Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

50 ml of THF and 5 g (0.153 mol) of 1- hydroxyethylpiperazine are placed in a 500 ml three-necked flask equipped with a thermometer, a condenser and a bubbler, with magnetic stirring and under a stream of nitrogen. After cooling to 0¡ãC, 1.539 g (0.064 mol) of sodium hydride are added and this medium is stirred for 1 hour to obtain the alkoxide. A solution derived from 250 ml of THF and 4.3 g (0.028 mol) of 3-fluoro-4-nitroaniline is added dropwise to this alkoxide. The medium obtained is stirred for 24 hours while monitoring by TLC (9/1 CH2Cl2/MeOH). The solvent is removed by evaporation on a rotavapor, followed by purification on a column of silica, eluting with dichloromethane/methanol. The compound thus obtained in the form of a yellow powder, in a mass of 9.3 g, corresponds to the expected compound. Analysis by mass spectrometry confirms the structure of the expected compound. The quasi-molecular ions [M+H]+ and [M+Na] + of the expected molecule C13H20N4O3 are mainly detected.

5464-12-0, As the paragraph descriping shows that 5464-12-0 is playing an increasingly important role.

Reference£º
Patent; L’OREAL; FADLI, Aziz; WO2013/87934; (2013); 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.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution of 4,6-dichloro-2-methylpyrimidine (2.86 g, 17.5 mmol) in 1,4- dioxane (200 niL) was added 2~(piperazin-l-yl)ethanol (1.14 g, 1.08 mmol) and N5N- diisopropylethylamine (12.2 mL, 70 mmol). The reaction mixture was stirred overnight at room temperature. The solvent was removed in vacuo. The residue was dissolved in EtOAc (150 mL) and washed with saturated NaHCO3 (2 x 50 mL). The organic layer was dried (Na2SO4). The solvent was removed in vacuo to afford the crude product (1.86 g, 83%) as yellow oil.

103-76-4, The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; TARGEGEN, INC.; WO2007/56023; (2007); 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.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

292To a solution of 1-137 (0.21 mmol, 0.10 g) in DCM (2 mL) is added l-methyl-piperazin-2-one hydrochloride (0.030 g , 0.26 mmol) followed by NaBH(OAc)3 (0.47 mmol, 0.10 g) and acetic acid (0.60 mmol, 0.035 mL). The mixture is stirred at room temperature for 6 days then concentrated under reduced pressure. The residue is purified by C18 reverse phase flash chromatography to provide 1-152 (0.044 g , 36%) as a clear film. To a suspension of 1-152 (0.076 mmol, 0.044g) in a 1 : 1 mixture of methanol : water (10 mL) is added LiOH (1.2 mmol, 0.050 g). The mixture is stirred at room temperature for 3 days during which time all of the solids went into solution. The pH of the mixture is then adjusted to approximately pH 5 by the addition of a 2N solution of hydrochloric acid and the mixture is concentrated under reduced pressure. The residue is purified by flash C18 reverse phase chromatography to provide the title compound (0.007 g, 16%) as a white powder., 109384-27-2

As the paragraph descriping shows that 109384-27-2 is playing an increasingly important role.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BERRY, Angela; BOSANAC, Todd; GINN, John David; HOPKINS, Tamara Denise; SCHLYER, Sabine; SOLEYMANZADEH, Fariba; WESTBROOK, John; YU, Maolin; ZHANG, Zhonghua; WO2013/25425; (2013); 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

0.5 mol of N-hydroxyethylpiperazine, 0.565 mol of sodium 2-hydroxyethanesulfonate and 500 mL of methanol were charged into a 1000 mL four-necked flask equipped with a reflux tube and subjected to a condensation reaction with sufficient stirring;First reacted at 50 for 2.5 hours, then gradually heated to reflux and continued to react for 3.0 hours;And then cooled to obtain a reaction mother liquor containing 4-hydroxyethylpiperazineethanesulfonate.The yield of sodium 4-hydroxyethylpiperazineethanesulfonate was calculated to be 93.6% by high performance liquid chromatography. 20 L of 4-hydroxyethylpiperazineethanesulfonate,Mass concentration of 15wt% raffinate, in the stirring effect,Diluted with deionized water to a concentration of 5 wt% by dialysis dialysis to remove sodium chloride,And finally concentrated by evaporation, cooling crystallization, filtration to get pure HEPES products,And finally washed once with anhydrous methanol, and dried by vacuum to obtain purified HEPES. The purified HEPES sample was formulated as a solution and then tested for purity:The purified HEPES sample was prepared as a solution and then tested for purity, 99.9%, yield 85.6%, pH = 6.46, Cl- concentration 6.8 mug / g., 103-76-4

The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Shandong Lianchuang Careful Chemicals Co., Ltd.; Wu Shaozu; (6 pag.)CN106905262; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21655-48-1, cis-2,6-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred suspension of 1?fluoro?4?nitrobenzene (562 mg, 3.98 mmol) and potassium carbonate (688 mg, 4.98 mmol) in anhydrous DMSO (2 mL) was added (2S,6R)?2,6? dimethylpiperazine (500 mg, 4.38 mmol) and the mixture heated at 100 ¡ãC for 16 h. After cooling the mixture wassuspended in water (40 mL) and filtered under vacuum to afford the title compound (889 mg, 95percent) . ?H NMR (500 MHz, DMSO?d6) : 3 8.03 (d, 2H) , 7.03 (d, 2H) , 3.88 (dd, 2H) 2.75?2.79 (m, 2H), 2.37?2.42 (m, 2H), 2.28 (br s, 1H),1.03 (d, 6H) . LCMS (Method C) : = 0.51 mi m/z = 236[M+H]., 21655-48-1

As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

Reference£º
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

109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 9: 3-(4-Methylpiperazin-1-yl)-propan-1-ol 1-Methylpiperazine (6.99 mL, 63 mol) was dissolved in toluene (30 mL). 3-Bromopropanol (2.62 mL, 30 mmol) was slowly and the mixture was stirred overnight at r.t. After heating to 80 C. for 2 h and cooling to r.t., the mixture was filtered and the filter cake was thoroughly washed with toluene. After removal of the solvent, the residue was subjected to distillation (b.p., 180 C./2 mbar) to obtain a colourless oil (4.08 g, 25.8 mmol, 86%). 1H NNR (CDCl3): delta=1.70 (Psi-quint, J?5.8 Hz, 2 H), 2.26 (s, 3 H), 2.35-2.6 (m, 8 H), 2.60 (Psi-t, J=5.8 Hz, 2 H), 3.77 (Psi-t, J=5.3 Hz, 2 H), 4.09 (s, br., 1 H)., 109-01-3

As the paragraph descriping shows that 109-01-3 is playing an increasingly important role.

Reference£º
Patent; 4SC AG; US2006/142570; (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.54699-92-2,4-Methyl-1-piperazineacetic acid,as a common compound, the synthetic route is as follows.

A solution of (1R,2R)-2-[[trans-2-[(1E,3E)-4-(4-cyano-2-fluorophenyl)-1,3-butadienyl]-1,3-dioxan-5-yl]thio]-1-(2,4-difluorophenyl)-1-[(1H-1,2,4-triazol-1-yl)methyl]propyl 2-(hydroxymethyl)benzoate (1.104 g, 1.63 mmol) obtained from Example 17-(4) in dichloromethane (25 ml) was cooled to 0C, and then 4-(N,N-dimethylamino)pyridine (299.1 mg, 2.45 mmol), 2-(4-methyl-1-piperazinyl)acetic acid (described in J. Med. Chem., 43, 1493 (2000); 387.3 mg, 2.45 mmol), and 1-ethyl-3-[3-(N,N-dimethylamino)propyl]carbodiimide (625.5 mg, 3.26 mmol) were added thereto. The reaction solution was stirred at room temperature for 4 hours, diluted with dichloromethane, and then the organic layer was washed successively with water and a saturated aqueous solution of sodium chloride. The solvent was evaporated under reduced pressure, and the residue was subjected to chromatography on a silica gel (40 g) column (eluent; ethyl acetate : methanol = 4 : 1) to give a mixture of the title target compound and 4-(N,N-dimethylamino)pyridine. The mixture was purified by recycle preparative HPLC [LC-908; Japan Analytical Industry Co., Ltd.; GPC column JAIGEL-1H (20 mm i.d. x 600 mm) and JAIGEL-2H (20 mm i.d. x 600 mm) connected in series for use; solvent, chloroform] to afford the title target compound (865.2 mg, 65% yield) as a colorless amorphous solid. NMR spectrum (400 MHz, CDCl3) delta ppm: 1.46 (3H, dd, J=7, 2 Hz), 2.29 (3H, s), 2.4-2.5 (4H, br s), 2.6-2.7 (4H, br s), 3.05 (1H, tt, J=12, 5 Hz), 3.31 (2H, s), 3.50 (1H, t, J=12 Hz), 3.53 (1H, t, J=12 Hz), 4.01 (1H, q, J=7 Hz), 4.12-4.21 (2H, m), 4 99 (1H, d, J=4 Hz), 5.45-5.55 (4H, m), 5.84 (1H, dd, J=15, 4 Hz), 6.57 (1H, dd, J=15, 10 Hz), 6.73 (1H, d, J=16 Hz), 6.93 (1H, dd, J=16, 10 Hz), 6.88-7.00 (2H, m), 7.34 (1H, dd, J=11, 1 Hz), 7.27-7.46 (3H, m), 7.53-7.60 (3H, m), 7.79 (1H, dd, J=8, 1 Hz), 7.90 (1H, s), 7.95 (1H, s) IR spectrum nu max KBr cm-1: 2230, 1726, 1503, 1275, 1257, 1051, 1140, 973 Mass spectrum m/z (FAB): 817 (M++1) Specific rotation [alpha]D25 +0.4 (c=0.99, CHCl3). A solution of (1R,2R)-2-[[trans-2-[(1E,3E)-4-(4-cyano-2-fluorophenyl)-1,3-butadienyl]-1,3-dioxan-5-yl]thio]-1-(2,4-difluorophenyl)-1-[(1H-1,2,4-triazol-1-yl)methyl]propyl 2-[[2-(4-methylpiperazin-1-yl)acetoxy]methyl]benzoate (280 mg, 0.343 mmol) obtained above in ethyl acetate (5 ml) was cooled to 0C, and hydrogen chloride (4N ethyl acetate solution; 95 mul, 0.38 mmol) was added thereto, and the mixture was stirred at 0C for 5 minutes. The solvent was evaporated under reduced pressure, and the residue was dried in vacuo to afford the mono hydrochloric acid salt of the title compound (298 mg, quantitative yield) as a pale yellow amorphous solid. NMR spectrum (400 MHz, CD3OD) delta ppm: 1.43 (3H, dd, J=7, 1 Hz), 2.87 (3H, s), 2.8-3.4 (8H, br), 3.04 (1H, tt, J=11, 5 Hz), 3.48 (1H, t, J=11 Hz), 3.53 (2H, s), 3.54 (1H, t, J=11 Hz), 4.06 (1H, q, J=7 Hz), 4.04-4.08 (2H, m), 4.17 (1H, ddd, J=11, 5, 2 Hz), 5.20 (1H, d, J=4 Hz), 5.46 (1H, d, J=14 Hz), 5.53 (1H, d, J=14 Hz), 5.58 (2H, s), 5.85 (1H, dd, J=15, 4 Hz), 6.57 (1H, dd, J=15, 10 Hz), 6.79 (1H, d, J=16 Hz), 7.01-7.11 (2H, m), 7.09 (1H, dd, J=16, 10 Hz), 7.46 (1H, td, J=8, 1 Hz), 7.50-7.61 (3H, m), 7.63 (1H, qd, J=7, 1 Hz), 7.78 (1H, t, J=8 Hz), 7.86 (1H, dd, J=7, 1 Hz), 7.95 (1H, s), 8.34 (1H, s) IR spectrum nu max KBr cm-1: 2230, 1726, 1503, 1274, 1257, 1140, 1050, 973 Mass spectrum m/z (FAB): 817 [M+(free base)+1] Specific rotation [alpha]D25 -1.9 (c=0.97, CHCl3). A solution of (1R,2R)-2-[[trans-2-[(1E,3E)-4-(4-cyano-2-fluorophenyl)-1,3-butadienyl]-1,3-dioxan-5-yl]thio]-1-(2,4-difluorophenyl)-1-[(1H-1,2,4-triazol-1-yl)methyl]propyl 2-[[2-(4-methylpiperazin-1-yl)acetoxy]methyl]benzoate (338.5 mg, 0.41 mmol) obtained above in ethyl acetate (5 ml) was cooled to 0C, and hydrogen chloride (4N ethyl acetate solution; 207 mul, 0.83 mmol) was added thereto, and the mixture was stirred at 0C for 5 minutes. The solvent was evaporated under reduced pressure, and the residue was dried in vacuo to afford the bis hydrochloric acid salt of the title compound (354 mg, quantitative yield) as a pale yellow amorphous solid. NMR spectrum (400 MHz, DMSO-d6) delta ppm: 1.35 (3H, dd, J=7, 2 Hz), 2.76 (3H, s), 2.82-2.92 (2H, br), 2.99 (1H, tt, J=11, 5 Hz), 3.06-3.16 (4H, br), 3.41 (2H, br d, J=15 Hz), 3.46 (1H, t, J=11 Hz), 3.47 (1H, t, J=11 Hz), 3.65 -3.75 (2H, br), 3.79 (1H, q, J=7 Hz), 3.96 (1H, ddd, J=11, 5, 2 Hz), 4.07 (1H, ddd, J=11, 5, 2 Hz), 5.05 (1H, d, J=5 Hz), 5.39 (1H, d, J=13 Hz), 5.40 (1H, d, J=14 Hz), 5.49 (1H, d, J=13 Hz), 5.56 (1H, d, J=14 Hz), 5.88 (1H, dd, J=15, 5 Hz), 6.56 (1H, dd, J=15, 11 Hz), 6.82 (1H, d, J=16 Hz), 7.16-7.20 (1H, m), 7.19 (1H, dd, J=16, 11 Hz), 7.31-7.37 (1H, m), 7.49-7.55 (1H, m), 7.55 (1H, td, J=9, 6 Hz), 7.60 (1H, d, J=7 Hz), 7.67-7.71 (2H, m), 7.84-7.89 (3H, m), 7.96 (1H, s), 8.44 (1H, s) Mass spectrum m/z (FAB): 817 [M+(free base)+1] Specific rotation [alpha]D25 -3.1 (c=1.87, CHCl3), 54699-92-2

The synthetic route of 54699-92-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Sankyo Company, Limited; EP1362856; (2003); 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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Step 1: 3,5-Dimethyl-l-(4-trifluoromethoxy-bepizyl)-piperazine: To a solution of 4-(trifluoromethoxy)- benzaldehyde (776 muL, 4.38 mmol) in dichloromethane (30 mL) was added 2,6-dimethy. piperazine (1.0 g, 8.77mmol). The reaction mixture was stirred for Ih. Sodium triacetoxy borohydride (2.45 g, 8.77 mmol) was added and the reaction mixture was stirred for 4h. The reaction mixture was concentrated in vacuo, diluted with ethyl acetate and extracted with IN HCl (2 x 50 mL). The combined aqueous solution was neutralized with NaOH and extracted with ethyl acetate (3 x 50 mL). The combined organic solution was dried (Ts^SO,)) and concentrated in vacuo to provide 3,5-dimethyl-l-(4- trifluoromethoxy-benzyl)-piperazine (1.01 g, 80percent) as a clear oil. 1H NMR (400 MHz, CD3OD) delta 7.42 (d, 2H), 7.23 (d, 2H), 3.54 (s, 2H), 2.98-2.88 (m, 2H), 2.82-2.74,(m, 2H), 1.69 (t, 2H), 1.05 (d,6H); LCMS 289.5 (M+l)+.

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; KALYPSYS, INC.; WO2007/47431; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13754-38-6, 1-Benzoylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Manufacturing example 9: (4-(2-hydroxy-2-methylpropyl)piperazine-1-yl)phenylmethanon e [Show Image] 500 mg (2.63 mmol) 1-benzoylpiperazine and 1.10 g (7.96 mmol, 3.0 eq.) potassium carbonate were suspended to 20 ml acetonitrile at room temperature. After adding 570 mg (7.90 mmol, 3.0 eq.) isobutylene oxide, it was heated at reflux and stirred overnight. After cooling to room temperature and adding 30 ml purified water, it was extracted twice with 30 ml ethylacetate. After collecting the organic layer and drying with anhydrous magnesium sulfate, it was concentrated with decompression. The obtained residue was purified by chromatography using silicagel (mobile phase: dichloromethane/methanol= 20:1) and 276 mg (40%) target compound as light-yellow solid were yielded. 1HNMR(400MHz,DMSO-d6) 1.10(6H,s), 2.23(2H,s), 2.43-2.52(2H,m), 2.53-2.62(2H,m), 3.35-3.45(2H,m), 3.55-3.65(2H,m), 4.13(1H,s), 7.35-7.38(2H,m), 7.43-7.46(3H,m), 13754-38-6

The synthetic route of 13754-38-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Yang Ji Chemical Co., Ltd.; EP2452939; (2012); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

EXAMPLES; Intermediate 1; (1H-Indol-5-yl)-(4-isopropyl-piperazin-1-yl)-methanone; A mixture of 3.23 g (20 mmol) indole-5-caboxylic acid (commercially available), 3.07 g (24 mmol) 1-(2-propyl)-piperazine (commercially available), 8.03 g (25 mmol) TBTU and 10.3 mL (60 mmol) DIPEA in 50 mL DMF was stirred for 2 h at room temperature. After evaporation of all volatiles the residue was extracted with ethyl acetate, the combined organic layers dried with MgSO4 and evaporated to dryness. The residue was subsequently purified by flash column chromatography eluting with a mixture formed from DCM, MeOH and NH3 aq. to yield after evaporation of the combined product fractions 5.1 g (94percent) of the title compound as light brown foam. MS (m/e): 272.3 (MH+).

4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Nettekoven, Matthias; Roche, Olivier; US2008/188486; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics