Month: September 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

Example 54 – Preparation of Intermediate 19 The synthesis of Intermediate 19 followed the procedure of General Procedure 15 following: Intermediate 18 Intermediate 19 To a cooled solution (0C) of 1-tert-butyl 2-methyl piperazine-1,2-dicarboxylate (Intermediate 18, 3.5 g, 14.3 mmol) in dry dichloromethane (70 mL) was added triethylamine (TEA, 5 mL, 35.9 mmol) followed by morpholine-4-carbonyl chloride (3.35 mL, 28.7 mmol). The reaction mixture was stirred at room temperature for 3 hours. To the mixture was added ice-cold water (20 mL), then it was extracted into EtOAc (2 x 50 mL). The combined organic layers were dried over sodium sulfate, filtered and concentrated under reduced pressure. The crude residue was purified by flash chromatography using 30% EtOAc/n-hexane to afford 1-tert-butyl 2-methyl 4- (morpholine-4-carbonyl)piperazine-1,2-dicarboxylate (Intermediate 19, 3.6 g, yield: 72%) as an off white solid; TLC: 50% ethyl acetate in hexane. Rf-0.5.

129799-15-1, 129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; VERSEON CORPORATION; SHORT, Kevin Michael; ESTIARTE-MARTINEZ, Maria de los Angeles; KITA, David Ben; SHIAU, Timothy Philip; (340 pag.)WO2016/138532; (2016); A1;,
Piperazine – Wikipedia
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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.

N-(5-tert-Butylisoxazol-3-yl)-N- {3- [ (2-chloropyrimidin-5-yl) ethynyl] phenyl} urea (Intermediate 9) (0.22 g) and tert-butyl 4-(2-aminoethyl)-piperazine-1-carboxylate (0.38 g) were stirred in MeCN (10 mL) and hydrogen chloride (I. OM solution in ether) (0.11 mL) was added dropwise. The reaction mixture was stirred and heated at 70¡ãC for 4 hours. The solvent was evaporated and the residue was dissolved in DCM (20 mL) and TFA (10 mL). The reaction mixture was stirred at ambient temperature for 2 hours, the solvent was evaporated and the product was purified by flash chromatography on silica using 1-20percent (7N NH3 in MeOH) in DCM as eluent. The product was triturated with ether to give the title compound as an off-white solid (274 mg, 99percent); ‘H NMR (DMSO-d6) 1.29 (s, 9H), 2.45-2. 57 (m, 2H), 2.57-2. 65 (m, 4H), 3.03-3. 10 (m, 4H), 3.39-3. 49 (m, 2H), 6.49 (s, 1H), 7.10-7. 16 (m, 1H), 7.29-7. 35 (m, 2H), 7.51 (t, 1H), 7.75 (s, 1H), 8.40-8. 52 (m, 3H), 8.99 (s, 1H), 9.62 (s, 1H) ; MS m/e MH+ 489.

192130-34-0, 192130-34-0 tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate 1514400, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/60970; (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.25057-77-6,1,2-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

To a stirred solution of (S)-l, 2-dimethylpiperazine (45g, 190.6mmol, leq) in EtOH (450mL) was added TEA (106.9mL, 762.7mmol, 4eq) under argon for 20min., then followed by addition of l-bromo-2,4-difluoro-5-nitrobenzene (47.8g, 286.0mmol, 1.5eq) at RT under argon atm and heated to 85C for 16h. TLC analysis indicated formation of less polar spot, then the reaction mixture was cooled to RT and solvent was evaporated under reduced pressure to give crude product, which was purified by column chromatography (silica gel, 100-200 mesh) using 0-30% EtOAc in pet ether as an eluent to afford (S)-4-(4-bromo-5-fluoro-2-nitrophenyl)-l,2- dimethylpiperazine (42g, 92%) as a yellow solid. LCMS: [M+H]+ 332.0.

25057-77-6, As the paragraph descriping shows that 25057-77-6 is playing an increasingly important role.

Reference£º
Patent; ONTARIO INSTITUTE FOR CANCER RESEARCH (OICR); AL-AWAR, Rima; ZEPEDA-VELAZQUEZ, Carlos Armando; PODA, Gennady; ISAAC, Methvin; UEHLING, David; WILSON, Brian; JOSEPH, Babu; LIU, Yong; SUBRAMANIAN, Pandiaraju; MAMAI, Ahmed; PRAKESCH, Michael; STILLE, Julia Kathleen; (1053 pag.)WO2017/147700; (2017); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.76003-29-7,1-Boc-3-Oxopiperazine,as a common compound, the synthetic route is as follows.

B) 4-(4-Iodo-benzyl)-3-oxo-piperazine-l-carboxylic acid tert-butyl ester: Sodium hydride (1.30 g, 33.5 mmol) was added to a slurry of 3-oxo-piperazine-l- carboxylic acid tert-butyl ester (6.70 g, 33.4 mmol) from step A in 25 mL dry N,N- dimethylformamide and 90 mL dry tetrahydrofuran under argon atmosphere and cooled to O0C. The mixture was stirred at room temperature until a solution was obtained after 30 minutes. 4-Iodobenzyl bromide (9.90 g, 33.4 mmol), dissolved in 20 mL tetrahydrofuran, was added dropwise. The reaction was stirred for 1 hour to give a white slurry. Ethyl acetate and water was added. The organic phase was washed three times with water, once with brine, dried (sodium sulfate) and evaporated. The crude was purified on a silica column using dichloromethane / methanol (97 : 3) as eluent to give 12.2 g of the sub-title product (yield 87 %). 1H NMR (400 MHz, chloroform-d as solvent and internal reference) delta(ppm) 1.46 (s, 9H), 3.24 (m, 2H), 3.58 (t, 2H, J= 5.2 Hz), 4.14 (s, 2H), 4.54 (s, 2H), 7.01 (d, 2H, J= 8.3 Hz), 7.66 (d, 2H, J= 8.4 Hz)., 76003-29-7

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; WO2007/8144; (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.53788-49-1,tert-Butyl 4-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

53788-49-1, Indole-2-carboxylic acid (5.2 g) in THF (200 mL) was treated with [CARBONYIDIIMIDAZOLE] (4.8 g) and stirred at ambient temperature for 10 min whereupon [4-METHYL-PIPERAZINE-1-CARBOXYLIC] acid tert-butyl ester (5.0 g) was added. The mixture was stirred at ambient temperature for 72 h and the solvent removed under reduced pressure. The residue was dissolved in ethyl acetate and washed with saturated sodium bicarbonate solution. The organic portion was separated, dried over sodium sulfate and filtered, and solvent was evaporated to afford a solid. Recrystallization from hot ethanol afforded [4- (1 H-] lndole-2-carbonyl)-piperazine-1-carboxylic acid ter-butyl ester (4. 2 g).

As the paragraph descriping shows that 53788-49-1 is playing an increasingly important role.

Reference£º
Patent; JANSSEN PHARMACEUTICA, N.V.; WO2004/22061; (2004); 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.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: In a 1 L round-bottom flask with a magnetic stir bar, compound 7 (46 g, 0.2014 mol, 1.0 eq.) was diluted in DIEA (41.64 mL, 0.2416 mol, 1.2 equivalents) and THF (700 mL). Solid N-Boc piperazine (39.38 g, 0.2114 mol, 1.05 eq.) was slowly added in portions. A mild exothermic reaction was observed. The reaction mixture was allowed to stir at room temperature for 2 hours then was quenched with saturated NaCl solution (100 mL), water (400 mL), and EtOAc (500 mL). The layers were separated and the aqueous layer was extracted with EtOAc (2 x 200 mL). The combined organic layers were dried (Na2SO4) and concentrated to give a gray solid. The crude solid was stirred in 2:1 TBME/hexanes (300/150 mL) overnight. The solids were filtered then washed with hexane (250 mL) to recover 52 g of impure product. The TBME/hexanes slurry was repeated to recover 46 g (59%) of compound 8. All remaining impure material was combined and purified via silica gel chromatography (4:1 hexane/EtOAc) to recover another 11.2 g (14%) of 8 for a total combined yield of 57.2 g (74%).

259808-67-8, 259808-67-8 1-Boc-3,3-Dimethylpiperazine 22710387, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; ARAXES PHARMA LLC; DENG, Xiaohu; LI, Liansheng; LONG, Yun Oliver; LIU, Yuan; REN, Pingda; MANI, Neelakandha S.; ALLISON, Brett D.; SALES, Zachary S.; LIANG, Jimmy T.; (71 pag.)WO2017/100546; (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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Reference Example 10 benzyl 3-methylpiperazine-1-carboxylate A 4 g portion of 2-methylpiperazine was dissolved in 40 ml of dichloromethane, and 1.71 g of benzyl chloroformate was added dropwise thereto at -78 C. After 1 hour of stirring, the mixture was washed by adding water and dried and then the solvent was evaporated to obtain 2.0 g of the title compound., 109-07-9

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

Reference£º
Patent; Yamanouchi Pharmaceutical Co. Ltd.; US6673799; (2004); B1;,
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.1235865-77-6,2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

Solution preparation prior to reaction: 10% Acetic Acid:Acetic Acid (37 mL) in water (333 g); 5% NaHCO3:NaHCO3 (9 g) in water (176 g); 5% NaCl:NaCl (9 g) in water (176 g). Compound (N) (13.5 g), DMAP (10.5 g), EDAC (10.7 g) and dichloromethane (300 mL) were combined in a suitable reactor and agitated at 25 C. In a second suitable reactor was charged the Acid (Compound (L), 25 g), Et3N (8.7 g) and dichloromethane (120 mL). The resulting Acid (Compound (L)) solution was slowly charged to the initial suspension of Compound (N) and agitated until reaction completion. N,N-dimethylethylenediamine (9.4 g) was then charged to the reaction mixture with continued agitation. The reaction mixture was warmed to 35 C. and washed with 10% Acetic acid solution (185 mL) twice. The lower organic layer was diluted with more dichloromethane (75 mL) and methanol (12.5 mL). The organic, product layer was then washed with 5% NaHCO3 solution (185 mL) and then washed with 5% NaCl solution (185 mL) at 35 C. The lower, organic layer was separated and then concentrated to 8 vol (256 mL) diluted with methanol (26 mL) and warmed to 38 C. Ethyl Acetate (230 mL) was slowly charged. The resulting suspension was slowly cooled to 10 C. and then filtered. The wet cake was washed twice with a 1:1 mix of dichloromethane and ethyl acetate (2 vol, 64 mL). After drying the wet cake at 90 C., 32 g (84%) of Compound (I) was isolated. 1H NMR (DMSO-d6): delta 0.90 (s, 6H), 1.24 (m, 2H), 1.36 (t, J=6.4 Hz, 2H), 1.60 (m, 2H), 1.87 (m, 1H), 1.93 (s, br, 2H), 2.12 (m, 2H), 2.19 (m, 4H), 2.74 (s, br, 2H), 3.06 (m, 4H), 3.26 (m, 4H), 3.83 (m, 2H), 6.17 (d, J=2.1 Hz, 1H), 6.37 (dd, J=3.4, 1.9 Hz, 1H), 6.66 (dd, J=9.1, 2.2 Hz, 1H), 7.01 (m, 2H), 7.31 (m, 2H), 7.48 (m, 3H), 7.78 (dd, J=9.3, 2.3 Hz, 1H), 8.02 (d, J=2.61 Hz, 1H), 8.54 (d, J=2.33 Hz, 1H), 8.58 (t, J=5.9 Hz, 1H, NH), 11.65 (m, 1H).

1235865-77-6, 1235865-77-6 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid 66713100, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; ABBVIE INC.; Chan, Vincent S.; Christesen, Alan C.; Grieme, Timothy A.; Ku, Yi-Yin; Mulhern, Mathew M.; Pu, Yu-Ming M.; US2014/275540; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1228780-72-0, 1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 102A (480 mg) and EXAMPLE 1B (457 mg) were taken up in dimethoxyethane (7.5 mL) in a microwave vial. Tris(dibenzylideneacetone)dipalladium(0) (37 mg), 2-(di-tert-butylphoshpino)biphenyl (48 mg) and potassium phosphate tribasic (423 mg) were added. The vial was capped and heated in a CEM Discover microwave reactor for 30 minutes at 150 C. The crude reaction mixture was filtered through celite and concentrated. The material was dissolved in 1:1 dimethylsulfoxide:methanol and purified by HPLC., 1228780-72-0

1228780-72-0 1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine 66713599, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; ABBOTT LABORATORIES; US2010/160322; (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.21043-40-3,1-Cyclopentylpiperazine,as a common compound, the synthetic route is as follows.

(4-Cyclopentylpiperazin-1-yl)(5-nitro-3-phenyl-1H-indol-2-yl)methanone (13) The title compound was synthesized according to Representative Procedure A from 1-cyclopentylpiperazine (6.9 muL, 0.044 mmol, 1.2 equiv.), NMM (5 muL, 0.045 mmol, 1.2 equiv.) and 5-nitro-3-phenyl-1H-indole-2-carboxylic acid (10.4 mg, 0.046 mmol, 1.0 equiv.). Purification of the crude product by prep. TLC (10% MeOH/CH2Cl2 then 10% MeOH/EtOAc) provided the title compound as a yellow solid (8.9 mg, 57%): 1H NMR (400 MHz, CDCl3) delta 10.54 (s, 1H), 8.68 (d, J=2.2 Hz, 1H), 8.18 (dd, J=9.0, 2.2 Hz, 1H), 7.56-7.47 (m, 5H), 7.47-7.40 (m, 1H), 3.76 (s, 2H), 3.13 (s, 2H), 2.44 (s, 2H), 2.32 (p, J=8.1 Hz, 1H), 1.73 (d, J=17.9 Hz, 3H), 1.66-1.58 (m, 1H), 1.54-1.42 (m, 2H), 1.25 (s, 4H); HRMS (ESI-TOF+) m/z calc’d for C24H27N4O3 [M+H]+: 419.2078. found 419.2077.

21043-40-3, The synthetic route of 21043-40-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; The Scripps Research Institute; Cravatt, Benjamin F.; Niphakis, Micah J.; Lum, Kenneth; Correia, Bruno; Cognetta, Armand; Hulce, Jonathan; (156 pag.)US10168342; (2019); B2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics