is playing an increasingly important role.

Reference：
Patent; AbbVie Inc.; Bogdan, Andrew; Cowart, Marlon D.; DeGoey, David A.; Jinkerson, Tammie K.; Koenig, John R.; Kort, Michael E.; Liu, Bo; Matulenko, Mark A.; Nelson, Derek W.; Patel, Meena V.; Peltier, Hillary; Scanio, Marc J.; Wakefield, Brian D.; US2015/218102; (2015); 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,76003-29-7

EXAMPLE 4 9-hydroxy-7-isopropyl-2- (quinolin-2-ylmethyl)-3, 4-dihydro-2H-pyrazino [1, 2-c] pyrimidine-1, 6,8 (7H) – trione Step 1 : 1- (2-Propenyl)-4-tert-butyloxycarbonyl-2-piperazinone To a stirred solution of 4-tert-butyloxycarbonyl-2-piperazinone (10 g, 50 mmol) and allyl bromide (7.25 g, 60 mmol) in DMF (75 mL) at 0 C was added sodium hydride (2.4 g of a 60% suspension in mineral oil, 60 mmol) in portions over a period of 10 min. The mixture was allowed to warm to ambient temperature and stirred for 18 h. The solvent was removed in vacuo and the residue was partitioned between EtOAc and water. The EtOAc layer was dried (MgS04), filtered, and the solvent was removed in vacuo. The residue was purified by silica gel column chromatography using a gradient elution of 33%, 40%, 50%, 60% EtOAc in hexanes. Concentration of product-containing fractions in vacuo gave the title compound as an oil. HPLC RT = 2.80 min (Method A), ES MS (M+H) = 241,’H NMR (400 MHz, CDC13) 8 5.76 (ddt, 1H), 5.2 (overlapping doublets, 2H), 4.10 (s, 2H), 4.04 (d, J = 6 Hz, 2H), 3.64 (t, J = 7 Hz, 2 H), 3.50 (t, J = 7 Hz, 2H), 1.47, (s, 9H).

The synthetic route of 76003-29-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK & CO., INC.; WO2005/92099; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

192130-34-0, tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 24; N-(2-methanosulfonylethyl)-piperazine hydrochloride; Methanesulfonyl chloride (0.7 mL, 9.0 mmol) was added to a cooled solution of 4-(2-amino-ethyl)-piperazine-1-carboxylic acid tert-butyl ester (1.33 g, 5.8 mmol) in pyridine (25.0 mL). The reaction was stirred for 12 h and partitioned between partitioned between aqueous sodium bicarbonate and methylene chloride. The organic phase was washed with 1 M hydrochloric acid, aqueous sodium bicarbonate, and brine, dried over anhydrous magnesium sulfate and concentrated. Purification of the crude residue by chromatography over silica gel using 0-5percent methanol in methylene chloride gave 4-(2-methanesulfonylamino-ethyl)-piperazine-1-carboxylic acid tert-butyl ester (0.70 g, 70percent)., 192130-34-0

As the paragraph descriping shows that 192130-34-0 is playing an increasingly important role.

Reference：
Patent; Fotouhi, Nader; Haley, Gregory Jay; Simonsen, Klaus B.; Vu, Binh Thanh; Webber, Stephen Evan; US2006/211693; (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.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of Intermediate H (190 mg, 0.67 mmol) in DMF (3 mL) were added tert-butyl 3,3-dimethylpiperazine-1-carboxylate (171.3 mg, 0.80 mmol), HATU (329.2 mg, 0.87 mmol) and DIPEA (232 tL, 1.3 mmol) and the mixture was stirred at rt ON. The reaction mixture was then diluted with EtOAc, washed with water and brine consecutively, dried over anhydrous sodium sulfate, filtered and concentrated to dryness. The residue was purified by flash chromatography eluting with EtOAc/hexanes 0-50% in 20 CV to obtain tertbutyl 4- [8-ethyl-6-(4-fluorophenyl)imidazo[ 1 ,2-b]pyridazine-2-carbonyl] -3,3 -dimethylpiperazine-1-carboxylate (235 mg) as a white solid. ?H NMR (400 MHz, CDC13) oe 8.32 (s, 1H), 8.04-7.86 (m, 2H), 7.26 (s, 1H), 7.22-7.11 (m, 2H), 4.39-3.92 (m, 2H), 3.73 -3.40 (m, 4H), 3.09 (m, 2H), 1.65 – 1.59 (m, 6H), 1.50 – 1.40 (m, 12H). LC-MS: 482.5 (M+H).

259808-67-8, As the paragraph descriping shows that 259808-67-8 is playing an increasingly important role.

Reference：
Patent; VERTEX PHARMACEUTICALS INCORPORATED; FARMER, Luc J.; FOURNIER, Pierre-Andre; LESSARD, Stephanie; LIU, Bingcan; ST-ONGE, Miguel; STURINO, Claudio; SZYCHOWSKI, Janek; YANNOPOULOS, Constantin; WO2015/48245; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics