Heterocyclic Building Blocks-piperazine

75336-86-6, (R)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

75336-86-6, In a nitrogen atmosphere, 115 mL of di-tert-butyl dicarbonate was dropwise added to chloroform (500 mL) solution of 50.0 g of (R)-2-methylpiperazine, over 1 hour. The reaction liquid was washed with water, and dried with anhydrous magnesium sulfate. The solvent was evaporated off under reduced pressure, and the residue was separated and purified through silica gel column chromatography (hexane/ethyl acetate = 2/1) to obtain 63.5 g of the entitled compound as a colorless oily substance.

The synthetic route of 75336-86-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BANYU PHARMACEUTICAL CO., LTD.; EP1726590; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

115761-79-0, 1-(2,4-Difluorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 2- (5-amino-2- (furan-2-yl) -7H-pyrazolo [4, 3-e] [1, 2, 4] triazolo [1, 5-c] pyrimidin-7-yl) -2-phenylpropanoic acid (50 mg, 0.13 mmol) , 1- (2, 4-difluorophenyl) piperazine (25 mg, 0.13 mmol) , HATU (59 mg, 0.16 mmol) and DIEA (33 mg, 0.26 mmol) in DMF (5 mL) was stirred at rt for 2 hrs. The solution was added with water (10 mL) , extracted with ethyl acetate (10 mL) and washed with brine (10 mL) . The organic layer was dried, concentrated and purified by column chromatography (PE: EA = 2: 1) and preparative TLC (DCM: MeOH = 20: 1) to get the desired product (20 mg, 28%) .1H NMR (400 MHz, DMSO-d6) delta 8.31 (s, 1H) , 8.08 (br. s, 2H) , 7.95 (d, J = 4.0Hz, 1H) , 7.30-7.11 (m, 7H) , 6.92-6.86 (m, 2H) , 6.74 (d, J = 4.0Hz, 1H) , 3.71 (br. s, 2H) , 3.45-3.40 (m, 2H) , 3.16-2.90 (m, 4H) , 2.35 (s, 3H) ppm. MS: M/e 570 (M+1)+

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

Reference£º
Patent; BEIGENE, LTD.; ZHANG, Guoliang; SUN, Hanzi; ZHOU, Changyou; (253 pag.)WO2020/20097; (2020); A1;,
Piperazine – Wikipedia
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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

The 5 – ((2,4-dioxo -3,4-dihydrochinazolines having antiviral properties -1 (2H)-yl) methyl) – 2-fluoro-benzoic acid (50 mg, 0 . 16mmol), EDCI (62 mg, 0 . 32mmol), HOBT (44 mg, 0 . 32mmol) and TEA (33 mg, 0 . 32mmol) into the reaction bottle in, addition of about 2 ml of the dissolution of water-free DMF, r.t. The lower stirring 60 min, then dropwise (2S, 6R) – 2,6-dimethyl piperazine (28 mg, 0 . 24mmol) in the DMF solution to the reaction solution, r.t. The lower stirring overnight, the reaction solution is poured into 100 ml water, using 100mLDCM extraction, an organic layer for sequentially 1MHCl (100 ml), saturated NaCl (100 ml) and water (100 ml) washing, concentrating under reduced pressure, column chromatography, to obtain 40 mg solid, yield 61.3percent.

21655-48-1, As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

Reference£º
Patent; Institute Of Materia Medica Chinese Academy Of Medical Sciences; Xu, Bailing; Chen, Xiaoguang; Yao, Haiping; Ji, Ming; Jin, Jing; Zhou, Jie; Wang, Ke; Zhao, Dalong; (55 pag.)CN105461697; (2016); A;,
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954388-33-1, (R)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,954388-33-1

(a) [2S]-1-Benzyloxycarbonyl-4-t-butoxycarbonyl-2-methoxycarbonylmethylpiperazine A solution of of [2R]-1-benzyloxycarbonyl-4-t-butoxycarbonylpiperazine-2-carboxylic acid (prepared as in Example 1(b) and 2(a)) (4.7g) in ethyl acetate (70ml) containing N-methylmorpholine (1.76ml) at 0C was treated with isobutyl chloroformate (2.37ml) for 3 hours and the solution was filtered and added to an excess of diazomethane and left at room temperature for 18 hours.. It was evaporated to dryness to afford the diazoketone, which was dissolved in dry methanol (120ml) and treated with silver benzoate (1.99g) in triethylamine (19.9ml), with cooling in ice.. The solution was stirred in the dark at room temperature for 18 hours, evaporated to dryness, dissolved in ethyl acetate, washed with sodium bicarbonate solution and dried over sodium sulfate.. It was chromatographed on silica gel, eluding with ethyl acetate-hexane to afford an oil (3.15g) (94% ee by chiral HPLC).

The synthetic route of 954388-33-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SmithKline Beecham plc; EP1187828; (2004); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of (3 ?)-3-methyl-6-(2- methyloxiran-2-yl)-3,4-dihydro-lH-isochromen-l-one (598 mg, 2.74 mmol) and tert-butyl (35)- 3 -(hydroxymethyl)piperazine-l -carboxylate (770 mg, 3.56 mmol dissolved in EtOH (15mL) was heated in a sealed tube to 110C for 14 hours. The reaction was cooled and concentrated to give crude product which was purified via MPLC (30-80%) EtOAc/Hexane) to give the title compound as a mixture of diastereomers: LC-MS: (M+l)+ 435;, 314741-40-7

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

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PIO, Barbara; PASTERNAK, Alexander; SHAHRIPOUR, Aurash; TANG, Haifeng; WALSH, Shawn; WO2013/90271; (2013); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.162046-66-4,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

4- (4- (tert-Butoxycarbonyl) pirhoerazin-1-yl) benzoic acid (10 g, 32.64 mmol) was dissolved in anhydrous THF (200 mL) under nitrogen at O0C and BH3. THF (IM in THF, 65.3 mL, 65.3 mmol) was added over 15 min. The reaction was EPO maintained at this temperature and after 3 h a further portion of BH3-THF (IM in THF, 10 mL, 10 itimol) was added. After 2 h, MeOH (30 mL) was added and the reaction was warmed to rt. The reaction mixture was partitioned between EtOAc (150 mL) and brine (200 mL) . The aqueous layer was re-extracted with EtOAc (100 ruL) and the combined organics were washed with a saturated aqueous solution of NaHCXb (150 mL) and then dried (MgSO/j) and filtered. On concentration of the solution the title compound (8.57 g, 90%) precipitated as a white solid and was collected by filtration. 1H NMR (CDCl3) 1.51 (9H, s), 8.14 (4H, t) , 3.62 (4H, t) , 4.62 (2H, d) , 6.94 (2H, d) , 7.31 (2H, d) .

162046-66-4, The synthetic route of 162046-66-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; VERTEX PHARMACEUTICALS INCORPORATED; WO2007/27528; (2007); A2;,
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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Add to the reaction flask6-bromo-3-aldehyde pyridine (2.43 g, 13 mmol) and(S) -2-methylpiperazine-1-carboxylic acid tert-butyl ester(2) (3.4 g, 17 mmol) and dichloromethane (30 mL)Sodium triacetoxyborohydride (4.3 g, 20 mmol) was added in portions.The mixture was stirred at room temperature for 12 hours, water (10 mL) was added,Dichloromethane extraction (20 mL x 3).The organic phase was washed with saturated Na2CO3 solution (40 mL)Saturated brine (40 mL), dried over anhydrous sodium sulfate, filtered,Concentrated under reduced pressure. The residue was purified by column chromatography (DCM / MeOH = 20: 1)The resulting residue was purified to give the title compound (2.2 g, white solid)Yield 45%., 169447-70-5

As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; Gan & Lee Pharmaceuticals; Liu, Wenjian; Yin, Lei; Li, Heng; (94 pag.)CN106608879; (2017); 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.182618-86-6,1-Boc-4-(4-Nitrophenyl)piperazine,as a common compound, the synthetic route is as follows.

tert-Butyl 4-(4-nitrophenyl)piperazine-1-carboxyiate (11) (3.24 g, 10.5 mmol) was dissolved in EtOAc (90 mL) under an atmosphere of nitrogen and a slurry of 10% Pd/C (0.500 g) in EtOAc (10 mL) was added. The resulting suspension was then stirred vigorously under an atmosphere of hydrogen at room temperature for 42 hours. The catalyst was removed by filtration through Celite, which was washed with EtOAc (7 x 10 mL) and the solvent was removed in vacuo to give the title compound (12) (2.92 g, 99 % yield) as a pale pink solid; 1H N R (400 MHz, afe-DMSO) delta 6.72 – 6.66 (m, 2H), 6.52 – 6.45 (m, 2H), 4.60 (s, 2H), 3.44 – 3.39 (m, 4H), 2.87 – 2.79 (m, 4H), 1.41 (s, 9H). LCMS Method C: rt 4.40 min; m/z 278.2 [M+H]+., 182618-86-6

The synthetic route of 182618-86-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CANCER THERAPEUTICS CRC PTY LTD; DEVLIN, Mark Graeme; STREET, Ian Philip; TONG, Warwick Bonner; WO2014/27199; (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.196811-66-2,tert-Butyl 4-carbamothioylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The production of compound No. 26 proceeds according to the sequence of reaction steps shown in the following schemes: The first sub-step shown above was performed at 20 C. during 2 hours with a molar excess of CH2N2 (about 2 molar equivalents) in dry ether, then in a second sub-step (shown below) performed at 5 C. HCl gas was bubbled into the reaction mixture for 15 minutes, and the desired intermediate was obtained in 71% yield. For the conversion from 3 to 4, the first sub-step shown above was performed at 20 C. during 1 hour with a molar excess of thio-carbonyldiimidazole (about 2 molar equivalents) in THF, then in a second sub-step performed at 20 C. for 12 hours a 25% aqueous NH3 solution was added, and the desired intermediate was obtained in 72% yield. The conversion from 4 to 5 was performed during 6 hours with 1 molar equivalent NaHCO3 at reflux in methanol, and the desired intermediate was obtained in 92% yield. The conversion from 5 to 6 was performed during 3 hours at 20 C., and the desired intermediate was obtained in 90% yield. The conversion from 6 to the final compound was performed during 6 hours at 20 C. in 1,2-dichloroethane (DCE) in the presence of a molar excess of triethylamine (1.2 molar equivalents).

196811-66-2, The synthetic route of 196811-66-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NV reMYND; US2010/197703; (2010); 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.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

To a solution of compound 8 (1.33 g, 4.66 mmol) and compound11 (1.03 g, 4.66 mmol) in anhydrous 1-butanol (20 mL), trifluoroacetic acid (0.36 mL, 4.66 mmol) was added. The reaction mixturewas heated to 100 C and stirred for 18 h. Subsequently, it wascooled to room temperature and saturated aqueous sodium bicarbonatesolution was added drop wise until basic pH was obtained.The volatiles were removed in vacuo and the obtained thick slurrywas dissolved in DCM (50 mL). The organic layer was washed withwater (20 mL), brine (20 mL), dried over anhydrous sodium sulfate,filtered and concentrated in vacuo. The crude was purified by flashsilica gel chromatography using DCM/MeOH (96:4, v/v) as eluentto afford 1.42 g of the desired product 12 (3.02 mmol, 65%) as white solid., 122833-04-9

122833-04-9 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline 20136253, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Basu, Debjit; Richters, Andre; Rauh, Daniel; Bioorganic and Medicinal Chemistry; vol. 23; 12; (2015); p. 2767 – 2780;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics