Heterocyclic Building Blocks-piperazine

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.

General procedure: A mixture of Palladium() acetate (6mg, 0.22mmol) 2-dicyclohexylphosphino-2?,6? -di-i-porpoxy-1,1?-biphenyl (22mg, 0.044mmol), and cesium carbonate (0.22g, 0.68mmol) were weighted out and the vial was purged with nitrogen, the bromo-contained intermediate 8d (0.44mmol) and a series of N-containing heterocyclic compounds (0.68mmol) solved in 1,4-dioxane (15mL) were added. The mixture was stirred at 100C for 16h. The reaction was filtered, concentrated and purified by silica gel column chromatography to give 18a-38a.

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

Reference£º
Article; Cao, Zhonglian; Fu, Wei; Ma, Xiaojun; Sun, Nannan; Wang, Yonghui; Xu, Jun; Zhou, Kaifeng; Zhu, Chen; European Journal of Medicinal Chemistry; vol. 187; (2020);,
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889939-92-8, 2-(1-Methylpiperazin-2-yl)ethanol is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

889939-92-8, 974 mg of Nu,Nu-diisopropylethylamine and 724 mg of 2-(1 -methylpiperazin-2-yl)ethanol are added to a suspension of 1 g of 4-fluoro-1 -nitro-2-(propan-2-yloxy)benzene in 10 ml of acetonitrile. The reaction medium is microwave-heated at 1 10C for 6 hours and then concentrated to dryness under reduced pressure. Purification is carried out by flash chromatography on silica gel (40-63 microns), elution being carried out with a mixture of dichloromethane and methanol (100/0) to (90/10). 1 .15 g of 2-{1 -methyl-4-[4-nitro-3- (propan-2-yloxy)phenyl]piperazin-2-yl}ethanol are obtained in the form of a yellow oil.

The synthetic route of 889939-92-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SANOFI; CARRY, Jean-Christophe; CHATREAUX, Fabienne; DEPRETS, Stephanie; DUCLOS, Olivier; LEROY, Vincent; MALLART, Sergio; MELON-MANGUER, Dominique; MENDEZ-PEREZ, Maria; VERGNE, Fabrice; WO2013/150036; (2013); 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.

To a solution of II-B-3 from Step 2 in THF (2 mL), was added N-(alpha,alpha,alpha-trifluoro-p-tolyl)piperazine (187 mg, 0.81 mmol, 1.0 equiv.), followed by Et3N (1.61 mmol, 2.0 equiv.). The reaction mixture was stirred at room temperature overnight. The solvent was evaporated and the residue was purified by chromatography. 1H NMR (400 MHz, CDCl3) delta ppm: 7.75 (m, 2H), 7.58 (m, 2H), 7.48 (d, 2H), 6.90(d, 2H), 3.76 (s, 3H), 3.74 (s, 2H), 3.65 (m, 4H), 3.22 (m, 4H)., 30459-17-7

The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Kalypsys, Inc.; US2005/234046; (2005); A1;,
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438049-35-5, N-Boc-3-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 3-1, Preparation of tert-butyl (3R)-3-ethyl-4-[3-fluoro-2-(methoxycarbonyl)-4-nitrophenyl]piperazine-1-carboxylate To a solution of tert-butyl-(3R)-3-ethylpiperazine-1-carboxylate (555 mg, 2.59 mmol) and methyl 2,6-difluoro-3-nitrobenzoate (843 mg, 3.89 mmol) in DMSO (2 mL) was added DIEA (0.90 mL, 5.2 mmol). The mixture was heated at 130 C. for 1 h. The mixture was purified by C18 reversed phase column chromatography to give the title compound (813 mg, 76% yield) as a brownish yellow gum. LCMS (M+H)+: 412.3., 438049-35-5

The synthetic route of 438049-35-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Crinetics Pharmaceuticals, Inc.; HAN, Sangdon; ZHU, Yunfei; KIM, Sun Hee; ZHAO, Jian; WANG, Shimiao; (146 pag.)US2019/367481; (2019); A1;,
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57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In a 100-ml flask, 500 mg (2.68 mmol) of t-butyl piperazine-1-carboxylate was dissolved in 5 ml of water, followed by stirring. 1.6 ml of acetic acid and 1.09 g (13.4 mmol, 5.0 eq) of potassium cyanate dissolved in water were added, followed by stirring at room temperature for 4 hours. After completion of the reaction, a solid was obtained by filtration while washing with water. The solid thus obtained was dissolved in dichloromethane, and then washed with water. An organic layer was separated and washed with a NaCl aqueous solution, dehydrated and dried over MgSO4, and concentrated under reduced pressure to obtain 282 mg (46%) of a title compound., 57260-71-6

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

Reference£º
Patent; Dong-A ST Co., Ltd.; CHOI, Sung Pil; CHOI, Seul Min; SON, Byoung Hwa; KIM, Hyun Jung; KIM, Ju Mi; JANG, Byung Jun; SUNG, Ji Hyun; LEE, Ji Hye; KIM, Eunjin; KANG, Kyung Koo; KIM, Soon-Hoe; (142 pag.)EP3135669; (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.21091-98-5,(4-Methylpiperazin-1-yl)(4-nitrophenyl)methanone,as a common compound, the synthetic route is as follows.

Step: 3A-2Synthesis of (4- Amino-phenyl)-(4-methy 1-piperazin-l – l)-methanone.Procedure:Pd-C (150mg) was added to a solution of (4-Methyl-piperazin-l-yl)-(4-nitro-phenyl)- methanone (440mg, 1.7670mmol) in MeOH and stirred for 2hrs in a hydrogen atmosphere. The reaction was monitored by the TLC (10% MeOH: CHC13). The resultant was filtered through celite bed and concentrated to afford 380mg (98% yield) of (4-Amino-phenyl)-(4- methyl-piperazin- 1 -y l)-methanone., 21091-98-5

As the paragraph descriping shows that 21091-98-5 is playing an increasingly important role.

Reference£º
Patent; AURIGENE DISCOVERY TECHNOLOGIES LIMITED; SENGUPTA, Saumitra; RAJAGOPALAN, Srinivasan; BELAVAGI, Ningaraddi; RAMACHANDRA, Muralidhara; WO2012/59932; (2012); A1;,
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Piperazines – an overview | ScienceDirect Topics

278788-66-2, (R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of /ert-butyl (3f?)-3-(hydroxymethyl)piperazine-l -carboxylate (80.0 g, 370 mmol, 1.0 eq) in Ethyl acetate (1400 mL) was added NaHCOa (93.2 g, 1.1 1 mol, 43.2 niL, 3.0 eq), H20 (700 mL) and benzyl carbonochloridate (82.0 g, 481 mmol, 68.4 mL, 1.30 eq). The mixture was stirred at 25 C for 12 hour. After completion, the organic phase was separated, washed with water (500 mL x 2) dried over Na2S04 and filtered. The solvent was removed under vacuum to give a residue. The residue was purified by column chromatography (Si02, Petroleum ether/Ethyl acetate=40/l to 1/1). The product 1 -benzyl 4-/ert-butyI ( 2R)-2 – (hydroxymethyl)piperazine-l,4-dicarboxylate (85.0 g, 235 mmol, 64% yield, 96% purity) was obtained as a yellow oil. LCMS [ESI, M-99]: 251., 278788-66-2

The synthetic route of 278788-66-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MIRATI THERAPEUTICS, INC.; ARRAY BIOPHARMA, INC.; MARX, Matthew, Arnold; BLAKE, James, F.; FELL, Jay, Bradford; FISCHER, John, P.; MEJIA, Macedonio, J.; (164 pag.)WO2020/47192; (2020); A1;,
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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.

(1035) A mixture of Compound 337J (3.0 g), Compound 337M (1.98 g), N,N-dimethylpyridin-4-amine (1.93 g) and N-((ethylimino)methylene)-N3,N3-dimethylpropane-1,3-diamine hydrochloride (1.31 g) in dichloromethane (50 ml) was stirred overnight and concentrated. The residue was purified by reverse chromatography, eluted with 40%-70% acetonitrile in 0.1% TFA water. The desired fractions were concentrated to remove acetonitrile, neutralized with NaHCO3 and extracted with dichloromethane. The organic layer was dried over Na2SO4, concentrated and dried to provide the title compound. 1H NMR (400 MHz, dimethylsulfoxide-d6) delta 11.68 (s, 1 H), 8.52-8.58 (m, 2 H), 8.04 (d, 1 H), 7.79 (dd, 1 H), 7.53 (d, 1 H), 7.47-7.52 (m, 2 H), 7.30-7.37 (m, 2 H), 7.07 (d, 1 H), 7.01-7.06 (m, 2 H), 6.68 (dd, 1 H), 6.39 (dd, 1 H), 6.19 (d, 1 H), 4.25 (s, 1 H), 3.25-3.32 (m, 4 H), 3.07 (s, 4 H), 2.75 (s, 2 H), 2.09-2.24 (m, 6 H), 1.95 (s, 2 H), 1.50-1.73 (m, 5 H), 1.28-1.43 (m, 4 H), 1.06-1.18 (m, 5 H), 0.92 (s, 6 H).

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; AbbVie Inc.; Catron, Nathaniel; Lindley, David; Miller, Jonathan M.; Schmitt, Eric A.; Tong, Ping; US10213433; (2019); B2;,
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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.

Intermediate 20: l-Cyclopropylmethyl-lH-[l ,2,4]triazole-3-carboxylic acid 20.1 : 3,3-Dimethyl-4-(l -phenyl- 1Eta-[ 1 ,2,4]triazole-3-carbonyl)-piperazine- 1 -carboxylic acid tert-butyl ester A mixture of 420 mg (2.22 mmol) l-phenyl-lH-[l ,2,4]triazole-3-carboxylic acid, 500 mg (2.22 mmol) 3,3-dimethyl-piperazine-l-carboxylic acid tert-butyl ester, 750 mg (2.22 mmol) TBTU and 500 mu (2.91 mmol) DIPEA in 5 mL DMF was stirred at RT for 2 h. The reaction mixture was poured into ice water. The precipitate was filtered off, taken up in EtOAc, dried over sodium sulfate, filtered and concentrated in vacuo. yield: 850 mg (99 %) ESI-MS: m/z = 386 (M+H)~ Rt(HPLC): 1.20 min (method 23), 259808-67-8

The synthetic route of 259808-67-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HEIMANN, Annekatrin; DAHMANN, Georg; GRUNDL, Marc; MUELLER, Stephan Georg; WELLENZOHN, Bernd; WO2013/87805; (2013); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of 1-(tert-butyl) 3-methyl piperazine-1,3-dicarboxylate (250 mg, 1.023 mmol) in acetonitrile (8 mL) were added DIPEA (0.536 mL, 3.07 mmol) and 4,4′-(bromomethylene)bis(chlorobenzene) (485 mg, 1.535 mmol). The reaction mixture was heated up to 85 C over 10 min and was stirred for 16 h. The reaction mixture was concentrated under high vacuum to yield a brown gum. The crude compound was purified by ISCO (using 24 g silica gel column; using 8 % -12 % ethyl acetate/ petroleum ether) to yield 1-(tert-butyl) 3-methyl 4-(bis(4-chlorophenyl)methyl) piperazine-1,3-dicarboxylate (280 mg, 57.1 % yield) as a brown gum. LCMS: m/z = 481.2 (M+2H); rt 1.803 min; LC-MS Method: Column-KINETEX-XB-C18 (75 x 3 mm- 2.6 ^m); Mobile phase A: 10 mM ammonium formate in water: acetonitrile (98:2); Mobile phase B: 10 mM ammonium formate in water: acetonitrile (2:98); Gradient: 80 % B over 0.5 minute, 80-98% B over 2.5 minutes, flow rate 1.0 mL/min, then a 1 minute hold at 98% B flow rate 1.0 mL/min, 129799-08-2

As the paragraph descriping shows that 129799-08-2 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;,
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