Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.27561-62-2,Cyclohexyl(piperazin-1-yl)methanone,as a common compound, the synthetic route is as follows.

TO 4- (3-PIPERIDIN-1-YLPROPOXY) BENZOYL CHLORIDE HYDROCHLORIDE (D3) (0.24g) in DCM (10 ML) was added 1- (CYCLOHEXANECARBONYL)-PIPERAZINE (0.155 g) and diethylaminomethyl polystyrene (3. 2MMOL/G, 0.69g). The mixture was stirred for 16h. The reaction mixture was then loaded directly onto a silica column and eluted with 0-10% MEOH (containing 10% 0.880 ammonia solution) in DCM. The isolated free base was dissolved in DCM (5ML) and treated with 4N HCI/DIOXANE solution (1 ml) with stirring for 10MIN. The reaction was concentrated, and the residue co-evaporated with toluene (3X10M1) and then dried at 50C under high vacuum for 16h to yield the title compound (E57) as a PALE SOLID (0.165G). MS ELECTROSPRAY (+ION) -442 (MH+). 1H NMR 8 (DMSO-D6): 9.71 (S, 1H), 7.39 (d, 2H, J=6.84Hz), 7.00 (d, 2H, J=6.84Hz), 4.10 (m, 2H), 3.47-3. 25 (m, 10H), 3.16 (m, 2H), 2.90 (m, 2H), 2.55 (m, 1H), 2.19 (m, 2H), 1.82-1. 62 (m, 10H), 1.40-1. 16 (m, 6H).

27561-62-2, As the paragraph descriping shows that 27561-62-2 is playing an increasingly important role.

Reference£º
Patent; GLAXO GROUP LIMITED; WO2004/37800; (2004); A1;,
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57184-25-5, 1-(Cyclopropylmethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-Cyclopropylmethyl-piperazine-1-carboxylic Acid 4-(3,3-dimethyl-butylcarbamoyl)-phenyl Ester The title product was prepared from 1-cyclopropylmethylpiperazine (0.35 mmol) dissolved in dichloromethane (5 ml). 4-(3,3-dimethyl-butylcarbamoyl)-phenyl chloroformate (0.35 mmol) was added at room temperature. The reaction mixture was stirred for 16 h and evaporated to dryness and subjected to preparative HPLC (metod C) (5%, white crystals). HPLC-MS m/z=388.2 (M+1), Rt: 2.43 min., 57184-25-5

57184-25-5 1-(Cyclopropylmethyl)piperazine 965875, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Ebdrup, Soren; de Jong, Johannes Cornelis; Jacobsen, Poul; Hansen, Holger Claus; Vedso, Per; US2003/166644; (2003); A1;,
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59702-07-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

The indazole (810 mg), Et3N (3.9 g), and amine (1.9 g) were taken up in DMSO (4 ml). The resulting solution was heated in a sealed tube at 100 ¡ãC for 16 hours. The solution was cooled, and it was partitioned between EtOAc and water. The aqueous layer was extracted with EtOAc. The combined organic layers were dried (MgS04), filtered, and concentrated. The residue was purified by flash chromatography (30/1 DCM MeOH, Si02) which provided the amino-pyridine.

59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; MILLER, Michael; BASU, Kallol; DEMONG, Duane; SCOTT, Jack; LIU, Hong; DAI, Xing; STAMFORD, Andrew; POIRIER, Marc; TEMPEST, Paul; WO2014/134776; (2014); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.,4318-42-7

Step D. [2-(3,4-Dichloro-phenoxy)-5-(4-isopropyl-piperazine-1- carbonvD-benzvH-methyl-carbamic acid tert-butyl ester.; To a solution of [5- bromo-2-(3,4-dichloro-phenoxy)-benzyl]-carbamic acid tert-butyl ester (327.0 mg, 0.71 mmol) in THF (2 ml.) were added DBU (0.30 ml_, 2.0 mmol), 1- isopropyl piperazine (0.30 ml_, 2.5 mmol), Hermann’s catalyst (31 .9 mg, 0.034 mmol), tri-f-butylphosphium tetrafluoroborate (26.4 mg, 0.091 mmol), and Mo(CO)6 (21 1.0 mg, 0.80 mmol). After 6 min in a microwave reactor at 125 0C, the mixture was cooled to rt and concentrated. Purification by FCC gave the desired product (212.5 mg, 56percent).

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2008/2820; (2008); A2;,
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109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Comparative Example 10 A 200 ml four-neck flask with a pH meter and dropping funnel was charged with 10.08 g (= 0.101 mole) of racemic 2-methylpiperazine, and 50.0 g of 1-butanol was added for dissolution, being followed by addition of 50.3 g of water (water content 50.1 wt%). With vigorous stirring, benzyl chlorocarbonate was added dropwise. In this case, 48 wt% sodium hydroxide aqueous solution was added dropwise to keep the pH value of the system at 10 to 11, and as required, the system was cooled with ice to keep the internal temperature at 23 to 26C (final water content 53.2 wt%). After completion of dropwise addition, with vigorous stirring, aging was carried out for 2.5 hours. The reaction solution was sampled and analyzed, and as a result, the conversion of 2-methylpiperazine was 85.5%, and the selectivity of 1-tert-butoxycarbonyl-3-methylpiperazine was 77.2% (reaction yield 66.0%).Comparative Example 11 A 200 ml four-neck flask with a pH meter and dropping funnel was charged with 10.22 g (= 0.102 mole) of racemic 2-methylpiperazine, and 80.5 g of 1-butanol was added for dissolution, being followed by addition of 27.5 g of water (water content 25.4 wt%). With vigorous stirring, benzyl chlorocarbonate was added dropwise. In this case, 48 wt% sodium hydroxide aqueous solution was added dropwise to keep the pH value of the system at 8 to 9.5, and as required, the system was cooled with ice to keep the internal temperature at 23 to 26 (final water content 26.9 wt%). After completion of dropwise addition, with vigorous stirring, aging was carried out for 2.5 hours. The reaction solution was sampled and analyzed, and as a result, the conversion of 2-methylpiperazine was 89.6%, and the selectivity of 1-tert-butoxycarbonyl-3-methylpiperazine was 73.5% (reaction yield 65.9%)., 109-07-9

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

Reference£º
Patent; Toray Fine Chemicals Co., Ltd.; EP1548010; (2005); A1;,
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181955-79-3, 1,4-Di-Boc-piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

181955-79-3, Step-2 [0552] Method-A [0553] (i) To a dichloromethane (DCM, 40 ml) solution of Boc-protected acid (5.0 g, 15.18 mmol) as prepared in step-1 is added a solution of N-hydroxysuccinimide (1.75 g, 15.21 mmol) in THF (20 ml) and a solution of DCC (3.6 g, 17.47 mmol) in DCM (20 ml) at 0 C. in the order specified. Reaction mixture stirred at 0-5 C. for 4-5 hrs, filtered, filtrate washed successively with water, aqueous sodium bicarbonate solution and finally with brine. Organic layer dried (Na2SO4) evaporated in vacuo to give the product as white solid. (Yield 5.8 g, 86.05%). [0554] (ii) To a solution of the succinimide derivative (1.92 g, 4.49 mmol) in DCM (20 ml) as prepared in (i) of step-2, is added a solution of L-prolinamide (0.6 g, 5.26 mmol). Reaction mixture stirred at 25 C. for 16 hrs. washed with aqueous NaHCO3 solution and brine, dried (Na2SO4), evaporated in vacuo yielding a crude residue. Desired coupled product was isolated by column chromatography (40% ethyl acetate/hexane), (Yield 0.53 g, 27.74%).

The synthetic route of 181955-79-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; TORRENT PHARMACEUTICALS LTD.; US2004/106802; (2004); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.115761-79-0,1-(2,4-Difluorophenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: Arylpiperazines (1.2 equiv) and potassium carbonate (4.0 equiv)were added to a solution of 2 (100 mg, 0.43 mmol) in acetonitrile(CH3CN, 15 mL). The reaction mixture was heated to 85 C and stirred for 16 h. Afterward the mixture was cooled to room temperature. The reaction mixture was filtered, and the filtrate was concentrated invacuo. Then the residue was purified by chromatography on silica-gel column (petroleum ether: ethyl acetate=3:1, v/v) to obtain the corresponding products (3-24).

115761-79-0, The synthetic route of 115761-79-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Chen, Hong; Zhang, Jingxiao; Hu, Peixin; Qian, Yuna; Li, Jing; Shen, Jianliang; Bioorganic and Medicinal Chemistry; vol. 27; 20; (2019);,
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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.

General procedure: Carbonyldiimidazole (0.97g, 0.006mol) in 5mL of dry THF was added to a solution of intermediates 1 (1.11g, 0.006mol), 2 (1.19g, 0.006mol), 3 (1.19g, 0.006mol) or 4 (1.28g, 0.006mol) dissolved in 10mL of anhydrous THF while stirring. After the end of gaseous (carbon dioxide) evolution (c.a. 0.5h), the respective secondary amines (0.006mol) dissolved in 5mL of anhydrous THF was added dropwise. The mixture was stirred at room temperature (approx. 24h) and evaporated to dryness. The crude product was purified by column chromatography (dichloromethane/methanol, 9:0.3, v/v). The final amides were obtained as solid substances followed by concentration of organic solvents under reduced pressure, and recrystallization from 2-propanol.

30459-17-7, As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference£º
Article; Kami?ski, Krzysztof; Zagaja, Miros?aw; Rapacz, Anna; ?uszczki, Jarogniew J.; Andres-Mach, Marta; Abram, Micha?; Obniska, Jolanta; Bioorganic and Medicinal Chemistry; vol. 24; 4; (2016); p. 606 – 618;,
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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

General procedure for Buchwald-Hartwig couplingIn a oven dried 20 mL round-bottomed flask 2,2′-bis(diphenylphosphino)-l,l’-binaphthyl (racemic) (0.07 g, 0.1 12 mmol) and palladium(II) acetate (0.02 g, 0.089 mmol) in dry toluene (3 ml) were added under N2 atm. followed by addition of (2No.,6S)-2,6-dimethylpiperazine (0.101 g, 0.888 mmol), 12a (0.2 g, 0.740 mmol) and cesium carbonate (0.338 g, 1.037 mmol). Reaction mixture was stirred at 100 ¡ãC for 16 h. After 16 h reaction mixture was cooled, diluted with EtOAc and filtered through celite pad, filtrate was concentrated and purified by column chromatography with a silica gel column and was eluted with 15 percent MeOH in CHC to obtain a pure product 13a, 0.1 g (45 percent)

21655-48-1, 21655-48-1 cis-2,6-Dimethylpiperazine 6950261, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CAMBRIDGE ENTERPRISE LIMITED; GLEN, Robert; HILEY, Robin; BELL, James; SPRING, David; KAPADNIS, Prashant, Bhimrao; WO2011/98776; (2011); A1;,
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674792-05-3, (S)-1-Boc-2-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,674792-05-3

[00339] To a solution of (5)-tert-butyl 2-isopropylpiperazine-1-carboxylate (400 mg, 1.76 mmol) in anhydrous toluene (10 mL) was added methyl 4-bromo-2-(methylsulfonyl)benzoate (1.03 g, 4.8 mmol), X-phos (80 mg, 0.17 mmol), Cs2CO3 (1.50 g, 4.62 mmol) and Pd2(dba)3 (200 mg, 0.22 mmol) under N2. The reaction mixture was stirred at 100 oC overnight. The reaction was quenched with water (20 mL), and extracted with EtOAc (4 X 20 mL). The combined organic layers were dried over anhydrous Na2504, filtered, concentrated and then purified by preparative TLC with petroleum ether / EtOAc 5/1 to afford (5)-tert-butyl 2- isopropyl-4- (4- (methoxycarbonyl)-3- (methylsulfonyl)phenyl)piperazine- 1 -carboxylate (500 mg, 65% yield) as a grey solid.

As the paragraph descriping shows that 674792-05-3 is playing an increasingly important role.

Reference£º
Patent; VITAE PHARMACEUTICALS, INC.; CLAREMON, David, A.; DONG, Chengguo; FAN, Yi; LEFTHERIS, Katerina; LOTESTA, Stephen, D.; SINGH, Suresh, B.; TICE, Colin, M.; ZHAO, Wei; ZHENG, Yajun; ZHUANG, Linghang; (185 pag.)WO2016/22521; (2016); A1;,
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Piperazines – an overview | ScienceDirect Topics