Heterocyclic Building Blocks-piperazine

21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1-cyclopentyl Piperazine(507 mg, 0.003 mmol) was added to a stirred solution of 6 (1 g, 0.0029 mmol) in dry 1,4-Dioxaneand DIPEA (0.7 mL,0.005 mmol). The solution was stirred for 4 h at room temperature. After adding water a precipitate was formed which was filtered to give compound 7 (1.1g, 86% yield) as white solid (m.p-156-159 C).1H NMR (300 MHz, CDCl3) ^ 1.39 – 1.50 (m, 2H), 1.58 (dd, J=7.72, 4.71 Hz, 2H), 1.68 – 1.75 (m, 2H), 1.88 (br. s, 2H), 2.51 – 2.60 (m, 1H), 2.64 – 2.70 (m, 4H), 3.66 – 3.71 (m, 1H), 3.76 – 3.82 (m, 4H), 3.96 (s, 3H), 5.25 (s, 2H), 7.06 (s, 1H), 7.18 (s, 1H), 7.31 – 7.41 (m, 3H), 7.42 – 7.48 (m, 2H).ESI [M+H]+:453.40., 21043-40-3

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

Reference：
Patent; COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH; TALUKDAR, Arindam; GANGULY, Dipyaman; PAUL, Barnali; MUKHERJEE, Ayan; ROY, Shounak; ROY, Swarnali; GHOSH, Amrit Raj; BHATTACHARYA, Roopkatha; RAHAMAN, Oindrila; KUNDU, Biswajit; (89 pag.)WO2017/163264; (2017); A1;,
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1001180-21-7, (R)-tert-Butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 4: (Reaction run in a 20-mL plastic bottle): To a solution of (R)-tert-butyl 4-(5- methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-l-carboxylate (0.250 g, 0.752 mmol) in 5 mL DCM was added DAST (0.795 mL, 6.02 mmol). The reaction mixture was capped and stirred at room temperature for 45 hours, after which it poured into ice saturated NaHCO3. The mixture was extracted with 2 x 40 mL DCM, and the combined extracts were dried (Na2SO4), filtered, and concentrated in vacuo. The crude was purified on silica gel (Biotage 40S) eluting with 6:1 to 3:1 hexanes:EtOAc to give (R)-tert-butyl 4-(7,7-difluoro-5-methyl-6,7-dihydro- SH-cyclopenta^pyrimidin^-ytypiperazine-l-carboxylate (0.092 g, 34.5% yield) as a yellow oil. MS (APCI+) m/z 355 [M+H]+.

1001180-21-7, 1001180-21-7 (R)-tert-Butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-1-carboxylate 59580350, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ARRAY BIOPHARMA INC.; GENENTECH, INC.; MITCHELL, Ian S.; BLAKE, James F.; XU, Rui; KALLAN, Nicholas C.; XIAO, Dengming; SPENCER, Keith Lee; BENCSIK, Josef R.; LIANG, Jun; SAFINA, Brian; LI, Jun; CHABOT, Christine; WO2008/6032; (2008); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

1-fluoro-4-nitrobenzene (1.460 g, 10.4 mmol) and potassium carbonate (4.29 g, 31.0 mmol) were suspended inanhydrous DMF (10 mL) . (S)-tert-butyl 3- (hydroxymethyl)piperazine-1-carboxylate (2.35 g, 10.9 mmol) was added and the mixture was heated at 90 C for 21 h. After cooling the mixture was partitioned between brine/water (100 mL) and ethyl acetate (25 mL) . Theaqueous layer was separated and further extracted with ethyl acetate (3 x 25 mL) . The combined ethyl acetate fractions were washed with brine/water (1:1, 4 x 25 mL), dried (anhydrous sodium sulfate), filtered and reduced in vacuo. The resulting residue was purified by silica gelchromatography (gradient 25-100% ethyl acetate incyclohexane) to afford the title compound (0.99 g, 28.4%) . ?H NMR (400 MHz, CDC13) : 3 8.12 (d, 2H), 6.83 (d, 2H),4.20-4.46 (m, 1H), 4.02-4.14 (m, 2H), 3.48-3.76 (m, 3H),3.08-3.30 (m, 3H), 2.86 (br s, 1H), 1.50 (s, 9H) . LCMS(Method C) : = 1.38 mi m/z = 338 [M+H]., 314741-40-7

As the paragraph descriping shows that 314741-40-7 is playing an increasingly important role.

Reference：
Patent; ALMAC DISCOVERY LIMITED; HARRISON, Timothy; TREVITT, Graham; HEWITT, Peter Robin; O’DOWD, Colin Roderick; BURKAMP, Frank; WILKINSON, Andrew John; SHEPHERD, Steven D.; MIEL, Hugues; WO2015/92431; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of intermediate 6 (200 mg, 0.53 mmol ) and 1-(methylsulfonyl)piperazine hydrochloride (87 mg, 0.53 mmol) in dry toluene (5 ml_), sodium tert butoxide (150 mg, 1.6 mmol) was added at RT and the resulting solution was flushed with nitrogen for 10 min. BINAP (66 mg, 0.1 mmol), Pd (dba (98 mg, 0.1 mmol) were added and the reaction mixture was flushed again with nitrogen for 10 min. It was then stirred at 100 C overnight. After completion of the reaction, the reaction mixture was diluted with EtOAc (20 mL) and filtered through celite pad. The filtrate was concentrated under vacuum and resulting crude product was purified by flash chromatography (Eluent: 47% EtOAC in pet ether) to afford the title compound. Yield: 5% (1 1 .3 mg, off-white solid). 1H NMR (400 MHz, DMSO-cfe): d 7.09 (d, J = 8.4 Hz, 2H), 6.92-6.90 (m, 3H), 6.85 (d, J = 2.0 Hz, 1 H), 6.82-6.80 (m, 1 H), 4.22 (s, 4H), 3.61 (d, J = 12.8 Hz, 1 H), 3.23-3.20 (m, 10H), 2.92 (s, 3H), 2.1 1 -2.06 (m, 2H), 1.72-1.68 (m, 2H), 1.56-1.48 (m, 1 H). LCMS: (Method A) 458.1 (M +H), Rt.1.570 min, 99.4% (Max). HPLC: (Method A) Rt. 3.038 min, 99.5% (Max), 99.4% (220 nm).

161357-89-7, 161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ASCENEURON S. A.; QUATTROPANI, Anna; WISHART, Grant; KULKARNI, Santosh S.; RAKESH, Paul; (338 pag.)WO2020/39027; (2020); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of the 3-(bromoacetyl)-6-methoxy-2- methylbenzonitrile (2.25 g, 8.40 mmol) in THF was added tert-butyl (35)-3- (hydroxymethyl)piperazine-l -carboxylate (2.18 g, 10.8 mmol) and Hunig’s Base (2.93 mL, 16.8 mmol). The reaction was allowed to stir at RT for 16 hours. TLC showed good reaction at that point. The crude reaction was adsorbed onto silica gel, and purified by silica gel flash chromatography to afford the title compound., 314741-40-7

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PIO, Barbara; PASTERNAK, Alexander; SHAHRIPOUR, Aurash; TANG, Haifeng; WALSH, Shawn; WO2013/90271; (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.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.

59878-57-8, To the reaction flask was added compound 6 (prepared in Example 3-2, 256.5g,0.86mol), CDI (139.45g, 0.86mol), 1.6LTHF, after stirring for 0.5h Compound 7 (138.8g,0.90mol) at room temperature The reaction 3h, after completion of the reaction, water was added to quench the reaction, of THF was distilled off under reduced pressure, theresidue was dissolved in ethyl acetate was added, the organic phase was separated,washed with water three times, the organic phase was dried over anhydrous Na 2SO 4Dried,filtered and concentrated to give Ola Trapani (356.3g, 0.82mol), yield 95%, HPLC purity 99.8%.

59878-57-8 1-(Cyclopropylcarbonyl)piperazine 2064235, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Shandong Luoxin Pharmaceutical Group Heng Xin Pharmaceutical Co. Ltd.; Li, Hua; Wang, Chunyan; Liu, Shuxin; (8 pag.)CN105820126; (2016); A;,
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.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

General procedure: To a solution of 3-iodo-4-methylbenzoyl chloride obtained above in dry DCM (10mL) at 0C was added Et3N (0.28mL, 2.0mmol) and 4-((4-methylpiperazin-1-yl) methyl)-3-(trifluoromethyl) aniline (328mg, 1.2mmol). The mixture was stirred at room temperature for 5h, and then the solvent was removed under reduced pressure. The residue was purified by using column chromatography to afford the corresponding product 6-1 (439mg, 2 steps yield: 85%)., 694499-26-8

694499-26-8 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 46838908, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Liu, Yang; Peng, Xia; Guan, Xiaocong; Lu, Dong; Xi, Yong; Jin, Shiyu; Chen, Hui; Zeng, Limin; Ai, Jing; Geng, Meiyu; Hu, Youhong; European Journal of Medicinal Chemistry; vol. 126; (2017); p. 122 – 132;,
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

21655-48-1, To a stirring suspension of 2?fluoro?5?nitrobenzaldehyde (2.69 g, 15.9 mmol) and potassium carbonate (8.80 g, 63.7 mmol) in anhydrous DMF (10 mL) was added (25,6R)?2,6?dimethylpiperazine (2 g, 17.51 mmol) and the mixture washeated at 90 °C for 16 h. After cooling the mixture was partitioned between brine/water (100 mL) and ethyl acetate (25 mL) . The aqueous layer was separated and extracted with ethyl acetate (3 x 25 mL) . The combinedethyl acetate fractions were washed with brine/water (1:1, 4 x 25 mL), dried (anhydrous sodium sulfate), filtered and reduced in vacuo. The resulting residue was chromatographed (gradient 20?100percent ethyl acetate in cyclohexane) to afford the title compound (2.77 g, 66.1 percent) . ?H NMR (400 MHz, CDC13) : 3 10.07 (s, 1H), 8.62 (d,1H), 8.28 (dd, 1H), 7.06 (d, 1H), 3.35 (d, 2H), 3.14?3.17 (m, 2H) , 2.72 (dd, 2H) , 1.13 (d, 6H) . LCMS (Method C) := 0.43 mi m/z = 264 [M+H].

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

Reference：
Patent; ALMAC DISCOVERY LIMITED; HARRISON, Timothy; TREVITT, Graham; HEWITT, Peter Robin; O’DOWD, Colin Roderick; BURKAMP, Frank; WILKINSON, Andrew John; SHEPHERD, Steven D.; MIEL, Hugues; WO2015/92431; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

3022-15-9, Piperazine-2-carboxylic acid dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Pyrazine-2-carboxylic acid hydrochloride (2 g, 9.8 mmol)And (Boc) 2O (8.6 g, 39.4 mmol)Was dissolved in THF (40 mL) and water (40 mL)Sodium bicarbonate (8.31 g, 79.8 mmol) was added,The reaction mixture was stirred magnetically at room temperature for 4 hours and then added with ethyl acetate.Poured into a separatory funnel, and the separated organic phase was washed with saturated brine, dried over anhydrous sodium sulfate,The solvent was concentrated under reduced pressure and purified by silica gel column chromatography to obtain 2.5 g of 1,4-di-tert-butoxycarbonylpiperazine-2-carboxylic acid (13-2) in a yield of 78%

3022-15-9, As the paragraph descriping shows that 3022-15-9 is playing an increasingly important role.

Reference：
Patent; Fujian Jinle Pharmaceutical Technology Co., Ltd.; Zhou Zhongxiang; Xing Yuanyuan; Chen Yingzhong; Deng Chengjun; Deng Honggui; Xue Wanhua; Zhang Shuzu; Chen Weipeng; Li Fang; (27 pag.)CN107174584; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

68104-63-2, 4-(Piperazin-1-yl)benzonitrile is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

68104-63-2, Preparation 23 tert-butyl 4-(4-cyanophenyl)piperazine-1-carboxylate 4-(piperazin-1-yl)benzonitrile (0.7g, 3.74mmol) was dissolved in a mixture of dioxane/water (15ml/7ml), then 1 N solution of NaOH was added (5.2ml) and finally BOC2O (0.82g, 3.78mmol). The reaction mixture was stirred at r.t. for 2h. The solvent was concentrated and the residue redissolved in water and the pH adjusted to 7 by adding 2N HCl. The aqueous layer was extracted with chloroform and the organic layer washed with brine, dried over magnesium sulphate and evaporated under reduced pressure to give 1 g of the desired compound (yield=93%) as a white solid. LRMS: m/z 288 (M+1)+ Retention time: 6.33 min (Method B) 1H NMR (300 MHz, CDCl3) delta ppm: 1.49 (s, 9H), 3.33-3.35 (m, 2H), 3.57-3.59 (m, 2H), 6.84-6.87 (m, 2H), 7.50-7.53 (m, 2H).

68104-63-2 4-(Piperazin-1-yl)benzonitrile 2733995, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Laboratorios Almirall, S.A.; EP2202232; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics