Category: piperazines

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 6-bromo-4,7-dichloro-2-methylquinazoline (435 mg, 1.49 mmol) and 1 -tert-butyl 2-methyl piperazine- 1 ,2-dicarboxylate (437 mg, 1.79 mmol) in 1,4-dioxane (30 mL), DIEA (769 mg, 5.96 mmol) was added. The mixture was stirred at 80C for 1.5 h. The mixture was allowed to cool to RT and partitioned between water and ethyl acetate. The organic layer was washed with brine, dried over Na2SO4 and concentrated. The residue was purified by flash column chromatography on silica gel (5-50 % ethyl acetate/petroleum ether) to afford the desired product (224 mg,30 % yield) as a yellow solid.

The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ARAXES PHARMA LLC; JANES, Matthew, Robert; PATRICELLI, Matthew, Peter; LI, Liansheng; REN, Pingda; LIU, Yi; (397 pag.)WO2016/44772; (2016); 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.161357-89-7,1-(Methylsulfonyl)piperazine hydrochloride,as a common compound, the synthetic route is as follows.

Intermediate 594-{2-[5-Chloro-2-(4-methanesulfonyl-piperazin-1 -yl)-pyrimidin-4-yl1-1 -hvdroxy-ethyl)- piperidine-1 -carboxylic acid tert-butyl esterA mixture of 4-[2-(2,5-dichloro-pyrimidin-4-yl)-1 -hydroxy-ethyl]-piperidine-1 – carboxylic acid tert-butyl ester (100 mg), 1 -methanesulfonyl-piperazine hydrochloride (70 mg), potassium carbonate (100 mg), and N,N-dimethylformamide (1 mL) is stirred for 4 h at 60C. After cooling to room temperature ethyl acetate is added. The organic phase is separated, washed with water and brine, dried over MgS04, and concentrated in vacuo. The residue is chromatographed on silica gel(cyclohexane/ethyl acetate 50:50? 0: 100) to give the title compound. LC (method 7): tR = 1 .46 min; Mass spectrum (EST): m/z = 504 [M+H]+.

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

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HIMMELSBACH, Frank; ECKHARDT, Matthias; HEINE, Niklas; LANGKOPF, Elke; NOSSE, Bernd; WO2012/80476; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 1 -benzhydrylazetidin-3-yl methanesulfonate (2.4 g, 7.56mmol), tert-butyl methyl piperazine-1,3-dicarboxylate (1.85 g, 7.56 mmol), K2C03 (1.6 g, 11.34 mmol) in CH3CN (40 mL)was stirred atreflux for 16 h. The mixture was partitioned between ethyl acetate and water. The organic layer was washed with waterand brine, dried over Na2504, and concentrated in vacuo. The residue was purified by flash column chromatography on silica gel (10% petroleum ether/ethyl acetate) to afford the desired product (1.85 g, 51% yield).

129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; ARAXES PHARMA LLC; JANES, Matthew, Robert; PATRICELLI, Matthew, Peter; LI, Liansheng; REN, Pingda; LIU, Yi; (397 pag.)WO2016/44772; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109384-27-2, 1-Methylpiperazin-2-one hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of ethyl 2-(4-methyl-3-oxopiperazin-l-yl)-2- phenylacetate (150). DIPEA (0.52 ml, 2.96 mmol) and l -methylpiperazin-2-one hydrochloride (0.22 g, 1.48 mmol) were sequentially added to a solution of ethyl 2-bromo-2-phenylacetate (0.22 ml, 1.23 mmol) in acetonitrile (4 ml). The reaction was stirred at room temperature for 1.5 hours. DIPEA (0.13 ml, 0.74 mmol) was added again and the reaction was stirred at room temperature overnight. The solvent was evaporated and the crude was purified by flash chromatography (DCM/Acetone = 9/1) to obtain ethyl 2-(4-methyl-3-oxopiperazin- l-yl)-2-phenylacetate (256 mg, 75 % yield) as a yellow oil. 1H NMR (300 MHz, DMSO-d6) ppm 6.91 – 7.66 (m, 5 H), 4.28 (s, 1 H), 3.99 – 4.22 (m, 2 H), 3.23 (t, 2 H), 3.00 (s, 2 H), 2.80 (s, 3 H), 2.61 – 2.71 (m, 2 H), 1.14 (t, 3 H).

As the paragraph descriping shows that 109384-27-2 is playing an increasingly important role.

Reference£º
Patent; CHIESI FARMACEUTICI S.P.A.; AMARI, Gabriele; PESENTI, Cristina; BOSSOLO, Stefano; WO2013/98145; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (S) – 4 – (2-hydroxy-1-phenyl-ethylamine) – 5-methyl-pyrrolo [2,1-f] [1, 2, 4] triazine-6-carboxylic acid (100 mg, 0 . 32mmol) and 1-cyclopropanecarboxylic formyl piperazine (74 mg, 0 . 48mmol) dissolved in N, N-dimethyl formamide (8 ml) in, then add 1-hydroxy benzotriazole (52 mg, 0 . 39mmol), 1-ethyl-3 – (3-dimethylamino-propyl) carbodiimide hydrochloride (74 mg, 0 . 39mmol) and triethylamine (98 mg, 0 . 96mmol), stirring the mixture at room temperature until the TLC reaction monitoring raw material the reaction is complete, to be added in to the reaction solution (100 ml), ethyl acetate (50 ml ¡Á 3) extraction, then by saturated sodium chloride solution (100 ml ¡Á 2) washing, the organic phase is dried with anhydrous sodium sulfate, concentrated under reduced pressure, the resulting residue is purified with silica gel column chromatography, to obtain (S) – (4-cyclopropyl carbonyl-piperazine-1-yl) – [4 – (2-hydroxy-1-phenyl-ethylamine) – 5-methyl-pyrrolo [2,1-f] [1, 2, 4] triazin-6-yl]-methyl ketone (99 mg, white solid), yield: 69.0%.

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

Reference£º
Patent; SHANGHAI CDYMAX PHARMACEUTICALS CO LTD; An, XiaoXia; Bie, PingYan; Yang, wuli; Liu, Jun; (49 pag.)CN103848833; (2016); B;,
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Piperazines – an overview | ScienceDirect Topics

31321-68-3, (R)-Piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The Boc protecting group of previous compound was removed at room temperature for one hour with a solution of AcOEt/HCl 4M. The mixture was then concentrated in vacuo, diluted with MeOH and concentrated several times in vacuo. The residue was then coupled with the corresponding acid (1.1 eq.), in the presence of BOP (1.1 eq.) and NMM (2.2 eq.) for two hours, in DCM. The mixture was then concentrated in vacuo and the residue dissolved in AcOEt. The organic layer was successively washed with aqueous solutions of 1M KHSO4, saturated NaHCO3 and brine. The organic layer was then dried over Na2SO4, filtered and concentrated in vacuo to yield the desired compound which was then treated with 4M AcOEt/HCl as already described if necessary. The final compound purified by preparative HPLC on a C18 column using a water/acetonitrile/TFA 0.1% gradient (yield around 50% for the three steps).

31321-68-3 (R)-Piperazine-2-carboxylic acid 6558437, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; AETERNA ZENTARIS GmbH; CENTRE NAT DE LA RECHERCHE SCIENTIFIQUE; University of Montpellier I; University of Montpellier II; US2009/239877; (2009); 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.1030377-21-9,(S)-1-Boc-2-(Hydroxymethyl)piperazine,as a common compound, the synthetic route is as follows.

Levofloxacin carboxylic acid (225.0mg, 0.8mmol) was dissolved in DMSO (dimethyl sulfoxide, 5.0mL), was added TEA (triethanolamine, 0.44mL, 3.2mmol) and Compound S1-5 (259.5mg, 1.2mmol), at 90 deg.] C in a microwave reactor 24h. After completion of the reaction, cooled to room temperature, dichloromethane (15 mL), then washed three times (15 mL), dried over anhydrous yellow solid was recrystallized from ethanol to give 105.1 mg, yield 27.51% calculated measured

1030377-21-9 (S)-1-Boc-2-(Hydroxymethyl)piperazine 22884145, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; Guangdong Zhong Hospital; Guangdong Experiment Animal Monitor Suo; Liu Bo; Xu Guangyu; Yu Jie; Wu Yue; Chen Cha; Xu Fangfang; Zhang Yu; Han Xiaodong; Lin Dongling; Huang Ren; Lu Jinjian; Zhang Yuqin; (62 pag.)CN106674254; (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.54699-92-2,4-Methyl-1-piperazineacetic acid,as a common compound, the synthetic route is as follows.

Example 13; General Method For The Preparation Of Active Esters Of N-Substituted Piperazine Acetic Acid From Trifluoroacetate Esters; A solution of the trifluoroacetate in THF (0.58 M, 1.2 equiv) was added to a solid sample of N-methyl piperazine acetic acid and mixed in a vortex or shaker until a homogeneous solution was obtained. The reaction of the carboxylic acid with the trifluoroacetate ester was generally complete within 30 min for all cases except N-hydroypyrrolidinone (NHP, 18 h). The progress of conversion to the active ester was monitored by ES-MS. The amount of product and any starting material (N-MPA) could be determined by direct infusion of a sample of the reaction (in ethanol) into the ES-MS. In some cases the active ester product was precipitated as dihydrochloride salt by the addition of a solution by addition of HCl solution in dioxane (4 M, 50% volume of the reaction) followed by washing with THF, ethyl acetate and hexanes. In other cases the product was isolated from the reaction as the mono TFA salt. Addition of TFA could be performed if the bis-TFA salt was desired. Dhbt ester, Calculated MH+ = 304.14 Found = 304.20 NHP ester, Calculated MH+ = 242.15 Found = 242.20 4-NP ester, Calculated MH+ = 280.13 Found = 280.20 1H NMR (400 MHz, CDCl3) d 8.20 (d, 2H, J=9.2 Hz, aromatic protons), 7.25 (d, 2H, J=9.2 Hz, aromatic protons), 3.69-3.40 (broad, 2H, ring protons), 3.57 (s, 2H, -CH-CO-), 3.15-2.90 (broad, 6H, ring protons), 2.78 (s, 3H, -CH3). Pfp ester, Calculated MH+ = 325.10 Found = 325.10 Pcp ester, Calculated MH+ = 404.95 Found = 405.90 3-NP ester, Calculated MH+ = 280.13 Found = 280.20 NHS ester, Calculated MH+ = 256.13 Found = 256.10

As the paragraph descriping shows that 54699-92-2 is playing an increasingly important role.

Reference£º
Patent; Applera Corporation.; US2005/148773; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1235865-77-6, 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(0104) Compound 5K (3.39 g), Compound 5A (1.87 g), 1-ethyl-3-[3-(dimethylamino)propyl]-carbodiimide hydrochloride (2.39 g), and 4-dimethylaminopyridine (1.09 g) were stirred in CH2Cl2 (40 ml) for 24 hours. The reaction was cooled and chromatographed on silica gel with 25-100% ethyl acetate/hexanes, then 10% methanol/ethyl acetate with 1% acetic acid, to give the product (1.62 g, 32%) as a white solid. 1H NMR (300 MHz, dimethylsulfoxide-d6) delta 11.65 (br s, 1H), 8.55 (br s, 1H), 8.04 (d, 1H), 7.89 (dd, 1H), 7.51 (m, 3H), 7.33 (d, 2H), 7.08 (m, 1H), 7.04 (d, 2H), 6.68 (dd, 1H), 6.39 (d, 1H), 6.19 (d, 1H), 3.84 (m, 1H), 3.30 (m, 4H), 3.07 (m, 4H), 2.73(m, 2H), 2.18 (m, 6H), 1.95 (m, 2H), 1.61 (dd, 2H), 1.38 (m, 2H), 1.24 (m, 4H), 0.92 (s, 6H).

As the paragraph descriping shows that 1235865-77-6 is playing an increasingly important role.

Reference£º
Patent; AbbVie Inc.; Catron, Nathaniel; Lindley, David; Miller, Jonathan M.; Schmitt, Eric A.; Tong, Ping; US10213433; (2019); B2;,
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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of 5-bromobenzofuran (250 mg, 1.27 mmol, 1.0 equiv.) and 2-methylpiperazine (508.4 mg, 5.08 mmol, 4.0 equiv.) in toluene (7 mL) was added PdCl2[P(o-Tol)3]2 (30 mg, 0.04 mmol, 0.04 equiv.) followed by sodium tert-butoxide (183 mg, 1.91 mmol, 1.5 equiv.). The resulting mixture was heated to 100 C. with stirring under nitrogen. After stirred at same temperature for 16 hours, the reaction mixture was cooled to room temperature and then diluted with ethyl acetate (100 mL). The resulting solution was washed with water, brine and then dried over Na2SO4. After removal of solvent, the crude product was purified by chromatography to give 132 mg (48% yield) of 1-Benzofuran-5-yl-3-methyl-piperazine. 1H NMR (400 MHz, CDCl3), delta (ppm): 7.56 (d, 1H), 7.39(d, 1H), 7.10 (d, 1H), 7.00 (dd, 1H), 6.69 (m, 1H), 3.44 (d, 2H), 306 (m, 3H), 2.72 (dt, 1H), 2.38 (d, 1H), 1.14 (d, 3H).

As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference£º
Patent; Kalypsys, Inc.; US2005/234046; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics