Month: April 2021

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.

A mixture of 2 g (14 mmol) 2-chloro-4-cyanopyridine and 2.34 g (15 mmol) 1- cyclopentylpiperazine in 5 ml DMF was heated to 80 0C for 16 h. The mixture was evaporated under reduced pressure and the residue was treated with 100 ml IM NaHCO3 aq. and extracted with two times 100ml ethyl acetate. The combined organic phases were dried with MgSO4 and evaporated under reduced pressure to yield 3.4 g (92 %) of the title compound as grey solid, (m/e): 257.3 (MH+; 100%).

21043-40-3, 21043-40-3 1-Cyclopentylpiperazine 806421, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; F.HOFFMANN-LA ROCHE AG; WO2006/63718; (2006); 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.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

Step A:6-Bromo-2-(4-cyclopropylpiperazin-1-yl)benzothiazole; To a solution of 6-bromo-2-chlorobenzothiazole (8.2 g, 33 mmol) in EtOH (115 mL) was added Et3N (16.7 g, 165 mmol), followed by 1-cyclopropylpiperazine (5 g, 39.6 mmol). The mixture was heated at reflux for 12 h. Then the mixture was evaporated to remove EtOH. Water (120 mL) was added to the residue and the mixture was extracted with CH2CI2 (3 x 50 mL). The combined organic extracts were washed with brine, dried (Na2SO4) and concentrated to give a residue, which was purified by column chromatography on silica gel eluting with a mixture of EtOAc/petroleum ether (1 :10 with 0.1 % NH4OH added) to give 3.46 g (31 %) 6-bromo-2-(4-cyclopropylpiperazin-1-yl)benzothiazole.1H NMR (300 MHz, CDCI3): delta 7.70 (t, 1 H), 7.38 (dd, 2 H), 3.60 (d, 4 H), 2.80 (d, 4 H), 1.68 (d, 1 H), 0.50-0.39 (m, 4 H).

20327-23-5, As the paragraph descriping shows that 20327-23-5 is playing an increasingly important role.

Reference£º
Patent; NOVO NORDISK A/S; WO2007/110364; (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.55276-43-2,1-Methanesulfonylpiperazine,as a common compound, the synthetic route is as follows.,55276-43-2

General procedure: To a solution of amine NHR4R5 (10.0 mmol) m MeOH was added acrylonitrile (1.5 mL). After 18 h at rt, the mixture was dry loaded onto silica gel. Elution with EtOAc provided the pure 3- aminopropionitriles 44. Reaction of acrylonitrile with l-(methylsulfonyl)piperazine provided 44a: lH NMR (200 MHz, CDCb) 3.30 – 3.20 (m, 4H), 2.78 (s, 3H), 2.80 – 2.42 (m, 8H).

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

Reference£º
Patent; DFH THERAPEUTICS; THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES; NITZ, Theodore J.; WILD, Carl T.; MARTIN, David E.; FREED, Eric O.; (0 pag.)WO2020/6510; (2020); A1;,
Piperazine – Wikipedia
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

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;,
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.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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
Piperazine – Wikipedia
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;,
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.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;,
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.

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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics