Month: June 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1: (S)-tert-butyl 2-methyl-4-(3-nitrophenyl)piperazine-1-carboxylate A mixture of K2CO3 (8.8 g, 63.8 mmol), 1-fluoro-3-nitrobenzene (3 g, 21.3 mmol), and (S)-tert-butyl-2-methylpiperazine-1-carboxylate (4.26 g, 21.3 mmol) in DMSO (80 mL) was stirred at 130 C. for 16 hrs. The mixture was then filtered and the filtrate was washed with water, extracted with EtOAc, and purified by chromatography (silica, EtOAc/PE=1/10) to afford (S)-tert-butyl-2-methyl-4-(3-nitrophenyl)piperazine-1-carboxylate (1.98 g, 6.18 mmol, 29%). ESI-MS (EI+, m/z): 222.2 [M-99]+., 169447-70-5

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (136 pag.)US2019/389843; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

181955-79-3, 1,4-Di-Boc-piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

DIEA (1.35 g, 10.46 mmol), HOBT (1.40 g, 10.37 mmol) sequentially added to piperazine acid (3.30 g, 10 mmol) and L-prolinamide (1.14 g, 10 mmol) in DCM (40 ml) at 0 C. A solution of DCC (2.40 g, 11.65 mmol) in DCM (30 ml) is added slowly at 0 C. over a period of 1 hr. Stirred another 1 hr. at 0 C. and then at 25 C. for 4 hrs. Filtered, DCM distilled off, diluted with ethyl acetate, washed sequentially with saturated aqueous solution of NaHCO3 and brine. Organic layer dried (Na2SO4), evaporated in vacuo purified by column chromatography (ethyl acetate). (Yield 2.6 g, 61.03%).

181955-79-3, As the paragraph descriping shows that 181955-79-3 is playing an increasingly important role.

Reference：
Patent; TORRENT PHARMACEUTICALS LTD.; US2003/225102; (2003); 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.115761-79-0,1-(2,4-Difluorophenyl)piperazine,as a common compound, the synthetic route is as follows.

115761-79-0, 5-CHLORO-2-FURAN-2-YL- [1, 2,4] triazolo [1, 5-a] pyrimidin-7-ylamine (1 g ; see Example L (b) above) was suspended in 22 mL OF DMSO along with 1.5 eq OF CSF ANZ 5 eq of aminoacetaldyde dimethyl acetal. The reaction mixture was stirred at 100 C for 10 hours. It was then cooled to room temperature and diluted with EtOAc and washed with H2O and brine, dried with NA2S04 and concentrated to afford N5-(2, 2- dimethoxy-ethyl)-2-furan-2-yl-[1, 2,4] triazolo [1, 5-a] pyrimidine-5,7-diamine. This dimethyl acetal intermediate (50 mg) was then unmasked to the corresponding aldehyde by suspending in a solution of 2 mL OF CH2CL2 and 0.2 mL of 2: 1 solution O : TFA/H20. The resulting reaction mixture was stirred at room temperature for 4 hours It was then neutralized with 0.3 mL OF ET3N. 1- (2, 4-Difluoro-phenyl) -piperazine (1.5 resulting reaction mixture was stirred at room temperature for 2 hours. It was then concentrated and then purified by preparative HPLC to afford the title compound. 1H NMR (DMSO-D6) 7.72 (d, J = 1.0 Hz, 1 H), 7.35 (br s, 2 H), 7.29 (d, J = 3.6 Hz, 1 H), 6. 7-7.4 (M, 3 H), 6.75 (dd, J = 3.6 Hz, 1.0 Hz, 1 H), 5.7 (S, 1H), 3.1 (BR S, 2 H), 2. 2- 3.6 (M, 12 H). MS : m/z: 441 [M + H]+.

As the paragraph descriping shows that 115761-79-0 is playing an increasingly important role.

Reference：
Patent; BIOGEN IDEC MA INC.; WO2004/92171; (2004); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109384-27-2, 1-Methylpiperazin-2-one hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

a) (4-Methyl-3-oxo-piperazin-l-yl)-carbamic acid t-butyl ester l-Methyl-2-piperazinone hydrochloride (1 : 1) (300 mg, 1.99 mmol) was combined with dichloromethane (20 mL) to give a light yellow suspension. N,N-Diisopropylethylamine (309 mg, 417 ??, 2.39 mmol) was added at 0 C. Subsequently 3-(4-cyanophenyl)-2-oxaziridinecarboxylic acid 1,1-dimethylethyl ester (441 mg, 1.79 mmol) in dichloromethane (10 mL) was added during 35 min at 0C and the reaction mixture was stirred for 1 h at 0 C. Afterwards the reaction mixture was concentrated in vacuo and the residue was purified by flash chromatography (silica gel, 20g, 0% to 100% ethyl acetate in n-heptane) to deliver an oil contaminated with 4-cyano- benzaldehyde. This material was purified by a second chromatography (aminophase 5 g, ethyl acetate/n-heptane 1 / 1) to give the title compound (67 mg, 15%) as white solid; GC-MS (EI) 229.0 (M)+.

109384-27-2, The synthetic route of 109384-27-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; GRETHER, Uwe; HEBEISEN, Paul; MOHR, Peter; RICKLIN, Fabienne; ROEVER, Stephan; WO2013/37703; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,13889-98-0

INTERMEDIATE 10( S)-ter t-Butyl 1 – |~2-(4-acetylpiperazin- 1 -yl)-7-fluoro-8-methylquinolin-3 – yl 1 ethylcarbamateIntermediate 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 (1H, s), 7.53 (1H, dd, J 8.9, 6.0 Hz), 7.16 (1H, t, J 8.9 Hz), 5.08-5.02 (1H, m), 3.95-3.90 (1H, m), 3.78-3.73 (2H, m), 3.64 (1H, 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).

As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference：
Patent; UCB PHARMA S.A.; BUeRLI, Roland; HAUGHAN, Alan, Findlay; MATTEUCCI, Mizio; OWENS, Andrew, Pate; RAPHY, Gilles; SHARPE, Andrew; WO2011/58110; (2011); 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.

Synthesis of compound 189.2. To a solution of 1-isopropylpiperazine (0.35 g, 2.7mmol, l .Oeq) in CH3CN (5ml) was added potassium carbonate (1.12g, 8.1mmol, 3.0eq). Compound 189.1 (0.5 g, 2.7 mmol, l .Oeq) in CH3CN (5 ml) was added dropwise to the reaction mixture. Reaction mixture was then stirred at 60°C for 6 hours. After completion of the reaction, mixture was poured into water and product was extracted with EtOAc. Organic layers were combined, washed with brine, dried over Na2S04 and concentrated under reduced pressure to obtain crude which was purified by column chromatography to furnish 189.2 (0.460 g, 61.56percent). MS (ES): m/z 277.32 [M+H]+.

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

Reference：
Patent; NIMBUS LAKSHMI, INC.; MASSE, Craig E.; GREENWOOD, Jeremy Robert; ROMERO, Donna L.; HARRIMAN, Geraldine C.; WESTER, Ronald T.; SHELLEY, Mee; KENNEDY-SMITH, Joshua Jahmil; DAHLGREN, Markus; WO2015/131080; (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.170911-92-9,tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,170911-92-9

A solution of 2-chloro-6-(2-chlorophenyl)-5H-pyrano[2,3-d]pyrimidin-5-one (42 mg, 0.14 mmol), tert-butyl 4-(4-aminophenyl)piperazine-1-carboxylate (40 mg,0.14 mmol) and DIPEA (50 1JL, 0.29 mmol) in anhydrous DMF (1 mL) was heated to 100 C under a nitrogen atmosphere for 60 mm. The reaction mixture was allowed to cool to RT, diluted with water (5 mL) and extracted into ethyl acetate (3 x 5 mL) . The combined organic phases werewashed with 1:1 water/brine (3 x 5 mL), dried over Na2504, filtered, and concentrated to dryness under reduced pressure. The residue was purified by flash chromatography (10-100%, MeOH in DCM) to give the title compound (50 mg, 65%) as a brown solid. ?H NMR (500 MHz,CDC13) : 6 9.24 (s, 1H), 7.94 (br s, 1H), 7.80 (s, 1H),7.54 (br d, 2H), 7.49 (dd, 1H), 7.30-7.38 (m, 3H), 6.96(d, 2H), 3.59 (t, 4H), 3.13 (t, 4H), 1.49 (s, 9H) . LCMS(Method A) : = 1.52 mi m/z = 534, 536 [M+H].

As the paragraph descriping shows that 170911-92-9 is playing an increasingly important role.

Reference：
Patent; ALMAC DISCOVERY LIMITED; ROUNTREE, James Samuel Shane; O’DOWD, Colin Roderick; BURKAMP, Frank; BELL, Mark Peter; WO2015/19037; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

159532-59-9, (S)-1-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step C (S)-1-(tert-Butyloxycarbonyl)-4-(dipentylcarbamoyl)piperazine-2-carboxylic acid A partial solution of 1.32 g (5.74 mmole) of (S)-1-(tert-butyloxycarbonyl)piperazine-2-carboxylic acid in 25 ml of dried DMF was treated dropwise over 5 min with 1.48 g (11.47 mmole of diisopropylethyl amine at 25 under nitrogen with stirring. The clear solution which resulted was treated dropwise over 15 min with a solution of 1.26 g (5.74 mmole) of dipentylcarbamoyl chloride in 5 ml of DMF and the mixture was stirred under nitrogen at 25 for 16 hr. The solution was concentrated in vacuo and the residue was dissolved in 100 ml of dichloromethane which was extracted with 2*100 ml of 0.5M citric acid and 2*25 ml of water. Without drying, the solution was concentrated in vacuo to 1.85g (78%) of medium yellow oil which was homogeneous by the (silica gel, 1:1:1:1 ethylacetate: n-butanol: acetic acid: water, Rf =0.50). Mass Spectrum (FAB): m/e 414 (M+1), 358 (loss of butyl) 1 H NMR (CDCl3, 400 MHz, ppm): delta0.86 (t, 6H), 1.20 (m, 4H), 1.27 (m, 4H), 2.46 (m, 13H), 2.82 (m, 1H), 3.10 (m, 4H), 3.16 (m, 2H), 3.42 (d of d, 1H), 3.84 (d of d, 1H), 4.04 (d, 1H), 4.61-4.77 (d, 1H).

159532-59-9, As the paragraph descriping shows that 159532-59-9 is playing an increasingly important role.

Reference：
Patent; Merck & Co., Inc.; US5348955; (1994); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

106261-48-7, 4-((4-Methylpiperazin-1-yl)methyl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[00130] To a solution of 5-(3-amino-phenylamino)-l,3-dihydro-indol-2-one (20 mg, 0.083 mmol) in DMF (2ml) is added 4-(4-methyl-piperazin-l-ylmethyl)-benzoic acid (31 mg, 0.1 mmol), N,N-diisopropylethylamin (54 mg, 0.42 mmol), EDCI (32 mg, 0.17 mmol) and HOBt (11 mg, 0.083 mmol). The reaction is stirred for 12 hours and EPO concentrated. The residue is purified by HPLC to afford the desired compound: LC-MS: 456.2 (MH+).

106261-48-7, Big data shows that 106261-48-7 is playing an increasingly important role.

Reference：
Patent; IRM LLC; WO2006/52936; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

55121-99-8, (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example B3Preparation, of .compound 3; Reaction under Ar flow. Dry DMSO (1.5 ml) was added to a mixture of intermediate 5 (0.000428 mol), l-(4-aminobenzoyl)-4-methyl- piperazine (0.000642 mol) and cesium carbonate (0.000642 mol). The reaction mixture was stirred for 3 hours at 100C. This mixture was extracted with a mixture of EtOAc/NaHCO3/H2O/NaCl. The extract’s solvent was evaporated. The residue (0.145 g) was purified by column chromatography over silica gel (eluent: DCM/MeOH gradient). The product fractions were collected and the solvent was evaporated, yielding 0.094 g of compound 3., 55121-99-8

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

Reference：
Patent; JANSSEN PHARMACEUTICA N.V.; WO2006/74985; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics