Month: September 2021

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of /ert-butyl (2-oxoethyl)carbamate (4.89 g, 30.7 mmol) in 1,2- dichloroethane (50 mL) was added to a solution of l-(tert-butyl) 3-methyl piperazine- 1,3- dicarboxylate (5 g, 20.5 mmol) in l,2-dichloroethane (25 mL). The solution stirred at 25 C under nitrogen atmosphere for 30 min. Sodium triacetoxyborohydride (8.69 g, 41.0 mmol) was added, and the resulting mixture stirred at 25 C for 15 h. The reaction was quenched by the addition of water (50 mL) at 25 C. The resulting mixture was extracted with dichloromethane (3 x 50 mL). The combined organic layers were washed with brine (50 mL), dried over anhydrous sodium sulfate, and the solids were filtered out. The filtrate was concentrated under vacuum. The residue was purified by silica gel chromatography (eluting with 1 : 1 ethyl acetate/petroleum ether) to afford l-ter/-butyl 3- methyl 4-(2-(/er/-butoxycarbonylamino)ethyl)piperazine-l,3-dicarboxylate as yellow oil (5.1 g, 64%). LCMS (ES, m/z): 388 [M+H]+.

129799-08-2, The synthetic route of 129799-08-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; FORMA THERAPEUTICS, INC.; MARTIN, Matthew W.; BUCKMELTER, Alexandre Joseph; (158 pag.)WO2019/222468; (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.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

4-[(4-methyl-1-piperidinyl) methyl] -3- (trifluoromethyl) -benzeneamine (360 mg, 1.33 mmol),N, N-Diisopropylethylamine (273 muL, 1.60 mmol),Dissolve DMAP (1.2 mg, 0.01 mmol) in THF (5.0 mL),3,5-Dibromo-4-methyl- benzoyl chloride (500 mg, 1.6 mmol) was added and stirred at room temperature for 2 hours.Add water and extract with ethyl acetate,It concentrated under reduced pressure with an evaporator.Silica gel column chromatography of the obtained residueThe compound 3 was purified by (chloroform: methanol = 10: 1).(540.0 mg, 0.98 mmol, 73.8%, pale yellow solid) were obtained., 694499-26-8

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Kyoto University; Arkray Corporation; Saji, Hideo; Kimura, Hiroyuki; Matsuda, Hirokazu; Nakanishi, Shuichi; (27 pag.)JP2019/64986; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

78818-15-2, Benzyl 3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

78818-15-2, Sodium hydride (60% dispersion in mineral oil, 281 mg, 7.0 mmol) was added to a solution of phenylmethyl 3-oxo-1-piperazinecarboxylate (1.5 g, 6.4 mmol) in dry dimethyl formamide (5 mL) and the mixture was stirred at room temperature for 30 minutes. 5-(Chloromethyl)-1-methyl-1H-1,2,4-triazole (WO0023449, 920 mg, 7.0 mmol) was added and the mixture was stirred at room temperature for 16 hours. The mixture was poured into water (150 mL) and extracted with diethyl ether (2×100 mL). The combined organic fractions were dried (MgSO4) and the solvent was evaporated under reduced pressure to give the title compound as a pale oil (2 g, 94%). m/z (ES+) 330 (M+1).

78818-15-2 Benzyl 3-oxopiperazine-1-carboxylate 736777, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Castro Pineiro, Jose Luis; Dinnell, Kevin; Elliott, Jason Matthew; Hollingworth, Gregory John; Shaw, Duncan Edward; Swain, Christopher John; US2003/236250; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

509073-62-5, tert-Butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of compound 8 (6.0 g, 20 mmol) in H2O (8 mL) andEtOH (24 mL) was added Fe (4.5 g, 80 mmol) and NH4Cl (1.5 g,28 mmol). The mixture was heated under reflux for 2 h. The solidwas filtered off and the liquid was concentrated under vacuum toafford the crude product. The crude product was purified by columnchromatography to provide compound 9 as yellow solid (5.7 g,yield: 93%). Mp: 155-156 C. 1H NMR (400 MHz, CDCl3) delta 7.25 (d,J = 8.4 Hz, 2H), 6.65 (d, J = 8.4 Hz, 2H), 3.94 (s, 2H), 3.59 (s, 4H), 3.44(s, 4H), 1.47 (s, 9H). 13C NMR (100 MHz, CDCl3) delta171.02, 154.54,148.36, 129.26, 124.44, 114.10, 80.15, 44.01, 43.30, 28.29.

509073-62-5, 509073-62-5 tert-Butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate 2764459, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Su, Yue; Li, Ridong; Ning, Xianling; Lin, Zhiqiang; Zhao, Xuyang; Zhou, Juntuo; Liu, Jia; Jin, Yan; Yin, Yuxin; European Journal of Medicinal Chemistry; vol. 177; (2019); p. 32 – 46;,
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.115619-01-7,4-(4-Ethylpiperazin-1-yl)phenylamine,as a common compound, the synthetic route is as follows.,115619-01-7

EXAMPLE IB5-bromo-N2-[4-(4-ethylpiperazin-l-yl)phenyl]-N4-[2-(trifluoromethyl)-lH-benzimidazol-5-yl]pyrimidine-2,4-diamineA scintillation vial was charged with EXAMPLE IA (98 mg, 0.25 mmol), 4- (4- ethylpiperazin-l-yl)aniline (66.7 mg, 0.325 mmol), n-butanol (4 ml) and 4 N hydrogen chloride in dioxane (62.5 muL, 0.250 mmol). The mixture was stirred at 80 0C overnight. The reaction mixture was cooled and quenched with water (10 mL), adjusted to pH -135089667 1 with slow addition of cone. aq. NaOH. The mixture was extracted with ethyl acetate and the extract was concentrated. The crude product was purified with HPLC on a Cl 8 reverse-phase column using a gradient of water and acetonitrile with 0.1% TFA as a buffer. The title compound was obtained as the TFA salt as an off-white solid (100 mg, 51%). MS: (ESI(+)) m/e 561.2, 563.2 (M+H)+; 1H NMR (500 MHz, DMSO-d6) delta ppm 9.53 (bs, IH), 9.39 (s, 1 H), 8.99 (s, IH), 8.22 (s, IH), 7.94 (s, IH), 7.73 (d, IH), 7.57 (d, IH), 7.43 (d, 2H), 6.76 (d, 2H), 6.51 (s, IH), 3.66-3.53 (m, 4H), 3.21-3.09 (m, 4H), 2.87 (U H), 1.26 (q, 3H).

115619-01-7 4-(4-Ethylpiperazin-1-yl)phenylamine 936738, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ABBOTT LABORATORIES; WANG, Gary, T.; MANTEI, Robert, A.; ERICKSON, Scott, A.; FIDANZE, Steve, D.; SHEPPARD, George, S.; WANG, Jieyi; BELL, Randy, L.; WO2010/138578; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1235865-77-6, 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In 25 ml water compound is added in the bottle (J) 100 mg, EDCI67mg, dichloromethane 10 ml, reaction solution stirring 30 minutes, the compound is added (K) (in accordance with WO2012058392 method preparation) 55 mg, finally adding catalytic DMAP, reaction solution adding stirring reaction sleepovers, to splines end of the detection reaction TLC solvent, ABT-199 HPLC purified to get the pure product 98 mg, yield 65%., 1235865-77-6

As the paragraph descriping shows that 1235865-77-6 is playing an increasingly important role.

Reference：
Patent; Nanjing Acesys Pharmatech Co., Ltd; GE, MIN; XU, YUNLEI; (8 pag.)CN104370905; (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.78818-15-2,Benzyl 3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

78818-15-2, [0713] To the solution of XXIV-1 (20 g, 85.5 mmol) in DMF (100 mL) was added NaH (60%, 4.1 g, 103 mmol) in portions. The mixture was stirred at rt for 30 mm. Then XXIV-2 (14.3 g, 85.5 mmol) was added. The reaction was stuffed at rt overnight. The reaction was quenched with ice- water carefully, and then extracted with EtOAc (100 mLx2). The combined organic layer was washed with brine, dried over anhydrous Na2SO4 and concentrated. The residue was used for next step directly (40 g, 140% crude yield).

The synthetic route of 78818-15-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; INTERMUNE, INC.; RAMPHAL, Johnnie, Y.; BUCKMAN, Brad, Owen; EMAYAN, Kumaraswamy; NICHOLAS, John, Beamond; SEIWERT, Scott, D.; WO2015/153683; (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.4318-42-7,1-Isopropylpiperazine,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°C 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 P58: 2-Nitro-3-[4-(propan-2-yl)piperazin-1 -yl]aniline; The compound was obtained by the method analogous to that described for Compound P42. Starting from 3-chloro-2-nitroaniline (0.459 g, 2.61 mmol), potassium carbonate (0.368 g, 2.66 mmol) and 1 -isopropylpiperazine (1.00 g, 0.741 mmol), 0.602 g of the title product in the form of a red solid were obtained (yield 91.9percent). MS-ESI: (m/z) calculated for Ci3H2iN402 [M + H]+: 265.16, found 265.1 1H NMR (500 MHz, DMSO-d6) delta 7.10 (dd, J = 8.1 Hz, 1 H), 6.52 (dd, J = 8.3, 1.0 Hz, 1 H), 6.35 (dd, J = 8.0, 1.0 Hz, 1 H), 5.83 (s, 2H), 2.85 (dd, J = 17.4, 12.8 Hz, 4H), 2.68 – 2.60 (m, 1 H), 2.47 (dd, 4H), 0.97 (d, J = 6.5 Hz, 6H).

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

Reference：
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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55121-99-8,(4-Aminophenyl)(4-methylpiperazin-1-yl)methanone,as a common compound, the synthetic route is as follows.

55121-99-8, Example No. 134Preparation of (4-methylpiperazin-l-yl) (4- ( (5- (thiophen-2-yl) – IH-pyrazolo [4 , 3 -d] pyrimidin-7-yl) amino) phenyl) methanone7-chloro-2- (4-methoxybenzyl) -5- (thiophen-2-yl) -2H- pyrazolo [4 , 3 -d] yrimidine (0.16 mmol) and (4 -aminophenyl) (4- methylpiperazin-l-yl) methanone (0.3 mmol 2 eq. , ) were suspended in MeOH (dry, 3mL) in a microwave vial (2-5mL) , HCl in dioxane (4M, 3 drops) was added. The reaction mixture was irradiated in a microwave reactor for 5 min at 140C. The reaction mixture was evaporated and used without further purification. The residue was dissolved in TFA (3mL) . The reaction mixture was irradiated in a microwave reactor for 5 min at 140C. The reaction mixture was concentrated and purified by semi -preparative HPLC-MS and freeze dried from water/t-BuOH 4/1. exact mass: 419.1830 g/molHPLC-MS: analytical method Crt: 1.97 min – found mass: 420 (m/z+H)

55121-99-8 (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone 231408, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ORIGENIS GMBH; ALMSTETTER, Michael; THORMANN, Michael; TREML, Andreas; TRAUBE, Nadine; WO2012/143144; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5521-39-1, 2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5521-39-1

EXAMPLE 39 6-Methoxy-8-(4-methyl-piperazin-1-yl)-4-oxo-4H-chromene-2-carboxylic acid {4-[4-(2hydroxy-ethyl)-piperazin-1-yl]-phenyl}-amide. This compound was prepared from 6-methoxy-8-(4-Methyl-piperazin-1-yl)-4-oxo-4H-chromene-2-carboxylic acid hydrochloride (Reference Example 2) and 2-[4-(4-amino-phenyl)-piperazin-1-yl]-ethanol (Reference Example 19) as prepared in Example 12, yielding a yellow solid. (80mg=60%). mp=211.5-212.2 (dec.), MS-base peak at m/z=492 by positive ion and m/z=490 by negative ion CI

5521-39-1 2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol 767100, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Pierson, Edward; Sohn, Daniel; Haeberlein, Markus; Davenport, Timothy; Chapdelaine, Marc; Horchler, Carey; McCauley, John P.; US2003/13708; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics