Month: April 2021

128102-16-9, (R)-4-Benzyl 1-Boc-2-methylpiperazine-4-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 1 15Btert-Butyl 2-methylpiperazine- 1 -carboxylate[00728] A solution of 4-benzyl 1-tert-butyl 2-methylpiperazine- 1,4-dicarboxylate (4.8 g, 14.4 mmol) in methanol (25 mL) was added 480 mg of 10% Pd/C and stirred at room temperature under hydrogen overnight. Filtered and concentrated to give the title product (2.8 g, yield 97%) as colorless oil. ^-NMR (400 MHz, CDC13) delta (ppm): 1.21 (d, J= 6.8 Hz, 3H), 1.46 (s, 9H), 2.64-2.70 (m, 1H), 2.74- 2.78 (m, 1H), 2.88-3.01 (m, 3H), 3.78 (d, J= 12.4 Hz, 1H), 4.16 (m, 1H); LC-MS (ESI) m/z: 201 (M+l)+., 128102-16-9

Big data shows that 128102-16-9 is playing an increasingly important role.

Reference£º
Patent; BIOMARIN PHARMACEUTICAL INC.; WANG, Bing; CHU, Daniel; WO2011/130661; (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.21091-98-5,(4-Methylpiperazin-1-yl)(4-nitrophenyl)methanone,as a common compound, the synthetic route is as follows.

Step 2: (4-Amino-phenyl)-(4-methy -piperazine-l-yl)-methanoneTo a solution of (4-Methyl-piperazin-l-yl)-(4-nitro-phenyl)-methanone (14 g, 0.05623 mol) in MeOH (100 mL) was added Pd/C 10% (1.4 g) in portions and the Parr reaction vessel was purged with nitrogen for 10 min. reaction vessel was fixed in Pan- shaker at 60 psi pressure for 3 h. The reaction mixture was filtered through the Celite pad and the filtrate was concentrated under reduced pressure to afford the title compound [11 g, 89%]; LC-MS (ESI): Calculated mass 219.1; Observed mass: 220.1 [M+H]+ (RT: 0.16 min).

21091-98-5, 21091-98-5 (4-Methylpiperazin-1-yl)(4-nitrophenyl)methanone 716396, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ENDO PHARMACEUTICALS INC.; SMITH, Roger, Astbury; THOMPSON, Scott, Kevin; HOSAHALLI, Subramanya; BEJUGAM, Mallesham; NANDURI, Srinivas; PANIGRAHI, Sunil, Kumar; MAHALINGAM, Natarajan; WO2012/58671; (2012); 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.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Intermediate 14 was dissolved in DMF (20 mL). DIPEA (1.021 mL, 5.85 mmol) was added, followed by HOBT (395 mg, 2.92 mmol), EDC (561 mg, 2.92 mmol) and tert-butyl 3,3-dimethylpiperazine-1-carboxylate (587 mg, 2.34 mmol). The reaction mixture was stirred at rt overnight, concentrated under reduced pressure, redissolved in DCM, washed with 1M HCl and sat NaHCO3, dried over MgSO4, filtered and concentrated under reduced pressure. The crude material was purified on preparative HPLC UV using the long high pH shallow gradient method (Mobile phase: 30-50% B; A: H2O with 10 mM NH4CO3 and 0.375% NH4OH v/v, B: CH3CN, 30 min run) on XBridge Prep C18 OBD, 50¡Á250 mm, 10 mum, Waters reverse phase column, giving 412 mg title compound (52.6%) as a solid. 1H NMR (400 MHz, CDCl3) delta ppm 1.22-1.35 (m, 1H) 1.38-1.55 (m, 9H) 1.71 (br. s., 1H) 1.94 (br. s., 1H) 2.47 (br. s., 1H) 2.88 (s, 3H) 2.96 (s, 3H) 3.32-3.59 (m, 4H) 3.65-3.85 (m, 2H) 5.77 (br. s., 1H) 6.16 (br. s., 1H) 7.17 (d, J=8.20 Hz, 2H) 7.75 (d, J=8.20 Hz, 2H); MS m/z 402.21 [M+H]+ (ESI).

259808-67-8, The synthetic route of 259808-67-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; US2010/216812; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0319] Reference Z [0320] Synthesis of N-cyclopropyl-3-(3-methylpiperazin-l-yl)quinoxalin-2-amine dihydrochloride [0322] Step 1 : tert-butyl 4-(3-(cyclopropylamino)quinoxalin-2-yl)-2-methylpiperazine-l- carboxylate [0323] To a solution of 3-chloro-N-cyclopropylquinoxalin-2-amine (100 mg, 0.455 mmol) in dioxane (455 mu) was added tert-butyl 2-methylpiperazine-l -carboxylate (137 mg, 0.683 mmol) and iP^EfN (1 19 mu, 0.683 mmol). The mixture was heated at 130 C for 60 h. Purification by ISCO (0-60% EtOAc/Hexanes) yielded the title compound as a yellow oil.

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

Reference£º
Patent; ENVOY THERAPEUTICS, INC.; HITCHCOCK, Stephen; MONENSCHEIN, Holger; REICHARD, Holly; SUN, Huikai; KIKUCHI, Shota; MACKLIN, Todd; HOPKINS, Maria; WO2014/28479; (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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

To a stirred solution of 2- methyl piperazine (l0g, lOOmmol, leq) in ethanol (200mL) was added DIPEA (43.5mL, 250mmol, and the reaction mixture stirred for 10 min.. To this Boc anhydride (21.8mL, lOOmmol, leq) was added at 0C and the resulting reaction mixture was stirred at room temperature overnight. The progress of reaction was monitored by TLC, which indicated formation of nonpolar spot. The reaction mixture was concentrated and dissolved in DCM (200mL) then washed with water (2 x 80mL) followed by brine solution. The combined organic layer was dried over Na2SC>4 and concentrated under reduced pressure to afford crude tert-butyl (S)-3-methylpiperazine-1-carboxylate (20g, crude yield 100%) as a yellow liquid. TLC: MeOH : DCM (0.5: 9.5); R,= 0.3., 109-07-9

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ONTARIO INSTITUTE FOR CANCER RESEARCH (OICR); AL-AWAR, Rima; ZEPEDA-VELAZQUEZ, Carlos Armando; PODA, Gennady; ISAAC, Methvin; UEHLING, David; WILSON, Brian; JOSEPH, Babu; LIU, Yong; SUBRAMANIAN, Pandiaraju; MAMAI, Ahmed; PRAKESCH, Michael; STILLE, Julia Kathleen; (1053 pag.)WO2017/147700; (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.129722-25-4,7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one,as a common compound, the synthetic route is as follows.

A mixture of compound 75 (1.2 g) in 4M HCl/dioxane (100 mL) was stirred at RT for 2 h. The solvent was removed under reduced pressure and the residue was dried under vacuum at 50 0C to afford the HCl salt of compound 75 (1.2 g) as a light-yellow solid. 1H-NMR (300 MHz, DMSO-de): delta 1.82-1.92 (m, 4H), 3.12-3.26 (m, 6H)3 3.45 (d, J = 9.4 Hz52H), 3.62 (d, J = 8.5 Hz, 2H), 4.07 (t, J = 5.5 Hz, 2H), 6.32 (d, J = 9.4 Hz, IH), 6.82 (dd, J1 = 4.5 Hz, J2 = 2.4 Hz, 2H), 7.22 (dd, J1 = 6.7 Hz, J2= 2.6 Hz, IH), 7.34-7.41 (m, 2H), 7.58 (d, J = 9.6 Hz, IH), 7.83 (d, J = 9.6 Hz, IH), 10.52 (bs, IH), 11.69 (bs, IH). 13C-NMR (75 MHz, DMSO-de): delta 20.84, 26.46, 48.44, 51.81, 55.84, 67.65, 99.33, 111.47, 114.09, 119.22, 120.53, 126.01, 126.72, 129.37, 129.99, 133.42, 140.76, 141.30, 150.18, 160.94, 162.94. HPLC (method: 20 mm C 18-RP column; mobile phase: 2-95% ACN + 0.1% formic acid in 3.3 min with 1.7 min hold at 95% ACN, Wavelength: 254 ran): retention time: 2.74 min. MS (M + H+): 446.1., 129722-25-4

129722-25-4 7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one 10114519, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CONCERT PHARMACEUTICALS INC.; WO2008/24481; (2008); A2;,
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,59702-07-7

General procedure: The following exemplary compounds were prepared analogously to Example 127.1 from Example 129A and the appropriate commercially available amines. In many cases, under the reaction conditions, mixtures of mono- and di-aminated products were obtained, and were separated by chromatography. Under argon, 1.30 g (3.01 mmol) of (4S)-1-(4-bromophenyl)-7,8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide (Example 49.2A) were initially charged in 65 ml of degassed toluene. 0.37 ml (331 mg, 3.31 mmol) of 1-methylpiperazine, 405 mg (4.21 mmol) of sodium tert-butoxide and 118 mg (0.15 mmol) of chloro-(2-dicyclohexylphosphino-2,4,6-triisopropyl-1,1-biphenyl) [2-(2-amino-1,1-biphenyl)]palladium(II) (CAS [1310584-14-5]) were added. The mixture was degassed again, saturated with argon and then stirred at 80¡ã C. for 12 hours. After cooling, the mixture was added to sat. sodium bicarbonate solution and extracted with ethyl acetate. The combined organic phases were washed with sat. sodium chloride solution and dried with sodium sulphate. The solvents were removed on a rotary evaporator and the residue (1.5 g orange foam) was purified by flash chromatography (SiO2, dichloromethane/methanol 0-3-10percent). This gave 850 mg (63percent of theory) of the desired product as a yellow solid.

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

Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; SIEGEL, STEPHAN; BAURLE, STEFAN; CLEVE, ARWED; HAENDLER, BERNARD; FERNANDEZ-MONTALVAN, AMAURY ERNESTO; MONNING, URSULA; KRAUSE, SABINE; LEJEUNE, PASCALE; SCHMEES, NORBERT; BUSEMANN, MATTHIAS; HOLTON, SIMON; KUHNKE, JOACHIM; (434 pag.)JP2015/529192; (2015); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,694499-26-8

A mixture of 3-iodo-4-difluoromethyl-nicotinic acid (860 mg, 2.88 mmol)was dissolved in N, N- dimethylformamide (5 mL), was added N, N- diisopropylethylamine(668 L , 4.04 mmol) was added and 2- (7-BTA) -Nu, Nu, Nu ‘, Nu’- tetramethyluroniumhexafluorophosphate (1.2 g, 3.2 mmol), stirred for 5 min 3-trifluoromethyl-4-(4-methyl-piperazin-1-ylmethyl) aniline (737 mg, 2.69 mmol), the reactionmixture was stirred at room temperature 26 h. After completion of thereaction system was added water, extracted with ethyl acetate twice. Thecombined organic layer was purified by column chromatography to give N- (4- (4-methyl-piperazin-1-ylmethyl) -3-trifluoromethylphenyl)-3-iodo-4-difluoromethyl-smoke amide (white solid, 1.5 g).

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Shanghai Pharmaceuticals Holding Co.,Ltd .; WAN, HUIXIN; LI, CHUNLI; SHI, Chen; Liu, Haiyan; Li, Ping; XIA, Guangxin; HAN, Yanan; (52 pag.)CN103420977; (2016); B;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

30 mL DMSO was stirred in room temperature and was added A1Sa (3.0 g, 18.8 mmol), compound A1Sb (3.0 g, 13.8 mmol, 100% ee) and KOH (2.4 g, 42.8 mmol) in turn. The reaction mixture was heated to 30 C. and stirred for 3 hours. The reaction was cooled to room temperature when it was finished, and was added 300 mL water, then the solid was precipitated from the solution, the mixture was stirred overnight at room temperature, and was filtrated. The filtrate were added to mixed solution (petroleum ether/EAOAc=5:1, 25 mL), and stirred for half hour at room temperature, and filtrated to afford yellow solid compound A1Sc (3.0 g, yield 64%). MS 336.2 [M+H]+., 314741-40-7

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Hangzhou Innogate Pharma Co., Ltd.; ZHANG, Hancheng; LIU, Shifeng; YE, Xiangyang; (92 pag.)US2019/308993; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

Step H: tert-butyl(3S)-3-(hydroxymethyl?j-4-[2-hydroxy-2-(6-methyl- 1-oxo- 1 ,3-dihydro-2- benzofuran-5-yl)ethyll piperazine- 1 -carboxylate: A mixture of 6-methyl-5- (oxiran-2-yl)-2- benzofuran-1(311)-one (750 mg, 3.95 mmol) and tert-butyl (3S)-3-(hydroxymethyl)piperazine-1- carboxylate (1.02 g, 4.74 mmol) in EtOH (5 mL) was reacted under microwave condition (140C) for 90 mm. After cooling to r.t., the mixture was concentrated to dryness. The residue was purified by prep-TLC to give title compound., 314741-40-7

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DEJESUS, Reynalda, Keh; FRIE, Jessica, L.; PIO, Barbara; TANG, Haifeng; WALSH, Shawn, P.; WO2014/99633; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics