Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,57260-71-6

INTERMEDIATE: Tert-butyl-4-r5-bromo-7H-pyrrolor2,3-dlpyrimidin-4- yPpiperazine- 1 -carboxylate.ChemicalF ormula C-IsH2OBrN5O2 Exact Mass 381 08 1H-NMR (CDC13/4OO MHz): 8.40 (s, IH), 7.26 (d, J= 1.7 Hz, IH), 3.66(s, 8H), 1.49 (s, 9H). MS (ES+, m/z): 384.1 (M++3, 40.0), 382.2 (M++l, 38.0).

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SUPERGEN, INC.; WO2008/128072; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

57260-71-6, General procedure: 1-Boc-piperazine (150 mg, 0.81 mmoles) was dissolved in anhydrous DMF (2 mL) and, under stirring, DIPEA (303 mL, 1.78 mmoles), PyBOP (461 mg, 0.89 mmoles) and 2-thiophenecarboxylic acid (114 mg, 0.89 mmoles) were added at room temperature. After complete conversion of 1-Boc-piperazine monitored by TLC analysis, the solution was diluted with DCM and washed with NaOH 0.5M, brine, HCl 0.1M and brine. Organic phase was dried over Na2SO4, filtered and concentrated under reduced pressure. The crude product was purified by chromatographic column (eluent DCM/MeOH = 96/4) to obtain 10e (188 mg, 79% yield).

As the paragraph descriping shows that 57260-71-6 is playing an increasingly important role.

Reference：
Article; Giannini, Giuseppe; Battistuzzi, Gianfranco; Vesci, Loredana; Milazzo, Ferdinando M.; De Paolis, Francesca; Barbarino, Marcella; Guglielmi, Mario Berardino; Carollo, Valeria; Gallo, Grazia; Artali, Roberto; Dallavalle, Sabrina; Bioorganic and Medicinal Chemistry Letters; vol. 24; 2; (2014); p. 462 – 466;,
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.57184-25-5,1-(Cyclopropylmethyl)piperazine,as a common compound, the synthetic route is as follows.

57184-25-5, To a solution of 4-(dibenzylamino)cyclohexan-1-one (273, 5 g, 17.0 mmol) and 1- (cyclopropylmethyl)piperazine (276, 2.4 g, 17.1 mmol) in DCM (30 mL) was added HOAc (1 mL). NaHB(OAc)3 (20 g, 94.4 mmol) was then added in portions. After stirring at room temperature for 48 h, the reaction mixture was neutralized with saturated sodium bicarbonatesolution and extracted with DCM (50 mL x 3). The combined organic phases were dried over Mg504 and concentrated in vacuo. The resulting residue was purified by column chromatography to afford (1 r,4r)-N,N-dibenzyl-4-(4-(cyclopropylmethyl)piperazin- 1- yl)cyclohexan-1-amine (277, 670 mg, 1.6 mmol) and (ls,4s)-N,N-dibenzyl-4-(4- (cyclopropylmethyl)piperazin- 1 -yl)cyclohexan- 1-amine (278, 1.2 g, 2.9 mmol).(1R,4R)-N,N-Dibenzyl-4-(4-(cyclopropylmethyl)piperazin- 1-yl)cyclohexan- 1-amine(277): ?H NMR (300 MHz, CDC13): 37.29-7.26 (m, 4H), 7.24-7.18 (m, 4H), 7.15 -7.10 (m,2H), 3.53 (s, 4H), 2.81- 2.60 (m, 6H), 2.44 – 2.36 (m, 2H), 2.29 (d, J= 6.6 Hz, 2H), 1.96 – 1.88(m, 4H), 1.58 – 1.29 (m, 4H), 1.21 – 1.10 (m, 2H), 0.88 – 0.77 (m, 1H), 0.50 – 0.42 (m, 2H),0.10-0.02 (m, 2H).(1S,4S)-N,N-Dibenzyl-4-(4-(cyclopropylmethyl)piperazin- 1-yl)cyclohexan- 1-amine(278): ?H NMR (300 MHz, CDC13): oe 7.29-7.27 (m, 4H), 7.23 -7.18 (m, 4H), 7.14-7.09 (m,2H), 3.57 (s, 4H), 2.96 – 2.49 (m, 8H), 2.40 (d, J= 6.6 Hz, 2H), 2.20 (s, 1H), 1.89 – 1.85 (m,2H), 1.77 – 1.66 (m, 2H), 1.48 – 1.44 (m, 2H), 1.26 – 1.17 (m, 3H), 1.00 – 0.82 (m, 1H), 0.55 -0.49 (m, 2H), 0.16-0.11 (m, 2H).

57184-25-5 1-(Cyclopropylmethyl)piperazine 965875, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; G1 THERAPEUTICS, INC.; STRUM, Jay, Copeland; JUNG, David; (250 pag.)WO2018/5860; (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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

5625-67-2, Piperazine-2-one (1.0 g, 10 mmol) was suspended in 10 mL DCM and Boc2O was slowly added.After the addition was completed, the reaction was allowed to stand at room temperature overnight.After completion of the reaction, it was washed three times with 0.1 N diluted hydrochloric acid, 20 ml each time, and washed three times with saturated potassium carbonate, 20 ml each time.Finally, anhydrous sodium sulfate was added and the solution was removed in vacuo to give a white solid.

As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

Reference：
Patent; Shaoxing University; Hu Chunqi; Li Xin; Shi Yaru; Du Wenting; Tong Jie; Su Wanting; Xia Weiqi; (21 pag.)CN108610333; (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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

General procedure: 6.1.15. General procedure IV, for preparation of 14a-f A mixture of aryl bromide (1.0 mmol), 4-methylpiperazin-2-one (for compounds 15-17)/morpholin-3-one (for compounds 18-20) (2.0 mmol), N,N0-dimethylethylene diamine (0.1 mmol), K2CO3 (2.0 mmol) and CuI (0.05 mmol) in anhydrous toluene was heated to reflux with stirring for 6 h. Then the reaction mixture was cooled to room temperature, poured into water, stirred vigorously and extracted thrice with ethyl acetate, dried over anhydrous Na2SO4, concentrated under reduced pressure and purified by flash chromatography to afford compounds 14a-f in 54-68% yields. 6.1.17 4-Methyl-1-(5-vinylpyridin-2-yl)piperazin-2-one (14b) A mixture of 2-bromo-5-vinylpyridine 3b (0.15 g, 0.81 mmol), 4-methylpiperazin-2-one (0.18 g, 1.63 mmol), N,N’-dimethylethylene diamine (0.007 g, 0.08 mmol), K2CO3 (0.22 g, 1.63 mmol) and CuI (0.007 g, 0.04 mmol) in anhydrous toluene was heated to reflux and the reaction was continued as described in general procedure IV to afford 14b (0.11 g) in 62.8% yield. 1H NMR (400 MHz, CDCl3): delta 8.40 (d, J = 2.3 Hz, 1H), 8.12 (dd, J = 8.6, 1.0 Hz, 1H), 7.80 (dd, J = 8.7, 2.4 Hz, 1H), 6.72 (dd, J = 17.7, 11.0 Hz, 1H), 5.81 (dd, J = 17.7, 0.7 Hz, 1H), 5.38 (dd, J = 11.0, 0.8 Hz, 1H), 3.66-3.76 (m, 2H), 3.28 (s, 2H), 2.76-2.82 (m, 2H), 2.41 (s, 3H); LC-MS: 218 (M++1).

34770-60-0, The synthetic route of 34770-60-0 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Rakesh; Bruhn, David; Maddox, Marcus; Lee, Robin B.; Yang, Lei; Lee, Richard E.; Madhura, Dora B.; Trivedi, Ashit; Meibohm, Bernd; Scherman, Michael S.; Gilliland, Janet C.; Gruppo, Veronica; McNeil, Michael R.; Lenaerts, Anne J.; Bioorganic and medicinal chemistry; vol. 20; 20; (2012); p. 6063 – 6072,10;,
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.34334-28-6,4-(4-Methylpiperazin-1-yl)benzonitrile,as a common compound, the synthetic route is as follows.

To a solution of 13 (1eq.) and CoCl2 6H20(2.1 eq.), NaBH4 (10 eq.) was added. The reaction mixture wasstirred for 5h and then filtered on a celite pad. The organic phase wasevaporated under reduced pressure. The yellow oil was purified by flashchromatography on silica gel (CH2Cl2:MeOH 8:2). Thedesired compound was obtained as a white solid (50%). 1H NMR (400MHz, MeOD): delta(ppm) 2.42(s, 3H); 2.74(t, J=8, 4H); 3.17(t, J=8, 4H), 4.43(s,2H); 6.89(d, J=8, 2H); 7.18(d, J=8, 2H). Anal. Calcd. for C12H19N3:C, 70.20; H, 9.33; N, 20.47; found; C, 70.10; H, 9.13; N, 20.27, 34334-28-6

34334-28-6 4-(4-Methylpiperazin-1-yl)benzonitrile 763205, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Radi, Marco; Bernardo, Vincenzo; Vignaroli, Giulia; Brai, Annalaura; Biava, Mariangela; Schenone, Silvia; Botta, Maurizio; Tetrahedron Letters; vol. 54; 38; (2013); p. 5204 – 5206;,
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

A vial was charged with (S)-tert-butyl 3 -(hydroxymethyl)piperazine-l -carboxylate (367.3 mg, 1.647 mmol) and 2-(tert-butoxymethyl)oxirane (243.3 mg, 1.850 mmol) in ethanol (3 mL). The mixture was heated at 120 C for 30 min using microwave. The mixture was cooled to room temperature, concentrated to remove all of solvents. The residue was purified with flash column chromatography on silica gel using 1-10% methanol in dichloromethane to afford the final product as colorless oil (497.5 mg) in 87% yield. NMR (500 MHz, Chloroforn /) delta 3.86 – 3.80 (m, 2H), 3.71 – 3.68 (m, lH), 3.53 – 3.41 (m, 2H), 3.40 – 3.35 (m, 2H), 3.24 (dd, J = 9.1, 6.6 Hz, 1H), 3.10 (br, 1H), 2.91 (m, 1H), 2.83 – 2.75 (m, 1H), 2.48 (dd, J = 13.1, 7.6 Hz, 2H), 2.39 – 2.30 (m, 1H), 1.44 (s, 9H), 1.18, 1.17 (2s, 9 H). MS for C17H34N2O5: 347.2 (MH+)., 314741-40-7

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

Reference：
Patent; NEKTAR THERAPEUTICS (INDIA) PVT. LTD.; NEKTAR THERAPEUTICS; SHARMA, PANKAJ; KHATRI, VIJAY KUMAR; GU, XUYUAN; SONG, YUAN; SHEN, MICHAEL LIXIN; SAUTHIER, JENNIFER RIGGS; ANAND, NEEL K.; KOZLOWSKI, ANTONI; ODINECS, ALEKSANDRS; RILEY, TIMOTHY A.; REN, ZHONGXU; MU. YONGQI; SHEN, XIAOMING; YUAN. XUEJUN; AURRECOECHEA, NATALIA; O’MAHONY, DONOGH JOHN ROGER; WO2015/92819; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

304897-49-2, tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

d: Ethyl 4-(4-((4-(tert-butoxycarbonyl)piperazin- 1 -yl)methyl)phenylamino)-2-chloro- 6-methylpyrimidine-5-carboxylate Ethyl 2,4-dichloro-6-methylpyrimidine-5-carboxylate (0.5 g, 2.1 mmol) and tert-butyl 4-(4-aminobenzyl)piperazine-l-carboxylate (0.6 g, 2.06 mmol) were dissolved in NMP and stirred at 0C for 2 hour. The reaction mixture was poured onto water and extracted with EtOAc. The organic layer was washed with water, dried over a2S04 and evaporated under vacuum to get the desired compound (0.62 g). XH NMR (400 MHz, CDC13): delta 10.58 (s, 1H), 7.58 (d, J = 6.4 Hz, 2H), 7.31 (d, J = 6.4 Hz, 2H), 4.45 (q, J = 6.8 Hz, 2H), 3.56 (s, 2H), 3.41 (m, 4H), 2.69 (s, 3H), 2.47 (m, 4H), 1.45 (s, 9H), 1.43 (t, J = 6.8 Hz, 3H); MS m/z 490.0 (M+l).

304897-49-2, As the paragraph descriping shows that 304897-49-2 is playing an increasingly important role.

Reference：
Patent; ENDO PHARMACEUTICALS INC.; VENKATESAN, Aranapakam; SMITH, Roger, Astbury; HOSAHALLI, Subramanya; POTLURI, Vijay; PANIGRAHI, Sunil, Kumar; BASETTI, Vishnu; KUNTU, Karunasree; WO2013/28818; (2013); 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.262368-30-9,N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide,as a common compound, the synthetic route is as follows.

Preparation of the Final Compounds: (cr) 3-Z-[1-(4-(N-(4-methyl-piperazin-1-yl-methylcarbonyl)-N-methyl-amino)-anilino)-methylene]-6-ethylcarbamoyl-2-indolinone 160 mg 3-(1-hydroxy-methylene)-6-ethylcarbamoyl-2-indolinone (starting material VIII) and 543 mg N-[(4-methyl-piperazin-1-yl)-methylcarbonyl]-N-methyl-p-phenylendiamine are dissolved in 3 ml of tetrahydrofuran, 506 ml trimethylsilylimidazole are added and the mixture is stirred for 25 minutes at 170 C. in a microwave oven. After cooling the solvent is evaporated and the residue is purified over an aluminum oxide column (activity 2-3) with methylene chloride/ethanol (19:1) as eluant. The residue is recrystallized from ether and vacuum-dried at 80 C. Yield: 0.17 g (52% of theory), Rf value: 0.60 (aluminum oxide, methylene chloride/methanol=9:1) Melting point: 255-260 C. C26H32N6O3 Mass spectrum: m/z=477 [m+H]+, 262368-30-9

As the paragraph descriping shows that 262368-30-9 is playing an increasingly important role.

Reference：
Patent; Boehringer Ingelheim International GmbH; US2006/142373; (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.25057-77-6,1,2-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

5-Chloro-N-[5-[(3,5-dimethoxyphenyl)methoxy]-2H-pyrazol-3-yl]pyrazine-2-carboxamide (390 mg, 1.00 mmol) was added in one portion to 1,2-dimethyl-piperazine (228 mg, 2.00 mmol) in anhydrous dimethylsulfoxide (2.00 ml) at 25 C. The resulting solution was stirred at ambient temperature for 2 h. The residue was purified by ion exchange chromatography, using an SCX column. The desired product was eluted from the column using 7M NH3/MeOH to afford impure material. The concentrated eluent was purified by silica column chromatography, eluting with a gradient of 0 to 10% 7M NH3/MeOH in DCM. Pure fractions were evaporated to dryness to afford the title compound (392 mg, 84%) as a yellow solid. 1H NMR (399.902 MHz, DMSO) delta 1.08 (3H, d), 2.06-2.12 (1H, m), 2.18 (1H, td), 2.23 (3H, s), 2.77-2.88 (2H, m), 3.14-3.21 (1H, m), 3.75 (6H, s), 4.32 (2H, t), 5.08 (2H, s), 5.84 (1H, s), 6.44 (1H, t), 6.59 (2H, d), 8.34 (1H, s), 8.71 (1H, s), 10.79 (1H, s), 11.35 (1H, s). MS: m/z 468 (MH+). Mean of n=1, FGFR Kinase assay-Caliper Echo Dosing, IC50 0.0015 muM.

25057-77-6, As the paragraph descriping shows that 25057-77-6 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; US2008/153812; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics