Month: September 2021

4318-42-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

Example 75 N-{2- [3 -Fluoro-5- (4-isopropyl-piperazin- 1 -yl) -phenyl] -3 ,3 -dimethyl- 1 ,2,3 ,4- tetrahydro-quinoline-6-carbonyl}-methanesulfonamideA mixture of 2-(3-bromo-5-fiuoro-phenyl)-3,3-dimethyl-l,2,3,4-tetrahydro-quinoline-6- carboxylic acid methyl ester (0.41 g, 1.0 mmol), 1-isopropyl piperazine (0.64 g, 5.0 mmol), copper (I) iodidie (120 mg, 0.6 mmol), L-proline (69 mg, 0.6 mmol) and potassium hydroxide (33.6 mg, 0.6 mmol) in DMSO (2 mL) was stirred at 120 °C for 2 hours. Then treated with saturated ammonium chloride (20 mL), extracted with ether (100 mL). After removal of solvent, the residue was purified on flash silica gel chromatography (silica gel from QingDao, 200-300 mesh, glass column from Shanghai SD company)(40percent ethyl acetate/hexanes) to afford 2-[3-fiuoro-5-(4-isopropyl-piperazin-l-yl)-phenyl] -3,3- dimethyl-l,2,3,4-tetrahydro-quinoline-6-carboxylic acid ethyl ester (0.27 g, 60percent) as a white solid: LC/MS m/e calcd for C27H36FN3O2 (M+H)+: 454.6, observed: 454.3.

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; CHEN, Li; FENG, Lichun; HUANG, Mengwei; LIU, Yongfu; WU, Guolong; WU, Jim, Zhen; ZHOU, Mingwei; WO2011/128251; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Synthesis of 3-methyl-1-thiazol-2-ylpiperazine 30.06 g (300.0 mmol) of 2-methylpiperazine were combined with 4.51 ml (50.0 mmol) of 2-bromothiazole. This mixture was fused and refluxed 5 min. The reaction mixture was cooled and taken up in 10% strength hydrochloric acid and washed with EA. The aqueous phase was set to pH>12 with a 10% strength aq. NaOH solution and then extracted with EA. The organic phase was dried over MgSO4 and conc. in vacuo. There were obtained 8.26 g (45.1 mmol, 90%) of 3-methyl-1-thiazol-2-ylpiperazine., 109-07-9

The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Gruenenthal GmbH; US2007/112011; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 9 In a 100 ml four-neck flask, 5.06 g (= 0.0505 mole) of racemic 2-methylpiperazine was placed, and 50.00 g of 1-butanol (water content 0.05 wtpercent) was added for dissolution. After cooling down to 0°C, 10.91 g (= 0.0500 mole, 0.99 molar time) of di-tert-butyl dicarbonate was added dropwise with the liquid temperature kept in a range from 5 to 15°C. Then, stirring was carried out at 5 to 10°C for 2 hours. The reaction solution was analyzed, and as a result, the conversion of 2-methylpiperazine was 94.7percent, while the selectivity of 1-tert-butoxycarbonyl-3-methylpiperazine was 89.3percent (reaction yield 84.6percent).Example 10 An experiment was carried out as described for Example 9, except that the amount of di-tert-butyl dicarbonate used was changed to 11.97 g (= 0.0548 mole, 1.10 molar times). As a result, the conversion of 2-methylpiperazine was 100.0percent, and the selectivity of 1-tert-butoxycarbonyl-3-methylpiperazine was 81.5percent (reaction yield 81.5percent)., 109-07-9

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

Reference：
Patent; Toray Fine Chemicals Co., Ltd.; EP1548010; (2005); 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.67455-41-8,4-(Piperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

67455-41-8, General procedure: A solution of 1mmol amine/thiol and 1.2mmol alpha,beta-unsaturated nitriles or carbonyl compounds was added to bucky gel (0.1mmol) and the mixture was stirred at 25C for 1min. Likewise, the completion of the reaction was monitored using TLC. The product formed in the one-phase system, was further extracted with ether. In the same way as in the above preparation, the resulting organic phase extract was washed with a saturated solution of NaHCO3, water, and dried over Na2SO4. After removal of the solvent, the residue was further purified by recrystallization or silica gel chromatography. The reaction products were then analyzed using 1H and 13C NMR spectroscopy.

67455-41-8 4-(Piperazin-1-yl)aniline 422925, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Attri, Pankaj; Bhatia, Rohit; Arora, Bharti; Kumar, Naresh; Park, Ji Hoon; Baik, Ku Youn; Lee, Geon Joon; Kim, In Tae; Koo, Je Huan; Choi, Eun Ha; Materials Research Bulletin; vol. 58; (2014); p. 6 – 9;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

674792-05-3, (S)-1-Boc-2-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,674792-05-3

The carboxylic acid was used directly in the next step without further purification. To a solution of the acid (340 mg, 1.5 mmol) in CH2Cl2 (15 mL), was added NEt3 (0.422 mL, 3 mmol), (2S)-N-Boc-2-Isopropyl-piperazine (350 mg, 1.5 mmol) and PyBroP (707 mg, 1.5 mmol). After stirring 18 h under nitrogen, the reaction mixture was diluted with CH2Cl2 (50 mL) and washed with a solution of HCl (0.1 M, 10 mL) and saturated NaHCO3 (10 mL). The organic layer was then dried with Na2SO4, filtered and concentrated under reduced pressure. The crude residue was purified by column chromatography (Hexane/AcOEt 1/0 to 6/4) and the desired piperazine adduct 13c was obtained as a pale yellow foam (452 mg, 1.04 mmol, 69%); HRMS: (ESI-TOF) C22H34N4O5H+ expected: 435.2602. found: 435.2598.

The synthetic route of 674792-05-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; The Scripps Research Institute; US2009/197895; (2009); 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.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 °C 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：
Patent; MODERNATX, INC.; BENENATO, Kerry E.; BUTCHER, William; (512 pag.)WO2018/232120; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

Step 3: 8-Fluoro-1,3,4,5-tetrahydro-2- (4-carboxyphenyl) -6H- pyrrolo [4,3,2-EF] [2] benzazepin-6 (100 mg, 0.31 mmol), benzotriazole-N, N, N ‘, N’- tetramethyluronium hexafluorophosphate (HBTU, 129 mg, 0.34 mmol), 1-(cyclopropanecarbonyl)piperazine (52 mg, 0.34 mmol), N, N-diisopropylethylamine (DIPEA, 80 mg, 0.62 mmol) and DMF (3 mL) were added to the reaction flask and stirred at room temperature for 2 h. H20 (5 mL) was added dropwise and the mixture was stirred to precipitate a solid which was filtered to give a gray solid which was recrystallized from methanol (10 mL) to give 8-fluoro-1,3,4,5-tetrahydro-2-(4-(4-(cyclopropanoyl)piperazine-1-carbonyl)phenyl)-6H-pyrrolo[4,3,2-EF][2]benzazepin-6-one (I-1) as a white solid (70 mg, yield 49.3%)., 59878-57-8

The synthetic route of 59878-57-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Shanghai Xunhe Pharmaceutical Technology Co., Ltd.; Zheng Yongyong; Jin Hua; Zhou Feng; Huang Meihua; Meng Xin; (23 pag.)CN107286166; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

630125-91-6,630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 4-Bromophenoxyacetic acid (1.20 g, 4.66 mmol) in anhydrous dichioromethane (10 mL) was added oxalyl chloride (0.59 g, 4.66 mmol)followed by a few drops of N,N-dimethylformamide at 0 C. After stirring at room temperature for one hour, a solution of 4-[(4-ethylpiperazin-1-yl)methyl]-3- (trifluoromethyl)aniline (2.50 g, 8.69 mmol) and triethylamine (2.63 g, 26.0 mmol) in anhydrous dichloromethane (10 mL) was added dropwise at 0 C and warmed to room temperature. After 16 h, the reaction mixture was partitioned between water (200 mL)and dichloromethane (100 mL). The aqueous layer was further extracted with dichloromethane (100 mL). The combined organic extracts were washed with brine (400 mL), dried (Na2SO4), the solvent evaporated and the residue purified by flash chromatography (Redisep silica gel, 97:3 CH2C12/MeOH) to afford 2-(4-bromophenoxy)- N- {4-[(4-ethylpiperazin- 1 -yl)methyl] -3 -(trifluoromethyl)phenyl } -acetamide (2.60 g). 1HNMR (400 MHz, DMSO-d6): 10.37 (s, 1H), 8.06 (s, 1H), 7.85-7.83 (dd, J= 8.4, 1.7Hz, 1H), 7.69-7.66 (a, J 8.5 Hz, 1H), 7.49-7.47 (d, J 9.2 Hz, 2H), 6.99-6.97 (d, J8.8 Hz, 2H), 5.75.(s, 2H), 4.72 (s, 2H), 3.53 (s, 2H), 2.37-2.27 (m, 1OH), 0.99-0.95 (t, J= 7.2 Hz, 3H); ESI MS, m/z 499 [M-H].

As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.

Reference：
Patent; AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH (A*STAR); CHERIAN, Joseph; DURAISWAMY, Athisayamani Jeyaraj; NACRO, Kassoum; WO2014/88519; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

Step 12.2: 3-Bromo-4-methyl-N-[4-(4-methyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-benzamide To a solution of 6.1 g (0.025 mol) 3-bromo-4-methylbenzoic acid chloride in 50 mL of acetonitrile are added at 10 C. 7 mL (0.05 mol) triethylamine followed by dropwise addition of a solution of 4-(4-methyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenylamine in 50 mL of acetonitrile (exothermic reaction). The brown suspension is stirred for 5 h at rt and is then allowed to stand over night. Ethyl acetate is added and the solution washed with saturated sodium bicarbonate solution and brine, dried with sodium sulphate and evaporated. Flash-chromatography on silica gel using dichloromethane/ethanol 93:7 containing 1% conc. ammonia gives pure title product: Rf (dichloromethane/ethanol 93:7 with 1% conc. ammonia)=0.4; HPLC tR=3.14 min; MS-ES+: (M+H)+=470, 472.

As the paragraph descriping shows that 694499-26-8 is playing an increasingly important role.

Reference：
Patent; Caravatti, Giorgio; Furet, Pascal; Imbach, Patricia; Martiny-Baron, Georg; Perez, Lawrence Blas; Sheng, Tao; US2006/35897; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-82-4, 4-(4-Methylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

70261-82-4, A solution [CONTAINING-50%] of propylphosphonic anhydride in N, N-dimethylformamide (Fluka, Buchs, Switzerland; 875 [UL, ~1.] 5 [MMOL)] is added within 20 minutes to a stirred mixture of 4- [METHYL-3- [ [4- (3-PYRIDINYL)-2-PYRIMIDINYL] AMINO]-BENZOIC] acid (306 mg, 1.0 [MMOL),] [4- [ (4-METHYL-] 1-piperazinyl) methyl] benzeneamine (Chem. Abstr. Reg. Number: 70261-82-4; 205 mg, 1.0 [MMOL)] and triethylamine (830 [ZL,] 6.0 [MMOL)] in 8 mL [N, N-DIMETHYLFORMAMIDE.] After stirring for 24 hours at room temperature, the mixture is treated with a saturated aqueous ammonium chloride and extracted three times with ethyl acetate. The solvent is evaporated off under reduced pressure and the residue dried in vacuo. The crude product is crystallised from ethanol-ethyl acetate to give the title compound as a crystalline solid, m. p. [153-155C.]

As the paragraph descriping shows that 70261-82-4 is playing an increasingly important role.

Reference：
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2004/5281; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics