Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13889-98-0,1-Acetylpiperazine,as a common compound, the synthetic route is as follows.,13889-98-0

A solution of the compound of formula 15 (9.0 g, 52.6 mmol) was added to the reaction flask at room temperature,30 mL of N, N-dimethylacetamide,The compound of formula 16 (7.4 g, 57.8 mmol)N, N-diisopropylethylamine (8.1 g, 63.1 mmol)90 reaction 5 ~ 6h,TLC monitoring reaction is complete,The reaction solution was poured into 200 mL of water,Extracted with ethyl acetate (60 mL x 3)Combined organic layer,Washed with saturated brine,Dried over anhydrous sodium sulfate,The compound of formula 17 (12.71 g) was obtained by steaming,As a yellow solid (yield 86.4%).

13889-98-0 1-Acetylpiperazine 83795, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Zhengda Tianqing Pharmaceutical Group Co., Ltd.; Zhang Yinsheng; Gao Yong; Ren Jing; Wang Qinglin; Wang Zhao; (67 pag.)CN106905245; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,4318-42-7

Step B/lntermediate B94: 1-[2-fluoro-3-(methyloxy)-4-nitrophenyl]-4-(1- methylethyl)piperazine; A pressure flask was charged with 1 ,2-difluoro-3-(methyloxy)-4-nitrobenzene (3.5 g, 18.5 mmol), dimethylsulfoxide (100 ml_), isopropyl piperazine (5.41 ml_, 22.2 mmol) and potassium carbonate (5.1g, 37.04 mmol). The resulting slurry was warmed to 7O0C and stirred overnight. The next morning, the orange solution was poured into water and extracted with diethyl ether. The organic layer was dried over sodium suflate, taken to a residue under reduced pressure, and purified via chromatography on SiO2 (0 to 10percent MeOH/CH2CL2 with 0.2percent NH3) to afford 1-[2-fluoro-3-(methyloxy)- 4-nitrophenyl]-4-(1-methylethyl)piperazine as a yellow solid (5.7g, quant, yield). 1 H NMR (400 MHz, CDCI3) delta ppm 1.10 (d, J=6.60 Hz, 6 H), 2.71 (s, 4 H), 2.76 (s, 1 H), 3.29 (s, 4 H), 4.03 (s, 3 H), 6.64 (dd, J=9.53, 8.07 Hz, 1 H), 7.70 (dd, J=9.35, 2.02 Hz, 1 H).

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

Reference：
Patent; SMITHKLINE BEECHAM CORPORATION; WO2009/20990; (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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Part A: 1,1 -Dimethylethyl (3R,5S)-3,5-dimethyl-1-piperazinecarboxylate. To a solution of c/s-2,6-dimethylpiperazine (1.142 g, 10 mmol) in dichloromethane (25 ml.) at 0 0C was added dropwise bis(1 ,1-dimethylethyl) dicarbonate (2.161 g, 9.9 mmol) in dichloromethane (6 ml_). The reaction mixture was allowed to warm to room temperature and stirred overnight before being diluted with dichloromethane and washed with saturated aqueous Na2CO3 solution. The aqueous layer was back extracted with dichloromethane once. The combined organic layers were washed with brine, dried (MgSO4) and evaporated to yield 1 ,1-dimethylethyl (3R,5S)-3,5-dimethyl-1- piperazinecarboxylate (2.04 g, 95%). LCMS: (M+H)+: 215.1., 21655-48-1

As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

Reference：
Patent; SMITHKLINE BEECHAM CORPORATION; WO2009/61879; (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.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

2-Mercaptoethylpiperazine [0383] To a suspension of piperizaine (30.00 g, 348.27 mmol) and sodium carbonate (106 g, 348.27 mmol) in dichloromethane (200 ml) was added dropwise a solution of Di- tert-butyl dicarbonate (18.98 g, 87.07 mmol) in dichloromethane (30 ml) at room temperature for one hour. Then the mixture was stirred at room temperature overnight. The mixture was mixed with water (100 ml) and separated. The dichloromethane layer was dried over magnesium sulfate and evaporated under reduced pressure. The residue was dissolved in dichloromethane (150 ml). Sodium carbonate (15.55 g, 146.77 mmol) and 1- bromo-2-chloroethane (21.05 g, 146.77 mmol) were added. The mixture was stirred at room temperature for a weekend. The mixture was mixed with water (100 ml) and separated. The dichloromethane layer was dried over magnesium sulfate and evaporated under reduced pressure. The residue was purified by chromatography on silica gel using hexane and ethyl acetate as eluent to give 6.85 g of l-Boc-4-(2-chloroethyl)piperazine., 57260-71-6

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SU, Zhuang; LONG, Zhengyu; YANG, Suizhou; WO2014/145686; (2014); A2;,
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

To a solution of 2-methyl-piperazine (2.0 g, 0.02 mol) and triethylamine (6 mL) in methylene chloride (15 mL) at 0° C. was added (Boc)2O (4.14 g, 0.019 mol) dropwise. The mixture was stirred at room temperature for 1 hour, and then the solvent was removed by rotary evaporation. The residue was dissolved in methylene chloride, washed with saturated sodium bicarbonate and brine, dried over Na2SO4, and purified by column chromatography on silica gel (DCM:MeOH:Et3N=75:1:0.2) to give an white solid (1.65 g, 42percent). LC-MS (ESI) m/z: 201 (M+1)+., 109-07-9

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

Reference：
Patent; LEAD THERAPEUTICS, INC.; US2010/35883; (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.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

Example 127. 2-[4-(6-Chloro-2-methvl-pyrimidin-4-vl)-piperaziii-l-vll-ethano?71); [0307] To a solution of 4,6-dichloro-2-methyl-pyrimidine (5.0 g, 31 mmol) and 2- pirhoerazin-1-yl-ethanol (2.7 g, 21 mmol) in dioxane (25 mL) was added DEPEA (3.0 mL, 17 mmol). The mixture was heated at reflux for 16 h. The mixture was allowed to cool to room temperature and poured into water. The resulting aqueous layer was extracted with EtOAc and the combined organic layers washed with brine, dried over Na2SO4 and filtered. The filtrate was concentrated and the residue purified by flash chromatography on silica gel (5-10% MeOH/DCM) to afford the title compound as a brown liquid (2.1 g, 39%). MS (ES+): m/z 257 (M+H)+.

103-76-4, As the paragraph descriping shows that 103-76-4 is playing an increasingly important role.

Reference：
Patent; TARGEGEN, INC.; WO2006/101977; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5464-12-0,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.

Step J: 1-f 2-f 2-Chloro-3-methyl-4-(4, 4, 5, 5-tetramethyl-l, 3, 2-dioxaborolan-2- yl)phenoxy] ethyl] -4-methyl-piperazine (0181) 10.0 g compound of Step I above (37.2 mmol), 8.7 g 2-(4-methylpiperazin-l-yl)ethanol (60.3 mmol) and 15.8 g triphenylphosphine (60.3 mmol) were dissolved in 100 mL dry toluene and then 27 mL diethyl azodicarboxylate (60.3 mmol, 40 percent solution in toluene) was added dropwise. The mixture was stirred at 50 °C under argon until no further conversion was observed. The volatiles were evaporated under reduced pressure and 100 mL diethyl ether was added. The precipitated white crystals were filtered off and washed with diethyl ether. The filtrate was concentrated under reduced pressure and purified via flash chromatography using chloroform and methanol as eluents. The resulting light brown oil was crystallized from hexane to give l-[2-[2-chloro-3-methyl-4-(4,4,5,5- tetramethyl-l,3,2-dioxaborolan-2-yl)phenoxy]ethyl]-4-methyl-piperazine as an off-white solid. 1H NMR (500 MHz, DMSO-d6) delta: 7.56 (d, 1H), 6.99 (d, 1H), 4.15 (t, 2H), 2.72 (t, 2H), 2.51 (s, 3H), 2.50 (br s, 4H), 2.29 (br s, 4H), 2.13 (s, 3H), 1.29 (s, 12H)

As the paragraph descriping shows that 5464-12-0 is playing an increasingly important role.

Reference：
Patent; LES LABORATOIRES SERVIER; VERNALIS (R&D) LIMITED; PACZAL, Attila; SZLAVIK, Zoltan; KOTSCHY, Andras; CHANRION, Maia; MARAGNO, Ana Leticia; GENESTE, Olivier; DEMARLES, Didier; BALINT, Balazs; SIPOS, Szabolcs; (81 pag.)WO2017/125224; (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.13889-98-0,1-Acetylpiperazine,as a common compound, the synthetic route is as follows.

INTERMEDIATE 19(S)-tert-Butyl 1 -|”2-(4-acetylpiperazin- 1 -yl)-8-methylquinolin-3-yllethylcarbamateIntermediate 9 (150 mg, 0.47 mmol), 1-acetylpiperazine (300 mg, 2.34 mmol), DIPEA (0.42 mL, 2.34 mmol) and NMP (3 mL) were combined in a sealed tube and heated to 1400C for 48 h. After cooling, the reaction mixture was dissolved in a 1 :1 mixture of EtOAc and Et2O (100 mL) and washed with saturated brine (3 x 25 mL). The organic layer was dried (MgSO4) and concentrated in vacuo. Purification by column chromatography (SiO2, 0-100% EtOAc in isohexane) afforded the title compound (151 mg, 78%) as a white solid. LCMS (ES+) 413 (M+H)+.

13889-98-0, As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference：
Patent; UCB PHARMA S.A.; ALLEN, Daniel, Rees; BROWN, Julien, Alistair; BUeRLI, Roland; HAUGHAN, Alan, Findlay; LANGHAM, Barry, John; MATTEUCCI, Mizio; OWENS, Andrew, Pate; RAPHY, Gilles; SHARPE, Andrew; WO2010/133836; (2010); 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,59878-57-8

To a solution of 2-Fluoro-5-((4-oxo3,4-dihydrophthalazin-l-yl)methyl)benzoic acid (50 mg, 0.168 mmol) in DMA (1 mL) was added DIPEA (56 L, 0.336 mmol) and HBTU (64 mg, 0.170 mmol). The reaction mixture was stirred for 1 hour before addition of cyclopropylpiperazine-l-ylmethanone (0.170 mmol) was carried out. The reaction mixture was stirred at room temperature for 48 h. The reaction mixture was then extracted with DCM (3 x 5 mL) and washed with water (3 x 20 mL). The organic layers were collected, dried with MgS04 and the excess solvent removed in vacuo. Purification via reverse phase HLPC was carried out affording 4-(3-(4 (cyclopropanecarbonyl) piperazine- l-carbonyl)-4- fluorobenzy phthalazin- 1 (2//)-one (olaparib) (25 mg, 34%) as a white solid. *H NMR (400 MHz, CDCh) d = 10.65 (s, 1H), 8.44 – 8.37 (m, 1H), 7.75 – 7.61 (m, 3H), 7.34 – 7.22 (m, 2H), 6.97 (t, J = 8.9 Hz, 1H), 4.22 (s, 2H), 3.90 – 3.09 (m, 8H), 1.79 – 1.52 (s, 3H), 0.99 – 0.88 (m, 2H), 0.81 – 0.63 (s, 2H); {}1^ NMR (376 MHz, CDCb) d = – 117.6; Mp: 69 – 7lC. Data is in accordance with known literature (Menear, K.A., et al., ibid.).

59878-57-8 1-(Cyclopropylcarbonyl)piperazine 2064235, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; OXFORD UNIVERSITY INNOVATION LIMITED; GOUVERNEUR, Veronique; CORNELISSEN, Bart; WILSON, Thomas Charles; (152 pag.)WO2019/186135; (2019); 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

Example 24 2-(4-Methylpiperazin-1-yl)ethyl 4-(2,4-difluorophenyl)piperazine-1-carboxylate trihydrochloride 2-(4-Methylpiperazin-1-yl)ethyl 4-nitrophenyl carbonate (Intermediate 4; 680 mg, 2.2 mmol) was dissolved in DMF (20.mL). DIPEA (0.76 mL, 4.4 mmol) and 4-(2,4-difluorophenyl)piperazine (508 mg, 2.2 mmol) were added and the reaction mixture was stirred at room temperature for 24 hours, and the reaction mixture was then concentrated in vacuo. The residue was purified by normal phase column chromatography (eluding with DCM, followed by a 200:8:1 mixture of DCM:EtOH:NH3) followed by reverse phase column chromatography (gradient eluding with MeOH in water, with 1% formic acid in each solvent, 0-100%). The residue was dissolved in DCM (10 mL) and 2M HCl in Et2O (3 mL) was added. The reaction mixture was then concentrated in vacuo to give the title compound 2-(4-methylpiperazin-1-yl)ethyl 4-(2,4-difluorophenyl)piperazine-1-carboxylate trihydrochloride (630 mg, 65%) as a white solid. Analytical HPLC: purity 100% (System A, RT=4.02 min); Analytical LCMS: purity 100% (System A, RT=5.76 min), ES+: 369.5 [MH]+; HRMS calcd for C18H26F2N4O2: 368.2024, found 368.2038.

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

Reference：
Patent; Biovitrum AB; US2009/281087; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics