Tag: M.W:200-300

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 solution of 1-bromononane (1.81 g, 8.72 mmol) in MeCN (44 mL) was added 4-(2-aminoethyl)-l -boc-piperazine (2.0 g, 8.72 mmol), K2CO3 (2.4 g, 17.4 mmol), and KI (145 mg, 0.872 mmol). The reaction was allowed to stir at 65 ¡ãC for 16 hours. The reaction mixture was cooled to room temperature, filtered, and the solids were washed with hexanes. The filtrate was extracted with hexanes, and the combined extracts were concentrated in vacuo. Purification by ISCO silica flash chromatography (0-20percent MeOH/DCM) provided fert-butyl 4- (2-(nonylamino)ethyl)piperazine-l -carboxylate (775 mg, 25percent).UPLC/ELSD: RT = 0.47 min. MS (ES): m/z (MH+) 356.41 for C20H41N3O21H NMR (300 MHz, CDCl3) delta: ppm 3.44 (br. m, 4H); 2.74 (t, 2H); 2.63 (t, 2H); 2.53 (t, 2H); 2.41 (br. m, 4H); 1.48 (br. m, 9H); 1.30 (br. m, 14H); 0.90 (t, 3H).

192130-34-0, The synthetic route of 192130-34-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MODERNATX, INC.; BENENATO, Kerry E.; BUTCHER, William; (512 pag.)WO2018/232120; (2018); 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.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

To a solution of Int-14 (100 mg, 0.335 mmol) and 2-methoxy-4-(4-methylpiperazin-l-yl)aniline (82 mg, 0.369 mmol) in 2- methoxyethanol (2 mL) was added 4 M HC1 in dioxane (0.086 mL, 0.343 mmol). The solution was stirred and heated at 110 C for 14 h. Then, additional 2-methoxy-4-(4-methylpiperazin-l- yl)aniline (40 mg, 0.180 mmol) and 1 drop of 4 M HC1 (aq) were added and the mixture was further irradiated under microwave conditions for 15 minutes at 160 C. Work up in the same way as Ex-20 provided the title compound as a light brown foam (97 mg, 60%). HPLC: 99% [tR = 8.7 min, 45% MeOH, 55% water (with 0.1% TFA), 20 min. NMR (400 MHz, DMSO-ifc): delta 7.83 (d, J = 8.8 Hz, 1H), 7.82 (s, 1H), 7.42 (s, 1H, disappeared on D20 shake), 7.18 (ddd, J = 8.2, 7.4, 1.7 Hz, 1H), 7.14 (t, / = 6.3 Hz, 1H, reduced by 50% on D20 shake), 7.07 (dd, / = 7.4, 1.7 Hz, 1H), 6.94 (dd, / = 8.2, 0.9 Hz, 1H), 6.85 (td, / = 7.4, 0.9 Hz, 1H), 6.60 (d, / = 2.5 Hz, 1H), 6.34 (dd, / = 8.8, 2.5 Hz, 1H), 3.79 (s, 3H), 3.76 (s, 3H), 3.50 (q, / = 6.3 Hz, 2H), 3.10- 3.03 (m, 4H), 2.82 (t, / = 6.3 Hz, 2H), 2.47-2.41 (m, 4H), 2.21 (s, 3H). HPLC-MS (ESI+): m/z 483.3 [50%, (M35C1+H)+], 242.2 [100%, (M35C1+2H)2+]. LC-MS (ESI+): 483.2 [100%, (M35C1+H)+]. HRMS (ESI+): m/z calcd for C25H31CI2N6O2 (M+H)+ 483.2270, found 483.2272., 122833-04-9

122833-04-9 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline 20136253, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; H. LEE MOFFITT CANCER CENTER & RESEARCH INSTITUTE; MAHAJAN, Nupam P.; MAHAJAN, Kiran N.; LAWRENCE, Nicholas J.; LAWRENCE, Hirshani R.; (85 pag.)WO2017/23899; (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.21416-67-1,4,4′-(Propane-1,2-diyl)bis(piperazine-2,6-dione),as a common compound, the synthetic route is as follows.

21416-67-1, EXAMPLE 1 dl-1,2-Bis(4-morpholinomethyl-3,5-dioxopiperazin-1-yl)-propane A mixture of dl-1,2-bis(3,5-dioxopiperazin-1-yl)-propane (26.8 g, 0.1 mole), morpholine (27 ml, 0.3 mole) and absolute ethanol (100 ml) was heated to reflux. To the mixture, 37% aqueous formaldehyde solution (27 ml) was added gradually and then the reaction mixture was refluxed for further 15 minutes. The cooled mixture was filtered and the filtrate was allowed to stand in the refrigerator. Then resulting white crystals were collected and washed with ethyl acetate to give the titled compound (39.6 g; yield 84.9%). Melting Point: 163 to 165 C. (recrystallized from ethyl acetate). Elementary Analysis (%). Calculated for C21 H34 N6 O6: C 54.06; H 7.35; N 18.01. Found: C 54.28; H 7.58; N 18.05.

As the paragraph descriping shows that 21416-67-1 is playing an increasingly important role.

Reference£º
Patent; Zenyaki Kogyo Kabushiki Kaisha; US4737497; (1988); A;,
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

6-fluoro-2-methoxy-3-(oxiran-2-yl)benzonitrile (1.4 g, 7.3 mmol) and (S)-4-N-BOC-2-hydroxymethylpiperazine(3.13 g, 14.5 mmol) were suspended in ethanol (15 mL) then heated in a microwave apparatus for 60min at 150 C. The reaction mixture was cooled and evaporated to dryness. The residue was purified by chromatographythrough a 40g Redi-sep column and eluting with 5%MeOH/95% EtOAc to yield the title compound: LCMS:M+1 = 410;, 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; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; (128 pag.)EP2744499; (2016); 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.120737-59-9,tert-Butyl 3-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of tert-butyl (S)-3-methylpiperazine-1-carboxylate (50 g, 250 mmol, leq) in DCM: AcOH (10: 3, 500 mL) was added 37percent HCHO (40.5 mL, 500 mmol, 2 eq) at 0¡ãC and the resulting reaction mixture was stirred at room temperature for 3h. NaCNBH3 (31.5 g, 500 mmol, 2 eq) was added portion wise at 0¡ãC and the resulting reaction mixture was stirred at room temperature for 2h. The progress of reaction was monitored with TLC, which indicated formation of nonpolar spot. The reaction mixture was basified with sat. aq, NaHCC solution and extracted with DCM (2 x 150 mL). The combined organic layer was washed with water, followed by brine solution and dried over Na2S04 then concentrated under reduced pressure to afford tert-butyl (S)-3,4-dimethylpiperazine-1-carboxylate (55g, crude) as colorless liquid. TLC system: MeOH : DCM (1 : 9); Rf.: 0.4.

120737-59-9, As the paragraph descriping shows that 120737-59-9 is playing an increasingly important role.

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

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Piperazine-1,2-dicarboxylic acid, 1-tert-butyl ester, 2-methyl ester (250 mg, 1.03 mmol) was added dropwise to a stirred suspension of 4-bromobenzyl bromide (283 mg, 1.14 mmol) and cesium carbonate (1.0 g, 3.09 mmol) in anhydrous DMF (10 mL) at room temperature. The reaction mixture was stirred at 40 C. for 3 hrs (TLC control) and then poured into water (25 mL) and extracted with diethyl ether (3¡Á25 mL). The combined extract was washed with water (2¡Á10 mL), brine (3¡Á10 mL), dried over anhydrous MgSO4, filtered and concentrated in vacuo. Purification of the product by flash column chromatography, using 40% ethyl acetate/hexane as eluent, afforded the title compound as a white foam (270 mg, 64%)

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; The Institutes for Pharmaceutical Discovery, LLC; US2006/122222; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

122323-88-0, Methyl piperazine-2-carboxylate dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Methyl 2-piperazine carboxylate dihydrochloride (20 g, 87 mmol) was suspended in tetrahydrofuran (300 mL), diisopropylethylamine (22 g, 0.17 mmol) was added thereto, and the mixture was stirred at room temperature for 1 hour. Next, a 2.0 M solution of phenylmagnesium bromide in tetrahydrofuran (260 mL, 0.52 mol) was added dropwise over 30 minutes, and the mixture was stirred at room temperature for 14 hours. The reaction solution was ice cooled, water (400 mL) was then added dropwise thereto, and the mixture was stirred for 30 minutes with ice cooling. Di-tert-butyl dicarbonate (13 g, 61 mmol) was added dropwise thereto, and the mixture was stirred at room temperature for 30 minutes. To the reaction solution was added an aqueous saturated ammonium chloride solution, and the resulting mixture was extracted with ethyl acetate. The extract was washed with water, and then concentrated under reduced pressure. The residue was purified with silica gel column chromatography (hexane: ethyl acetate = 3: 1) to obtain the title compound (9.7 g, yield 30%).

122323-88-0, The synthetic route of 122323-88-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Takeda Pharmaceutical Company Limited; EP1661898; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

639068-43-2, tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,639068-43-2

A solution of compounds of general structure 1 (1 equiv), Boc protected amine (1-3 equiv) and DIPEA (3 equiv) in DMSO were reacted at 100-110 ¡ãC. The reaction mixture was cooled to room temperature and quenched by addition of water and crude residue extracted with EtOAc. Combined organic layers were washed with brine, dried over Na2S04, filtered and concentrated under reduced pressure to provide crude compound of general strucutre 2, which was used in the following step without further purification. To a solution of compounds of general structure 2 in CH2C12 was added HCl/dioxane (4 N) or TFA. The reaction was stirred at room temperature for 2 hrs and mixture was concentrated under reduced pressure. The residue was purified by reverse phase preparative HPLC to afford final compounds of general structure 3.

The synthetic route of 639068-43-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; KADMON CORPORATION, LLC; SKUCAS, Eduardas; LIU, Kevin, G.; KIM, Ji-In; POYUROVSKY, Masha, V.; MO, Rigen; (345 pag.)WO2019/45824; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

438631-77-7, (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To degassed solution of 68 1,4-dioxane (71.6 mL) and 56 DIPEA (5.65 mL, 32.46 mmol) at rt was added 505 7-bromo-4-chloro-6,8-difluoro-3-nitroquinoline (3.5 g, 10.82 mmol) followed by 272 1-tert-butyl 3-methyl (3R)-piperazine-1,3-dicarboxylate (3.96 g, 16.23 mmol). The reaction was heated at 100 C. for 16 h. The reaction was cooled to rt and the solvent removed in vacuo. The resulting residue was diluted with EtOAc (300 mL), washed with water (2¡Á250 mL) and brine (100 mL). The organic layer was dried (phase separator) and concentrated in vacuo to afford crude material which was purified by flash silica chromatography (0 to 50% 57 EtOAc in 58 heptane) to give 507 1-tert-butyl 3-methyl (3R)-4-(7-bromo-6,8-difluoro-3-nitroquinolin-4-yl)piperazine-1,3-dicarboxylate (3.89 g, 68%) as an orange dry film; 1H NMR (400 MHz, DMSO, 30 C.) 1.45 (9H, s), 3.18-3.29 (2H, m), 3.54 (3H, s), 3.57-3.66 (1H, m), 3.72-3.95 (2H, m), 4.05 (1H, s), 4.33 (1H, s), 8.06 (1H, dd), 9.13 (1H, s); m/z: ES+ [M+H]+ 530.9.

438631-77-7, 438631-77-7 (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 6558432, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; Kettle, Jason Grant; Bagal, Sharanjeet; Robb, Graeme Richard; Smith, James Michael; Goldberg, Frederick Woolf; Cassar, Doyle Joseph; Feron, James Lyman; US2019/177338; (2019); 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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

70261-81-3, EXAMPLE 3 4-((4-methyl-1-piperazinyl)methyl)aniline (I-c) Crude I-a (8.5g, 36.2mmol), FeO(OH)/C, 2.0 g as catalyst and 95% ethanol (100 ml) were added into a 500 mL single neck flask, which was refluxed. Into the reaction system were added slowly and dropwise a mixture of 25 mL hydrazine hydrate and 20 mL 95% ethanol. The depletion of the starting materials was confirmed by TLC (methanol: chloroform = 1:15). Suction filtration was performed while the reaction mixture was hot. The filter cake was washed with hot ethanol twice (30 ml *2). After removal of the solvent under reduced pressure, white solid was obtained, which was dried under vacuum to give 6.7 g (I-c); Yield: 90.3%. The product was used for subsequent reaction without further purification. 1H-NMR[300MHz, DMSO-d6]: delta2.1 (3H, s, -CH3), 2.3-2.5 (8H, m, -CH2-*4), 3.5 (2H, s, -CH2-), 4.0(2H, s, -NH2), 7.5 (2H, d, J = 8.7 Hz, ArH), 8.1 (2H, d, J = 8.7 Hz, ArH).

As the paragraph descriping shows that 70261-81-3 is playing an increasingly important role.

Reference£º
Patent; China Pharmaceutical University; LU, Tao; WANG, Yue; CHEN, Yadong; LU, Yi; WANG, Zhanwei; JIN, Qiaomei; YANG, Taotao; LIN, Guowu; GUO, Qinglong; ZHAO, Li; EP2955185; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics