Sep 2021 News Brief introduction of Butyl piperazine-1-carboxylate

The synthetic route of 50606-32-1 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.50606-32-1,Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

50606-32-1, 2-{[Methyl(5,6,7,8-tetrahydro-8-quinolinyl)amino]methyl}-1H-benzimidazole-4-carboxylic acid (190 mg, 0.56 mmol), bis(2-oxo-3-oxazolidinyl)phosphinic chloride(220 mg, 0.85 mmol), /V-butoxycarbonylpiperizine (104 mg, 0.56 mmol), and N,N-diisopropylethylamine (110 mg, 0.85 mmol) were dissolved in acetonitrile (5mL) andA/,/V-dimethylformamide (2ml_) and the reaction was stirred for 16 h at 35 C. Thereaction mixture was concentrated and purified using reverse phase HPLC (0% to70% acetonitrile/water/0.1% trifluoroacetic acid gradient) to provide the protectedamine (56 mg). The amine was dissolved in dichloromethane (3mL) andtrifluoroacetic acid (2mL) and stirred for 3 h. The reaction was concentrated,dissolved in water and lyophilized to provide the product (68 mg, 30%) as an off-white trifluoroacetate salt: 1H-NMR (DMSO-cf6) 8 8.62 (d, 1H), 7.94 (d, 1H), 7.72 (d,1H), 7.58-7.54 (m, 1H), 7.41-7.35 (m, 2H), 4.74-4.70 (m, 1H), 4.60 (d, 1H), 4.48 (d,1H), 4.38 (s, 2H), 3.25 (br s, 4H), 3.13 (br s, 4H), 2.88-2.80 (m, 2H), 2.65 (s, 3H),2.36-2.30 (m, 1H), 2.08-1.96 (m, 2H), 1.82-1.72 (m, 1H). MS m/z405 (M+1).

The synthetic route of 50606-32-1 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; SMITHKLINE BEECHAM CORPORATION; WO2006/23400; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Brief introduction of 1-Methylpiperazin-2-one

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

59702-07-7, A mixture N [5-chloro-7- (3-methoxyprop-1-yn-1-yl)-1, 3-benzodioxol-4-yl]-7- (3- chloropropoxy) -5-isopropoxyquinazolin-4-amine (0.320 g, as a 1: 1.3 wt.: wt. mixture with triphenylphosphine) and 1-methylpiperazin-2-one (0.280 g) was dissolved in 2- methoxyethanol (7 ml), then sodium iodide (0.040 g) was added and the reaction mixture was then heated at 110°C with stirring for 24 hours. The reaction mixture was then cooled to room temperature, diluted with dichloromethane (70 ml) and washed with water: brine (1: 1) then water then brine and dried over magnesium sulfate before filtration and evaporation of solvents under reduced pressure. The residues so resulting were then purified by column chromatography on silica using increasingly polar mixtures of methanol in dichloromethane as eluent. There was thus obtained 4- (3- {4- [5-chloro-7- (3-methoxy-prop-1-ynyl)- benzo [1, 3] dioxol-4-ylamino]-5-isopropoxy-quinazolin-7-yloxy}-propoxy)-1-methyl- piperazin-2-one (0.086 g) as a white foam; NMR Spectrum: (CDC13) 1.53 (d, 6H), 2.02 (quin, 2H), 2.61 (t, 2H), 2.72 (t, 2H), 2.96 (s, 3H), 3.18 (s, 2H), 3.33 (t, 2H), 3.45 (s, 3H), 4.15 (t, 2H), 4.35 (s, 2H), 4.83 (sept, 1H), 6.10 (s, 2H), 6.49 (d, 1H), 6.82 (d, 1H), 7.05 (s, 1H), 8.51 (s, 1H), 9.41 (s, 1H); Mass Spectrum: M+H+ 596/598.

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

Reference:
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2004/4732; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News New learning discoveries about 1-(2-Methoxyethyl)piperazine

As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution containing 2.7 g (18.9 mmol) of 1-[2-(methyloxy)ethyl]piperazine and 20 ml. of THF at O0C was added 0.9 g (23 mmol) of a 60% suspension of NaH in mineral oil. The reaction mixture was allowed to stir for 15 min and 3.0 g (18.9 mmol) of 2- chloro-5-nitropyridine was added. The reaction mixture was heated at 6O0C overnight and then quenched by the addition of water and extracted with EtOAc. The combined organic layers were dried over MgSO4 and the solvents were removed under reduced pressure. The residue was subjected to silica gel chromatography to give 2.7 g (54%) of 1-[2-(methyloxy)ethyl]-4-(5-nitro-2-pyridinyl)piperazine as a yellow solid: 1H NMR (400 MHz, DMSO-d6) delta 2.50-2.53 (m, 6H), 3.24 (s, 3 H), 3.46 (t, J = 5.7 Hz, 2 H), 3.71 – 3.78 (m, 4 H), 6.94 (d, J = 9.7 Hz, 2 H), 8.21 (dd, J = 9.6 and 2.8 Hz, 1 H), and 8.95 (d, J = 2.75 Hz, 1 H)., 13484-40-7

As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

Reference:
Patent; SMITHKLINE BEECHAM CORPORATION; WO2009/32667; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Downstream synthetic route of 1-Acetylpiperazine

As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Method 25 1-Acetyl-4- piperazine; 1-Butyl-3-methylimidazolium tetrafluoroborate (1.75g, 7. 74mmol) was added to a stirred solution of l-fluoro-2-methyl-4-nitrobenzene (12g, 77. 35mmol) and 1-acetylpiperazine (39.7g, 309. 4mmol) in acetonitrile (3ml). The reaction mixture was then heating at 95C overnight. The reaction mixture was allowed to cool down to room temperature. The solution was diluted with EtOAc and water. The precipitate formed was filtered off to give a solid corresponding to the required product. The organics were washed with water (4 times), brine, dried and evaporation of solvent to give a solid. Both solids were combined and after trituration with isohexane/ether and filtration, the title compound was obtained as a yellow solid which was dried in vac oven overnight at 50C. (19. 61g, 96%). NMR (400MHz) 2.06 (s, 3H), 2.38 (s, 3H), 2.99 (dt, 4H), 3.61 (m, 4H), 7.14 (d, 1H), 8.04 (dd, 1H), 8.07 (d, 1H); m/z 264., 13889-98-0

As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference:
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/75461; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Brief introduction of 3-(4-Methylpiperazin-1-yl)propan-1-ol

The synthetic route of 5317-33-9 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.5317-33-9,3-(4-Methylpiperazin-1-yl)propan-1-ol,as a common compound, the synthetic route is as follows.,5317-33-9

4-Toluenesulphonyl chloride (3.2 g) was added to a stirred mixture of 1-(3-hydroxypropyl)4-methylpiperazine (2.4 g), triethylamine (4.6 ml) and methylene chloride (60 ml) and the resultant mixture was stirred at ambient temperature for 2 hours. The solution was washed in turn with a saturated aqueous sodium bicarbonate solution and with water and filtered through phase separating paper. The organic filtrate was evaporated to give 3-(4-methylpiperazin-1-yl)propyl 4-toluenesulphonate as an oil which crystallized on standing (3.7 g); Mass Spectrum: M+H+ 313.

The synthetic route of 5317-33-9 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Lambert, Christine Marie Paul; Ple, Patrick; US2004/44015; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Brief introduction of 1-Ethylpiperazine

The synthetic route of 5308-25-8 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.5308-25-8,1-Ethylpiperazine,as a common compound, the synthetic route is as follows.,5308-25-8

General procedure: A solution of compound 2 (0.55 mmol), 1-substituted piperazine (0.83 mmol) and pyridine (0.8 mmol) in 10 mL THF (tetrahydrofuran) was stirred at room temperature overnight. When the reaction was completed, the solvent was evaporated under reduced pressure. The residues were dissolved in ethyl acetate and washed with water and saturated sodium chloride solution. After drying over anhydrous Na2SO4, the solvent was removed under reduced pressure to get crude product. The pure products were obtained by recrystallizing from ethanol.

The synthetic route of 5308-25-8 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Wu, Zhilin; Ding, Na; Tang, Yuting; Ye, Jiao; Peng, Junmei; Hu, Aixi; Research on Chemical Intermediates; vol. 43; 8; (2017); p. 4833 – 4850;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Downstream synthetic route of 1-Acetylpiperazine

13889-98-0, As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2-[(4-Bromo-2-fluoro-phenyl)methyl]-6-phenyl-thiazinane 1,1-dioxide (208 mg, 0.52 mmol), Pd(OAc)2 (5.8 mg, 0.026 mmol), 2-dicyclohexylphosphine-2′,6′-di-iso-propoxy-1,1′-biphenyl (24.8 mg, 0.052 mmol) and cesium carbonate (254 mg, 0.78 mmol) were weighed out in a vial and the vial was purged with nitrogen. 1,4-Dioxane (2.5 mL) and 1-piperazin-1-ylethanone (100 mg, 0.78 mmol) were then added and the reaction was stirred at 80 C. for 2 hours. The reaction was then filtered through diatomaceous earth, concentrated and purified by reverse-phase HPLC to give 1-(4-(4-((1,1-dioxido-6-phenyl-1,2-thiazinan-2-yl)methyl)-3-fluorophenyl)piperazin-1-yl)ethanone (210 mg, 89% yield).

13889-98-0, As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference:
Patent; Genentech, Inc.; Fauber, Benjamin; Gobbi, Alberto; Rene, Olivier; Bodil van Niel, Monique; Gancia, Emanuela; Gaines, Simon; Laddywahetty, Tammy; Vesey, David; Ward, Stuart; Winship, Paul; US2015/197529; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Brief introduction of Piperazine-1-carboxamide hydrochloride

The synthetic route of 474711-89-2 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.474711-89-2,Piperazine-1-carboxamide hydrochloride,as a common compound, the synthetic route is as follows.,474711-89-2

A mixture of (S) -2- (3- (benzyloxy) -4- (difluoromethoxy) phenyl) -5- (1- ( (tert-butoxy carbonyl) amino) ethyl) oxazole-4-carboxylic acid (300 mg, 0.595 mmol) , EDCI (171 mg, 0.892 mmol) and HOAT (121 mg, 0.892 mmol) in DCM (20 mL) was stirred at rt for 30 min, and piperazine-1-carboxamide hydrochloride (200 mg, 0.892 mmol) was added, and then DIPEA (1.5 mL, 9.52 mmol) was added dropwise at 0 . After the addition, the mixture was stirred at rt for 10 h and washed with water (25 mL × 3) . The organic layer was dried over anhydrous Na2SO4 and concentrated. The residue was purified by silica gel chromatography eluted with Petroleum ether/EtOAc (v/v) 1/1 to give the title compound as a white solid (176 mg, 48) .1H NMR (400 MHz, CDCl3) : delta ppm 7.66 (d, J 2.0 Hz, 1H) , 7.61 (d, J1 8.4 Hz, J2 2.0 Hz, 1H) , 7.36-7.50 (m, 5H) , 7.29 (d, J 8.4 Hz, 1H) , 6.66 (t, JF-H 74.4 Hz, 1H) , 5.25-5.28 (m, 1H) , 5.25 (s, 2H) , 4.56 (s, 2H) , 3.83-4.00 (m, 4H) , 3.53-3.55 (m, 4H) , 1.57 (d, J 6.8 Hz, 3H) , 1.44 (s, 9H) and MS-ESI: m/z 616.30 [M+H] +.

The synthetic route of 474711-89-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

17 Sep 2021 News Analyzing the synthesis route of 1-(2-Hydroxyethyl)-4-methylpiperazine

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5464-12-0, Compound 132 was synthesized according to the following production scheme.

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; SBI BIOTECH CO., LTD.; CRYSTALGENOMICS, INC.; US2011/190299; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

17 Sep 2021 News Simple exploration of 1-tert-Butylpiperazine

38216-72-7, 38216-72-7 1-tert-Butylpiperazine 3530572, apiperazines 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.38216-72-7,1-tert-Butylpiperazine,as a common compound, the synthetic route is as follows.

A. Synthesis of l-(4-(4-fert-butylpiperazin-l-yl)(phenyl)methyl)piperidin-l-yl)ethanone; [0092] 1-tert-butylpiperazine (4.48 g, 20.8 mmol), l-(4-(chloro(phenyl)methyl)piperidin-l-yl)ethanone (5.77 g, 22.9 mmol), K2CO3 (7.2 g, 52.1 mmol), and KI (22.9 mmol) were combined in dry DMF (150 mL). The reaction was refluxed overnight. Upon completion of the reaction, the DMF was removed under reduced pressure. The resulting crude was taken up in water (75 mL) and washed with EtOAc (3 x 100 mL). The organic portions were combined, dried (Na2SO4) and concentrated. The product was purified by silica gel chromatography (2.5:2.5:95 Et3N/MeOH/EtOAc, Rf 0.4) and isolated as a red oil (2.66 g, 36%).

38216-72-7, 38216-72-7 1-tert-Butylpiperazine 3530572, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; NEUROMED PHARMACEUTICALS LTD.; WO2008/31227; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics