Tag: M.W:100-200

55276-43-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55276-43-2,1-Methanesulfonylpiperazine,as a common compound, the synthetic route is as follows.

To a stirred suspension of N-methanesulfonylpiperazine (1.0 g, 6.1 mmol) in isopropanol (15 mL) at rt was added trimethylsilylisocyanate (1.4 mL, 11 mmol) and the resulting suspension stirred overnight before the precipitate was filtered and dried to give 4-methanesulfonyl-piperazine-1-carboxylic acid amide (1.35 g, quant.) as a solid; 1H-NMR (300 MHz, d6-DMSO) 6.10 (2H, s), 3.37-3.40 (4H, m), 3.03-3.06 (4H, m), 2.90 (3H, s).

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

Reference：
Patent; Schering Aktiengesellschaft; EP1657241; (2006); A1;,
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

To a solution of l-(2,4-difluorophenyl)piperazine [C.A.S. 115761-79-0] (0.088 g, 0.446 mmol) in DCE (2.14 ml) stirred at r.t. was added D88 (0.1 g, 0.371 mmol) and the resulting mixture was stirred at r.t. overnight. Then, acetic acid (0.037 ml) was added and stirred at r.t. for 4 h more. Then, sodium triacetoxy-borohydride (0.87 g, 0.409 mmol) was added and stirred at r.t. overnight. The reaction mixture was neutralized with Na2CO3 (aqueous sat. solution) and extracted with DCM. The organic layer was dried (Na2SO4) and concentrated in vacuo. The crude product thus obtained was purified by column chromatography (silica gel; DCM/EtOAc from 100/0 to 50/50 as eluent). The desired fractions were collected and concentrated in vacuo. The residue obtained was triturated with DIPE to yield final compound E224 (0.107 g, 64%).

115761-79-0 1-(2,4-Difluorophenyl)piperazine 2734637, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ORTHO-MCNEIL-JANSSEN PHARMACEUTICALS, INC; ADDEX PHARMA S.A.; CID-NUNEZ, Jose, Maria; OEHLRlCH, Daniel; TRABANCO-SUAREZ, Andres, Avelino; TRESADERN, Gary, John; VEGA RAMIRO, Juan, Antonio; MACDONALD, Gregor, James; WO2010/130424; (2010); 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.109-01-3,1-Methylpiperazine,as a common compound, the synthetic route is as follows.

4-nitrobenzylbromide (4.30 g, 20 mmol) was dissolved in 40 ml of acetonitrile solvent,Then K2CO3 (5.52 g, 40 mmol) was added,KI (0.33 g, 2 mmol),Then, 4-methylpiperazine (2.20 g, 22 mmol) was added thereto,After 5 h, the reaction was complete.The reaction solution was concentrated and dried,And further adding 100 ml of H2O thereto,Extracted with ethyl acetate (150 ml x 3)The organic layer was collected, concentrated,4.32 g of a solid was obtained in 92% yield., 109-01-3

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

Reference：
Patent; Nantong University; Ling, Yong; Mou, Jiefei; Xu, Qibing; Feng, Jiao; Zhu, Peng; Liu, Ji; Wang, Tingting; Ge, Xiang; Liang, Shanshan; (26 pag.)CN106432235; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

74879-18-8,74879-18-8, (S)-(+)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2.23 Example 23 (Prepared according to Scheme 4); (S)-4-(3-Chloropyridin-2-yl)-2-methyl-N-(4-(trimethylsilyl)phenyl)piperazine-l-carboxamide; A solution of 2,3-dichloropyridine (3mmol), (5)-(+)-2-methylpiperazine (3mmol) and TEA (9mmol) in DMSO (20 ml) was heated to 100 C for 18 hrs. The reaction mixture was diluted with MeOH (20 ml) and put onto an SCX cartridge. The cartridge was washed with MeOH before eluting the product off with 2M ammonia in MeOH. The appropriate fractions were collected and concentrated under reduced pressure. The resulting residue was purified by flash chromatography (60-80 % ethyl acetate in petroleum ether on KPNH cartridge) yielding (S)-l-(3-chloropyridine-2-yl)-3-methylpiperazine (2.1mmol).MS: ES+ 212.10. 1H NMR (400 MHz, DMSO-d6) delta 8.14 – 8.28 (m, IH), 7.67 – 7.87 (m, IH), 6.84 – 7.08 (m, IH), 3.49 – 3.62 (m, 2H), 2.87 – 2.96 (m, IH), 2.77 – 2.87 (m, 2H), 2.62 – 2.77 (m, IH), 2.51 (s, IH), 2.34 – 2.44 (m, IH), 0.92 – 1.10 (m, 3H)A solution of (,S>;-l-(3-chloropyridine-2-yl)-3-methylpiperazine (0.53mmol) and Intermediate 1 (0.53mmol) in ethanol (2 ml) was heated in the microwave to 100 0C for 30 min. The reaction mixture was concentrated under educed pressure and the resulting residue was purified by flash chromatography (20-40 % ethyl acetate in petroleum ether) yielding the title compound (0.32 mmol).MS ES- 401.20. 1H NMR (400 MHz, DMSO-d6) delta 8.32 (s, IH), 8.00 – 8.07 (m, IH), 7.57 – 7.66 (m, IH), 7.22 – 7.30 (m, 2H), 7.1 1 – 7.20 (m, 2H), 6.78 – 6.88 (m, IH), 4.26 (br. s., IH), 3.77 (br. s., IH), 3.41 – 3.52 (m, 2H), 2.98 – 3.08 (m, IH), 2.55 – 2.77 (m, 2H), 1.04 – 1.13 (m, 3H), 0.00 (s, 9H)

As the paragraph descriping shows that 74879-18-8 is playing an increasingly important role.

Reference：
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; AYSCOUGH, Andrew Paul; SHOWELL, Graham Andrew; TEALL, Martin Richard; TEMPLE, Hannah Elizabeth; AHMED, Saleh; WO2010/92342; (2010); 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.39539-66-7,4-Methylpiperazine-1-carbonyl chloride,as a common compound, the synthetic route is as follows.

EXAMPLE 28 Triethylamine (3.4 cc. equivalent to 2.44 g.), followed by pyridine (15 cc.) are added to a suspension of 2-(7-chloro-1,8-naphthyridin-2-yl)-5-fluoro-3-hydroxy-1-isoindolinone (2 g.) and 4-chlorocarbonyl-1-methyl-piperazine hydrochloride (3.6 g.) in methylene chloride (30 cc.). The suspension obtained is heated to the reflux temperature (55 C) for 1 hour and further 4-chlorocarbonyl-1-methylpiperazine (3.6 g.) and triethylamine (3.4 cc.) are then added. The mixture is further heated to the reflux temperature for 45 minutes. After cooling, methylene chloride (30 cc.) and water (60 cc.) are added. After phase separation, the aqueous layer is extracted with methylene chloride (60 cc.). The organic extracts are dried over anhydrous sodium sulphate. After filtration and concentration, the residue is triturated in water (30 cc.). The precipitate is filtered off and dried in air. The crude product is recrystallized from acetonitrile (64 cc.). The product is filtered off and then washed with isopropyl ether (60 cc.). This gives 2-(7-chloro-1,8-naphthyridin-2-yl)-5-fluoro-3-(4-methylpiperazinyl)-carbonyloxy-1-isoindolinone (0.8 g.) melting at 247-248 C. 2-(7-chloro-1,8-naphthyridin-2-yl)-5-fluoro-3-hydroxy-1-isoindolinone can be prepared in the following manner:

39539-66-7, The synthetic route of 39539-66-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Rhone-Poulenc S.A.; US4016274; (1977); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

59702-07-7, Example 70: (+/-)-4-(c/’s-4-(4-amino-5-(2-phenylchroman-7-yl)-7H-pyrrolo[2,3-d]pyrimidin-7- yl )cyclohexyl)- 1 – methyl piperazin-2-oneTo a mixture of 4-(4-amino-5-(2-phenylchroman-7-yl)-7H-pyrrolo[2,3-d]pyrimidin-7- yl)cyclohexanone (Intermediate AL, 100 mg, 0.23 mmol), 1-methylpiperazin-2-one (137 mg, 0.92 mmol), diisopropyiethylamine (1.84 mmol, 327 uL) in dichloroethane (3 mL), was added sodium triacetoxyborohydride (195 mg, 0.92 mmol). The mixture was stirred at room temperature for 2 h and then concentrated. The resulting residue was purified to a mixture of the cis and trans isomers via reverse phase preparative HPLC (Method S). Preparative silica TLC, eluting with 10percent MeOH in DCM with 0.1 N ammonia, was used to isolate the cis (lower band) isomer. MS m/z 537.3 (M+H+) (Method M).

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

Reference：
Patent; NOVARTIS AG; IRM LLC, a Delaware Limited Liability Company; CHEN, Bei; FAIRHURST, Robin, Alec; FLOERSHEIMER, Andreas; FURET, Pascal; JIANG, Songchun; LU, Wenshuo; MARSILJE, Thomas, H.; VAUPEL, Andrea; WO2011/64211; (2011); 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.109-01-3,1-Methylpiperazine,as a common compound, the synthetic route is as follows.

Example 8Synthesis of [F- 18]- 1 -methyl- l-(4-fluorophenyl)piperazinium saltt-BOC-Protected methylpiperizine was heated in the presence of l-fluoro-4- nitrobenzene under pressure in benzene to give 4-t-BOC-protected 1 -methyl- 1 -(4- nitrophenyl)piperazinium salt. The piperazinium salt was heated in the presence of potassium [18F]fluoride and Krytofx at 2000C for 10 minutes. The oil was treated with aq. 3 M HCl for 20 minutes to give [F-18]- 1 -methyl- l-(4-fluorophenyl)piperazinium chloride., 109-01-3

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

Reference：
Patent; THE GENERAL HOSPITAL CORPORATION; WO2008/22319; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 95: l-Methyl-4-[4-(methylsuIfonylmethyl)-6-morpholin-4-yl-pyrimidin-2-yl]piperazin-2- oneA mixture of 2-chloro-4-(methylsulfonylmethyl)-6-morpholin-4-yl-pyrimidine (200 mg), l-methylpiperazin-2-one (157 mg) and sodium carbonate (146 mg) in DMA (4 mL) was heated in a microwave reactor at 16O0C for 10 minutes. The reaction mixture was loaded onto a SCX-2 column and product removed with 7N ammonia in methanol. The solution was evaporated to dryness and chromatographed on silica, eluting with 0 – 2.5percent methanol in DCM, to give the desired material (179 mg) as a white solid. Mass Spectrum; MH+ 370NMR Spectrum: 1H NMR (DMSOd6) 52.89 (3H, s), 3.13 (3H, s), 3.38 (2H, t), 3.55 – 3.56 (4H, m), 3.67 – 3.68 (4H, m), 3.93 (2H, t), 4.19 (2H, s), 4.28 (2H, s), 6.28 (IH, s)

59702-07-7, As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2007/80382; (2007); 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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.,21655-48-1

[5013] A solution of (2S,6R)-2,6-dimethylpiperazine (10.000 g, 87.573 mmol) and tri- ethylamine ( 18.309 mL, 131.360 mmol) in dichloromethane (300 inL) was mixed at 0 °C with benzyl chloroformate ( 13.752 mL, 96.331 mmol) and stirred at the same temperature for 2 hr. Then, saturated aqueous potassium bicarbonate solution was added to the reaction mixture, followed by extraction with dichloromethane. The organic layer was washed with aqueous saturated sodium chloride solution, dried with anhydrous MgS0 , filtered, and concentrated in vacuo. Benzyl (3S,5R)-3,5-dimethylpiperazine- l -carboxylate was used without further purification ( 1 1.000 g, 50.6 percent, pale yellow oil).

21655-48-1 cis-2,6-Dimethylpiperazine 6950261, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; LEE, Jaekwang; KIM, Yuntae; LEE, Chang Sik; SONG, Hyeseung; GWAK, Dal-Yong; LEE, Jaeyoung; OH, Jung Taek; LEE, Chang Gon; KIM, II Hyang; (1041 pag.)WO2017/23133; (2017); A2;,
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.21043-40-3,1-Cyclopentylpiperazine,as a common compound, the synthetic route is as follows.

Step 1: 6-(4-Cyclopentyl-piperazin-1-yl)-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid ethyl ester A mixture of 1 g (3.7 mmol) 6-bromo-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid ethyl ester (prepared according to the method described in WO 2003/064423 A1) and 2.8 g (18.6 mmol) 1-cyclopentyl-piperazine (commercially available) was heated to 140 C. for 1 h. The mixture was absorbed on isolute and purified by flash column chromatography on silica eluting with a gradient formed from n-heptane and ethyl acetate (0.1% NEt3). Evaporation of the product fractions yielded 501 mg (39%) of the title compound as white solid. MS: (m/e): 343.4 (MH+)., 21043-40-3

As the paragraph descriping shows that 21043-40-3 is playing an increasingly important role.

Reference：
Patent; Nettekoven, Matthias; Roche, Olivier; US2007/142358; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics