Month: May 2021

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.

4.1.4.12 (S)-1-(2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)pyridin-4-yl)-N-(4-(trifluoromethoxy)benzyl)piperidine-3-carboxamide (2d) Compound 5d (257?mg, 0.56?mmol) was reacted with 2-methoxy-4-(4-methylpiperazin-1-yl)aniline (137?mg, 0.62?mmol) according to the general procedure B to give compound 2d (177?mg, yield: 53%).

122833-04-9, As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference：
Article; Liu, Siming; Jiang, Ying; Yan, Ruohong; Li, Zhonghuang; Wan, Shanhe; Zhang, Tingting; Wu, Xiaoyun; Hou, Ju; Zhu, Zhengguang; Tian, Yuanxin; Zhang, Jiajie; European Journal of Medicinal Chemistry; vol. 179; (2019); p. 358 – 375;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

115761-79-0, 1-(2,4-Difluorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,115761-79-0

General procedure: To a solution of methyl hydrazinecarbodithioate 1 (0.34 g, 3 mmol) in ethanol (5 mL) was added the appropriate 1-substituted piperazine 2a-m (6 mmol), and the reaction mixture was stirred at reflux until the evolution of methyl mercaptan almost ceased (it took 5-10 h, and methyl mercaptan was detected by the moistened Pb(OAc)2 paper placed at the upper end of the reflux condenser). After cooling to room temperature, the precipitate was collected by filtration, dried in air. The crude product was purified by recrystallization from the appropriate solvent to give compounds 3a-m.

The synthetic route of 115761-79-0 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Lin, Hui-Hui; Wu, Wei-Yao; Cao, Sheng-Li; Liao, Ji; Ma, Li; Gao, Man; Li, Zhong-Feng; Xu, Xingzhi; Bioorganic and Medicinal Chemistry Letters; vol. 23; 11; (2013); p. 3304 – 3307;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

859518-35-7, tert-Butyl 3-cyanopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

859518-35-7, A solution of tert-butyl 3-cyanopiperazine-1-carboxylate, prepared as described in the previous step, (10 g, 0.047 mol) and 2-(2-hydroxyethoxy)acetaldehyde (14.8 g) (see: Bodin, A.,Contact Dermatitis, 2001,44:207) in dichloromethane was treated with formic acid (12.7 g), and the reaction mixture was stirred at room temperature overnight. Sodium cyanoborohydride (7.2 g, 0.118mol) was added in portions. The reaction mixture was stirred at room temperature for 3 hours followed by the addition of water and extraction with dichloromethane. The organic layer was w·ashed with brine, dried over sodium sulfate, filtered, and concentrated. The crude product was purified by column chromatography to provide the product. 1H NMR: (CDCl3, 400 MHz): delta (ppm) 4.15 (s, 1H), 3.69-3.63 (m, 4H), 3.58 (d, J=4.4 Hz, 2H), 3.47-3.44 (m, 4H), 2.61 (d, J=5.2 Hz, 2H), 2.51-2.48 (m, 4H), 1.43 (s, 9H).

As the paragraph descriping shows that 859518-35-7 is playing an increasingly important role.

Reference：
Patent; JANSSEN PHARMACEUTICA NV; ORTHO-CLINICAL DIAGNOSTICS, INC; DONAHUE, Matthew Garrett; GONG, Yong; SALTER, Rhys; HRYHORENKO, Eric; DECORY, Thomas R.; REMMERIE, Bart M.; SANKARAN, Banumathi; WO2014/31600; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,21043-40-3

(General Procedure 16)4-Cyclopentyl-piperazine-1-carboxylic Acid 4-iodo-pyrazol-1-yl Ester The title compound was prepared from 1-hydroxy-4-iodopyrazole and N-cyclopentylpiperazine applying the general procedure 16. The crude product was purified by flash chromatography (Quad flash 12, EtOAc-heptane-3% Et3N) (61%, crystals). 1H NMR (300 MHz; CDCl3): delta 1.33-1.94 (m, 8H), 2.46-2.61 (m, 5H), 3.57 (bt, 2H), 3.67 (bt, 2H), 3.63 (bs, 2H), 3.77 (bs, 2H), 7.40 (d, 1H), 7.44 (d, 1H); HPLC-MS: m/z=391.1 (M+1); Rt=1.31 min.

21043-40-3 1-Cyclopentylpiperazine 806421, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Ebdrup, Soren; de Jong, Johannes Cornelis; Jacobsen, Poul; Hansen, Holger Claus; Vedso, Per; US2003/166644; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

350 ml of ethanol was added to 155 g (1.547 mol) of N-methylpiperazine. At room temperature (25+/-3 C.), 60 g (0.351 mol) of 4-chloromethylbenzoic acid was added thereto and stirred for 6-7 hours. The reaction was analyzed by HPLC, and then the reaction solution was distilled under reduced pressure to remove ethanol, and 60 ml of 1-butanol was added thereto. The mixture was azeotropically distilled at 70+/-2 C. and concentrated to produce a solid. 600 ml of 2-propanol was added thereto and the mixture was stirred at room temperature (25+/-3 C.) for 30 minutes, stirred under reflux for 15 minutes, and then stirred at room temperature (25+/-3 C.) for 12 hours with slow cooling. The produced precipitate was cooled to 19+/-3 C., stirred for 1 hour and then filtered. The filtrate was washed with 50 ml of cooled 2-propanol and dried in an oven at 60 C., thereby obtaining a white compound of formula (2) (60 g, yield: 72%, purity: 95% or higher).HPLC purity: 99.123% (desmethyl impurity: 0.042%, starting material 0.42%).Thin layer chromatography: Methanol-Dichloromethane (7:5), Rf: 0.2., 109-01-3

109-01-3 1-Methylpiperazine 53167, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BCWORLD PHARM. CO., LTD.; US2012/330014; (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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

Intermediate 8 tert-Butyl (3R)-4-(chlorocarbonyl)-3 -methylpiperazine- 1 -carboxylateTo a mixture of triphosgene (23 g, 75 mmol) in anhydrous DCM (250 mL) was added pyridine (18 g, 225 mmol) drop-wise followed by addition of tert-butyl (3R)-3- methylpiperazine-1 -carboxylate (15 g, 75 mmol) at 0 C. The mixture was stirred overnight at RT. TLC showed the starting material had been consumed. The mixture was concentrated to afford Intermediate 8 as yellow solid, which was used without further purification., 163765-44-4

As the paragraph descriping shows that 163765-44-4 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; LI, David, Yunzhi; WANG, Jiabing; YANG, Zhenfan; ZENG, Qingbei; ZHANG, Xiaolin; WO2014/135876; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

25057-77-6, 1,2-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Reference Example 7 To a solution of N-benzyl-4-piperidone (8.0 g) and 3,4-dimethylpiperazine (9.5 g) in ethanol (100 ml) are added 5% platinum-carbon (2 g) and acetic acid (14.4 ml), and the mixture is subjected to catalytic hydrogenation at room temperature under atmospheric pressure. The catalyst is removed by filtration, and the filtrate is concentrated under reduced pressure. Water is added to the resultant, and the mixture is basified with a 5% aqueous sodium hydroxide solution, and the mixture is extracted with diethyl ether. The extract is washed with water, dried and concentrated under reduced pressure to remove the solvent. The residue is dissolved in ethanol, and thereto is added to conc. hydrochloric acid to give a hydrochloride. The resulting white powder is collected by filtration, dissolved in water, and basified with a 5% aqueous sodium hydroxide solution. The mixture is extracted with diethyl ether, washed with water, dried, and concentrated under reduced pressure to give 4-(3,4-dimethyl-1-piperazinyl)-1-benzylpiperidine (4.2 g). 1 H-NMR (CDCl3) deltappm: 1.04 (3H, d, J=6 Hz), 1.45-2.5 (12H, m), 2.27 (3H, s), 2.7-3.05 (4H, m), 3.48 (2H, s), 7.31 (5H, m).

25057-77-6, The synthetic route of 25057-77-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Otsuka Pharmaceutical Company, Limited; US6140330; (2000); 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.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of tert-butyl 3,3-dimethylpiperazine-l-carboxylate (500 mg, 2.333 mmol) in DCM (11 ml) at 0 C was added TEA (0.976 ml, 7.00 mmol) and methanesulfonyl chloride (321 mg, 2.80 mmol) and the resulting mixture was stirred RT for 3 h. The volatiles were removed under reduced pressure. The residue was purified via silica gel chromatography (5 – 100 % EtOAc in hexanes) to give tert-butyl 3,3-dimethyl-4-(methylsulfonyl)piperazine-l-carboxylate (600 mg, 2.052 mmol, 88 % yield) as a colorless liquid. MS (ES+) C^H^C^S requires: 292, found: 293 [M+H] +., 259808-67-8

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

Reference：
Patent; TESARO, INC.; LEWIS, Richard T.; JONES, Philip; PETROCCHI, Alessia; REYNA, Naphtali; HAMILTON, Matthew; CROSS, Jason; TREMBLAY, Martin; LEONARD, Paul Graham; (216 pag.)WO2018/136887; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

123987-13-3, (3-(4-Methylpiperazin-1-yl)phenyl)methanol is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 18 (5.00 g, 19.1 mmol), /V-methylpiperazine (5.73 g, 57.2 mmol), Pd2(dba)3(3.49 g, 3.82 mmol), Cs2C03(12.4 g, 38.2 mmol) and 2,2′-bis(diphenylphosphino)-1 ,1 ‘-binaphthalene (3.56 g, 5.72 mmol) in 1 ,4-dioxane (5 mL) was degassed and purged with N2for 3 times, and then the mixture was stirred at 80 C for 18 h under N2atmosphere. Then the mixture was cooled to 15 C, filtered and concentrated in vacuum. The residue was purified via column chromatography (DCM/MeOH = 20:1) to give 19 (1.40 g, 31 %) as brown oil.1H NMR (400 MHz, DMSO-d6) 7.60 (s, 1 H), 7.52 (d, J = 7.5 Hz, 1 H), 7.34 – 7.30 (m, 1 H), 7.12 (dd, J = 7.7, 2.4 Hz, 1 H), 3.91 (s, 3H), 3.29 – 3.25 (m, 4H), 2.62 – 2.65 (m, 4H), 2.37 (s, 3H). To a solution of 19 (1.40 g, 5.98 mmol) in THF (10 mL) was added LiAIH4(454 mg, 12.0 mmol) at 0 C. The mixture was stirred at 70 C for 2 h. The mixture was cooled to 0 C and quenched by saturated solution of potassium sodium tartrate (3 mL), the precipitate formed was collected, filtered to remove the precipitate. The organic phase was concentrated in vacuum. The residue was purified via column chromatography (DCM/MeOH = 20:1) to give 20 (530 mg, 43%) as brown solid.1H NMR (400 MHz, DMSO-de) 7.26 (s, 1 H), 6.96 (s, 1 H), 6.91 – 6.80 (m, 2H), 4.66 (s, 2H), 3.32 – 3.05 (m, 4H), 2.66 – 2.48 (m, 4H), 2.36 (s, 3H). To a solution of 20 (530 mg, 2.57 mmol) in DCM (10 mL) was added /V-Boc- (S)-valine (670 mg, 3.08 mmol), DCC (795 mg, 3.86 mmol) and DMAP (62.8 mg, 0.514 mmol). The mixture was stirred at 15 C for 24 h. The mixture was filtered and concentrated in vacuum. The residue was purified by column chromatography (DC / eOH = 20:1) to give 21 (600 mg, 58%) as a brown solid. To a solution of 21 (200 mg, 0.493 mmol) in EtOAc (5 mL) was added HCI/EtOAc (4 , 2 mL). The mixture was stirred at 15 C for 15 h. Then the mixture was concentrated in vacuum, the precipitate formed was collected by filtration to give 22 (120 mg, 71 %) as a yellow solid.

123987-13-3, The synthetic route of 123987-13-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ANACOR PHARMACEUTICALS, INC.; AKAMA, Tsutomu; CARTER, David Scott; HALLADAY, Jason S.; JACOBS, Robert T.; LIU, Yang; PLATTNER, Jacob J.; ZHANG, Yong-Kang; WITTY, Michael John; (149 pag.)WO2017/195069; (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.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.,75336-86-6

i) tert-Butyl (3/?)-3-methylpiperazine-l-carboxylate;To a solution of (2No.)-2-methylpiperazine (Ig) in THF (10ml) was added di-tert-butyldicarbonate (1.45g). The reaction mixture was allowed to stir at room temperaturefor 18h.The reaction mixture was then partitioned between DCM (100 ml) and HaO (100 ml). Theorganics were separated and the aqueous layer was re-extracted with DCM (2 x 150ml).Organics were combined, dried (MgSO4) and reduced in vacuo to give the subtitle compoundas a clear oil. Yield: 1. Ig’H NMR: (DMSO) 8 0.92 (d, 3H), 1.38 (s, 9H), 2.57-2.70 (m, 1H), 2.76-2.81 (m, 1H), 2.87-2.99 (m, 1H), 3.66-3.74 (m, 4H)

The synthetic route of 75336-86-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2006/24823; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics