Heterocyclic Building Blocks-piperazine

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.

4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)benzoic acid 54 (0.022 mmol), HATU (0.027 mmol) and l-methylpiperazin-2-one (0.022 mmol) are dissolved in dry DMF (0.5 mL) at rt. Diisopropylethylamine (0.06 mmol) is added to the solution. The reaction mixture is stirred for 1 h at rt. HPLC purification affords 4-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)benzoyl)- l-methylpiperazin-2-one Gl as a TFA salt. 1H NMR (400MHz, J6-DMSO) delta 10.1 (s, IH), 8.87 (s, 2H), 7.90 (d, J = 8.4 Hz, 2H), 7.79 (d, J = 8.7 Hz, 2H), 7.43 (d, J = 8.4Hz, 2H), 7.29 (d, J = 8.0 Hz, 2H), 7.12 (t, J = 51.2 Hz, IH), 4.1 (s, 2H), 2.87 (s, 3H), 2.55 (m, 4H). MS (m/z) (M+l)+: 454.2., 59702-07-7

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

Reference：
Patent; IRM LLC; WO2009/26276; (2009); A1;,
Piperazine – Wikipedia
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34770-60-0, 4-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The reaction conditions for 1-4.3.28 differ: Under argon atmosphere 1-2.2 (250 mg, 0.54 mmol), potassium carbonate (150 mg, 1.07 mmol), copper (I) iodide (10 mg, 0.05 mmol), Nu,Nu’- dimethylethylendiamine (25 L, 0.23 mmol) and 4-methyl-piperazin-2-one (75 mg, 0.66 mmol) in dioxane (10 mL) are heated to 80 C for 8 d. The reaction mixture is filtered and the solution is concentrated. The residue is purified by reversed phase HPLC. Yield 30%, m/z 500 [M+H]+, rt 0.98 min, LC-MS Method V011 S01.

34770-60-0, As the paragraph descriping shows that 34770-60-0 is playing an increasingly important role.

Reference：
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; ANDERSKEWITZ, Ralf; GRAUERT, Matthias; GRUNDL, Marc; HAEBEL, Peter, Wilhelm; OOST, Thorsten; PAUTSCH, Alexander; PETERS, Stefan; BINDER, Florian; VINTONYAK, Viktor; WO2014/140075; (2014); 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.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The 100 mg compound II, 120 mg compound III by adding 5 ml dichloromethane (DCM) in, stirring, 40 C reaction 2 hours, TLC monitoring, after the reaction, the solvent turns on lathe does, the reactant putting into the 100 ml water, ethyl acetate (20 ml × 3) extraction, standing liquid, organic phase are respectively 5% of NaHCO3 (20 Ml × 3), saturated salt water (20 ml × 3) washing, then drying water-free magnesium sulfate, filtered, reduced pressure to remove the ethyl acetate to get the yellow oily compound IV 90 mg.

120737-78-2, As the paragraph descriping shows that 120737-78-2 is playing an increasingly important role.

Reference：
Patent; Southern Medical University; Chen Jianjun; Cheng Binbin; (22 pag.)CN109456284; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound (Z) -1- acetyl-3- (methoxy (-2H- tetrahydro-thiopyran-4-yl) methylene) -2-oxo-indole-6-carboxylate Lin ( 600mg, 1.6mmol), 4- (N- methyl-2- (4-methyl-piperazin-1-yl) acetamide) aniline (251mg, 0.96mmol) and potassium hydroxide (50mg, 0.8mmol) was dissolved in 50mL of methanol, the reaction was stirred overnight at 50 deg.] C, the solvent was spin, 50mL of water was added, the mixture with dichloromethane (20mL × 3). the organic phase was dried over anhydrous sodium sulfate, the solvent was spin, the crude product was purified by silica gel column (dichloromethane: methanol = 50: 1) isolated as a dark red solid.(26mg, 3%)

262368-30-9, The synthetic route of 262368-30-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Shandong Hengli medical science and Technology Co Ltd; Luo, haoxian; Wang, aichen; (42 pag.)CN103848814; (2016); B;,
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78551-60-7, tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,78551-60-7

To a solution of oxalyl chloride (1.08 g, 8.30 mmol) in CH2CI2 (7 ml) in a dryice-acetone bath was added DMSO (1.14 g, 14.6 mmol). After 5 min, a solution ofthe product of Step 3 (3.01 g, 7.34 mmol) in CH2CI2 (7 ml) was added and the mixturewas stirred for 1 h. Diisopropylethylamine (3.28 g, 25.4 mmol) was added and after 2min the cooling bath was removed. The mixture was stirred for 30 min and dilutedwith water (50 ml). CH2CI2 (40 ml) was added and the aqueous layer was extractedwith CH2CI2 (40 ml). The combined organic layer was washed with brine, dried(MgSC>4), and concentrated to give the aldehyde, which was not further purified.To a solution of diisopropylamine (896 mg, 8.85 mmol) in THF (5 ml) in a dryice-acetone bath was added 1.6 M butyllithium in hexanes (5.5 ml, 8.8 mmol). After 5min the mixture was put in an ice-water bath and stirred for 20 min. The solution wascooled in the dry ice-acetone bath again and a solution of the product of Step 5 (2.14g, 7.37 mmol) in THF (8 ml) was added. The mixture was stirred for 1 h. A solutionof the above aldehyde in THF (10 ml) was added and the mixture was stirred for 1.5h. The reaction was quenched with water and partitioned between ether (4×50 ml)and water (50 ml). The combined organic layer was washed with brine (50 ml), dried(MgSO4), concentrated, and purified by column chromatography (gradientEtOAc/Hexanes 0-20%) to give the product (2.67 g, 52%). MS m/e 698 (M+H)+

The synthetic route of 78551-60-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SCHERING CORPORATION; WO2006/14762; (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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A solution of iert-butyldimethylsilyl chloride (1.53 g, 10.17 mmol) in DCM (10 ml) was added dropwise to (5)-4-A/-Boc-2-hydroxymethyl-piperazine (2 g, 9.25 mmol) and triethylamine (2.58 ml, 18.49 mmol) in DCM (50 ml) at 20C over a period of 5 minutes under air. The resulting solution was stirred at 20C for 16 hours then evaporated to dryness. The residue was purified by flash silica chromatography, elution gradient 0 to 5% EtOH in EtOAc. Pure fractions were evaporated to dryness to afford te/t-butyl (S)-3-(((ieri-butyldimethylsilyl)oxy)methyl)piperazine-l-carboxylate (2.84 g, 93%) as a colourless oil. 1H NM (500 MHz, CDCI3) 0.00 (s, 6H), 0.84 (s, 9H), 1.40 (s, 9H), 2.48 (s, 1H), 2.6 – 2.87 (m, 3H), 2.92 (d, J = 11.5 Hz, 1H), 3.41 (dd, J = 7.2, 9.8 Hz, 1H), 3.52 (s, 1H), 3.85 (s, 2H).

314741-40-7, The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; BOYD, Scott; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; RAUBO, Piotr, Antoni; (144 pag.)WO2018/206539; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

115619-01-7, 4-(4-Ethylpiperazin-1-yl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 5 (0.10g, 0.48mmol), DIPEA (0.08ml, 0.48mmol) and EtOH (5ml) was mixed with the 85 (0.07g, 0.48mmol) and refluxed for 2.5hrs. The reaction was quenched by saturated NaHCO3 (aq.) and the mixture was extracted by ethyl acetate (30ml x 3). The residue was purified by flash column over silica gel (dichloromethane: methanol = 9: 1, Rf = 0.28) to afford 89 (0.05g, 33.24%) as a pale yellow solid. 1H-NMR (300MHz, CDCl3): delta 1.13 (t, J= 7.2 Hz, 3H), 2.46 (q, J= 7.2 Hz, 2H), 2.62 (t, J= 5.1 Hz, 4H), 2.98 (d, J= 5.1 Hz, 3H), 3.19 (t, J= 5.1 Hz, 4H), 5.17-5.29 (m, 1H), 5.55 (br, 1H), 6.91 (d, J= 8.7 Hz, 2H), 7.37 (d, J= 8.1 Hz, 1H), 7.46 (s, 1H), 8.20 (d, J= 44.7 Hz, 1H)., 115619-01-7

The synthetic route of 115619-01-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TAIPEI MEDICAL UNIVERSITY; YEN, Yun; LIOU, Jing-Ping; CHEN, Chun-Han; (70 pag.)WO2017/15400; (2017); 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.

4-Cyclopropylmethyl-piperazine-1-carboxylic Acid 4-(5-trifluoromethyl-pyridin-2-yloxy)-phenyl Ester The hydrochloride of the title compound was prepared from 4-(5-trifluoromethyl-pyridin-2-yloxy)-phenyl chloroformate and 1-cyclopropylpiperazine, yield 62%. Recrystallisation from 0.2 M HCl gave white crystals, m.p. 238-239 C.; 1H NMR (DMSO-d6): delta 11.51 (br s, 1H), 8.61-8.55 (m, 1H), 8.30-8.20 (m, dd, 1H), 7.32-7.19 (m, d+s, 5H), 4.44-4.00 (br, 2H), 3.80-3.40 (br m, 4H), 3.29-2.93 (br m, 4H), 1.28-1.05 (br m, 1H), 0.75-0.58 (m, 2H), 0.50-0.35 (m, 2H).IR (KBr): nu 1730, 1713 (C=O) cm-1.

20327-23-5, The synthetic route of 20327-23-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Ebdrup, Soren; de Jong, Johannes Cornelis; Jacobsen, Poul; Hansen, Holger Claus; Vedso, Per; US2003/166644; (2003); 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

4) Preparation of benzyl 3-oxopiperazine-1-carboxylate 1.4; 10 g of piperazin-2-one and 90 g of sodium carbonate were dissolved in 250 ml of water; 500 ml of ethyl acetate were added to this solution, and 20.45 g of benzyl chloroformate were added dropwise with vigorous stirring. After the addition had ended, the mixture was stirred at room temperature overnight. For workup, the organic phase was removed, dried over magnesium sulfate, filtered and concentrated under reduced pressure. This afforded benzyl 3-oxopiperazine-1-carboxylate 1.4. Molecular weight 234.10 (C12H14N2O3); retention time Rt=1.18 min. [B]; MS (ESI): 235.11 (MH+)., 5625-67-2

As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

Reference：
Patent; SANOFI-AVENTIS; US2011/46105; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

To mixture of (2S)(‘/WJ-5-(-1-(tert-butoxy)-2-methoxy-2-oxoethyl)-4-(8-fluoro-5-methylchroman- 6-yl)-1 ,6-dimethyl-1 H-pyrrolo[2,3-b]pyridine-2-carboxylic acid (30 mg, 0.060 mmol) and 1- cyclopentylpiperazine (8.67 pL, 0.060 mmol) in ethyl acetate (1 mL) was added DIEA (0.026 mL, 0.150 mmol) followed by addition of 1-propanephosphonic acid cyclic anhydride (T3P) (0.072 mL, 0.120 mmol) as a 50% solution in ethyl acetate and stirred at room temperature for 30 min. Diluted with ethyl acetate, added water and saturated ammonium chloride and extracted with ethyl acetate. Organic phase was washed with brine, dried over IS^SC^, filtered and concentrated to give (2S (7WJ-methyl 2-(tert-butoxy)-2-(2-(4-cyclopentylpiperazine-1-carbonyl)-4- (8-fluoro-5-methylchroman-6-yl)-1 ,6-dimethyl-1 H-pyrrolo[2,3-b]pyridin-5-yl)acetate (37 mg, 97% yield) as a colorless oil. 1H NMR (400 MHz, CHLOROFORM-d) delta = 6.74 (br. s., 1 H), 5.99 (br. s., 1 H), 5.14 (s, 1 H), 4.32 (t, J=5.0 Hz, 2 H), 3.93 (br. s., 3 H), 3.78 – 3.88 (m, 1 H), 3.59 (s, 3 H), 2.78 – 2.86 (m, 3 H), 2.74 (br. s., 2 H), 2.53 (br. s., 2 H), 2.17 (br. s., 2 H), 1.89 (br. s., 2 H), 1.78 (s, 3 H), 1.57 (br. s., 12 H), 1.06 – 1.17 (m, 9 H); LC/MS (m/z) ES+ = 635 (M+1)

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

Reference：
Patent; VIIV HEALTHCARE UK LIMITED; DE LA ROSA, Martha Alicia; JOHNS, Brian, Alvin; KAZMIERSKI, Wieslaw, Mieczyslaw; SAMANO, Vicente; SUWANDI, Lita; TEMELKOFF, David; VELTHUISEN, Emile; WEATHERHEAD, Jason, Gordon; WO2014/9794; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics