Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.,59878-57-8

General procedure: A solution of 1,1?-carbonyldiimidazole (CDI) in THF (3 ml, 3.7 mmol) was added to indole-2-carboxylic acid (3.1 mmol) in THF (5 ml) at room temperature and stirred for 1 hunder N2. Then, the reaction mixture was cooled to 0d fC andN-substituted piperazine derivatives (3.7 mmol) in THF (3ml) were added and stirred for further 17-18 h at roomtemperature. Basic workup (CHCl3, sat. NaHCO3) wasapplied, evaporated under vacuo and recrystallization fromethyl acetate:n-hexane provided the desired compounds (1,4-15, Scheme 1).

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

Reference£º
Article; Altuntas, Tunca Gul; Yilmaz, Niluefer; Coban, Tuelay; Oelgen, Suereyya; Letters in drug design and discovery; vol. 14; 4; (2017); p. 380 – 386;,
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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Step 1: CbzCl (17 g, 0.1 mol) was added into a solution of compound 219-1 (30 g, 0.3 mol) and DIPEA (40 g, 0.3 mol) in DCM (200 mL) at 0C, then the mixture was stirred at room temperature for 3h and the solvent was removed, the crude product was purified by column chromatography to deliver compound 2 (11 g, yield 47%) as yellow oil. MS ESI calcd for C13H18N2O2 [M+H]+ 235, found 235., 109-07-9

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GUANGDONG ZHONGSHENG PHARMACEUTICAL CO., LTD; WU, Hao; LIN, Jun; LI, Yunhui; WEI, Changqing; CHEN, Shuhui; LONG, Chaofeng; CHEN, Xiaoxin; LIU, Zhuowei; CHEN, Lijuan; (212 pag.)EP3124482; (2017); A1;,
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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;,
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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.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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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;,
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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.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

5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A 2-l Erlenmeyer flask was charged with 2-piperazinone (36.5 g, 364 mmol), sodium carbonate (116 g, 1.10 mol), 600 ml dioxane, and 150 ml water at room temperature. To this was slowly added benzyl chloroformate (62.1 g,364 mmol) over 20 min. After the addition was complete, the mixture was stirred for 2 h, diluted with water and extracted with 2 l of ethyl acetate. The combined organic extracts were dried (MgSO4), filtered and concentrated to give a white solid.To this solid was added 500 ml CH2Cl2, triethylamine (92.6 g, 128 ml, 911 mmol), 4-dimethylaminopyridine (4.45 g, 36.4 mmol), and di-tert-butyl dicarbonate (119 g,546 mmol). After 1 h at room temperature, the mixture was diluted with water and the organics were separated, dried (MgSO4), filtered and concentrated to give a brown oil. To this oil was added 100 ml CH2Cl2 followed by 1 l hexane. The resulting white solid was collected by filtration to give 4-benzyl 1-tert-butyl 2-oxo-1,4-piperazinedicarboxylate (101 g, 81%). 1H-NMR (400 MHz, CDCl3) delta 7.45-7.29 (m, 5 H), 5.15 (s, 2H), 4.24 (s, 2 H), 3.88-3.74 (m, 2 H), 3.74-3.59 (m, 2 H), 1.54 (s, 9H).

5625-67-2, The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Lloyd, David J.; St Jean, David J.; Kurzeja, Robert J. M.; Wahl, Robert C.; Michelsen, Klaus; Cupples, Rod; Chen, Michelle; Wu, John; Sivits, Glenn; Helmering, Joan; Komorowski, Renee; Ashton, Kate S.; Pennington, Lewis D.; Fotsch, Christopher; Vazir, Mukta; Chen, Kui; Chmait, Samer; Zhang, Jiandong; Liu, Longbin; Norman, Mark H.; Andrews, Kristin L.; Bartberger, Michael D.; Van, Gwyneth; Galbreath, Elizabeth J.; Vonderfecht, Steven L.; Wang, Minghan; Jordan, Steven R.; Veniant, Murielle M.; Hale, Clarence; Nature; vol. 504; 7480; (2013); p. 437 – 440;,
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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Reference Example 7 0.65 g of 2-methylpiperazine was added to a solution of 0.48 g of 1-cyclopropyl-6,7-difluoro-5-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid in 5 ml of N-methyl-2-pyrrolidone, followed by heating at 90 C. for 20 minutes. After distilling off the solvent under reduced pressure, the residue was added with ethanol. The resulting crystals were filtered and recrystallized from ethyl acetate-ethanol to give 231 mg of 1-cyclopropyl-6-fluoro-7-(3-methyl-1-piperazinyl)-5-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid. m.p.: 206 C.-208 C., white powder

109-07-9, 109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Otsuka Pharmaceutical Co., Ltd.; US6333431; (2001); B1;,
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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

To the 1200 L reactor was added [60C] racemic 2-methylpiperazine (100 kg) from a drum. H20 (240 L) was added, and the solution was cooled to [13C.] To the 1200 L receiver was added L-tartaric acid (150 kg). [H20] (140 L) was added, and the slurry was stirred for 1 h 35 min until dissolution of the solids was complete. The L-tartaric acid solution was transferred to the 1200 L reactor over 2 h while maintaining a temperature of [10-22C] in the 1200 L reactor followed by a [H20] rinse (20 L). Ethanol (163 kg) was added to the 1200 L reactor, and the solution was cooled to [2C.] The resulting slurry was stirred for 2 h at [2C,] and filtered through a 36″Nutsche filter sending the filtrate into the 1200 L receiver. The 1200 L reactor and 36″Nutsche filter were washed with H20 (200 L), and the solids were dried to yield 214 kg of 12% ee [(171%] based on the title compound). These solids were recharged to a clean 1200 L receiver and H20 (630 L) was added to the 1200 L receiver, which was heated to [85C] until all the solids had dissolved. The solution was filtered through an in-line filter (C) into the 1200 L reactor, cooled to [5C,] and stirred for 2 h. The resulting slurry was filtered through a clean 36″Nutsche filter sending the filtrate into the 1200 L receiver. The 1200 L reactor and 36″Nutsche filter were washed with [H20] (200 L), and the solids were dried to yield 104 kg of 93% ee (83% based on the title compound). These solids were recharged to a clean 1200 L receiver and [H20] (254 L) was added to the 1200 L receiver, which was heated to [85C] until all the solids had dissolved. The solution was filtered through an in-line filter (C) into the 1200 L reactor, cooled to [5C,] and stirred for 2 h. The resulting slurry was filtered through a clean 36″Nutsche filter sending the filtrate into the 1200 L receiver. The 1200 L reactor and 36″Nutsche filter were washed with H20 (200 L), and the solids were dried to yield 92 kg of 99% ee (74% based on the title compound). [D1] does not describe the preparation of the title compound but makes reference [TO J.] Med. Chem. 1990, 33, 1645-1656 (D2). The yield of the title compound according to D2, starting from racemic 2-methylpiperazine was 35%. M. Pt. 255.0-257. [0C.] ‘H NMR (400 MHz, [D20)] : [6] 4.79 [(D20,] reference), 4.36 (2H, s), 3.73-3. 64 (4H, [M),] 3.43 [(1H,] td J = 13.7, 3.0 Hz), 3.34 [(1H,] td, J = 12.7, 3.1 Hz), 3.17 [(1H,] dd, J = 14.2 12.8 Hz), 1.41 (3H, d, J = 6.1 Hz), 0.00 (TMS, reference). [13C] NMR (100 MHz, [D20)] : [6] 178.46 (s), 73.91 (d), 49.02 (d), 49.00 [(MEOH,] reference), 45.82 (t), 40.56 (t), 40.10 (t), 15.42 (q). IR (diffuse reflectance) 3426 (s), 3011 (s), 2999 (s), 2888 (s), 2785 (s, b), 2740 (s, b), 2703 (s, b), 2649 (s, b), 2483 (s, b), 2483 (s, b), 2361 (s), 2354,2340, 2248,1638 (s), cm HRMS (FAB) [CALCD FOR C5HL2N2 +HI 101.] 1079, found [101.] 1080. [[A]] [25D] = [24] (c 1.00, water). Anal. Calcd for [C4H606.] [C5HL2N2C,] 43.20 ; H, 7.25 ; N, 11.19. Found: C, 41.25 ; H, 7.45 ; N, 10.71.

109-07-9, As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference£º
Patent; BIOVITRUM AB; WO2004/829; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics