Month: February 2021

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

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.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

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.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

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

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.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of tert-butyl 14-((6-(tert-butylsulfonyl)-4-((4,5-dimethyl-lH-pyrazol-3- yl)amino)quinazolin-7-yl)oxy)-3,6,9,12-tetraoxatetradecan-l-oate (200 mg, 0.300 mmol) in DCM (2 mL) was added hydrochloric acid (2.253 mL, 9.01 mmol) 4M in dioxane and the reaction was stirred at 20 C under an atmosphere of nitrogen for one hour. The volatiles were removed under vacuum, and to the resulting residue was added DCM (2 mL) and DMF (200ul), DIPEA (0.210 mL, 1.202 mmol), tert-butyl 2-methylpiperazine-l-carboxylate (0.085 mL, 0.360 mmol) and l-ethyl-3-(3- dimethylaminopropyl)carbodiimide (69.1 mg, 0.360 mmol). The reaction was stirred at room temperature under an atmosphere of nitrogen for 3 days. The reaction was diluted in 50 mL EtOAc, washed with 50 mL saturated sodium bicarbonate solution, 50 mL water, 50 mL 2 M HCI and 50 mL brine. The aqueous layer was neutralised with saturated sodium bicarbonate solution, and washed with 3 x 100 mL EtOAc. The organic layer was passed through a Biotage phase separator and concentrated under vacuum to afford the title compound (75 mg, 0.095 mmol, 32 % yield). LCMS RT= 0.83 min, ES+ve 792. (2R,5S)-Tert-butyl 5-((4-(14-((6-(tert-butylsulfonyl)-4-((3,4-dimethyl-lH-pyrazol-5- yl)amino)quinazolin-7-yl)oxy)-3,6,9,12-tetraoxatetradecan-l-oyl)-2-methylpiperazin-l-yl)methyl)- 4-(2-(6-(4-fluorobenzyl)-3,3-dimethyl-2,3-dihydro-lH-pyrrolo[3,2-b]pyridin-l-yl)-2-oxoethyl)-2- m thylpiperazine-l-carboxylate, 120737-78-2

As the paragraph descriping shows that 120737-78-2 is playing an increasingly important role.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; CASILLAS, Linda N.; HARLING, John David; MIAH, Afjal Hussain; SMITH, Ian Edward David; RACKHAM, Mark David; (204 pag.)WO2017/182418; (2017); 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.171504-98-6,Methyl 1,4-Bis(Boc)-2-piperazinecarboxylate,as a common compound, the synthetic route is as follows.

(B) 1,4-Di-(N-tert-Butoxycarbonyl)-2-Piperazinecarboxylic Acid A solution of 1 N sodium hydroxide (1.2 mL) was added to a solution methyl 1,4-di-(N-tert-butoxycarbonyl)-2-piperazinecarboxylate (A, 290 mg) in methanol (10 mL). The mixture was stirred at room temperature for 12 hr and evaporated in vacuo. The residue was diluted with water and washed with ether. The aqueous layer was acidified with 10% citric acid and extracted with ethyl acetate. The organic layer was washed with brine, dried over anhydrous sodium sulfate, and evaporated in vacuo to give the title compound (230 mg) as a colorless foam: 1H NMR (400 MHz, CDCl3) delta 1.44 (s,18H) and 4.56-4.75 (m, 1H)., 171504-98-6

The synthetic route of 171504-98-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Microcide Pharmaceuticals, Inc.; US6399629; (2002); B1;,
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.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: 1) (Cyanomethylene)tributylphosphorane (262 muL, 1.00 mmol) was added to a solution of (tetrahydrofuran-3-yl)methanol (51 mg, 0.50 mmol) and 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (97 mg, 0.5 mmol) in degassed 1,4-dioxane (2 mL) sealed in a microwave tube at rt under nitrogen. The solution was heated to 150¡ãC for 30 min in the microwave reactor and cooled to rt. 2) 1-Bromo-4-methoxybenzene (94 mg, 0.50 mmol), potassium carbonate (207 mg, 1.50 mmol) and [1,1?-Bis(diphenylphosphino)ferrocene]dichloropalladium(II) complex with CH2Cl2 (40.8 mg, 0.05 mmol) were added to the solution. The tube was sealed, evacuated and backfilled with nitrogen. Degassed water (1 mL) was added under nitrogen. The resulting mixture was stirred at 120¡ãC for 20 min. The reaction mixture was diluted with EtOAc (25 mL) and water (15 mL), the layers were separated, and the aqueous layer was extracted with EtOAc (15 mL). The combined organic layers were washed with saturated brine (15 mL). The organic layer was dried with MgSO4, filtered and evaporated to afford the crude product. The crude product was purified by preparative HPLC (Waters XSelect CSH C18 ODB column, 5mu silica, 30mm diameter, 100mm length), using decreasingly polar mixtures of water (containing 1percent by volume NH3OH (28-30percent in H2O)) and MeCN as eluents to afford 4-(4-methoxyphenyl)-1-((tetrahydrofuran-3-yl)methyl)-1H-pyrazole (89mg, 69percent) as a beige solid., 5464-12-0

Big data shows that 5464-12-0 is playing an increasingly important role.

Reference£º
Article; Mosallanejad, Arash; Lorthioir, Olivier; Tetrahedron Letters; vol. 59; 18; (2018); p. 1708 – 1710;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics