Heterocyclic Building Blocks-piperazine

182618-86-6, 1-Boc-4-(4-Nitrophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A suspension of 4-(4-nitro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (Step 8.3) (1.26 g, 4.1 mmol) and palladium on carbon (200 mg) in MeOH (30 ml.) was stirred for 30 min at rt, under a hydrogen atmosphere. The reaction mixture was filtered through a pad of celite and concentrated to afford 1.1 g of the title compound as a pink solid: ESI-MS: 278.2 [M+H]+; tR= 2.85 min (System 1 )., 182618-86-6

182618-86-6 1-Boc-4-(4-Nitrophenyl)piperazine 3380696, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; NOVARTIS AG; WO2009/141386; (2009); 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.

(0413) To a solution of Compound 3J (90 mg), Compound 130C (64.2 mg), triethylamine (0.077 ml), N,N-dimethylpyridin-4-amine (38.5 mg) in a mixture of dichloromethane (5 ml) and N,N-dimethylformamide (0.5 ml) was added N1-((ethylimino)methylene)-N3,N3-dimethylpropane-1,3-diamine, hydrochloric acid (60.4 mg) and the mixture was stirred 18 hours. This was concentrated on high vacuum and the crude was purified by reverse phase chromatography with ammonium acetate buffer/acetonitrile. 1H NMR (500 MHz, pyridine-d5) delta 13.03 (s, 1H), 9.27 (d, 1H), 8.59 (d, 1H), 8.43 (d, 1H), 8.37 (dd, 1H), 8.11 (d, 1H), 7.65-7.67 (m, 2H), 7.44 (d, 2H), 7.07 (d, 2H), 6.88 (d, 1H), 6.76 (dd, 1H), 6.54 (d, 1H), 6.48 (m, 1H), 4.06 (m, 1H), 3.98 (d, 2H), 3.35 (t, 2H), 3.07 (m, 4H), 2.73-2.80 (m, 4H), 2.68-2.72 (m, 1H), 2.36 (q, 1H), 2.11-2.30 (m, 9H), 1.97 (m, 2H), 1.62-1.71 (m, 3H), 1.48-1.58 (m, 2H), 1.39 (t, 2H), 0.94 (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：
Patent; AbbVie Inc.; Catron, Nathaniel; Lindley, David; Miller, Jonathan M.; Schmitt, Eric A.; Tong, Ping; US10213433; (2019); B2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

548762-66-9, (2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

548762-66-9, To a stirred solution of 64 mg (0.3 mmol) tert-butyl (25,5R)-2,5-dimethylpiperazine-1- carboxylate in 2 mL DOE were added at RT 160 pL DIPEA (0.9 mmol, 3 eq) and 86 mg 4-methylbenzenesulfonyl chloride (0.45 mmol, 1.5 eq) and the mixture was stirred overnight at RT. The organic phase was washed three times with water, dried andevaporated to yield 110 mg (100%) of the crude title compound which was used in the next step without further purification.[C-MS (Method 1): Rt = 1.39 mm; MS (ESIpos): m/z = 369 [M÷H]

As the paragraph descriping shows that 548762-66-9 is playing an increasingly important role.

Reference：
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; KOPPITZ, Marcus; SIEBENEICHER, Holger; STEUBER, Holger; TER LAAK, Antonius; NUBBEMEYER, Reinhard; ROTTMANN, Antje; IRLBACHER, Horst; BADER, Benjamin; PETERS, Michaele; WAGENFELD, Andrea; (74 pag.)WO2018/114672; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-34-8, tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step A. 4-(4-Amino-2-fluoro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester. 4-(2-Fluoro-4-nitro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (4.0 g, 12.3 mmol), was dissolved into EtOH (200 ml.) and Pd/C 10% (300 mg) was added carefully. The resulting mixture was stirred under hydrogen atmosphere provided by hydrogen balloon for 24 h. The catalyst was removed and the concentration of the filtrate yield the title compound.MS (ESI) mass calculated for C15H22FN3O2, 295.35; m/z measured, 296.5 [M+H]+1H NMR (CDCI3): 6.76 (t, J = 9.2, 1 H), 6.44-6.35 (m, 2H), 3.62-3.49 (m, 6H), 2.93-2.82 (m, 4H), 1.47 (s, 9H).

154590-34-8, 154590-34-8 tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate 16203508, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; JANSSEN PHARMACEUTICA N.V.; WO2009/79597; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

N-(4-(2-(Chloromethyl)-5-methyl-4-oxo-4,5-dihydrofuro[3,2-c]pyridin-7-yl)p (for a preparation see Intermediate 82, 50 mg, 0.151 mmol) was dissolved in DMF (5 mL), potassium carbonate (62.5 mg, 0.452 mmol) was added, followed by 1-methylpiperazin-2-one (17.20 mg, 0.151 mmol). The mixture was stirred for 3 h at room temperature. The mixture was diluted with water (10 mL) and extracted with a mixture of methanol (3 mL) and DCM (15 mL), the organic layer was dried, 59702-07-7

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

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED; AMANS, Dominique; BAMBOROUGH, Paul; BARKER, Michael David; BIT, Rino Antonio; BROWN, John Alexander; CAMPBELL, Matthew; GARTON, Neil Stuart; LINDON, Matthew J; SHIPLEY, Tracy Jane; THEODOULOU, Natalie Hope; WELLAWAY, Christopher Roland; WESTAWAY, Susan Marie; WO2014/140077; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

934-98-5,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.

A solution of 2,4-dichloro-5,7-difluoro-3-nitroquinoline (5.58 gm, 2.0×10?2 moles) in 2-methyl tetrahydrofuran (50 mL) is stirred as diisopropylethylamine (2.84 gm, 2.2×10?2 moles) and N-2-aminoethyl-N? methylpiperazine (3.15 gm, 2.2×10?2 moles) are added. This solution is stirred at room temperature overnight. The yellow reaction mixture is diluted with more 2-methyl-tetrahydrofuran (50 mL) and this is washed with water (100 mL) followed by brine (50 mL). After being dried over magnesium sulfate, the solution is filtered and the solvent is removed under reduced pressure. The oily residue is stirred with diethyl ether (25 mL) and this is cooled on ice causing the product to crystallize. The solid yellow product is isolated by filtration, washed with ether and dried. The yield is about 4.32 gm.

The synthetic route of 934-98-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; JANUS BIOTHERAPEUTICS, INC.; Lipford, Grayson B.; Zepp, Charles M.; (72 pag.)US9873694; (2018); B2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129779-30-2, (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Bubbled N2 through a suspension of 6-(4-bromophenyl)pyrazolo[l,5-a]pyrimidine (1.14 g, 4.16 mmol) (WO 2009/114180 Al, 2009) and (3R,5S)-tert-butyl 3,5-dimethylpiperazine-l- carboxylate (2.25 g, 10.50 mmol) in toluene (16 mL). Added bis(tri-t- butylphosphino)palladium (0) (0.106 g, 0.208 mmol) then sodium 2-methylpropan-2-olate (0.600 g, 6.24 mmol). Heated in 100 degree bath under N2. After 5 h, removed solvent. Partitioned between EA and water. Filtered through Celite, washing with ethyl acetate. Washed org layer with brine, dried (Na2S04), filtered and concentrated. Purified on Biotage (50 g) eluting with 25-75% EA/hex. Solid obtained from later peak was triturated in EtOH and filtered to obtain (3R,5S)-tert-butyl 3,5-dimethyl-4-(4-(pyrazolo[l,5-a]pyrimidin-6- yl)phenyl)piperazine-l-carboxylate (0.234 g, 0.574 mmol, 13.81 % yield) as a faint yellow solid.

129779-30-2, 129779-30-2 (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 10822535, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; THE BRIGHAM AND WOMEN’S HOSPITAL, INC.; THE U.S.A., AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH & HUMAN SERVICES; ALIMARDANOV, Asaf; CUNY, Gregory, D.; GREWAL, Gurmit, Singh; LEE, Arthur; MCKEW, John, C.; MOHEDAS, Agustin, H.; SHEN, Min; XU, Xin; YU, Paul, B.; WO2014/160203; (2014); 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.54699-92-2,4-Methyl-1-piperazineacetic acid,as a common compound, the synthetic route is as follows.,54699-92-2

Example 13; General Method For The Preparation Of Active Esters Of N-Substituted Piperazine Acetic Acid From Trifluoroacetate Esters; A solution of the trifluoroacetate in THF (0.58 M, 1.2 equiv) was added to a solid sample of N-methyl piperazine acetic acid and mixed in a vortex or shaker until a homogeneous solution was obtained. The reaction of the carboxylic acid with the trifluoroacetate ester was generally complete within 30 min for all cases except N-hydroypyrrolidinone (NHP, 18 h). The progress of conversion to the active ester was monitored by ES-MS. The amount of product and any starting material (N-MPA) could be determined by direct infusion of a sample of the reaction (in ethanol) into the ES-MS. In some cases the active ester product was precipitated as dihydrochloride salt by the addition of a solution by addition of HCl solution in dioxane (4 M, 50% volume of the reaction) followed by washing with THF, ethyl acetate and hexanes. In other cases the product was isolated from the reaction as the mono TFA salt. Addition of TFA could be performed if the bis-TFA salt was desired. Dhbt ester, Calculated MH+ = 304.14 Found = 304.20 NHP ester, Calculated MH+ = 242.15 Found = 242.20 4-NP ester, Calculated MH+ = 280.13 Found = 280.20 1H NMR (400 MHz, CDCl3) d 8.20 (d, 2H, J=9.2 Hz, aromatic protons), 7.25 (d, 2H, J=9.2 Hz, aromatic protons), 3.69-3.40 (broad, 2H, ring protons), 3.57 (s, 2H, -CH-CO-), 3.15-2.90 (broad, 6H, ring protons), 2.78 (s, 3H, -CH3). Pfp ester, Calculated MH+ = 325.10 Found = 325.10 Pcp ester, Calculated MH+ = 404.95 Found = 405.90 3-NP ester, Calculated MH+ = 280.13 Found = 280.20 NHS ester, Calculated MH+ = 256.13 Found = 256.10

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

Reference：
Patent; Applera Corporation.; US2005/148773; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

149057-19-2, 4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General Process for the Preparation of Compound O-In-3 from O-In-2:; [00169] A three necked round bottom flask was charged with O-In-2 (1 eq.), triethyl amine (2 eq.) and dry dichloromethane under nitrogen atmosphere. The reaction mixture was cooled to 0 0C and methyl chloroformate (1.3 eq.) was added into the reaction mixture very slowly. The reaction mixture was stirred at -10 0C for 30min and further cooled to -30 0C. Ammonia gas was purged in the reaction mixture for 30min at -30 0C. The reaction mixture was allowed to stir at room temperature for 16h. After consumption of starting material, ice-cold water was added to reaction mixture. The organic layer was separated and aqueous layer was extracted with dichloromethane. The combined organic layers was washed with water, brine and dried over anhydrous sodium sulfate. The organic layer was filtered and concentrated under reduced pressure. The resulting crude product was purified by column chromatography using 60-120 silica gel and chloroforrrDeltamethanol (6%) as eluant to afford O-In-3.

149057-19-2, As the paragraph descriping shows that 149057-19-2 is playing an increasingly important role.

Reference：
Patent; BRISTOL-MYERS SQUIBB COMPANY; WO2009/158394; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6.1. Example 1(S)-N-(3-bromo-4-fluorophenyl)-2-methyl-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazine-1-carboxamide The captioned compound was prepared in several steps.A. Preparation of (S)-tert-butyl 2-methyl-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazine-1-carboxylate. (S)-tert-butyl 2-methylpiperazine-1-carboxylate (3 g, 15 mmol), N,N-diisopropylethylamine (3 ml), and 4-chloro-5-methyl-7H-pyrrolo[2,3-d]pyrimidine (2 g, 12 mmol) were added to isopropanol (10 ml). The solution was heated at 120 C. in a sealed pressure tube for 12 hours. The reaction was concentrated under vacuum, and the residue was purified by flash chromatography (80 g SiO2, 0-5% MeOH: CH2Cl2, 50 min) to give clean (S)-tert-butyl 2-methyl-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazine-1-carboxylate (1.5 g, 4.5 mmol, 38%).1H NMR (400 MHz, chloroform-d) delta ppm 10.42 (br. s., 1H), 8.39 (s, 1H), 6.96 (s, 1H), 4.40 (d, J=6.06 Hz, 1H), 3.83-4.01 (m, 2H), 3.43 (td, J=12.57, 3.41 Hz, 1H), 3.32 (dd, J=12.76, 3.92 Hz, 1H), 3.07 (td, J=12.32, 3.41 Hz, 1H), 2.44 (s, 3H), 1.50 (s, 9H), 1.24 (d, J=6.82 Hz, 3H); MS (ES+) [M+H]+=332.

169447-70-5, As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference：
Patent; Harrison, Bryce Alden; Kimball, Spencer David; Mabon, Ross; Rawlins, David Brent; Rice, Dennis S.; Voronkov, Michael Victor; Zhang, Yulian; US2009/42893; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics