Heterocyclic Building Blocks-piperazine

502649-32-3, 1-Boc-3-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

502649-32-3, A solution of compounds of general structure 1 (1 equiv), Boc protected amine (1-3 equiv) and DIPEA (3 equiv) in DMSO were reacted at 100-110 C. The reaction mixture was cooled to room temperature and quenched by addition of water and crude residue extracted with EtOAc. Combined organic layers were washed with brine, dried over Na2S04, filtered and concentrated under reduced pressure to provide crude compound of general strucutre 2, which was used in the following step without further purification. To a solution of compounds of general structure 2 in CH2C12 was added HCl/dioxane (4 N) or TFA. The reaction was stirred at room temperature for 2 hrs and mixture was concentrated under reduced pressure. The residue was purified by reverse phase preparative HPLC to afford final compounds of general structure 3.

The synthetic route of 502649-32-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; KADMON CORPORATION, LLC; SKUCAS, Eduardas; LIU, Kevin, G.; KIM, Ji-In; POYUROVSKY, Masha, V.; MO, Rigen; (345 pag.)WO2019/45824; (2019); A1;,
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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 round bottom flask containing 2-(4,4,5,5-Tetramethyl-l,3,2-dioxaborolan-2-yl)benzoic acid (1.00 g, 4.03 mmol) was added DCM (40 mL), diisopropylethylamine (1.05 mL, 6.04 mmol) and HBTU (2.29 g, 6.04 mmol). The reaction mixture was stirred for 30 min before adding cyclopropylpiperazine-l-ylmethanone (0.86 mL, 6.04 mmol). The reaction was stirred overnight before the excess solvent with removed in vacuo and the crude material purified via flash column chromatography (EtOAc:MeOH 10:1) affording (4- (Cyclopropanecarbonyl)piperazin-l-yl)(2-(4,4,5,5-tetramethyl-l,3,2-dioxaborolan-2- yl)phenyl)methanone as a white solid (1.08 g, 2.82 mmol, 70%) in a mixture of rotamers (2:1). The shifts relating to the minor rotamer has been donated with an asterisk.* *H NMR (400 MHz, CDCh) d = 7.81 (d, J = 7.4 Hz, 1H + 1H*), 7.45 (td, J = 7.6, 1.5 Hz, 1H + 1H*), 7.35 (td, / = 7.5, 1.3 Hz, 1H + 1H*), 7.22 (d, J = 7.5 Hz, 1H + 1H*), 3.86 – 3.69 (m, 4H, 4H*), 3.67 – 3.50 (m, 2H, 2H*), 3.34 – 3.07 (m, 2H, 2H*), 1.81 – 1.52 (m, 1H + 1H*), 1.29 (s, 12H + 12H*), 1.04 – 0.95 (m, 2H + 2H*), 0.67 – 0.87 (m, 2H + 2H*); 13C NMR (100 MHz, CDCh) d = 172.3 (1C + 1C*), 171.3 (1C + 1C*), 142.3 (1C + 1C*), 135.7 (1C + 1C*), 131.2 (1C + 1C*), 128.2 (1C + 1C*), 125.4 (1C + 1C*), 84.1 (2C + 2C*), 47.3 (1C*), 47.0, 45.2 (1C*), 44.9, 41.9 (2C), 41.6 (2C*) 24.9 (4C + 4C*), 11.0 (1C + 1C*), 7.65 (2C + 2C*) (the carbon bearing the boron substituent is not observed); IR (v, cm 1): 2970, 1634, 1467, 1213, 1014, 741; HRMS (ESI) for C2iH3o10BN204 [M+H]+ requires 384.2220 found 384.2218; Mp: 85 – 87C.

As the paragraph descriping shows that 59878-57-8 is playing an increasingly important role.

Reference£º
Patent; OXFORD UNIVERSITY INNOVATION LIMITED; GOUVERNEUR, Veronique; CORNELISSEN, Bart; WILSON, Thomas Charles; (152 pag.)WO2019/186135; (2019); A1;,
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25057-77-6, 1,2-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5-Chloro-N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]pyrazine-2-carboxamide (388 mg, 1.00 mmol) was added in one portion to 1,2-dimethyl-piperazine (228 mg, 2.00 mmol) in anhydrous dimethylsulfoxide (2.00 ml) at 25 C. The resulting solution was stirred at ambient temperature for 2 h. The residue was purified by ion exchange chromatography, using an SCX column. The desired product was eluted from the column using 7M NH3/MeOH to afford impure material. The concentrated eluent was purified by silica column chromatography, eluting with a gradient of 0 to 10% 7M NH3/MeOH in DCM. Pure fractions were evaporated to dryness to afford the title compound (375 mg, 81%) as a yellow solid. 1H NMR (399.9 MHz, DMSO-d6) delta 1.07-1.09 (3H, d), 2.06-2.20 (2H, m), 2.23 (3H, s), 2.76-2.86 (2H, m), 2.87 (4H, s), 3.13-3.19 (1H, m), 3.72 (6H, s), 4.27-4.30 (2H, m), 6.33 (1H, t), 6.42 (2H, d), 6.46 (1H, s), 8.35 (1H, d), 8.70 (1H, d), 9.75 (1H, s), 12.18 (1H, s). MS: m/z 466 (MH+). Mean of n=1, FGFR Kinase assay-Caliper Echo Dosing, IC50 0.0022 muM., 25057-77-6

25057-77-6 1,2-Dimethylpiperazine 198037, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; US2008/153812; (2008); A1;,
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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.

A mixture of intermediate 47 (0.49 g; 0.85 mmol) and cis 2,6-dimethylpiperazine (0.2 g; 1.7 mmol) in MeOH (6 mL) was stirred at room temperature overnight. Sodium triacetoxyborohydride (0.54 g; 2.6 mmol) was added to the reaction mixture and stirred 3 hours at room temperature. The solution was poured into cooled water and basified with K2CO3 powder and the product was extracted with EtOAc. The organic layer was separated, dried over MgSC , filtered and evaporated to dryness. The residue (0.625 g) was purified by chromatography over silica gel (Irregular SiOH, 15-40 muiotaeta, gradient from 97percent DCM 3percent CH3OH 0.1percent NH4OH to 85percent DCM 15percent CH3OH 0.1percent NH4OH). The fractions containing the product were collected and evaporated to dryness to afford 0.347 g (61percent) of intermediate 49., 21655-48-1

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

Reference£º
Patent; JANSSEN PHARMACEUTICA NV; MEVELLEC, Laurence, Anne; MEERPOEL, Lieven; COUPA, Sophie; PONCELET, Virginie, Sophie; PILATTE, Isabelle, Noelle, Constance; PASQUIER, Elisabeth, Therese, Jeanne; BERTHELOT, Didier, Jean-Claude; QUEROLLE, Olivier, Alexis, Georges; MEYER, Christophe; ANGIBAUD, Patrick, Rene; DEMESTRE, Christophe, Gabriel, Marcel; MERCEY, Guillaume, Jean, Maurice; (203 pag.)WO2016/97359; (2016); A1;,
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414910-15-9, tert-Butyl 4-(cyclopropanecarbonyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1-Tertbutoxycarbonyl-4-(cyclopropanecarbonyl) piperazine (190 mg, 0.75 mmol) was dissolved in dichloromethane, and then trifluoroacetic acid (1 mL) was added. The reaction mixture was stirred at room temperature until complete reaction, and then washed with saturated sodium bicarbonate solution for three times. The organic phases were concentrated to give 112 mg (yield 97%) pale yellow solid of N-(cyclopropanecarbonyl) piperazine for use.

414910-15-9, As the paragraph descriping shows that 414910-15-9 is playing an increasingly important role.

Reference£º
Patent; Chengdu Di’ao Pharmaceutical Group Co. Ltd.; JI, Jianxin; GUO, Na; XUE, Ting; KANG, Bingqiang; YE, Xinfa; CHEN, Xin; ZHANG, Tao; EP2799435; (2014); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

EXAMPLE 7 9-{4-[4-(4-Trifluoromethyl-phenyl)-piperazin-1-yl]-butyl}-9H-fluorene-9-carboxylic acid-(2,2,2-trifluoroethyl)-amide Prepared analogously to Example 2 b from 1-(4-trifluoromethyl-phenyl)-piperazine and 9-(4-bromo-butyl)-9H-fluorene-9-carboxylic acid-(2,2,2-trifluoroethyl)-amide. Yield: 0.23 g (48.7% of theoretical). Melting point: 176 C., 30459-17-7

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

Reference£º
Patent; Boehringer Ingelheim Pharm GmbH & Co, KG; US6818644; (2004); B1;,
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Piperazines – an overview | ScienceDirect Topics

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 is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2-(lH-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4- chlorophenyl)-4,4-dimethylcyclohex- 1 -enyl)methyl)piperazin- 1 -yl)benzoic acid( 16g,28mmol) and 3-nitro-4-((tetrahydro-2H-pyran-4-yl)methylamino)benzenesulfonamide(8.83g, 28mmol) in DCM(300mL) was added EDCI(10.74g, 56mmol) and DMAP(6.85g, 56mmol). The mixture was stirred at r.t. overnight. LC/MS showed the expected product as a single peak. The mixture was diluted with DCM(500ml) and washed with aq. NaHC03, water, brine and dried over Na2S04. The residue after evaporation of solvent was dissolved in DCM and loaded on a column and eluted with 30% ethyl acetate in DCM followed by 1 to 2% MeOH in DCM to give 24.5g pure product(95% purity) which was dissolved in DMSO and MeOH(l :l) and TFA(2eq) and loaded on a 330g C18 column (6g a time)to give 13.5g pure(>99.7% purity) product(55%yield). The API was extracted using dichloromethane and then, the solvent was removed using rotary evaporator. The resulting solid was suspended in acetonitrile at ambient temperatures to reach its solubility. After equilibrating, the solids were isolated at ambient temperature., 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 fields.

Reference£º
Patent; ABBOTT LABORATORIES; CATRON, Nathaniel D.; CHEN, Shuang; GONG, Yuchuan; ZHANG, Geoff G.; WO2012/71336; (2012); A1;,
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Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.,74879-18-8

[1646] A solution of (S)-(+)-2-methylpiperazine (0.50 g, 0.005 mol, CAS 74879-18-8, Aldrich 39,717-2, 99%) and 2-bromopyridine (5 mL, 0.05 mol) was heated to 120 C. for 14 hours. The reaction mixture was cooled to 23 C. and partitioned between ethyl acetate and water. The layers were separated, and the water layer extracted twice more with ethyl acetate. The aqueous phase was adjusted to pH 11 with a solution of saturated sodium bicarbonate and solid sodium carbonate. Sodium chloride was added, and the saturated aqueous solution was extracted with ethyl acetate (2¡Á) and dichloromethane (2¡Á). The combined organic extracts were dried over sodium sulfate, filtered, and concentrated under reduced pressure to afford 0.6 g (67% yield) of the title compound. 1H NMR (400 MHz, DMSO-d6) delta1.02 (d, J=6.0 Hz, 3H), 2.27 (dd, J=12, 10 Hz, 1H), 2.67 (m, 3H), 2.92 (m, 1H), 4.07 (m, 2H), 6.58 (dd, J=8, 6 Hz, 1H), 6.77 (d, J=8 Hz, 1H), 7.49 (m, 1H), 8.08 (m, 1H); MS (ESI) m/e 178 (M+H)+.

74879-18-8 (S)-(+)-2-Methylpiperazine 2734219, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Bhatia, Pramila A.; Daanen, Jerome F.; Hakeem, Ahmed A.; Kolasa, Teodozyj; Matulenko, Mark A.; Mortell, Kathleen H.; Patel, Meena V.; Stewart, Andrew O.; Wang, Xueqing; Xia, Zhiren; Zhang, Henry Q.; US2003/229094; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

639068-43-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.639068-43-2,tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

General procedure: To a stirred solution of compound 13a-b, 17a-b (1.0 mmol) inCH3CN (20 mL) were added N-Boc-piperazine (180.9 mg,0.9 mmol), K2CO3 (205.9 mg, 1.5 mmol), KI (166.0 mg, 1.0 mmol)and 18-crown-6 (26.4 mg, 0.1 mmol) at room temperature. Themixture was stirred overnight at 80 C and filtered. The filtrate wasdiluted by DCM and washed by brine. The organic layer was concentrated for next step. To a stirred solution of the abovecompounds in DCM (20 mL) was added TFA (3 mL) at room temperature.The mixture was stirred for 3e4 h and concentrated toafford the crude products 15a-o and 19a-f in a yield of 35%e42%. Toa stirred solution of above crudes in anhydrous MeOH (10 mL) wasadded BTZ core compound 11 (403.2 mg, 1.0 mmol) and Et3N(0.2 mL, 1.5 mmolj) at room temperature. The mixture was stirredfor 1e3 h at 40 C and concentrated. The residue was purified bysilica gel column (DCM: MeOH 20: 1) to give 1a-f and 2a-e (25%e41% for two steps).

The synthetic route of 639068-43-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Wang, Apeng; Lv, Kai; Tao, Zeyu; Gu, Jian; Fu, Lei; Liu, Mingliang; Wan, Baojie; Franzblau, Scott G.; Ma, Chao; Ma, Xican; Han, Bing; Wang, Aoyu; Xu, Shijie; Lu, Yu; European Journal of Medicinal Chemistry; vol. 181; (2019);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

142-64-3, Piperazine Dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A 250 mL round bottom flask was charged with 40 mmol of compound (4), 80 mL of tetrahydrofuran and n-hexane (v / v = 1: 1)20 mmol of compound (2) (R is ethyl) was added dropwise under stirring at 20 C for 1 hour. The mixture was heated to reflux for further stirring. After about 6 hours, the solid no longer increased. The mixture was distilled and ethanol was distilled off to recover the compound 2) (R is ethyl). The solution was cooled to below 30 C and an ethanol solution containing 60 mmol of sodium ethoxide in 30% sodium ethoxide was added dropwise. The mixture was stirred for another hour after the addition was completed for 1 hour. , Ethanol, and piperazine (3). The product was distilled off under reduced pressure to give a pale yellow transparent liquid to obtain piperazine methylmethyldiethoxysilane represented by the formula (1) (R is an ethyl group) b in a yield of 88 % (In (2) dollars), high performance liquid chromatography analysis content of 98.5%.

142-64-3, 142-64-3 Piperazine Dihydrochloride 8893, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Yancheng Technology College; Sun Guoxiang; (6 pag.)CN106046041; (2016); A;,
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Piperazines – an overview | ScienceDirect Topics