Category: piperazines

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.

0Example 1 4- [6- (4-ISOPROPYLPIPERAZIN-1-YL)-PYRIDAZIN-3-YL] BENZONITRILE A suspension OF 4- (6-CHLORO-PYRIDAZIN-3-YL)-BENZONITRILE (1 g, 4.64 mmol ; prepared as de- scribed in US patent No. 4,112, 095), isopropylpiperazine (0.654 g, 5.1 MMOL), DIPEA (1.199 g, 9.27 MMOL) and 4- (DIMETHYLAMINO) PYRIDINE (0.057g, 0.464 MMOL) in DMSO (4 mi) was stirred and heated to 100 ¡ãC for 20h. After cooling to room temperature, the mixture was di- luted with DICHLOROMETHANE (25 ml) and water (35 ml) and stirred for 5 min. The organic phase was separated, washed with water (50 ml) and brine (50 ML), and acidified to pH 2 by addition of 1 N hydrochloric acid. The mixture was extracted with water (30 ML), and the aque- ous phase was washed with DICHLOROMETHANE (10 mi) and concentrated in vacuo to give a solid, which was collected and stripped with ethanol to afford the title compound as a crys- talline hydrochloride (1.33 g, 76percent). ‘H NMR (D2O) 51. 30 (d, 6H), 3.26 (broad t, 2H), 3.45-3. 68 (m, 5H), 4.52 (broad d, 2H), 7.75 (d, 1H), 7.77 (d, 2H), 7.87 (d, 2H), 8.12 (d, 1H) ; HPLC-MS: M/Z 308.2 (MH+) ; Rt : 1.76 min., 4318-42-7

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NOVO NORDISK A/S; WO2005/9976; (2005); A1;,
Piperazine – Wikipedia
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181955-79-3, 1,4-Di-Boc-piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 1,4-bis(tert-butoxycarbonyl)piperazine-2-carboxylic acid (4.88 g, 14.7 mmol) in DMF (49 mL) was added K2CO3 (2.65 g, 19.2 mmol), and the mixture cooled to 0 C. To the mixture was then slowly added methyl iodide (1.38 mL, 22.1 mmol). The reaction stirred was stirred at room temperature for 18 hours and quenched with saturated aqueous NH4Cl (100 mL). The mixture was diluted with water and extracted with EtOAc twice. The combined organic layers were washed with water and brine, dried over Na2SO4, filtered and concentrated in vacuo. The residue was purified by column chromatography on SiO2 (Hex:EtOAc=7:1 to 5:1 to 3:1) to afford 1,4-di-tert-butyl 2-methyl piperazine-1,2,4-tricarboxylate (5.09 g, 100%) as a pale brown viscous oil. 1H-NMR (CDCl3, Varian, 400 MHz): delta 1.44 (18H, s), 2.80 (1H, br. s), 3.12-3.24 (1H, m), 3.21 (1H, br. s), 3.74 (3H, s), 3.80-4.10 (2H, m), 4.48-4.73 (2H, m).

181955-79-3, The synthetic route of 181955-79-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; HANDOK INC.; CMG Pharmaceutical Co., Ltd.; Kim, Moonsoo; Lee, Chaewoon; Lee, Gilnam; Yoon, Cheolhwan; Seo, Jeongbeob; Kim, Jay Hak; Lee, Minwoo; Jeong, Hankyul; Choi, Hyang; Jung, Myung Eun; Lee, Ki Nam; Kim, Hyun Jung; Kim, Hye Kyoung; Lee, Jae Il; Lee, MinWoo; Kim, Misoon; Choi, Soongyu; (124 pag.)US2016/168156; (2016); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2815-34-1,trans-2,5-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

A mixture of 0.20 g (0.38 mmol) 2- (3, 5-BIS-TRIFLUOROMETHYL-PHENYL)-N- [6-CHLORO-4- (4- fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide, 87 mg (0.75 mmol) (2RS, 5SR) -dimethyl-piperazine, 0.01 g (0.03 mmol) cetyltrimethylammonium bromide, 0.01 g (0.02 mmol) bis (tri-t-butylphosphine) palladium (0), 0.075 ml NaOH 50 % and 3 ml toluene was degassed by two freeze-thaw cycles. The reaction mixture was heated under argon at 90 C for 48 h. After cooling to room temperature the mixture was diluted with water and brine and extracted with three portions of tert-butyl methyl ether. The combined organic layers were dried over sodium sulphate and concentrated in vacuo. Flash column chromatography gave 96 mg (42%) of the title compound as a light yellow solid. MS m/e (%): 611 (M+H+, 100)

2815-34-1, As the paragraph descriping shows that 2815-34-1 is playing an increasingly important role.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; WO2005/2577; (2005); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A solution of 1, 1-dimethylethyl (2S)-2-methyl-1-piperazinecarboxylate (Intermediate 26,100 mg, 0.5 mmol) in CH2CI2 (5 mL) was mixed with 3-bromo benzaldehyde (0.06 mL, 0.5 mmol) and NaB (OAc) 3H (0.16 g, 0.75 mmol). The resulting mixture was stirred for 12 hours, diluted with dichloromethane (30 mL) and washed with brine (50 mL). The organic layer was collected, dried over Na2SO4 and concentrated. Separation via a combiflash system then afforded the title compound (150 mg, 81%). LC/MS : m/z, 369 (M+H) ;’HNMR (MeOD) 1.26 (3H, d), 1.47 (9H, s), 2.0 (1H, m), 2.1 (1H, m), 2.6 (1H, m), 2.8 (1H, m), 3.1 (1H, m), 3.3 (2H, s), 3.4 (1 H, m), 3.5 (1 H, m), 3.8 (1 H, m), 4.2 (1 H, m), 4.88 (1 H, s), 7.25 (1 H, m), 7.3 (1 H, m), 7.4 (1 H, m), 7.55 (1 H, s)., 169447-70-5

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

Reference£º
Patent; GLAXO GROUP LIMITED; WO2005/87236; (2005); A1;,
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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.

A l-liter-3-neck flask was loaded with 4-nitrobenzoyl chloride (50.5 g, 267 mmol) and THF (500 ml) and cooled to 0 C. Pyridine (44 ml, 544 mmol), then 1-methyl-piperazine (35 ml, 316 mmol) were added while mechanically stirring at 0 C. After the addition was completed the ice bath was removed and the mixture stirred for 1 hour, while warming to room temperature. A voluminous precipitate forms. The slurry was diluted with dichloromethane and 1 M aq. KOH and the layers separated. The organic layer was washed one more time with 1 M aq. KOH, then with brine and dried over MgSO4, filtered and concentrated in vacuum. 31.5 g yellow solid (4-methylpiperazin- l-yl)(4-nitrophenyl)methanone were isolated. MS (ESI) m/z 250 (M+H). 1H NMR (CDCl3) delta ppm 8.27 (d, 2 H, J= 7.9), 7.56 (d, 2 H, /= 7.9), 3.81 (bs, 2 H), 3.37 (bs, 2 H), 2.50 (bs, 2H), 2.34 (bs, 2H), 2.32 (s, 3H)., 109-01-3

The synthetic route of 109-01-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; PURANDARE, Ashok, Vinayak; BATT, Douglas, G.; LIU, Qingjie; JOHNSON, Walter, L.; MASTALERZ, Harold; ZHANG, Guifen; ZIMMERMANN, Kurt; WO2010/80474; (2010); A1;,
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30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 9 (2-Iodo-5-methanesulfonyl-phenyl)-[4-(4-trifluoromethyl-phenyl)-piperazin-1-yl]-methanone To a solution of 2-Iodo-5-methanesulfonyl-benzoic acid (Example C, 3.0 g, 9.2 mmol) in dimethylformamide (20 ml) were successively added TBTU (3.8 g, 11.5 mmol), N-ethyldiisopropylamine (8.0 ml, 46.0 mmol) and 1-(4-trifluromethylphenyl)piperazine (ABCR F07741NB, [30459-17-7], 2.5 g, 11.0 mmd). The reaction was then stirred at room temperature for two hours, then concentrated in vacuo and purified by column chromatography (SiO2, 50 g, CH2Cl2/MeOH/NH3=100/0/0 to 95/4.5/0.5), to give the title compound as a pale brown foam; MS (m/e): 539.1 (M+H+). TBTU=2-(1 H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium tetrafluoroborate

30459-17-7, As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference£º
Patent; Alberati-Giani, Daniela; Jolidon, Synese; Narquizian, Robert; Nettekoven, Matthias Heinrich; Norcross, Roger David; Pinard, Emmanuel; Stalder, Henri; US2005/59668; (2005); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

Reference Example 46] 1-Methylpiperazin-2-one [Show Image] An aqueous 1 N sodium hydroxide solution was added to a suspension of 1-methylpiperazin-2-one hydrochloride (19.6 g) of Reference Example 21-(3) in dichloromethane, and the resultant mixture was partitioned. Further, sodium chloride was added to the aqueous layer to saturate the layer, and then the aqueous layer was extracted with dichloromethane. The organic layers were combined and dried over anhydrous sodium sulfate. After separation by filtration, the solvent was evaporated under reduced pressure, and the title compound (5.90 g) was obtained as an oily product. ESI-MSm/z: 115(M+H)+.

109384-27-2, 109384-27-2 1-Methylpiperazin-2-one hydrochloride 17060766, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1785418; (2007); A1;,
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Piperazines – an overview | ScienceDirect Topics

848482-93-9, (S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of (S)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (500 mg, 2.171 mmol) in 1,4-dioxane (5 mL) and water (20 mL) was added potassium carbonate (1200 mg, 8.69 mmol) followed by (9Hfluoren-9-yl)methyl carbonochloridate (562 mg, 2.171 mmol) at 0 C. The mixture was stirred at RT for 18hrs and then treated with water (10 ml). The resulting mixture was extracted with diethyl ether (2¡Á15 ml).The aqueous phase was acidified with aq. HCl (1M) to pH 2-3, and extracted with DCM (3¡Á20 ml). Thecombined organic layers were dried over MgSO4 and concentrated to give the crude product. The crudeproduct was purified via prep HPLC (10-100% CH3CN:Water with 0.1% TFA buffer) to afford the product(S)-1-(((9H-fluoren-9-yl)methoxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (294 mg,30% yield) as a white solid. 1H NMR (500 MHz, methanol-d4) d 7.83 (t, J=6.6 Hz, 2H), 7.68-7.58 (m,2H), 7.45-7.38 (m, 2H), 7.38-7.30 (m, 2H), 4.65 (br. s., 1H), 4.58 (d, J=13.7 Hz, 1H), 4.55-4.39 (m, 3H),4.33-4.18 (m, 1H), 2.91-2.85 (m, 4H), 1.47 (s, 9H). ESI-MS(+) m/z=475 (M+Na)., 848482-93-9

848482-93-9 (S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid 1501850, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Bristol-Myers Squibb Company; Miller, Michael Matthew; Mapelli, Claudio; Allen, Martin Patrick; Bowsher, Michael S.; Boy, Kenneth M.; Gillis, Eric P.; Langley, David R.; Mull, Eric; Poirier, Maude A.; Sanghvi, Nishith; Sun, Li-Qiang; Tenney, Daniel J.; Yeung, Kap-Sun; Zhu, Juliang; Reid, Patrick C.; Scola, Paul Michael; (892 pag.)US9308236; (2016); B2;,
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34770-60-0, 4-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 3-14-2 Preparation of 1-(2-Amino-1-(3-methoxy-4-((6-methoxypyridin-3-yl)methoxy)benzyl)-1H-benzo[d]imidazol-5-yl)-4-methylpiperazin-2-one To a stirred suspension of 5-iodo-1-(3-methoxy-4-((6-methoxypyridin-3-yl)methoxy)benzyl)-1H-benzo[d]imidazol-2-amine (0.25 g, 0.48 mmol) in 1,4-dioxane (8 mL) was added 4-methylpiperazin-2-one (0.11 g, 0.96 mmol), CuI (0.036 mg, 0.19 mmol), trans-N,N’-dimethylcyclohexane-1,2-diamine (0.044 g, 0.38 mmol), and tribasic potassium phosphate (0.32 g, 1.52 mmol). The mixture was heated to 145 C. in a microwave reactor. After 3 h, the mixture was allowed to cool to room temperature and was filtrated through Celite. The filtrate was concentrated, and the residue was purified by silica gel chromatography (2-5% methanol/dichloromethane elute) followed by prep-HPLC to afford 0.030 g (12%) of the product as a white solid: 1H NMR (500 MHz, CDCl3) delta 8.17 (s, 1H), 7.66 (dd, J=8.0, 2.0 Hz, 1H), 7.25 (s, 1H), 7.01 (d, J=8.0 Hz, 1H), 6.86 (d, J=8.0 Hz, 1H), 6.79 (d, J=8.0 Hz, 1H), 6.76-6.74 (m, 2H), 6.64 (d, J=7.5 Hz, 1H), 4.99 (s, 2H), 4.89 (br s, 2H), 4.81 (s, 2H), 3.94 (s, 3H), 3.79 (s, 3H), 3.72 (t, J=5.0 Hz, 2H), 3.30 (s, 2H), 2.82 (t, J=5.0 Hz, 2H), 2.44 (s, 3H) ppm; (M+1)=503., 34770-60-0

34770-60-0 4-Methylpiperazin-2-one 13704283, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; KANE, JR., John L.; MATTHEWS, Gloria; METZ, Markus; KOTHE, Michael; LIU, Jinyu; SCHOLTE, Andrew; US2015/158847; (2015); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.149057-19-2,4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

Stage 1: 4-Benzyl 1 -tert-butyl 2-cyclopentyl piperazi ne-i ,2,4-tricarboxylate 4-[(Benzyloxy)carbonyl]- 1 -(tert-butoxycarbonyl)piperazi ne-2-carboxylic acid (9.96 g, 27 mmol) was dissolved in DCM (50 mL) and cooled to 0CC. Cyclopentanol (7.4 mL, 82 mmol), EDO (7.86 g, 41 mmol) and DMAP (0.33 g, 2.7 mmol) were then added and the reaction allowed to warm to RT, and stirred for 24 hrs. Water (100 mL) and DCM (50 mL) were then added and the layers separated. The aqueous layer was reextracted with DCM (2 x 50 mL) and the combined organic layers were then dried over Mg504 and concentrated in vacuo. Purification by column chromatography (40% EtOAc/heptane) afforded the title compound as a colourless oil (10.4 g, 88%). LCMS: m/z 455 [M+Na]., 149057-19-2

The synthetic route of 149057-19-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CHROMA THERAPEUTICS LTD; DAVIES, Stephen John; PINTAT, Stephane; NORTH, Carl Leslie; MOFFAT, David Festus Charles; WO2014/1802; (2014); A1;,
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Piperazines – an overview | ScienceDirect Topics