Heterocyclic Building Blocks-piperazine

438631-77-7, (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Method 4:Synthesis of methyl (2R)-l-r5-(3-{l-r6-(2-aminopyrimidin-5-yl)pyridin-3- yl1cvclobutyl}-l,2,4-oxadiazol-5-yl)pyridin-2-yl1piperazine-2-carboxylate (Example 38, Table 1)Ex. 99 R30Example 99 (120 mg, 0.296 mmol) is treated with R30 (361 mg, 1.48 mmol) and NMP (0.150 mL) and heated at 80 C for 48 hours. The resulting mixture is cooled to room temperature and treated with 4N HC1 in 1,4-dioxane (1.50 mL) and stirred for 1.5 hours The resulting mixture is purified by reverse-phase preparative HPLC (C-18 silica, 10- 30% acetonitrile/water/0.1% trifluoroacetic acid over 20 minutes) to afford the title compound as a trifluoroacetic acid salt (110 mg), m/z 514.8 [M+H].

438631-77-7, As the paragraph descriping shows that 438631-77-7 is playing an increasingly important role.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BARTOLOZZI, Alessandra; BOSANAC, Todd; CHEN, Zhidong; DE LOMBAERT, Stephane; DINES, Jonathon, Alan; HUBER, John, D.; LIU, Weimin; LOKE, Pui Leng; MORWICK, Tina, Marie; OLAGUE, Alan; RIETHER, Doris; TYE, Heather; WU, Lifen; ZINDELL, Renee, M.; WO2012/40139; (2012); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1: (S)-tert-butyl 4-(3,5-difluorophenyl)-2-methylpiperazine-1-carboxylate A solution of (S)-tert-butyl-2-methylpiperazine-1-carboxylate (1.2 g, 6 mmol), 1,3-difluoro-5-iodobenzene (1.685 g, 7.2 mmol), t-BuONa (865 mg, 9 mmol), BINAP (150 mg, 0.24 mmol), Pd2(dba)3 (110 mg, 0.12 mmol) in dry toluene (40 mL) was stirred under N2 at 80 C. for 16 hrs. The reaction mixture was concentrated and the mixture was purified by chromatography (silica, EtOAc/PE=1/10) to afford (S)-tert-butyl-4-(3,5-difluorophenyl)-2-methylpiperazine-1-carboxylate (1.1 g, 3.52 mmol, 59%) as a yellow oil. ESI-MS (EI+, m/z): 257.0 [M-55]+.

169447-70-5, As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (136 pag.)US2019/389843; (2019); A1;,
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216144-45-5, 4-(4-Methylpiperazin-1-yl)benzylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To 4,9-dioxo-4,9-dihydrothiazolo [5,4-g] quinoline-2-carboxylic acid (27 mg, 0.1 mmol) of N, N-dimethylformamide ( 2.0mL) solution was added DIPEA (27mg, 0.21mmol), HATU (59mg, 0.15mmol), 4- (4-methylpiperazin-1-yl) benzylamine (21mg, 0.1mmol), and the reaction system was stirred at 40 C. 2 hours.The reaction system was diluted with water, extracted with ethyl acetate, and the organic phase was concentrated under reduced pressure andpurifiedby prep-HPLC (NH4HCO3system) to obtain compound 30 (2.25 mg, yield: 5%) as a gray-black solid., 216144-45-5

As the paragraph descriping shows that 216144-45-5 is playing an increasingly important role.

Reference£º
Patent; Shanghai Dinuo Pharmaceutical Technology Co., Ltd.; Zhao Zhiming; (42 pag.)CN110467629; (2019); A;,
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Piperazines – an overview | ScienceDirect Topics

438631-77-7, (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Representative Synthesis I; (R)-l-(4-Chloro-benzyl)-piperazine-2-carboxylic acid methyl ester; R-4N-Boc-piperazine 2-carboxylic acid methyl ester (679.4mg, 2.78mmol) and 4- chlorobenzaldehyde (390.94mg, 2.78mmol) are mixed in dichloromethane(lthetaml) for 30 minutes. Sodium triacetoxyborohydride (800mg, 3.77mmol) is added. The mixture is stirred at room temperature for 16 hf . Water is added. The aqueous layer is extracted with dichloromethane twice (3OmL x2). The dichloromethane solution is treated with trifluoracetic acid (30ml). After 4 hrs the solvent is evaporated and re-disolved in water. The water solution is basified by adding K2CO3 (solid). The water solution is extracted with EtOAc three times. The organic layer is dried over NaSO4. The product is colorless oil (748mg, 100% ) after removing solvent to dryness. Found reta/z ES+=269 . ‘ . .

438631-77-7, 438631-77-7 (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 6558432, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GmbH; WO2007/120595; (2007); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5271-27-2,1-Methyl-3-phenylpiperazine,as a common compound, the synthetic route is as follows.,5271-27-2

1-Methyl-3-phenyl-piperazine (31.7 mg, 0.18 mmol) were weighted into a reaction vial and dissolved in 1 ml THF. 1 ml of a DMF stock solution containing N-methylmorpholine (51 mg, 0.5 mmol), 6-(4-Hydroxy-phenyl)-3-methyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid (48 mg, 0.18 mmol), and HOBt (28 mg, 0.21 mmol) was added, followed by EDC (32 mg, 0.21 mmol). The vial was closed with a screw cap and shaken at r.t. over night. The mixture was treated with 0.1 ml TFA, filtered and purified by preparative HPLC to give the TFA salt. Conversion of the TFA salt into the HCl salt (and deprotection of amines containing a BOC-protection group) was achieved by shaking the compound with 2 ml 4M HCl in dioxane at r.t. overnight. Then 5 ml water were added and the mixture was freeze-dried to obtain the final product as the hydrochloride salt (17 mg, 19percent). LC/MS (Method LC10): Rt=2.23 min; m/z=428.22 [M+H]+. 1H-NMR (500 MHz, d6-DMSO): 2.30 (s, 1H), 2.63 (s, 3H), 2.85-2.95 (m, 2H), 3.62-3.68 (m, 4H), 4.31-4.43 (m, 1H), 6.22 (m, 1H), 6.90 (d, 2H), 7.2-7.6 (m, 4H), 7.70 (s, 1H), 8.07 (d, 2H).

The synthetic route of 5271-27-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SANOFI; HACHTEL, Stephanie; PLETTENBURG, Oliver; SCHOENAU, Christian; LOEHN, Matthias; PFEIFFER-MAREK, Stefania; MENDEZ-PEREZ, Maria; KANNT, Aimo; DEDIO, Juergen; KOHLMANN, Markus; SCHIFFER, Alexander; BEGIS, Guillaume; DUCLOS, Olivier; JEANNOT, Frederic; US2013/85128; (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.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.

The sulfonamide (compound 3, 158.9 g), DMAP (123.7 g), EDCI (126.5 g) and dichloromethane (3678 mL) were combined at 25C (reactor I). In a second reactor (reactor II), the benzoic acid derivative (compound 2, 340.0 g), Et3N (140 mL) and dichloromethane (2936 mL) were combined and stirred for 15 minutes. The resulting acid solution (reactor II) was slowly added to the suspension of the sulfonamide (reactor I) within 120 minutes and reaction mixture agitated until reaction completion. After 22 hours the reaction mixture was washed with 10% acetic acid solution twice (2×2056 mL). The lower organic layer was diluted with more dichloromethane (882 mL) and methanol (146 mL), before separation of the organic layer. After phase separation the organic layer was washed with 5% aq. NaHCO3 (2059 mL) and then with 5% NaCl solution (2059 mL) at room temperature. The lower organic layer was separated and the concentrated to dryness, resulting a yellow solid. Dichloromethane (2014 mL) and methanol (206 mL) were added, the suspension was heated to 38C under stirring. Ethyl acetate (1840 mL) was added slowly within 40 minutes to the yellow solution. Heating was turned off and the suspension was cooled to 0-5 C and stirred at 5C overnight. The filtrated product was washed with Ethyl acetate (735 ml) and dried under vacuum (100 mbar) at 50C overnight to yield Venetoclax as yellow solid (273.6 g; 62.5 %, HPLC purity 95.36 A%).

1235865-77-6, The synthetic route of 1235865-77-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASSIA CHEMICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; POTARINE JUHASZ, Zsuzsa; STRUBA, Szabolcs; NEMETHNE RACZ, Csilla; TOTH, Zoltan Gabor; SZILAGYI, Andrea; KERTI-FERENCZI, Renata; MOLNAR, Sandor Janos; PASZTOR-DEBRECZENI, Nora; HAJKO, Janos; (100 pag.)WO2017/156398; (2017); A1;,
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21655-48-1, cis-2,6-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(Formula 12-7: methyl 4-(((3S,5R)-3,5-dimethyl-N-(3-(trifluoromethyl)phenyl)piperazine-1-carboxamido)methyl)benzoate)[1793][1794]Compound ofFormula 1-3(methyl 4-((((4-nitrophenoxy)carbonyl)(3-(trifluoromethyl)phenyl)amino)methyl)benzoate; 1.263 g, 2.662 mmol), (2S,6R)-2,6-dimethylpiperazine (1.520 g, 13.309 mmol) and potassium carbonate (0.736 g, 5.323 mmol) were dissolved in N,N-dimethylformamide (5 mL) at 40 ¡ãC and stirred at the same temperature for 16 hours. Then, the temperature was lowered to room temperature, and the reaction was completed. Then, water was poured into the reaction mixture, and the organic layer was extracted with ethyl acetate. Then, the organic layer was washed with saturated sodium chloride aqueous solution, dehydrated with anhydrous magnesium sulfate, filtered, and then concentrated under reduced pressure. The concentrate was purified and concentrated by column chromatography (silica; ethyl acetate/hexane=20-50percent) to give the desired compound ofFormula 12-7(0.726 g, 60.7percent) in the form of a yellow liquid.

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

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; LEE, Changsik; YANG, Hyun-Mo; CHOI, Hojin; KIM, Dohoon; KIM, Soyoung; HA, Nina; LIM, Hyojin; KO, Eunhee; YOON, Seongae; BAE, Daekwon; WO2014/178606; (2014); A1;,
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Piperazines – an overview | ScienceDirect Topics

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of 1-tert-butyl 3-methyl 4-(5-chloro-2-nitrobenzyl)piperazine-1,3-dicarboxylate (52)1.5 g (8.2 mmol) of the aldehyde 51 and 2.0 g (8.2 mmol) of the amine 5 are initially introduced in a mixture of 50 ml of dichloroethane and 50 ml of THF. 0.940 ml of glacial acetic acid are then added, and the mixture is stirred at RT for about 3 h. 5.5 g (24.6 mmol) of NaB(OAc)3 and a further 0.940 ml of acetic acid are subsequently added, and the mixture is stirred overnight at room temperature. The batch is stirred with saturated NaHCO3 solution, diluted with dichloromethane and extracted by shaking. The organic phase is again washed by shaking with water, the aqueous phase is again extracted by shaking with DCM. The combined organic phases are dried over Na2SO4, filtered off with suction and evaporated to dryness in vacuo. The 3.5 g of crude product obtained are dissolved in THF, adsorbed onto Isolute and separated on silica gel 60 (Flashmaster). The relevant fractions are combined and evaporated to dryness in a rotary evaporator, thus giving the desired product 52 (1.6 g, 21% yield) in a purity of 45% (mass: [M+]=414; HPLC method D, RT=3.86 min) as yellow oil, which is reacted further without further purification., 129799-08-2

129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Merck Patent Gesellschaft Mit Beschrankter Haftung; US2012/115852; (2012); A1;,
Piperazine – Wikipedia
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115619-01-7, 4-(4-Ethylpiperazin-1-yl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The reaction vessel was charged with 5-((3-fluorophenyl)sulfonyl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole-3-carboxylic acid(29 mg, 0.16 mmol), diisopropylethylamine (0.035 mL, 0.2 mmol), 1-hydroxybenzotriazole monohydrate (19 mg, 0.12 mmol) and dichloromethane (2 mL) were added and stirred. 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDCI ?? HCl, 23 mg, 0.12 mmol) was added thereto and stirred at room temperature. The reaction mixture was diluted with dichloromethane (10 mL), water (10 mL) was added, and the mixture was stirred. The organic layer was washed with brine, dried over anhydrous magnesium sulfate and concentrated. The residue was purified by column chromatography (silica gel, dichloromethane: methanol = 30: 1) to obtain the desired compound (50 mg, 90% yield).

115619-01-7, As the paragraph descriping shows that 115619-01-7 is playing an increasingly important role.

Reference£º
Patent; Korea Institute of Science and Technology; Sim Tae-bo; Noh Eun-ju; Yang Han-yong; (33 pag.)KR101936851; (2019); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

197638-83-8, 1-Boc-4-(4-Formylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 4-(4-formyl-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (1.3 g, 4.47 mmol) in THF (50 mL) was mixed with LAH (0.7 g, 17.87 mmol) and stirred at reflux for 14 h. The reaction was quenched at room temperature by adding KOH aqueous (14 N, 20 mL). The supernatant was decanted and combined with DCM washings, then diluted with water (50 mL). The mixture was extracted with DCM (3¡Á50 mL) followed by concentration using a rotary evaporator to give [4-(4-methyl-piperazin-1-yl)-phenyl]-methanol (0.82 g, 89%). To a solution of DMSO (0.56 mL, 7.96 mmol) in DCM (50 mL) at -78 C. was added oxalyl chloride (0.7 mL, 7.96 mmol) and the resulting mixture was stirred at -78 C. for 0.5 h. A solution of [4-(4-methyl-piperazin-1-yl)-phenyl]-methanol (0.82 g, 3.98 mmol) in DCM (20 mL) was slowly added. The reaction was stirred at -78 C. for 1.5 h. Triethylamine (1.7 mL, 11.94 mmol) was added and the reaction was allowed to gradually warm up to room temperature. After stirring for 4 h the reaction was quenched by adding sodium bicarbonate aqueous (1 N, 50 mL). The mixture was extracted with DCM (3¡Á50 mL) followed by concentration to afford a residue, which was further purified by column chromatography to yield 4-(4-methyl-piperazin-1-yl)-benzaldehyde (0.5 g, 61%)., 197638-83-8

As the paragraph descriping shows that 197638-83-8 is playing an increasingly important role.

Reference£º
Patent; RVX Therapeutics Inc.; McLure, Kevin G.; Young, Peter Ronald; US2013/281397; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics