Heterocyclic Building Blocks-piperazine

169448-87-7, (R)-tert-Butyl 2-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of the product of Example 75 step i) (300mg), (f?>2-(hydroxymethyl)piperazine- 1-carboxylic acid, terf-butyl ester (465mg) and sodium triacetoxyborohydride (608mg) in dichloromethane (2OmL) was stirred under nitrogen for 16 hours. The reaction was partitioned between dichloromethane and water, the organics were then collected and concentrated to dryness. The residue was purified by HPLC to give the title compound (230mg) as a solid. MS: APCI(+ve) 519 (M+H)+1H NMR DMSO-Cl6 8.54 (d, J = 4.2 Hz, 1 H), 8.35 (d, J = 8.3 Hz, 1 H), 7.97 (d, J = 1.5 Hz, 1 H), 7.69 – 7.64 (m, 2H), 7.54 (dd, J = 8.2, 1.4 Hz, 1 H), 7.49 (s, 1 H), 4.46 (t, J = 5.4 Hz, 1 H), 3.93 – 3.79 (m, 2H), 3.55 – 3.44 (m, 2H), 3.28 – 3.20 (m, 2H), 2.89 – 2.77 (m, 3H), 2.75 – 2.67 (m, 1H), 2.63 – 2.52 (m, 2H), 2.25 (d, J = 2.3 Hz, 3H), 2.07 – 1.87 (m, 2H), 1.67 – 1.58 (m, 1 H), 1.31 – 1.19 (m, 1H), 0.74 – 0.66 (m, 2H), 0.60 – 0.54 (m, 2H), 0.52 – 0.45 (m, 2H), 0.44 – 0.38 (m, 2H), 169448-87-7

As the paragraph descriping shows that 169448-87-7 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2008/122765; (2008); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13889-98-0,1-Acetylpiperazine,as a common compound, the synthetic route is as follows.

Intermediate 9 (3.0 g, 0.89 mmol) in NMP (15 mL) was treated with 1-acetyl- piperazine (2.8 g, 22 mmol) and DIPEA (5.7 g, 44 mmol) and heated in a sealed tube at 140C for 72 h. The reaction mixture was cooled to r.t. and diluted with ethyl acetate/ water. The organic phase was washed (water, brine), dried (phase separation cartridge) and evaporated in vacuo. The resulting residue was purified by silica flashchromatography, eluting with 50-60% EtOAc in isohexane, to give the title compound (3.4 g 89%) as a cream solid. deltaEta (CDC13) 7.95 (IH, s), 7.53 (IH, dd, J 8.9, 6.0 Hz), 7.16 (IH, t, J 8.9 Hz), 5.08-5.02 (IH, m), 3.95-3.90 (IH, m), 3.78-3.73 (2H, m), 3.64 (IH, m), 3.61-3.40 (2H, m), 3.19-3.15 (2H, m), 2.59 (3H, d, J2.4 Hz), 2.17 (3H, s), 1.58 (3H, d, J 6.5 Hz), 1.48-1.42 (9H, m).

13889-98-0, 13889-98-0 1-Acetylpiperazine 83795, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; UCB PHARMA S.A.; ALLEN, Daniel, Rees; BUeRLI, Roland; HAUGHAN, Alan, Findlay; MATTEUCCI, Mizio; OWENS, Andrew, Pate; RAPHY, Gilles; SHARPE, Andrew; WO2011/58108; (2011); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.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,as a common compound, the synthetic route is as follows.

Compound L, the free base of venetoclax (4-(4-{[2-(4-chlorophenyl)-4,4- dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4- ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide), may be prepared as follows. Compound K (3.39 g), Compound A (1.87 g), 1-ethyl-3-[3- (dimethylamino)propyl]-carbodiimide hydrochloride (2.39 g), and 4-dimethylaminopyridine (1.09 g) were stirred in CH2Cl2 (40 mL) for 24 hours. The reaction was cooled and chromatographed on silica gel with 25-100% ethyl acetate/hexanes, then 10% methanol/ethyl acetate with 1% acetic acid, to give the product (1.62 g, 32%) as a solid.1H NMR (300 MHz, dimethylsulfoxide-d6) 11.65 (br s, 1H), 8.55 (br s, 1H), 8.04 (d, 1H), 7.89 (dd, 1H), 7.51 (m, 3H), 7.33 (d, 2H), 7.08 (m, 1H), 7.04 (d, 2H), 6.68 (dd, 1H), 6.39 (d, 1H), 6.19 (d, 1H), 3.84 (m, 1H), 3.30 (m, 4H), 3.07 (m, 4H), 2.73 (m, 2H), 2.18 (m, 6H), 1.95 (m, 2H), 1.61 (dd, 2H), 1.38 (m, 2H), 1.24 (m, 4H), 0.92 (s, 6H)., 1235865-77-6

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 66713100, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ACERTA PHARMA B.V.; HAMDY, Ahmed; ROTHBAUM, Wayne; IZUMI, Raquel; LANNUTTI, Brian; COVEY, Todd; ULRICH, Roger; JOHNSON, Dave; BARF, Tjeerd; KAPTEIN, Allard; (732 pag.)WO2016/24230; (2016); A1;,
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5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5625-67-2, Boc2O (2.0 mmol, 436mg, 1.0 eq) was added in portions under stirring and cooling on an ice bath to a suspension of piperazin-2-one (2.0 mmol, 200 mg, 1.0 eq) in anhydrous dichloromethane (10.0 mL). The reaction mixture was stirred overnight at room temperature, during which a homogeneous solutionformed. The solvent was evaporated and the solid residue was vacuum-dried tofurnish a yellow solid (300.0 mg, 100%). 1H NMR (300 MHz, CDCl3) delta (ppm): 1.51(s, 9 H); 3.37-3.46 (m, 2 H); 3.66 (t, J= 5.2 Hz, 2 H); 4.12 (s, 2 H); 6.39 (bs, 1 H). 13C NMR (75 MHz, CDCl3) delta (ppm):27.4 (CH2); 28.3 (3 x CH3); 41.2 (CH2); 77.1(CH2); 80.9 (C); 153.9 (C); 168.0 (C). MS (DCI/NH3) m/z: 201.1 [M+H+]; 218.1 [M + NH4+].

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Chollet, Aurelien; Mori, Giorgia; Menendez, Christophe; Rodriguez, Frederic; Fabing, Isabelle; Pasca, Maria Rosalia; Madacki, Jan; Kordulakova, Jana; Constant, Patricia; Quemard, Annaik; Bernardes-Genisson, Vania; Lherbet, Christian; Baltas, Michel; European Journal of Medicinal Chemistry; vol. 101; (2015); p. 218 – 235;,
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Piperazines – an overview | ScienceDirect Topics

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

To a solution of l-tert-butyl 3-methyl piperazine- 1, 3 -dicarboxy late (compound I-3a, 1.22 g, 5 mmol) in anhydrous CH2CI2 (15 mL) was added trimethylsilyl isocyanate (634 mg, 5.5 mmol). The resulting mixture was stirred at room temperature for 64 h. The reaction mixture was directly concentrated under reduced pressure to afford crude O l-tert-butyl 03 -methyl 4- carbamoylpiperazine-l,3-dicarboxylate (1.51 g) as a light-yellow foam which was directly used for next step without purification. MS obsd. (ESI+) [(M+H)+]: 288., 129799-08-2

129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; HAN, Xingchun; JIANG, Min; WANG, Yongguang; YANG, Song; (83 pag.)WO2019/129681; (2019); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.76003-29-7,1-Boc-3-Oxopiperazine,as a common compound, the synthetic route is as follows.

76003-29-7, In a 500 mL three-necked flask, 12.70 g (63.0 mmol, 1.0 eq.) of Compound 1 was dissolved in 280 mL of dimethylformamide and cooled to 0 C in an ice bath;1.73 g (73.0 mmol, 1.15 equivalents) of sodium hydride were added and stirred under ice cooling for 1 hour.Then 6.60 mL (69.0 mmol, 1.10 equivalents) of methyl bromoacetate was added via syringe.After further stirring for 20 minutes under ice cooling, the reaction solution was warmed to room temperature. After 18 hours, 10 mL of methanol, 10 mL of deionized water and 180 mL of a saturated sodium chloride solution were added to the reaction solution.The aqueous phase the organic phase was extracted once with 250mL to 140mL extracted three times with ether, and the combined dried over magnesium sulfate, and the solvent was evaporated under reduced pressure.Subsequently, it was removed under reduced pressure at a water temperature of 55 C in 2 hours.Residual dimethylformamide. Obtaining 13.4 g of an orange liquid, purified by flash chromatography using petroleum ether/ethyl acetate 4:1? petroleum ether/ethyl acetate 2:1 as eluent.Got a white solid,Yield: 14.16g (82%, 52.0mmol),White solid,

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

Reference£º
Patent; Shaoxing University; Hu Chunqi; Li Xin; Shi Yaru; Du Wenting; Tong Jie; Su Wanting; Xia Weiqi; (21 pag.)CN108610333; (2018); A;,
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548762-66-9,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.548762-66-9,(2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of(2S,5R)-1-Boc-2,5-dimethylpiperazine (3.5 g, 16.3 mmol, Astatech) in dichloromethane (35 ml), anhydrous triethylamine (4.59 ml, 32.7 mmol) was added and the mixture was cooled to 0 C. in ice-water bath. Acryloyl chloride (1.46 ml, 18.0 mmol) was added dropwise over ?5 min at which point the reaction mixture became yellow and viscous and formation of a white precipitate was observed. Water (10 ml) was added and the mixture was removed from the ice bath and was allowed to stir for 10 min. The organic layer was separated, quickly washed with 2N HCl (40 ml), water and brine, filtered through pad of MgSO4 and concentrated to afford crude tert-butyl (2S,5R)-4-acryloyl-2,5-dimethylpiperazine-1-carboxylate (4.4 g) as yellow oil. This material was redissolved in DCM (40 ml) and TFA (12.6 ml, 163 mmol) was added and the mixture was stirred at rt for 4 h at which point complete deprotection was observed. The mixture was concentrated under reduced pressure and dried under vacuum to afford 1-((2R,5S)-2,5-dimethylpiperazin-1-yl)prop-2-en-1-one 2,2,2-trifluoroacetate (Intermediate 160, ?9 g) as an oil.

548762-66-9 (2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate 11745988, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; Amgen Inc.; ALLEN, John Gordon; LANMAN, Brian Alan; CHEN, Jian; REED, Anthony B.; CEE, Victor J.; LIU, Longbin; LOPEZ, Patricia; WURZ, Ryan Paul; NGUYEN, Thomas T.; Booker, Shon; ALLEN, Jennifer Rebecca; CHU-MOYER, Margaret; AMEGADZIE, Albert; CHEN, Ning; GOODMAN, Clifford; LOW, Jonathan D.; MA, Vu Van; MINATTI, Ana Elena; NISHIMURA, Nobuko; PICKRELL, Alexander J.; WANG, Hui-Ling; SHIN, Youngsook; SIEGMUND, Aaron C.; YANG, Kevin C.; TAMAYO, Nuria A.; WALTON, Mary; XUE, Qiufen; US2019/374542; (2019); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

Example 10 Procedure for preparation of (R)-l-amino-N-( l-cyano-2-(4′-((4-cyclopropyl- piperazin-l-yl) methyl) biphenyl-4-yl) ethyl)cyclohexanecarboxamide (PZ1050)The preparation of PZ1050-1: To a solution of 1-cyclopropylpiperazine (2.0 g, 15.9 mmol) in EtOH (20 ml) was added 4-bromobenzaldehyde (2.9 g, 15.9 mmol) and CH3COOH (1.1 g, 19.1mmol). Then this mixture was stirred at room temperature overnight. This mixture was adjusted pH = 9 with NaHC03 and extracted with DCM. Then the organic phase was washed with IN HCI. The organic phase were combined, dried and concentrated in vacuo. The residue was purified by Pre-HPLC to give PZ1050-1 (1.1 g, 23.5%) as yellow solid., 20327-23-5

The synthetic route of 20327-23-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PROZYMEX A/S; PEDERSEN, John; LAURITZEN, Conni; WO2012/119941; (2012); 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.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,as a common compound, the synthetic route is as follows.

1235865-77-6, (0848) Compound 277J (0.063 g), Compound 277O (0.042 g), 1-ethyl-3-[3-(dimethylamino)propyl]-carbodiimide hydrochloride (0.032 g), and 4-dimethylaminopyridine (0.027 g) were combined in a 4-ml vial with dichloromethane (1.0 ml) and stirred overnight at ambient temperature. The reaction mixture was chromatographed directly without aqueous workup on silica gel with 0-4% methanol in dichloromethane as the eluent. Fractions containing the desired product were concentrated, slurried in acetonitrile, concentrated and dried overnight in a vacuum oven at 80 C. to give the title compound. 1H NMR (500 MHz, pyridine-d5) delta 13.05 (s, 1H), 9.13 (d, 1H), 8.72 (d, 1H), 8.41 (d, 1H), 8.10 (d, 1H), 7.67 (m, 1H), 7.66 (d, 1H), 7.44 (m, 2H), 7.07 (m, 2H), 6.76 (dd, 1H), 6.51 (m, 2H), 4.63 (m, 4H), 4.53 (d, 2H), 3.39 (m, 1H), 3.07 (m, 4H), 2.77 (s, 2H), 2.51 (m, 2H), 2.25 (m, 2H), 2.18 (m, 2H), 2.13 (m, 4H), 2.06 (t, 2H), 1.97 (s, 2H), 1.89 (m, 2H), 1.39 (t, 2H), 0.93 (s, 6H).

The synthetic route of 1235865-77-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AbbVie Inc.; Catron, Nathaniel; Lindley, David; Miller, Jonathan M.; Schmitt, Eric A.; Tong, Ping; US10213433; (2019); B2;,
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31166-44-6, 1-Cbz-Piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step A: Benzyl 4-(2-methoxy-2-oxoethyl)piperazine-l-carboxylate.To a solution of benzyl piperazine-1 -carboxylate (0.5 g, 2.270 mmol) and TEA (0.949 mL, 6.81 mmol) in THF (10 mL) was added methyl 2-bromoacetate (0.230 mL, 2.497 mmol) dropwise. The reaction was stirred at 65¡ãC. After 1 hour, the reaction mixture was concentrated, and the residue was partitioned between EtOAc and saturated aqueous NaHC03. The organic layer was dried over anhydrous magnesium sulfate, filtered, and concentrated to generate benzyl 4-(2-methoxy-2-oxoethyl)piperazine-l -carboxylate as a clear oil (0.61 g, 92 percent yield).

31166-44-6, 31166-44-6 1-Cbz-Piperazine 643495, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; AMGEN INC.; BODE, Christiane, M.; CHENG, Alan, C.; CHOQUETTE, Deborah; LEWIS, Richard, T.; POTASHMAN, Michele, H.; ROMERO, Karina; STELLWAGEN, John, C.; WHITTINGTON, Douglas, A.; WO2012/18668; (2012); A1;,
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Piperazines – an overview | ScienceDirect Topics