Month: September 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.930782-89-1,(R)-4-Benzyl 1-tert-butyl 2-(hydroxymethyl)piperazine-1,4-dicarboxylate,as a common compound, the synthetic route is as follows.

930782-89-1, Compound 28 (4.74 g, 13.53 mmol) was dissolved in anhydrous DCM (45 mL) and triethylamine (7.54 mL, 54.11 mmol) added and the mixture was cooled to 0 C. A solution of pyridine sulfur trioxide (6.46 g, 40.58 mmol) in DMSO (45 mL) was added at 0 C and stirred for 1 hour. The reaction was quenched with a saturated NaHCCb solution and diluted with ether. The aqueous phase was extracted with ether (3x). Combined organic layers were extracted with sodium phosphate dibasic (Na2HP04), 1M HC1 and brine; dried over anhydrous Na2S04, filtered and evaporated. The crude product was used for the next step without purification.

930782-89-1 (R)-4-Benzyl 1-tert-butyl 2-(hydroxymethyl)piperazine-1,4-dicarboxylate 16124590, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; EMORY UNIVERSITY; LIOTTA, Dennis C.; JECS, Edgars; ALTAS TAHIROVIC, Yesim; WILSON, Lawrence; PELLY, Stephen Christopher; (102 pag.)WO2019/183133; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

20327-23-5, 1-Cyclopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 6(4-Cvclopropyl-piperazin-1 -yl)-(4-morpholin-4-ylmethyl-phenyl)- methanone bis-hvdrochloride saltStep A: PreparationA 100-L glass-lined reactor was charged with toluene (45.00 kg) and stirred at ~20-25C. To the stirring toluene was added 4-(4- morpholinylmethyl)benzoic acid hydrochloride (6.50 kg, 93.5%, 24.04 mol), 1- hydroxybenzothazole monohydrate (2.32 kg, 15.13 mol), 1 – cyclopropylpiperazine (3.50 kg, 27.07 mol) and acetonitrile (9.00 kg). The resulting off-white slurry was stirred under N2 at ~20-25C for 40 minutes. N- (3-Dimethylaminopropyl)-N’-ethylcarbodiimide hydrochloride (3.50 kg, 27.07 mol) was added, followed by an acetonitrile (1 .20 kg) rinse. After the addition, the reaction mixture was stirred at ~20-25C overnight. Water (32.50 kg) and aqueous saturated sodium carbonate (19.50 L) were then added to the stirring suspension. The suspension was stirred for an additional 30 minutes. The resulting biphasic solution was allowed to settle. The aqueous phase was discarded and the organic phase was washed with a 50% brine solution [water (19.50 L) / brine (19.50 L)]. To the stirred organic phase was then added anhydrous sodium sulfate (2.86 kg) and the resulting mixture was stirred at ~20-25C for 1.5 hours. The solid sodium sulfate was filtered off and the filter cake was washed with acetonitrile (15.30 kg). The filtrate was transferred to a clean 100-L glass-lined reactor and stirred at ~20-25C. Water (0.47 kg) and 5/6N HCI in 2-propanol were added to precipitate the title compound as the corresponding bis-hydrochloride salt as a solid. The solid was filtered, washed with acetonitrile (10.2 kg) and dried (60 Torr, ~40-45C) to a constant weight to yield the title compound as a white solid.Step B: PurificationIn a 50-L glass reactor, the white solid prepared as in Step A above (15.0 kg, 37.28 mol) was dissolved in 1 :1 (v/v) mixture of ethanol :water (15.0 L: 15.0 L) at ~20-25C. The resulting mixture was stirred for 45 minutes and polish filtered (to remove any foreign particles) into a clean 100-L glass-lined reactor. The filtrate was transferred to a clean reaction vessel. Upon stirring, (polish filtered) ethanol (75.0 L) was added and the title compound precipitated as a bis-HCLmono-hydrate salt. The resultant white slurry was stirred at -20- 25C overnight. The solid was filtered, washed with ethanol (7.5 L) and dried at ~20-25C under vacuum to yield the title compound as a monohydrate bis- hydrochloride salt as a white solid.Karl Fisher analysis showed 3.4-3.6% water present. Chromatographic Purity (%w/w) showed 96.6%, 20327-23-5

As the paragraph descriping shows that 20327-23-5 is playing an increasingly important role.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2008/76685; (2008); 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.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

8-tert-butyl-6-(4-fluorophenyl)imidazo[l,2-b]pyridazine-2-carboxylic acid (5g, 16 mmol), DMF (l20mL), HATU (7.3g, 19.2 mmol), tert-butyl 3, 3 -dimethylpiperazine-l -carboxylate (4.lg, 1.92 mmol) and DIPEA (lOmL, 57.4 mmol) afforded tert-butyl 4-(8-(tert-butyl)-6- (4-fluorophenyl)imidazo [l,2-b]pyridazine-2-carbonyl)-3 ,3 -dimethylpiperazine- 1 – carboxylate that was dissolved in 4N HC1 solution in l,4-dioxane (60 mL) affording 4-(8- (tert-butyl)-6-(4-fluorophenyl)imidazo[l,2-b]pyridazine-2-carbonyl)-3,3- dimethylpiperazine hydrochloride (6.5g, 97%) as a solid. 1H NMR (401 MHz, DMSO) d 9.71 (bs, 2H), 8.57 (s, 1H), 8.17 – 8.10 (m, 2H), 7.50 (s, 1H), 7.44 – 7.36 (m, 2H), 4.16 – 4.08 (m, 2H), 3.35 – 3.27 (m, 2H), 3.23 – 3.14 (m, 2H), 1.61 (s, 6H), 1.59 (s, 9H)., 259808-67-8

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

Reference£º
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; AURELIO, Luigi; BUNNETT, Nigel; FLYNN, Bernard Luke; GIANG, Le; (125 pag.)WO2019/124567; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1 : To a lOOmL three-necked flask was added 20mL toluene and compound 13a (3g, 0.014mol, l .Oeq), compound 13b (4.3g, 0.022mol, 1.5eq) and t-BuONa (2.064g, 0.022mol, 1.5eq). The reaction was heated to 80oC with nitrogen. Then BINAP (0.3g, 0.42mmol, 0.03eq) and Pd2(dba)3.CHCl3 (0.15g, 0.14mmol, O.OOleq) was added to the stirred mixture . The reaction was heated to reflux for 18h. The solution was cooled, concentrated and extracted with 30 EA from lOmL water. The organic layer was washed with brine , dried , concentrated in vacuum and purified by column chromatography on silica gel eluted with PE: EA= 10: 1 to afford the compound 13c (4g, HPLC: 98%) as a white solid. Yield: 86%.

120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; LIANG, Congxin; (62 pag.)WO2018/5713; (2018); 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.692058-21-2,1-Boc-4-(2,2,2-trifluoroethyl)piperazine,as a common compound, the synthetic route is as follows.

Hydrogen chloride gas was bubbled through a solution of tert-butyl 4- (2, 2, 2-TRIFLUOROETHYLPIPERAZINE-1-CARBOXYLATE (8 g) in ethyl acetate (50 ml) during 1.5 hours. A precipitate formed as carbon dioxide gas was evolved. The precipitate was collected by filtration, washed with ethyl acetate and dried under vacuum. There was thus obtained 1- (2, 2, 2-trifluoroethyl) piperazine hydrochloride (7 g); NMR Spectrum : (DMSOd6 and CF3CO2D) 2.85 (m, 4H), 3.1 (m, 4H), 3.35 (q, 2H), 692058-21-2

692058-21-2 1-Boc-4-(2,2,2-trifluoroethyl)piperazine 16748694, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2004/41829; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

118753-66-5, tert-Butyl 4-aminopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a well-stirred solution of intermediate 5a (2.0 g,5.29 mmol) in ethanol (10 mL) was added 1-amino-4-methylpiperazine 9a (0.61 g, 5.29 mmol) and a drop of acetic acid,and the mixturewas stirred at 78 C for 2 h. The mixturewas cooledto room temperature and the resulting solid was collected byfiltration and purified by column chromatography to give the targetcompounds 6a-1 as a yellow solid in 75% yield. M.p: 228-230 C;

118753-66-5, As the paragraph descriping shows that 118753-66-5 is playing an increasingly important role.

Reference£º
Article; Wu, Yachuang; Ding, Xiudong; Yang, Yifeng; Li, Yingxiu; Qi, Yinliang; Hu, Feng; Qin, Mingze; Liu, Yajing; Sun, Lu; Zhao, Yanfang; European Journal of Medicinal Chemistry; vol. 185; (2020);,
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

To a solution of Intermediate?B? (150 mg, 0.41 mmol) in CH2CI2 (5 mL) was added Et3N (126 mg, 1.25 mmol), in portions, followed by the addition of l-[4-(trifluoro- methyl)phenyl]piperazine (96 mg, 0.42 mmol), in portions. The resulting solution was stirred for 16 h at rt, then quenched by the addition of 20 mL H2O and extracted with 2×20 mL of EtOAc. The combined organic layers were concentrated under vacuum to afford 180 mg (90%) of the title compound as an off-white solid. LC-MS: (ES, m/z) 480, 30459-17-7

30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CENTAURUS THERAPEUTICS; ROMERO, Donna, L.; BLITZER, Jeremy; (242 pag.)WO2019/140188; (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.78818-15-2,Benzyl 3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

78818-15-2, EXAMPLE 89 1-(4-Chloroquinolin-7-ylmethyl)-piperazin-2-one. 4-(Benzyloxycarbonyl)-piperazin-2-one (1.1 g, 4.6 mmol) is dissolved in THF (50 ML), cooled in an ice bath and treated with tretrabutylammonium iodide (0.18 g, mmol) and 60% sodium hydride (0.24 g, 6.0 mmol).The reaction mixture is stirred at 0 C. for 30 minutes then treated dropwise with a solution of 7-bromomethyl-4-chloroquinoline (1.2 g, 4.6 mmol), Example 14, in THF (50 ML).The resulting solution is stirred at 0 C. for 2 h then quenched with ammonium chloride solution and concentrated.Dilution with ethyl acetate is followed by a water wash; the organic layer is dried (sodium sulfate) and concentrated.The residue is chromatographed (4% methanol/methylene chloride) to yield solid 4-(benzyloxycarbonyl)-1-(4-chloroquinolin-7-ylmethyl)-piperazin-2-one (1.2 g, 2.9 mmol).A portion of this material (0.75 g, 1.8 mmol) is dissolved in acetonitrile (20 ML) and treated with iodo trimethylsilane (0.78 ML, 5.4 mmol) at room temperature for 3 hours.The reaction is quenched with methanol and concentrated to dryness.methanol addition and concentration is repeated four times.The final residue is taken up is 2M aqueous HCl; the solution is washed with ether and concentrated.The residue is recrystallized from isopropanol and ether to yield the title compound (0.63 g, 2.3 mmol) MS m/z: M+=275; 1HNMR (CD3OD, 300 MHz) delta9.1 (d, 1H), 8.5 (d, 1H), 8.2-8.3 (m, 2H), 8.0 (d, 1H), 5.2 (s, 2H), 4.1 (s, 2H), 3.7-3.8 (m, 2H), 3.6-3.7 (m, 2H).

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

Reference£º
Patent; AVENTIS PHARMACEUTICALS INC.; US2004/102450; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 128 4-Amino-2-[4-(cyclopropylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline N-(Cyclopropylcarbonyl)piperazine (3.08 g., 0.02 mole) and 2-chloro-4-amino-6,7-dimethoxyquinazoline (4.74 g., 0.02 mole) are reacted according to the procedure of Example 127(a). The crude product crystallized from ethanol affords analytically pure 4-amino-2-[4-(cyclopropylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline, m.p. 283.5 C. (corr.). Analysis, Calcd. for C18H23N5O3 (percent): C, 60.49; H, 6.49; N, 19.59. Found (percent): C, 60.56; H, 6.46; N, 19.41., 59878-57-8

The synthetic route of 59878-57-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Cell Pathways, Inc.; US6262059; (2001); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

76003-29-7,76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1 4-Benzyl-3-oxo-piperazine-1-carboxylic acid tert-butyl ester Sodium hydride (60%, 18.11 g, 452 mmol) in mineral oil was triturated with 35 hexanes, dried under a stream of nitrogen and taken up in 1500 mL of THF. To the slurry at 0 C. was added 3-oxo-piperazine-1-carboxylic acid tert-butyl ester (75.057 g, 200.4 mmol) in portions over 15 min. After 90 minutes benzyl bromide (71.01 g, 415.1 mmol) was added and the mixture was warmed to room temperature for 18 hours. The solution was quenched with H2O and extracted with Et2O. The combined organic layers were washed with H2O, washed with brine, dried over MgSO4. Concentration in vacuo gave a crude solid which was recrystallized from hexane to afford 4-benzyl-3-oxo-piperazine-1-carboxylic acid tert-butyl ester (83.5 g, 76%) as a white crystalline solid.

76003-29-7 1-Boc-3-Oxopiperazine 3157178, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Roche Palo Alto LLC; US2009/209553; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics