Category: piperazines

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

To a solution of tert-butyl (3S, 5R)-3,5-dimethylpiperazine-1-carboxylate (1 g, 4.67 mmol, 1 eq) and ethyl 2-bromoacetate (701 mg, 4.20 mmol, 0.9 eq) in acetonitrile (10 mL) was added diisopropyl ethyl amine (1.81 g, 14.00 mmol, 3 eq). The reaction mixture was stirred at 80C for 12 hours. The reaction mixture was diluted with water (50 mL) and extracted with ethyl acetate (50 mL x 3). The combined organic layers were washed with brine (80 mL x 2), dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (Petroleum ether/Ethyl acetate=30/1 to 1/1). tert-butyl (3S,5R)-4-(2-ethoxy-2-oxo-ethyl)-3,5-dimethyl-piperazine-1-carboxylate (1.09 g, 3.63 mmol, 77% yield) was obtained as a white solid. LC/MS (ESI) m/z: 301.1 [M+1] +; 1H-NMR (400MHz, CDCl3) d 4.16 (q, J=7.2 Hz, 2H), 4.02 – 3.72 (m, 2H), 3.56 (s, 2H), 2.96 – 2.82 (m, 2H), 2.53 (s, 2H), 1.46 (s, 9H), 1.27 (t, J=7.2 Hz, 3H), 1.08 (d, J=6.4 Hz, 6H).

129779-30-2, As the paragraph descriping shows that 129779-30-2 is playing an increasingly important role.

Reference£º
Patent; ARVINAS OPERATIONS, INC.; YALE UNIVERSITY; CREW, Andrew P.; HORNBERGER, Keith R.; WANG, Jing; CREWS, Craig M.; JAIME-FIGUEROA, Saul; DONG, Hanqing; QIAN, Yimin; ZIMMERMAN, Kurt; (1451 pag.)WO2020/51564; (2020); 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.381242-61-1,1-(4-Nitro-2-(trifluoromethyl)phenyl)piperazine,as a common compound, the synthetic route is as follows.

According to scheme 1, step 2: 1-(4-nitro-2-(trifluoromethyl)phenyl)piperazine (5.0 mmol) was taken in ethyl acetate (20 mL), to this, aqueous sodium hydroxide (6.2 mmol, 30%) was added keeping the temperature 0 C, carbon disulfide (6.2 mmol) dissolved in ethylacetate (5 mL) was added drop-wise with stirring at 0 C. The reaction mixture was further stirred at room temperature for one hour to furnish a yellow solid. Solvent was distilled off and the crude was recrystallised by methanolic ether to get sodium 4-(4-nitro-2- (trifluoromethyl)phenyl)piperazine-1 -carbodithioate as a yellow powder., 381242-61-1

The synthetic route of 381242-61-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH; SHARMA, Vishanu Lal; LAL, Nand; SARSWAT, Amit; JANGIR, Santosh; BALA, Veenu; KUMAR, Lalit; RAWAT, Tara; JAIN, Ashish; KUMAR, Lokesh; MAIKHURI, Jagdamba Prasad; GUPTA, Gopal; WO2014/122670; (2014); 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.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

200 mg (0.63 mmol) of 1-chloro-3-methyl-2-phenylpyrido[1,2-a]benzimidazole-4-carbonitrile (I-8) was suspended in dimethylsulfoxide (4 ml), and 0.19 ml (1.32 mmol) of triethylamine and 82 mg (0.82 mmol) of (S) – (+) -2-methylpiperazine were added thereto, and heated with stirring at 90C for 5 hours. After restored to room temperature, water was added to the reaction mixture, and the resulting precipitate was collected by filtration and washed with n-hexane. The thus-obtained crude crystal was recrystallized from a mixed solvent of chloroform/ethyl acetate/n-hexane to obtain 141 mg (58 %) of the entitled compound as a yellow solid. MS(ESI)m/z:382(M+1)+.1H-NMR(DMSO-d6)delta: 0.76(3H, d, J=6.1Hz), 1.89(1H, t, J=10.5Hz), 2.17(3H, s) , 2.30(1H, dt, J=2.7, 11.2Hz), 2.70(1H, d, J=12.4Hz), 2.98-3.11(4H, m), 7.37-7.42(3H, m), 7.52-7.57(4H, m), 7.88(1H, d, J=8.0Hz), 8.80(1H, d, J=8.5Hz). IR(ATR): 2833, 2220, 1481, 1442 cm-1., 74879-18-8

74879-18-8 (S)-(+)-2-Methylpiperazine 2734219, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1479681; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

474711-89-2,474711-89-2, Piperazine-1-carboxamide hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

56c. Lambda/1-Methyl-Lambda/1-((2,6,6-trimethylcyclohex-1-en-1-yl)methyl)piperazine- 1,4-dicarboxamide3-Methyl-1 -(methyl((2,6,6-trimethylcyclohex-1 -en-1 – yl))methyl)carbamoyl)-1 H-imidazol-3-ium iodide (0.200 g, 0.470 mmol), piperazine-1-carboxamide hydrochloride (78.0 mg, 0.470 mmol) and triethylamine (0.130 ml_, 0.930 mmol) were dissolved in a 1 :4 mixture of acetonitrile: dichloromethane. The reaction mixture was stirred at room temperature under argon for 2 days. The reaction mixture was poured into saturated ammonium chloride (30 mL) and the organic layer was removed. The aqueous layer was extracted with dichloromethane (4 x 15 mL). The combined organic phases were dried over sodium sulfate, filtered and concentrated in vacuo. The product obtained as a white solid (11 mg, 0.03 mmol, 7%) was purified by preparative plate thin layer chromatography (1000 mum thickness Sitheta2 gel, 20 cm x 20 cm plate, eluent 10:90 methanol: ethyl acetate + 0.1 % (v/v) ammonium hydroxide. Mp = 139.6-140.30C; Rf = 0.62 (10:90 methanol: ethyl acetate + 0.1 % (v/v) ammonium hydroxide); 1H-NMR (400 MHz, DMSO) delta 6.00 (s, 2H), 3.93 (s, 2H), 3.32-3.28 (m, 4H), 3.01-3.00 (m, 4H), 2.66 (s, 3H), 1.99-1.96 (m, 2H), 1.65 (s, 3H), 1.59-1.57 (m, 2H), 1.41- 1.40 (m, 2H), 0.96 (s, 6H); Mass spectrum (ESI +ve) m/z 323.0 (MH+).

The synthetic route of 474711-89-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIKAM PHARMACEUTICALS, INC.; GARVEY, David, S.; LAROSA, Gregory, J.; GREENWOOD, Jeremy, Robert; BREWER, Mark, L.; QUACH, Tan; COTE, Jamie, B.; BERMAN, Judd; WO2010/147653; (2010); 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.252990-05-9,Methyl (R)-1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

(R)-Piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester (120 mg, 0.49 mmol) and 2-Bromo-5-trifluoromethyl-pyridine (133 mg, 0.59 mmol) were dissolved into 2.0 mL of anhydrous toluene (degassed). In a separate, septum-equipped vial were placed tri(dibenzylideneacetone)dipalladium (0) (22 mg, 0.024 mmol), 1,3-bis(2,6-di-i-propylphenyl)imidazolium chloride (42 mg, 0.1 mmol) and sodium t-butoxide (57 mg, 0.59 mmol). This “catalytic” vial was equipped with a magnetic stir bar and flushed with dry nitrogen. The reactant solution was next transferred to the “catalytic” vial and the mixture was stirred at 100 C. for 5 h. After this period the mixture was combined with 20 mL of hexane/EtOAc (2:1) and was passed through a pad of Celite. The resulting filtrate was evaporated in vacuo and purified using flash silica chromatography (0-20% EtOAc/Hexane) to yield 110 mg (58%) of (R)-4-(5-Trifluoromethyl-pyridin-2-yl)-piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester, intermediate IX-B, as a yellow residue. 1H NMR (400 MHz, CDCl3) delta 8.39-8.38 (m, 1H), 7.65 (d, 1H), 6.68 (m, 1H), 4.89-4.68 (m, 2H), 4.29 (dd, 1H), 3.95 (dd, 1H), 3.69 (s, 3H), 3.43-3.26 (m, 2H), 3.12-2.97 (m, 1H), 1.51-1.46 (m, 9H)., 252990-05-9

The synthetic route of 252990-05-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Kalypsys, Inc.; US2005/234046; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

74879-18-8, (S)-(+)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,74879-18-8

To a solution of (S)-methylpiperazine (400 mg) in dichloromethane (20 mL) at0 C was added di-tert-butyl dicarbonate (871 mg). The reaction was stirred at room temperature for 4 h and then quenched with water (20 mL) and extracted into dichloromethane (2 x 40 mL). The combined organics were washed with saturated aqueous brine solution (40 mL), dried (MgSO4) and concentrated to give (S)-3-methyl-piperazine-l- carboxylic acid tert-butyl ester as a white solid (669 mg, 84%).

As the paragraph descriping shows that 74879-18-8 is playing an increasingly important role.

Reference£º
Patent; PIRAMED LIMITED; GENENTECH, INC.; BAYLISS, Tracy; CHUCKOWREE, Irina; FOLKES, Adrian; OXENFORD, Sally; WAN, Nan, Chi; CASTANEDO, Georgette; GOLDSMITH, Richard; GUNZNER, Janet; HEFFRON, Tim; MATHIEU, Simon; OLIVERO, Alan; STABEN, Steven; SUTHERLIN, Daniel, P.; ZHU, Bing-Yan; WO2008/70740; (2008); 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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

In the following order 6.82 g (29.9 mmol) of the methylated bromo compound, 4.03 g (35.9 mmol) of the dimethyl piperazine, 13.6 g (41.9 mmol) of Cs2CO3, 1.42 g (2.99 mmol) of X-Phos (see Huang et al., J. Am. Chem. Soc., 125(2003)6653). and 0.55 g (0.6 mmol) of Pd2(dba)3 were added to 225 ml of toluene which was degassed for 4 hours prior to usage. While stirring and under a nitrogen atmosphere the temperature was raised to 100¡ã C. for 20 hours, after which it was allowed to reach room temperature. The mixture was diluted with CH2Cl2 after which it was filtered and concentrated in vacuo. The residue was put on top of a flash chromatography column (SiO2) using DMA 0.25. The combined product containing fractions yielded after concentration in vacuo 0.73 g (9percent) of the desired pure piperazine VIII-H., 21655-48-1

As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

Reference£º
Patent; SOLVAY PHARMACEUTICALS B.V.; US2006/122189; (2006); 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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Preparation 6 (5-Bromo-l,2-benzothiazol-7- l)-[cz5,-3,5-dimethylpiperazin-l-yl]methanone To a mixture of 5-bromo-l,2-benzothiazole-7-carboxylic acid (10 g, 0.039 mol) and DMF (100 mL) is added cw-2,6-dimethylpiperazine (6.64 g, 0.058 mol) at 28 ¡ãC. The resulting mixture is cooled to 0 ¡ãC and HATU (22.1 g, 0.058 mol) is added in portions (internal temperature is 0 to 2 ¡ãC). The mixture is warmed to 25 ¡ãC and stirred at this temperature for 16 h. The mixture is concentrated under vacuum, poured into water (30 mL) and extracted with ethyl acetate (3 chi 50 mL). The combined organic portions are washed with saturated sodium bicarbonate solution (30 mL) and brine (30 mL). The organic portion is concentrated and the resulting residue is dissolved in a mixture of dichloromethane (30 mL) and water (30 mL). 6 N HC1 is added dropwise until a majority of the solid appears. The solid is collected by filtration. The aqueous phase of the filtrate is separated and combined with the solid cake, basified with sodium bicarbonate solution to pH 8, and then extracted with dichloromethane (3 chi 50 mL). The organic phase is concentrated to give the title compound (10.1 g, 74percent). LC-ES/MS m/z (79Br/81Br) 354/356 [M+H]+., 21655-48-1

As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

Reference£º
Patent; ELI LILLY AND COMPANY; GENIN, Michael James; HOLLOWAY, William Glen; REKHTER, Mark David; (41 pag.)WO2016/81311; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1228780-72-0, 1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Under nitrogen protection, Compound 20 (1.0 g, 3.13 mmol), Compound 1 (0.9 g, 3.13 mmol) and dipotassium hydrogen phosphate (1.10 g, 6.26 mmol) Add to a solution of dimethyl sulfoxide (DMSO, 25 ml), The reaction solution was reacted at 140 C for 12 h, and cooled to room temperature. The reaction was quenched with water (50 mL). Dry over anhydrous sodium sulfate, remove the solvent,The concentrate is subjected to column separation (eluent: petroleum ether/ethyl acetate (v/v) = 3:1), Obtained 1.4 g of a yellow oil, The yield was 76%.

1228780-72-0, As the paragraph descriping shows that 1228780-72-0 is playing an increasingly important role.

Reference£º
Patent; Shenzhen Tajirui Bio-pharmaceutical Co., Ltd.; Wang Yihan; Liu Zhiqiang; (35 pag.)CN108658983; (2018); A;,
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.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Example 49; l-{2-[(2R)-4-benzhydryl-2-methylpiperazin-l-yl]-2-oxoethyl}-3,3-diphenylpyrrolidin-2- one; Example 49A; (R)-l-benzhydryl-3-methylpiperazine; A solution of the dihydrochloride of i?-methylpiperazine (Tetrahedron Lett. 1994, 35, 16, 2533-2536)(0.42 g, 2.42 mmol) in N,JV-dimethylformamide (3 mL) was treated with bromodiphenylmethane (0.6 g, 2.42 mmol), potassium carbonate (1.17 g, 8.5 mmol), and a catalytic amount of potassium iodide. The resultant reaction mixture was then stirred at ambient temperature overnight. Then the reaction mixture was concentrated and partitioned between water/methylene chloride. The organic layer was dried over magnesium sulfate, concentrated and the residue was purified by preparative HPLC on a Waters Nova-Pak.(R). HR Cl 8 6um 6psiA Prep-Pak.(R). cartridge column (40mm x 100mm) using a gradient of 10percent to 100percent acetonitrile in 10 mM aqueous ammonium acetate over 12 minutes at a flow rate of 70 mL/min to provide the title compound., 75336-86-6

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

Reference£º
Patent; ABBOTT LABORATORIES; BHATIA, Pramila, A.; DOHERTY, George, A.; DRIZIN, Irene; MACK, Helmut; PERNER, Richard, J.; STEWART, Andrew, O.; ZHANG, Qing Wei; WO2010/39947; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics