Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

[0253] 4-(fe/7-Butoxycarbonyl)-l-(4-(tert-butoxycarbonyl)-l-(4-((4-((8A,l 1/?,13L’,- 14L’, 1 IS)- 17-hyd roxy- 13-methy 1-3-oxo- 17-(p rop- 1 -yn-1 -yl)- 2,3,6,7,8,ll,12,13,14,15,16,17-dodecahydro-l -cyclopenta[fl]phenanthren-ll- yl)phenyl)(methyl)amino)butanoyl)piperazine-2-carbonyl)piperazine-2-carboxylic acid (0380) To a solution of Intermediate C (132 mg, 0.263 mmol) and 1 -(tert-butyl) 3-methyl piperazine-l,3-dicarboxylate in DMF (1 ml) were added iPnNEt (0.092 ml, 0.526 mmol) and HATU (110 mg, 0.289 mmol) and the resulting mixture was stirred at room temperature for 12 h. The reaction mixture was diluted with EtOAc (20 mL) and washed with sat NH4CI (20 mL), water (20 mL x 3), and brine (20 mL). The organic layer was dried over Na2S04, filtered and concentrated under reduced pressure. The residue was dissolved in 1.0 mL of THF and 0.4 mL of water and treated with LiOH and stirred at room temperature for 1 hour. The residue was purified by reverse phase preparative HPLC (Mobile phase: A = 0.1% TFA/H2O, B = 0.1% TFA/MeCN; Gradient: B = 10 – 90%; 20 min) to give the title compound (13.1 mg, 0.014 mmol, 5.38 % yield) as a brown amorphous material.

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; BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM; LINK, James, T.; LISSANU DERIBE, Yonathan; (91 pag.)WO2019/200217; (2019); A1;,
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.34334-28-6,4-(4-Methylpiperazin-1-yl)benzonitrile,as a common compound, the synthetic route is as follows.

4-Fluorobenzonitrile (12 g, 99 mmol, 1 eq.) and 100 mL of DMF are placed in a 250 mL round-bottomed flask. N-Methylpiperazine (16 mL, 1.6 eq., 123 mmol) is added to this solution. The orange solution is heated at a temperature in the region of 90 C. for 15 hours. The solvent is then evaporated to dryness and the residue is diluted with 500 mL of diethyl ether. The solution is washed with sodium hydrogen carbonate solution (2*100 mL) and then with saturated sodium chloride solution (100 mL). After evaporation, the 4-(4-methylpiperazin-1-yl)benzonitrile (orange solid, 10 g, 77%) is used without further purification in the following hydrolysis step. It is added at a temperature in the region of 0 C. to a solution of 98% sulfuric acid (25 mL) and 5 mL of water. The purple solution is then heated at a temperature in the region of 100 C. for 8 hours. The solution is cooled and then hydrolyzed by pouring onto ice. The pH is adjusted to 9-10 with sodium hydroxide pellets. The precipitate obtained is filtered off and washed thoroughly with water and then with tetrahydrofuran, which partially dissolves the product. The water is separated out by settling. After evaporating the organic phase to dryness, a solid is obtained, which is purified by chromatography on silica gel, eluding with a methanol/dichloromethane mixture (15/85 by volume). 4-(4-Methylpiperazin-1-yl)benzamide (8.7 g, 80%) is thus obtained in the form of a white solid, which is used directly in the following step., 34334-28-6

The synthetic route of 34334-28-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Aventis Pharma S.A.; US2008/146542; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

76003-29-7,76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Will be 49.94mmol3-oxo-1-piperazinecarboxylic acid tert-butyl ester1 dissolved in 100 mL of tetrahydrofuran,Add 51.4 mmol of 60% NaH to the temperature below zero, stir for 30 minutes, then add 25.5 mL of ethyl bromide and reflux for 3 hours.It was quenched by cooling with water, extracted with ethyl acetate and dried.Spin dry to obtain 10.8 g of compound 2, the recovery of compound 2 was 95%;

The synthetic route of 76003-29-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Shanghai Changtai Biological Technology Co., Ltd.; Lu Qian; Kuang Yi; Li Guohua; (9 pag.)CN108822048; (2018); 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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

mixture of 4-methyl-2-piperazinone (200 mg, 1.75 mmol), 4-iodoaniline (384 mg, 1.75 mmol), K3PO4 (848 mg, 4.00 mmol) and 1,2-trans-diaminocyclohexane (98 uL, 0.80 mmol) in dioxane (6 mL) was degassed with Ar before being charged with CuI (76 mg, 0.40 mmol). The mixture in a sealed tube was heated at 110 0C for 4 h. It was then purified by a silica gel prep-TLC using CH2C12/MeOH (95/5) as solvents to give the desired product (25 mg). MS 206.2 (M+H)., 34770-60-0

The synthetic route of 34770-60-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PORTOLA PHARMACEUTICALS, INC.; WO2006/55951; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

67455-41-8, 4-(Piperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

67455-41-8, To a solution of 2-chloro-N-cyclohexyl-9-(tetrahydro-2H-pyran-2-yl)-9H- purin-6-amine (0.50 g, 1.5 mmole) in 7.5 ml toluene was added 4-(piperazin-l-yl)aniline (317 mg, 1.8 mmole) and 2-di-tert-butylphosphino-2′,4′,6′-triisopropylbiphenyl (63 mg, 0.15 mmole). The reaction mixture was degassed using Argon for 10 min after which Pd(dppf)Cl2 complex with CH2C12 (61mg, 0.075 mmole) was added, followed by sodium t-butoxide (286 mg, 3.0 mmole). The reaction flask was put into a preheated oil-bath at 100 C and stirred overnight. The mixture was cooled to room temperature. To the mixture, water and EtOAc were added. The layers were separated and the aqueous layer was extracted with EtOAc. The combined organic layer was dried over Na2S04 and concentrated. The crude product was purified on a silica gel column, eluted EtOAc, then 10% MeOH in EtOAc, then 20%MeOH in EtOAc to get 480mg (68% yield) of N6-cyclohexyl-N2-(4-(piperazin-l- yl)phenyl)-9-(tetrahydro-2H-pyran-2-yl)-9H-purine-2,6-diamine

As the paragraph descriping shows that 67455-41-8 is playing an increasingly important role.

Reference£º
Patent; THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE; LIU, Xuedong; ZHANG, Gan; CHAN, Daniel, Chuen-Fong; PISCOPIO, Anthony, D.; (117 pag.)WO2015/175813; (2015); 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.

General procedure: To a solution of 14 (200 mg, 0.63 mmol) in DMA (60 mL), HOBt(170 mg, 1.26 mmol), EDCI (242 mg, 1.26 mmol), and DIPEA(0.208 mL, 1.26 mmol) and then the corresponding piperazine wereadded, and the mixture was stirred overnight. Water (10 mL) wasadded to the mixture, which was stirred for an additional 1 h. Then,the mixture was extracted with ethyl acetate (50 mL x 3). Thecombined organic layers were washed with brine, dried overanhydrous sodium sulfate and concentrated to give the crudeproduct, which was purified by column chromatography to affordthe corresponding compounds in good yields., 21043-40-3

The synthetic route of 21043-40-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Chen, Wenhua; Guo, Ne; Qi, Minghui; Dai, Haiying; Hong, Minghuang; Guan, Longfei; Huan, Xiajuan; Song, Shanshan; He, Jinxue; Wang, Yingqing; Xi, Yong; Yang, Xinying; Shen, Yanyan; Su, Yi; Sun, Yiming; Gao, Yinglei; Chen, Yi; Ding, Jian; Tang, Yun; Ren, Guobin; Miao, Zehong; Li, Jian; European Journal of Medicinal Chemistry; vol. 138; (2017); p. 514 – 531;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-59-9, tert-Butyl 3-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2) 3,4-Dimethylpiperazine-1-carboxylic acid tert-butyl ester 36percent Aqueous formalin (833 muL) and sodium triacetoxyborohydride (3.18 g) were added at room temperature to the above-obtained 3-methylpiperazine-1-carboxylic acid tert-butyl ester (2.0 g) in methylene chloride (40 mL), followed by stirring for 3 hours. Saturated aqueous sodium hydrogencarbonate was added thereto for partitioning the reaction mixture. The organic layer was washed with brine, and dried over magnesium sulfate anhydrate. After a filtration step, the solvent was removed under reduced pressure, to thereby give a 3,4-dimethylpiperazine compound as an oily product (1.95 g, 91percent). 1H-NMR(300MHz, CDCl3) delta:1.05 (3H, d, J=6.24Hz), 1.49(9H,s), 1.96-2.05(2H,m), 2.11-2.24(1H, m), 2.28(3H,s), 2.72(1H, d, J=11.75Hz), 3.00(1H, t, J=11.20Hz), 3.81(2H,br s). MS (FAB)m/z:215 (M+H)+., 120737-59-9

The synthetic route of 120737-59-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1621537; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a solution of isocyanate (1.877mmol) in toluene (2.5mL) was added a solution of a monosubstituted piperazine (1.877mmol) in toluene (1.0mL). The reaction mixture was heated at 40-45C for 30 to 60min. The reaction mixture was then cooled down to room temperature (22-25C) and the resulting solids were filtered and washed with more toluene (2.0mL). The wet solids were then placed in 2.0mL of toluene, stirred at room temperature for about 30min, filtered and washed with toluene (1.0mL) to obtain the crude disubstituted piperazine derivative. Finally, all crude derivatives were purified by silica-gel column chromatography using a mixture of dichloromethane/methanol (9:1) to afford pure piperazines products., 5747-48-8

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Patil, Mahadev; Noonikara Poyil, Anurag; Joshi, Shrinivas D.; Patil, Shivaputra A.; Patil, Siddappa A.; Bugarin, Alejandro; Bioorganic Chemistry; vol. 92; (2019);,
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.5521-39-1,2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol,as a common compound, the synthetic route is as follows.

5521-39-1, To a solution of Example 7 compound 1b (313 mg, 1 mmol) and TFE (2,2,2-trifluoroethanol, 4 mL) was added 2-[4- (4-aminophenyl)piperazin-1-yl]ethanol (265 mg, 1.2 mmol) and TFA (trifluoroacetic acid, 342 mg, 3 mmol). The resulting mixture was heated to reflux and stirred overnight, then cooled to room temperature. EtOAc (50 mL) was added and the mixture was washed with saturated NaHCO3 (50 mL). The organic layer was dried over magnesium sulfate, filtered, and concentrated in vacuo to obtain the crude compound. Then purify with silica gel column, dichloromethane: methanol = 20: 1 rinse, after concentration to obtain the target compound 2o.

As the paragraph descriping shows that 5521-39-1 is playing an increasingly important role.

Reference£º
Patent; Guangdong University of Technology; Chen Huixiong; Yan Longjia; Li Yongliang; Chen Anchao; Deng Minggao; (30 pag.)CN110724137; (2020); 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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

6-Bromo-3,4-dihydroisoquinolin-2(1H)-carboxylic acid tert-butyl ester (300 mg, 0.96 mmol), (2S,6R)-2,6-dimethylpiperazine at room temperature (131 mg, 1.15 mmol), BINAP (119 mg, 0.19 mmol),Sodium tert-butoxide (276 mg, 2.88 mmol), Pd2 (dba) 3 (87.9 mg, 0.10 mmol) and toluene (6 mL) were added to the reaction flask. Sealed, replaced with nitrogen 3 times,The mixture was heated to 100 ¡ã C for 4 hours. After the reaction solution is cooled to room temperature,Diluted with ethyl acetate (50 mL) and the organic phase was washed with brine.Dry over anhydrous sodium sulfate, filter, and the filtrate was evaporated.The residue was purified by EtOAc EtOAc EtOAc EtOAcYield 6-((3S,5R)-3,5-dimethylpiperazin-1-yl)-3,4-dihydroisoquinoline-2(1H)-tert-butyl carboxylic acid (330 mg, yellow solid, yield: 99.79percent)., 21655-48-1

The synthetic route of 21655-48-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Beijing Yue Zhi Kangtai Bio-pharmaceutical Technology Co., Ltd.; Duan Maosheng; Xiong Yanlin; Liu Jiale; Tian Shihong; Dai Quan; (57 pag.)CN109232533; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics