Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.154590-35-9,tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1: Cool in ice a solution of the product of Preparation 13, Step 3 (1.53 g, 5.2 mmol) and DIPEA (1.10 ml, 6.2 mmol) in THF (40 ml). Add dropwise 4-bromobutyryl chloride (1.01 g, 5.4 mmol). Stir 2 h and partition with ether and satd. NaHCO3. Dry (MgSO4) and concentrate to obtain the carbamate as a yellow solid

154590-35-9, As the paragraph descriping shows that 154590-35-9 is playing an increasingly important role.

Reference£º
Patent; Schering Corporation; US2004/220194; (2004); A1;,
Piperazine – Wikipedia
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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.

4-chloro-3-(3-fluorophenyl)-1-[2-(4-methylpiperazin-1-yl)ethyl]-5-phenyl-pyrazolo[3,4-c]pyridazine (Compound 8) A mixture of 4-chloro-3-(3-fluorophenyl)-5-phenyl-1H-pyrazolo[3,4-c]pyridazine (0.33 mmol), 2-(4-methylpiperazin-1-yl)ethanol (0.65 mmol), diethyl azodicarboxylate (114 mg, 0.65 mmol) and triphenyl phosphine (171 mg, 0.65 mmol) in 1,4-dioxane (2 mL) was heated using microwave irradiation to a temperature between 85 and 120¡ã C. for a 30 to 90 min period. The reaction mixture was concentrated in vacuo and the residue was purified by preparative HPLC to provide Compound 8. 1H NMR delta (ppm)(CHCl3-d): 7.81-7.77 (2H, m), 7.57-7.44 (6H, m), 7.20-7.18 (1H, m), 4.95 (2H, t), 3.07 (2H, t), 2.65 (4H, bs), 2.35 (4H, bs), 2.25 (3H, s). LCMS (10 cm_Formic_ACE 3 C18 AR_HPLC_CH3CN) Rt 9.93 min; m/z 451 [M+H] 99.18percent purity., 5464-12-0

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Usher III Initiative; Buerli, Roland Werner; Krishna Esmieu, William Rameshchandra; Lock, Christopher James; Malagu, Karine Fabienne; Owens, Andrew Pate; Harte, William E.; US2014/121205; (2014); A1;,
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163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To 188 (15 mg, 0.039 mmol) in DMF (3 mL) was added (5)-l-N- Boc-2-methylpiperazine (9.4 mg, 0.047 mmol) and Et3N (10 mu, 0.072 mmol) and heated at 90 C for 2 h. Solvent was removed under reduced pressure and the residue was purified by preparatory TLC (CH2Cl2:MeOH, 10:1) to afford Boc-protected intermediate in quantitative yield. To this was added 1 mL of a solution of CH2Ci2:TFA (7:3) and stirred at rt for 4 h. Solvent was removed under reduced pressure and the residue was purified by preparatory TLC (CH2Cl2:MeOH-NH3 (7 N), 20: 1) to afford 17 mg (98%) of 191. 1H NMR (500 MHz, CDC13): delta 8.17 (s, 1H), 7.35 (d, J= 8.4 Hz, 2H), 7.10 (t, J= 7.8 Hz, 1H), 7.04 (d, J= 8.4 Hz, 2H), 6.72 (dd, J= 8.1, 1.7, 1H), 6.67 (d, J= 7.5 Hz, 1H), 6.60 (s, 1H), 5.29 (d, J= 12.7 Hz, 1H), 5.24 (d, J = 12.7 Hz, 1H), 4.76 (m, 1H), 4.42-4.47 (m, 1H), 3.65 (s, 3H), 3.00-3.12 (m, 2H), 2.84-2.94 (m, 2H), 2.67-2.73 (m, 1H), 1.22 (d, J= 6.8 Hz, 3H); MS (ESI) m/z [M+H]+ 448.3., 163765-44-4

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MEMORIAL SLOAN KETTERING CANCER CENTER; CHIOSIS, Gabriela; KANG, Yanlong; PATEL, Hardik J.; PATEL, Maulik; OCHIANA, Stefan; RODINA, Anna; TALDONE, Tony; SHRESTHA, Liza; (288 pag.)WO2015/175707; (2015); A1;,
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70261-81-3, 1-Methyl-4-(4-nitrobenzyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General Procedure 3-1 : Synthesis of (4-((4-methylpiperazin-l-yl)methyl)aniline)[00187] The synthesis of the title compound was conducted as described in U.S. Pat. Appl. Publ.No. 2006058341 (March 16, 2006). Specifically, to a solution of 4-nitrobenzyl chloride in THF at the room temperature was added 1 -methyl piperazine. The solution was stirred for 3 hours after which time the crude reaction was diluted with ethyl acetate and washed repeatedly with water. The dried organics were concentrated to give directly the 4-nitrobenzylamine adduct.This was subsequently treated with Rainey Nickel in THF at 75PSI for 12 hours to give the title compound., 70261-81-3

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

Reference£º
Patent; BIOGEN IDEC MA INC.; WO2008/94575; (2008); A2;,
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Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.325145-35-5,(S)-tert-Butyl 2-ethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Boc-2-S-ethyl piperazine 22 (prepared as per Kiley et al Org. Prep. Proc- Int. 1990, 22, 761 ; 4.2 g, 18.6 mmol), tris(dibenzylideneacetone)dipalladium (340 mg, 0.37 mmol), racemic-2,2′-bis(diphenylphosphino)-1 ,1′-binaphthyl (BINAP) (495 mtf, 0.74 mmol), cesium carbonate (12 g, 37.2 mmol) and toluene (80 ml). After the mixture was heated at 100 0C for 16 h, fresh tris(dibenzylideneacetone)- dipalladium (340 mg, 0.37 mmol) and BINAP (495 mg, 0.74 mmol) were added and the heating was continued for 3 days. The solvent was removed in vacuo, and the residue was suspended in a 100 ml portion of ethyl acetate. This mixture was extracted with water and brine. The separated organic layer was dried over sodium sulfate and concentrated in vacuo. Purification of the residue via silica gel flash chromatography (5percent methanol/ 95percent DCM) yielded 5.3 g of a partially purified material 23 which was used directly in the next step. M.S. M+H = 350

325145-35-5, As the paragraph descriping shows that 325145-35-5 is playing an increasingly important role.

Reference£º
Patent; SCHERING CORPORATION; PHARMACOPEIA, INC.; WO2007/109238; (2007); A1;,
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Piperazines – an overview | ScienceDirect Topics

59878-57-8,59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3-(4-oxo-3,4-dihydro-phthalazin- 1 -yl-oxyl)benzoic acid (54 mg, 0.3 mmol) was dissolved in N,N-dimethylformamide, and then 1-(3-dimethylaminopropyl)-3-ethylcar- bodiimide hydrochloride (EDCI) (220 mg, 1.2 mmol), triethylamine (150 pL, 1.2 mmol) and 1 -hydroxy-7-azaben- zotriazole (HOAt) (165 mg, 1.2 mmol) were added successively. The mixture was stirred at room temperature for half an hour, and then N-(cyclopropanecarbonyl) piperazine was added and reacted at room temperature overnight, and then the reaction was quenched with water, extracted with ethyl acetate, and washed with water for three times. The organic phases were combined and washed with saturated saline, dried with anhydrous sodium sulfate, and concentrated for colunm chromatography isolation (dichloromethane:methanol=20: 1) to give Compound 7. A white solid was obtained. ?H NMR (600 MHz, DMSO-d5): oe 11.98 (s, 1H), 8.27 (d, 1H, J=7.38 Hz), 8.10 (d, 1H, J=7.74 Hz), 7.99-8.01 (m, 1H), 7.94-7.96 (m, 1H), 7.52 (t, 1H, J=7.86 Hz), 7.39-7.38 (m, 2H), 7.28 (d, 1H, J=7.62 Hz), 3.33-3.81 (m, 8H), 1.96 (brs, 1H), 0.69-0.74 (m, 4H); ESI-MSm/z: calculated for4l8.16. found 417.89 [M-H].

As the paragraph descriping shows that 59878-57-8 is playing an increasingly important role.

Reference£º
Patent; CHENGDU DI’AO PHARMACEUTICAL GROUP CO., LTD.; Ji, Jianxin; Guo, Na; Xue, Ting; Kang, Bingqiang; Ye, Xinfa; Chen, Xin; Zhang, Tao; US2015/51211; (2015); 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.113028-17-4,Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate,as a common compound, the synthetic route is as follows.

EXAMPLE 5 Ethyl 7-(4-acetonyl-1-piperazinyl)-6-fluoro-1-methyl-4-oxo-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate Ethyl 6-fluoro-1-methyl-7-(1-piperazinyl)-4-oxo-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate (3.8 g) was suspended in 50 ml of N,N-dimethylformamide, 1.66 g of potassium carbonate was added thereto, 1.65 g of bromoacetone was dropped in with ice cooling and stirring, and the mixture was stirred at room temperature for 20 hours. The reaction solution was poured over into ice water and the crystals separated out were collected by filtration, washed with water, dried and recrystallized from ethanol to give 3.7 g of desired compound in colorless powdery crystals, m.p. 196-200 C. (decompn.). Elementary analysis calculated for C21 H24 FN3 O4 S: Calcd (%): C 58.18, H 5.58, N 9.69. Found (%): C 57.93, H 5.39, N 9.46., 113028-17-4

The synthetic route of 113028-17-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Nippon Shinyaku Co., Ltd.; US4843070; (1989); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

169447-70-5, To a solution of 2,6-difluorobenzonitrile (0.8g, 5.7 mmol) in DMF (10 mL) was added (S)-tert-butyl 2-methylpiperazine-l-carboxylate (1.14 g, 5.7 mmol) and K2CO3 (2.35g, 17. Immol). The solution was stirred for 17 hrs at 100C, then concentrated to give the crude. The crude was purified by chromatography (silica, EtOAc/PE = 1/10) to afford (S)-/er/-butyl-4-(2- cyano-3-fluorophenyl)-2-methylpiperazine-l-carboxylate (0.6 g, 1.88 mmol, 33%) as a white solid. MS (EI+, m/z): 320 [M+H]+.

As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; NAVITOR PHARMACEUTICALS, INC.; O’NEILL, David John; SAIAH, Eddine; KANG, Seong Woo Anthony; BREARLEY, Andrew; BENTLEY, Jonathan; (184 pag.)WO2018/89493; (2018); A1;,
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Piperazines – an overview | ScienceDirect Topics

215309-01-6, 3-(4-Methylpiperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a suspension of 3-(4-methylpiperazin-1-yl)benzoic acid (0.58 g, 2 mmol) in dichloromethane (50 mL) and DMF (2 drops), oxalyl chloride (0.9 mL, 10 mmol) was added dropwise at RT. After addition the reaction mixture was heated at 60 C. for 2 h. After concentration and stripping with toluene the crude acyl chloride was dissolved in dry THF (7 mL)/triethylamine (3 mmol) and t-butylglycinate (0.286 mL, 2.1 mmol) was added at RT and the reaction mixture was stirred at RT overnight. After concentration obtained 0.66 g (2 mmol, quant.) of tert-butyl N-[3-(4-methylpiperazin-1-yl)benzoyl]glycinate. The above obtained t-butyl ester (0.1 g, 0.3 mmol) was stirred at RT in dichloromethane (4 mL) and trifluoroacetic acid (3 mL) overnight. The solvents were removed under reduced pressure and the crude material stripped three times with toluene. Obtained the corresponding acid (0.080 g. 96% yield). The acid was then reacted as described in Example 1 to afford the title compound. H-NMR (DMSOd6), delta ppm: 2.87 (s, 3 H) 3.13-4.03 (m, 8 H) 7.24-7.95 (m, 6 H) 8.36 (dd, J=4.63, 1.59 Hz, 1 H) 8.52 (d, J=2.44 Hz, 1 H) 9.11 (d, J=7.32 Hz, 1 H) 10.48 (s, 1 H) 11.83-11.96 (m, 1 H) 12.58 (s,1 H), 215309-01-6

As the paragraph descriping shows that 215309-01-6 is playing an increasingly important role.

Reference£º
Patent; Pharmacia Italia S.p.A.; US2007/112020; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a suspension of methyl (Z)-1-acetyl-3-(ethoxy(phenyl)methylene)-2-oxoindoline-6-carboxylate (6) (500 mg,1.368 mmol) in DMF (3.5 mL) was added N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide (14) (395 mg,1.505 mmol, 1.1 equiv.) at RT. After heating the reaction mixture at 80 C for 1 h, it was allowed to cool to RT. Piperidine (297 lL,3.010 mmol, 2.2 equiv.) was then added and stirred for 2 h. Volatiles were removed in vacuo and water was added to the obtained residue and stirred for 15 min. The precipitate was then filtered under suction and cake was washed with water, then with minimum amount of cold methanol, and then ether. The obtained product was purified by column chromatography (neutral Al2O3,0-10% methanol in CH2Cl2) to afford 532 mg (72%) of target molecule 15. Major conformer 1H NMR (400 MHz, DMSO-d6): d 12.22 (s,1H), 10.98 (s, 1H), 7.66-7.47 (m, 5H), 7.42 (s, 1H), 7.24-7.09 (m,3H), 6.89 (d, J = 8.0 Hz, 2H), 5.83 (d, J = 8.0 Hz, 1H), 3.77 (s, 3H),3.06 (s, 3H), 2.69 (s, 2H), 2.34-2.06 (brs, 8H), 2.10 (s, 3H). HRMSm/z found 540.2606, calcd for C31H34N5O4 [M+H]+ 540.2605.

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

Reference£º
Article; Edupuganti, Ramakrishna; Taliaferro, Juliana M.; Wang, Qiantao; Xie, Xuemei; Cho, Eun Jeong; Vidhu, Fnu; Ren, Pengyu; Anslyn, Eric V.; Bartholomeusz, Chandra; Dalby, Kevin N.; Bioorganic and Medicinal Chemistry; vol. 25; 9; (2017); p. 2609 – 2616;,
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Piperazines – an overview | ScienceDirect Topics