Tag: M.W:200-300

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[005961 To a stirring solution of 1 -bromo-4-(heptyloxy)benzene (447 mg. 1.65 nunol) in dioxane (5 niL) were added tert-butyl 3-oxopiperazine-1-carboxylate (330 mg, 1.65 mmol), copper I iodide (31.4 mg, 0.17 mmol), (1R,2R)-Nl .N2-dimethylcyclohexane- 1,2- diarnine (234 mg. 1.65 nmiol) and potassium carbonate (456 rng, 3.30 mmol). The reaction mixture was heated at 120C for 16 h. The reaction mixture was passed through a plug of celite, eluted with EA (50 mL). The organics were washed with ammonium chloride (25 niL), water (25 niL) and brine (25 mL) then dried over MgSO4 and concentrated to afford 602 mg (89%) of tert-butyl 4-(4-(heptyloxy)phenyl)-3- oxopiperazine-l-carboxylate. LCMS-ESI (m/z) calculated for C22H34N204: 390.5; found 319.0 [M+Hf. 1R= 2.90 mi (i1vlethod4).

76003-29-7, The synthetic route of 76003-29-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CELGENE INTERNATIONAL II SARL; BOEHM, Marcus, F.; MARTINBOROUGH, Esther; MOORJANI, Manisha; TAMIYA, Junko; HUANG, Liming; YEAGER, Adam, R.; BRAHMACHARY, Enugurthi; FOWLER, Thomas; NOVAK, Andrew; MEGHANI, Premji; KNAGGS, Michael; GLYNN, Daniel; MILLS, Mark; (851 pag.)WO2016/94729; (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.502649-29-8,1-Boc-3-Benzylpiperazine,as a common compound, the synthetic route is as follows.

To a flask was added tert- butyl 3-benzylpiperazine-1-carboxylate (CAS: 502649-29-8, Vendor: BePharm, 300 mg, 1.09 mmol), TEA (330 mg, 454 pL, 3.26 mmol) and DCM (2 mL). Then it was cooled with ice bath and Cbz-Cl (278 mg, 232 pL, 1.63 mmol) was added drop-wise. After being warmed to rt slowly and stirred for 2 hrs, the reaction mixture was diluted with 20 mL water and extracted with EA (15 mL) twice, the organic layer was dried over Na2S04 and concentrated to give a brown oil. After purification by flash column (EA/PE= 0 to 20%), the compound 39a (268 mg) was obtained as an oil. MS: calc’d 411 (MH+), measured 411 (MH+)., 502649-29-8

Big data shows that 502649-29-8 is playing an increasingly important role.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; LIU, Haixia; SHEN, Hong; ZHU, Wei; HU, Taishan; ZHANG, Zhisen; ZHANG, Zhiwei; DEY, Fabian; WANG, Xiaoqing; (89 pag.)WO2019/238629; (2019); 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.132710-90-8,1-Boc-4-(3-hydroxypropyl)piperazine,as a common compound, the synthetic route is as follows.

e-1 – carboxylate0.61 ml (3.07 mmol) of diisopropyl diazene-l,2-dicarboxylate is added drop by d r o p a t 0 C under argon to 0.5 g (2.05 mmol) of tert-butyl 4-(3- hydroxypropyl)piperazine-l -carboxylate, 0.3 g (2.46 mmol) of 4-hydroxybenzaldehyde and 1 g (3.07 mmol) of supported triphenylphosphine (3 mmol/g of resin) diluted in 14.5 ml of anhydrous tetrahydrofuran. The reaction mixture is stirred at room temperature for 20 hours, and then the solid is filtered and rinsed with dichloromethane. The filtrate is concentrated and diluted in sodium hydroxide solution (1 M), the product is extracted several times with ethyl acetate, and then the organic phases are combined, dried on magnesium sulfate and concentrated. The residue is purified by silica gel chromatography (eluent: 4:6 cyclohexane/ethyl acetate to 100% ethyl acetate) to yield 0.58 g of tert-butyl 4-(3-(4-formylphenoxy)propyl)piperazine-l -carboxylate in the form of a colorless oil.LCMS (ESI, m/z): (M+l) 348.91H MR: 6H pm 400 MHz, DMSO: 9.87 (1H, s, CHO), 7.86 (2H, d, CHarom), 7.12 (2H, d, CHarom), 4.13 (2H, t, CH2), 3.28-3.31 (4H, m, 2CH2), 2.44 (2H, t, CH2), 2.31-2.34 (4H, m, 2CH2), 1.91 (2H, q, CH2), 1.40 (9H, s, 3CH3)., 132710-90-8

132710-90-8 1-Boc-4-(3-hydroxypropyl)piperazine 16217800, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; PIERRE FABRE MEDICAMENT; RABOT, Remi; BEDJEGUELAL, Karim; KALOUN, El Bachir; SCHMITT, Philippe; RAHIER, Nicolas; MAYER, Patrice; FOURNIER, Emmanuel; WO2012/140114; (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.53788-49-1,tert-Butyl 4-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,53788-49-1

Deprotection; A solution of 1:1 TFA, DCM with 0.5% water was prepared. This solution was added to the material isolated from the reduction, above (10 mL/g starting material). The reaction was stirred for 30 minutes then the solvent was removed with a rotoevaporator. Solvent evaporation was terminated when no more solvent was observed to be collecting on the condenser. TFA was added to the product residue (2 mL/g starting material) to form a free flowing solution. The TFA solution was transferred to a centrifuge tube and diethyl ether was added to precipitate the product salt. The solution was mixed using a vortex. The solution was then centrifuged and the supernatant decanted to collect the precipitate. The filtrate was then washed 1 time with ether by resuspending the product, vortexing, and re-centrifugation. Product was dried under low vacuum to remove residual ether.

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

Reference£º
Patent; Applera Corporation.; US2005/148774; (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.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The mixture of 4-(4-chloro-1,6-naphthyridin-2-yl)-N,N-diethylbenzamide (278 mg, 0.82 mmol), tert-butyl 4-(2-aminoethyl)piperazine-1-carboxylate (281 mg, 1.23 mmol) and K2C03 (226 mg, 1.64 mmol) in DMF (1 mL) was heated at 100¡ãC for l8hrs. The reaction mixture was poured into water (20 mL), extracted with EA (10 mL x 3). The combined organic layers were washed by water (10 mL x 3) and brine (10 mL), dried over Na2SO4. Filtered and the filtrate was concentrated under the reduced pressure to give the residue which was purified prep-TLC to afford tert-butyl 4-(2-(2-(4- (diethylcarbamoyl)phenyl)- 1 ,6-naphthyndin-4-ylamino)ethyl)piperazine- 1 -carboxylate (90 mg, 20percent). LC-MS (ESI): 533.3(M + 1)., 192130-34-0

As the paragraph descriping shows that 192130-34-0 is playing an increasingly important role.

Reference£º
Patent; SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE; PINKERTON, Anthony B.; ARDECKY, Robert J.; ZOU, Jiwen; (256 pag.)WO2018/204176; (2018); 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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

Example 97′ {3-[6-(6-Methoxy-pyridin-3-yl)-quinazolin-4-yl]-phenyl}-((R)-2-methyl-piperazin-1-yl)-methanone To a stirred solution of 3-[6-(6-methoxy-pyridin-3-yl)-quinazolin-4-yl]-benzoic acid (100 mg, 0.254 mmol) in 2 mL of DMF, was added HBTU (144 mg, 0.381 mmol) and DIPEA (0.177 mL, 1.016 mmol). The reaction mixture was stirred at rt for 30 min, (R)-3-methyl-piperazine-1-carboxylic acid tert-butyl ester (76 mg, 0.381 mmol) was added and the resulting reaction mixture stirred for a further 2 h at rt. The reaction was quenched with H2O, and extracted with CH2Cl2. The organic layer was washed with brine, dried over MgSO4, filtered and evaporated under vacuum. The residue was dissolved in 3 ml of CH2Cl2 and TFA (1 ml) was added. The reaction mixture was stirred at ambient temperature for 2 h. After this period of time, the mixture was concentrated and purified by preparative reverse phase Gilson HPLC and subsequent neutralization of the combined fractions over PL-HCO3 MP gave the title compound (29 mg, 26% yield) as a white powder. 1H-NMR (400 MHz, DMSO-d6, 298 K): delta ppm 1.23 (d, 3H) 2.55-3.2 (m, 7H) 3.91 (s, 3H) 6.95 (d, 1H) 7.62 (d, 1H) 7.72 (t, 1H) 7.81 (s, 1H) 7.98 (d, 1H) 8.11 (d, 1H) 8.22 (d, 2H) 8.38 (d, 1H) 8.59 (s, 1H) 9.38 (s, 1H). MS: 440.1 [M+1]+, Rt(2′)=0.89 min.

163765-44-4, As the paragraph descriping shows that 163765-44-4 is playing an increasingly important role.

Reference£º
Patent; NOVARTIS AG; COOKE, Nigel Graham; FERNANDES GOMES DOS SANTOS, Paulo Antonio; FURET, Pascal; HEBACH, Christina; HOGENAUER, Klemens; HOLLINGWORTH, Gregory; KALIS, Christoph; LEWIS, Ian; SMITH, Alexander Baxter; SOLDERMANN, Nicolas; STAUFFER, Frederic; STRANG, Ross; STOWASSER, Frank; TUFFILLI, Nicola; VON MATT, Anette; WOLF, Romain; ZECRI, Frederic; US2015/342951; (2015); 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.118753-66-5,tert-Butyl 4-aminopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

(ii) 4-({1-[5-(5-Chloro-thiophen-2-yl)-isoxazol-3-ylmethyl]-1H-indole-2-carbonyl}-amino)-piperazine-1-carboxylic acid tert-butyl ester To a solution of 1 g 1-[5-(5-Chloro-thiophen-2-yl)-isoxazol-3-ylmethyl]-1H-indole-2-carboxylic acid and 1.3 ml NEM in 8 ml DCM, 914 mg TOTU were added and the mixture was stirred for 30 min at RT. Then 673 mg 4-Amino-piperazine-1-carboxylic acid tert-butyl ester were added and the reaction was stirred over night. After removal of the solvent under reduced pressure the residue was directly purified by chromatography on silica gel eluding with an ethyl acetate/heptane gradient. Yield: 1.1 g., 118753-66-5

The synthetic route of 118753-66-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Nazare, Marc; Essrich, Melanie; Will, David William; Matter, Hans; Ritter, Kurt; Wehner, Volkmar; US2003/199689; (2003); A1;,
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Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Amine 15 (hydrochloride) (4.3 mmol) was dissolved in CH2Cl2 (5 ml), and the solution was cooled with an ice bath. A solution of ethyl chloroglyoxylate (4.7 mmol) in CH2Cl2 (2 ml) was added dropwise, and the mixture was stirred at 0C for 0.5-1 hour. The reaction solution was diluted with ethyl acetate. The organic layer was washed with an aqueous saturated sodium chloride solution and dried with anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure to obtain crude product. This crude product was dissolved in ethanol (13 ml), 2 mol/L sodium hydroxide (6.5 ml 13 mmol) was added, and the mixture was stirred at room temperature for 1.5 hour. The solvent was distilled off under reduced pressure, and 2 mol/L hydrochloric acid was added to the residue to acidic, and the precipitated crystal was collected by filtration. The crystal was washed with water and dried to obtain carboxylic acid 16 (yield 77-99%). To carboxylic acid 16 (1.0 mmol) were added DMF (10 ml), aniline (1.2 mmol), HOBt (1.2 mmol), triethylamine (1.2 mmol), DMAP (0.05 mmol) and WSCD¡¤HCl (1.2 mmol). The mixture was stirred at room temperature for overnight. An aqueous saturated sodium bicarbonate solution was added, and the aqueous layer was extracted with EtOAc. The organic layer was washed with brine, dried over MgSO4, and concentrated under reduced pressure. The residue was purified by amino silica gel column chromatography (CHCl3/MeOH, gradient: 0-10% MeOH) to afford oxamide 6a-v (yield 46-91%).

30459-17-7, 30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Anan, Kosuke; Masui, Moriyasu; Tazawa, Aya; Tomida, Minoru; Haga, Yoshihiro; Kume, Masaharu; Yamamoto, Shoichi; Shinohara, Shunji; Tsuji, Hiroki; Shimada, Shinji; Yagi, Shigenori; Hasebe, Nobuyoshi; Kai, Hiroyuki; Bioorganic and Medicinal Chemistry Letters; vol. 29; 9; (2019); p. 1143 – 1147;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

548762-66-9,548762-66-9, (2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 4-fluorobenzoyl chloride(1.0 g, 7.14 mmol) in acetonitrile (10 mL) were added DIPEA (3.74 mL, 21.41 mmol) and HATU (3.53 g, 9.28 mmol) at room temperature. After 30 min., tert-butyl (2S,5R)-2,5-dimethylpiperazine-1- carboxylate (1.83 g, 8.56 mmol) was added and the reaction mixture was stirred overnight. The reaction mixture was concentrated under reduced pressure to remove volatiles and the residue dissolved in ethyl acetate (100 mL) and washed with water (50 mL). The aqueous layer was back extracted with ethyl acetate (100 mL x 2) and the combined organic layer was washed with brine, dried over anhydrous Na2SO4, concentrated under reduced pressure to obtain the crude product, which was purified by silica gel chromatography (50-100% EtOAc in petroleum ether; 40 g column) to afford tert-butyl (2S,5R)-4-(4-fluorobenzoyl)-2,5-dimethylpiperazine-1-carboxylate (1.99 g, 83 % yield). LCMS: m/z = 337.1 (M+H); retention time 1.62 min. [LCMS Condition: Column: Waters Acquity UPLC BEH C18 (2.1 x 50 mm) 1.7 mm, Mobile phase A: 10 mM NH4OAc:acetonitrile (95:5); Mobile phase B: 10 mM NH4OAc:acetonitrile (5:95), Gradient = 20-90 % B over 1.1 minute, then a 0.6 minute hold at 90 % B; Temperature: 50 C; Flow rate: 0.7 mL/min; Detection: UV at 220 nm].

As the paragraph descriping shows that 548762-66-9 is playing an increasingly important role.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; VELAPARTHI, Upender; CHUPAK, Louis S.; DARNE, Chetan Padmakar; DING, Min; GENTLES, Robert G.; HUANG, Yazhong; KAMBLE, Manjunatha Narayana Rao; MARTIN, Scott W.; MANNOORI, Raju; MCDONALD, Ivar M.; OLSON, Richard E.; RAHAMAN, Hasibur; JALAGAM, Prasada Rao; ROY, Saumya; TONUKUNURU, Gopikishan; VELAIAH, Sivasudar; WARRIER, Jayakumar Sankara; ZHENG, Xiaofan; TOKARSKI, John S.; DASGUPTA, Bireshwar; REDDY, Kotha Rathnakar; RAJA, Thiruvenkadam; (0 pag.)WO2020/6018; (2020); 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.300543-56-0,(R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine,as a common compound, the synthetic route is as follows.

A mixture containing (4-chlorophenyl)phenyl methylamine free base (4.1 g, 18.8 mmol), N,N-bis(2-chloroethyl)benzyl carbamate (7 g, 26.7 mmol) potassium iodide (1.7 g, 10 mmol) and diisopropyl ethylamine (10 ml) was stirred at 135 C. (oil bath), for 4 hours.While cooling down, 60 ml dichloromethane was added. The mixture was stirred at ambient temperature for 20 min. 35 ml HCl (1M) was added to the dichloromethane. The organic layer was separated, washed with NaCl (10 ml) dried and concentrated to give an oily material (10 g). The impure material was purified with AcOEt/heptane column (3?50%).0.5 grams of above pure material was dissolved in a solution containing 1.3 g NaOH in 1.2 ml H2O and 5 ml 2-propanol. The mixture was heated til 100 C. for 5 h. The mixture was concentrated in vacuo to get rid of 2-propanol and redissolved in 10 ml toluene and 5 ml H2O. The mixture was stirred for 20 min and layers were separated. The organic layer was dried over Na2SO4 and concentrated. To the crude product ethyl acetate (10 ml) was added, followed by addition of 0.2 g oxalic acid dissolved in 1 ml EtOH. The suspension was stirred 4 h at ambient temperature and overnight at 5 C. The solid obtained was filtered off and dried at air to give a solid material (0.3 g, 38.5% yield). 98.86% ee purity.

300543-56-0, 300543-56-0 (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine 668697, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Zhu, Jie; US2009/143582; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics