Sep 2021 News Simple exploration of (R)-2-Methylpiperazine

The synthetic route of 75336-86-6 has been constantly updated, and we look forward to future research findings.

75336-86-6, (R)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 1; Synthesis of 2-((lambda)-2-methyl-4-(6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-yl)- piperazin-l-yl)acetic acid Step 1A mixture of 1 -benzosuberone (0.803 ml, 5.01 mmol), (/?)-2-methylpiperazine (1.505 g, 15 mmol) in titanium (4+) isopropoxide (4.399 ml, 15 mmol) was heated at 800C overnight. After cooling to RT, the reaction mixture was diluted with 30 mL of MeOH and sodium borohydride (0.529 ml, 15 mmol) was slowly added. After stirring at rt for 20 min, the solvent was evaporated to dryness. The residue was redissolved in 50 mL of EtOAc and to this solution was added 1O g OfNaHCO3 and 0.5 mL of water to generate a white slurry. After stirring at rt for 2 h, the mixture was filtered with the help of excess EtOAc and the filtrate was evaporated to dryness. Column chromatography (SiO2, DCM/MeOH = 100:5 to 100:10 to 100:15 to 100:20) gave (3lambda)-3-methyl-l-(6,7,8,9-tetrahydro-5H-benzo[7]annulen-5- yl)piperazine (860 mg, 70percent yield) as an off white gum., 75336-86-6

The synthetic route of 75336-86-6 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; AMGEN INC.; WO2009/75857; (2009); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

28 Sep 2021 News Brief introduction of 4-(4-Ethylpiperazin-1-yl)phenylamine

115619-01-7, The synthetic route of 115619-01-7 has been constantly updated, and we look forward to future research findings.

115619-01-7, 4-(4-Ethylpiperazin-1-yl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(5-Chlorothieno[2,3-c]pyridin-2-yl)(2,6-difluoro-3,5-dimethoxyphenyl)methanol (730 mg, 1.96 mmol), 4 -(4-ethylpiperazin-1-yl)aniline (590 mg, 2.36 mmol), Pd2 (dba) 3 (360 mg, 0.393 mmol), XantpHos (454 mg, 0·785 mmol), Cs2CO3 (1.28 g, 3.93 mmol) It was mixed with toluene (10 ml) and stirred at 110 C under Ar protection overnight. The reaction solution was directly dried by column chromatography (dichloromethane:methanol = 95:5) to give compound (2,6-difluoro-3,5-dimethoxyphenyl) (5-((4-(4-) Ethyl piperazin-1-yl)phenyl)amino)thieno[2,3-c]pyridine-2-yl)methanone 1 g, purity 80%, yield 86.8%.

115619-01-7, The synthetic route of 115619-01-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Shanghai Xin Qibo Biological Technology Co., Ltd.; Wang Zhaoyin; Ma Jianbin; (39 pag.)CN110092798; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

28 Sep 2021 News New learning discoveries about 4-Methylpiperazine-1-carbonyl chloride

As the paragraph descriping shows that 39539-66-7 is playing an increasingly important role.

39539-66-7, 4-Methylpiperazine-1-carbonyl chloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The 4′-OH was protected using methyl pipirazine carbonyl chloride (11 mg, 0.054 mMoles) in 2mL DCM, 200 muL Allyl alcohol and pyridine (21 muL) for 2 hours. The product was purified by silica gel column chromatography and Identified by Mass Spec, MS+1 = 654, 39539-66-7

As the paragraph descriping shows that 39539-66-7 is playing an increasingly important role.

Reference:
Patent; MEDAREX, INC.; WO2005/112919; (2005); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Downstream synthetic route of 1-Methylpiperazine

The synthetic route of 109-01-3 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.109-01-3,1-Methylpiperazine,as a common compound, the synthetic route is as follows.

A l-liter-3-neck flask was loaded with 4-nitrobenzoyl chloride (50.5 g, 267 mmol) and THF (500 ml) and cooled to 0 C. Pyridine (44 ml, 544 mmol), then 1-methyl-piperazine (35 ml, 316 mmol) were added while mechanically stirring at 0 C. After the addition was completed the ice bath was removed and the mixture stirred for 1 hour, while warming to room temperature. A voluminous precipitate forms. The slurry was diluted with dichloromethane and 1 M aq. KOH and the layers separated. The organic layer was washed one more time with 1 M aq. KOH, then with brine and dried over MgSO4, filtered and concentrated in vacuum. 31.5 g yellow solid (4-methylpiperazin- l-yl)(4-nitrophenyl)methanone were isolated. MS (ESI) m/z 250 (M+H). 1H NMR (CDCl3) delta ppm 8.27 (d, 2 H, J= 7.9), 7.56 (d, 2 H, /= 7.9), 3.81 (bs, 2 H), 3.37 (bs, 2 H), 2.50 (bs, 2H), 2.34 (bs, 2H), 2.32 (s, 3H)., 109-01-3

The synthetic route of 109-01-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; PURANDARE, Ashok, Vinayak; BATT, Douglas, G.; LIU, Qingjie; JOHNSON, Walter, L.; MASTALERZ, Harold; ZHANG, Guifen; ZIMMERMANN, Kurt; WO2010/80474; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Downstream synthetic route of 1-Boc-3-Oxopiperazine

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

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

76003-29-7, A mixture of 1 ,1 -dimethylethyl 3-oxo-1 -piperazinecarboxylate (0.489 g, 2.44 mmol), 3-bromothiophene (0.332 g, 2.036 mmol), copper(l) iodide (0.019 g, 0.102 mmol), potassium carbonate (0.563 g, 4.07 mmol) and trans-N,N-dimethyl-cyclohexane-1 ,2- diamine (0.029, 0.204 mmol) in 1 ,4-dioxane (5 mL) was heated at reflux under nitrogen for 24 hours. After cooling to room temperature, the reaction mixture was filtered through silica ge. eluting with DCM:EtOAc/1 :1 , The filtrate was concentrated and the residue was purified by silica gel chromatography to afford 1 ,1 -dimethylethyl 3-oxo-4-(3-thienyl)-1 – piperazinecarboxylate (0.305 g, 53%) as a white solid.

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

Reference:
Patent; GLAXOSMITHKLINE LLC; BANKA, Anna; CATALANO, John, G.; CHONG, Pek, Yoke; FANG, Jing; GARRIDO, Dulce, Maria; PEAT, Andrew, James; PRICE, Daniel, J.; SHOTWELL, John, Brad; TAI, Vincent; ZHANG, Huichang; WO2011/41713; (2011); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

28 Sep 2021 News New learning discoveries about Piperazin-2-one

5625-67-2, 5625-67-2 Piperazin-2-one 231360, 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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

Reference Example 50: 3 -Oxo-4-(2-trimethylsilanyl-ethoxymethyl)-piperazine-l -carboxylic acid benzyl ester.; Piperazin-2-one (2.00 g, 20.0 mmol) was dissolved in H2O (10 ml) – 1,4-dioxane (10 ml); and NaHCO3 (1.85 g, 22.0 mmol) and benzylchloroformate (3.42 g, 20.0 mmol) was added thereto. After stirring at room temperature for 13 h, the reaction mixture was diluted with H2O and EtOAc. The aqueous layer was extracted with EtOAc and the combined organic layer was washed with brine, dried over MgSOphi The desiccant was removed through filtration and the filtrate was concentrated under reduced pressure to obtain crude 3 -Oxo-piperazine-1 -carboxylic acid benzyl ester as pale brown oil. This oil was used for the next step without further purification. The crude 3 -Oxo-piperazine-1 -carboxylic acid benzyl ester was dissolved in DMF (40 ml) and NaH (55% in oil, 1.05 g, 24.0 mmol) and SEMCl (5.01 g, 30.0 mmol) was added thereto at room temperature. After stirring at 500C for 18 h, the reaction mixture was diluted with EtOAc. The mixture was washed with H2O and brine, dried over MgSOphi The desiccant was removed through filtration and the filtrate was concentrated under reduced pressure. The EPO residue was purified by silica gel column chromatography (hexane / EtOAc = 8 / 2 to 5 / 5, to obtain the intended compound as a colorless oil.

5625-67-2, 5625-67-2 Piperazin-2-one 231360, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; MERCK & CO., INC.; BANYU PHARMACEUTICAL CO., LTD.; WO2007/11809; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Downstream synthetic route of 4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid

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

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

To a solution of piperazine-1,2,4-tricarboxylic acid 4-benzyl ester 1-tert-butyl ester (0.364 g, 1 mmol) in dichloromethane (3 mL) was added O-Methyl Hydroxylamine HCl (95 mg, 1.13 mmol), EDC HCl (0.3 g, 1.57 mmol) and DIEA (0.28 g, 2.17 mmol). The resulting mixture was stirred at room temperature overnight and partitioned between dichloromethane and water. The combined organic extracts were washed with brine, dried, and evaporated. The residue was purified by flash column chromatography on silica gel, eluting with EtOAc/n-Hexane (30/70) to afford the title product.LC/MS (m/z) [M]+ 394.2 (calculated for C19H27N3O6, 393.19).

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

Reference:
Patent; BIGNAN, Gilles; Gaul, Micheal; Xu, Guozhang; Zhao, Bao-Ping; US2011/150864; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Some tips on (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate

314741-40-7, 314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6-(Bromoacetyl)-3 ?4-dihydro- 1 H35 isochromen-1-one (-1.54 g, 5.72 mmol, presence of a-chloroketone was noted, -10%) andcommercially ayailable (S)-4-N-BOC-2-hydroxymethylpiperazine (1.24 g, 5.72 mmol) were added to a round bottom fiask and diluted with THF (50 m). Diisopropylethylamine (1.30 m, ?7.44 mmol) was then introduced and the mixture left stirring for 14 h at RT during which time a considerable amount of solid had formed (presumably HBr salt of DIPEA). The reaction mixture was diluted with EtOAc, then washed with saturated NH4Claq followed by H20. Both aqueous layers were sequentially back extracted once with another portion of EtOAc, the organics werethen combined, dried with MgSO4, filtered, and concentrated in yacuo. The recoyered crude product was subjected to purification by flash chromatography (Biotage, 50% EtOAc/Hex) to afford the title compound.

314741-40-7, 314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DE JESUS, Reynalda, Keh; DING, Fa-xiang; DONG, Shuzhi; FRIE, Jessica; GU, Xin; JIANG, Jinlong; SHAHRIPOUR, Aurash; PIO, Barbara; TANG, Haifeng; WALSH, Shawn; WO2014/126944; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Brief introduction of Piperazin-2-one

As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

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, Reference Example 3 4-(Tert-butoxycarbonyl)-2-piperazinone To a mixture of 2-piperazinone (3.00 g) and acetonitrile (50 ml) was added dropwise di-tert-butylbicarbonate (7.20 g), and the mixture was stirred at room temperature for 2 hours. The reaction solution was concentrated under reduced pressure, and precipitated crystals were washed with ether to give colorless crystals of the title compound (4.77 g). 1H-NMR (CDCl3) delta: 1.48 (9H, s), 3.33-3.43 (2H, m), 3.64 (2H, t, J=5.3 Hz), 4.09 (2H, s), 6.40-6.70 (1H, br). IR (KBr): 1696, 1667, 1400, 1341, 1130 cm-1.

As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

Reference:
Patent; Takeda Chemical Industries, Ltd.; US6403595; (2002); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

28 Sep 2021 News Brief introduction of tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate

As the paragraph descriping shows that 192130-34-0 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.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a mixture of 61 (131 mg, 0.303 mmol, 1.0 equiv), Pd2dba3 (27 mg, 0.0303 mmol, 0.10 equiv), 2-Dicyclohexylphosphino-2′, 4′, 6′-tri-1-propyl-1,1′-biphenyl (17 mg, 0.036 mmol, 0.12 equiv), and NaOtBu (58 mg, 0.606 mmol, 2.0 equiv) was added toluene (5 mL) which was first purged with argon. After 1 min of vigorous stirring, tert-butyl 4-(2-aminoethyl)piperazine-1-carboxylate (63 muL, 0.606 mmol, 2.0 equiv) was added and the mixture was heated to 90° C. After starting material was consumed as indicated by TLC, the solvent was removed in vacuo. The resulting residue was taken up in EtOAc (50 mL) and washed with water and brine. After drying with MgSO4 and concentration in vacuo, the crude mixture was purified by silica gel chromatography (10percent MeOH:CH2Cl2) to afford amine 10v [MS (MH+) 625; Calculated 624.3 for C36H44N6O4] and amine 15 [MS (MH+) 398; Calculated 397.2 for C25H23N3O2]., 192130-34-0

As the paragraph descriping shows that 192130-34-0 is playing an increasingly important role.

Reference:
Patent; Nunes, Joseph J.; Martin, Matthew W.; White, Ryan; McGowan, David; Bemis, Jean E.; Kayser, Frank; Fu, Jiasheng; Liu, Jinqian; Jiao, Xian Yun; US2006/46977; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics