Month: June 2021

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The mixture of Pd2(dba)3 (377 mg, 0.410 mmol), piperidine (500 mg, 5.87 mmol), t-BuOK (851 mg, 7.58 mmol), X-Phos (418 mg, 0.877 mmol) and intermediate M-2 (1000 mg, 3.35 mmol) in toluene (40 mL) was heated under a nitrogen atmosphere at 110 C until complete by TLC. Upon completion, the reaction solution was cooled to ambient temperature, concentrated under vacuum, and purified by flash chromatography (3:1 petroleum ether: ethyl acetate eluent) to yield N-(2,6-dimethyl-4-(piperidin-1-yl)phenyl)-3,3-dimethylbutanamide (293mg, 29% yield)., 30459-17-7

As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference：
Article; Yang, Shaoning; Lu, Dingqiang; Ouyang, Pingkai; Bioorganic and Medicinal Chemistry Letters; vol. 28; 10; (2018); p. 1731 – 1735;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,59702-07-7

To 188 (10 mg, 0.026 mmol) in DMF (800 mu) was added 1- methylpiperazin-2-one (14.8 mg, 0.130 mmol) and the reaction mixture was heated at 90 °C for 2 h. Solvent was removed under reduced pressure and the residue was purified by preparatory TLC (CH2Cl2:MeOH-NH3 (7 N), 20: 1 to afford 10 mg (83percent) of 189t. MS (m/z): [M+H]+ 462.1.

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MEMORIAL SLOAN KETTERING CANCER CENTER; CHIOSIS, Gabriela; KANG, Yanlong; PATEL, Hardik J.; PATEL, Maulik; OCHIANA, Stefan; RODINA, Anna; TALDONE, Tony; SHRESTHA, Liza; (288 pag.)WO2015/175707; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

170911-92-9, tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

170911-92-9, Step 3. 4-[4-(6-Bromo-imidazo[1,2-a]pyrazin-8-ylamino)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester [0167] A mixture of 6, 8-dibromoimidazo [1, 2-a] pyrazine (12. 5 MMOL), 4- (4-AMINO- PHENYL)-PIPERAZINE-L-CARBOXYLIC acid tert-butyl ester (12) (13. 1 mmol), potassium carbonate (25 mmol), acetonitrile (50 ML) and N, N-DIMETHYLACETAMIDE (20 mL) is heated at 65 C for 16 hrs. The mixture is cooled to room temperature, treated water (100 mL), and extracted with ethyl acetate (3 x 80 mL). The extracts are washed with water (3 x 60 mL) and brine (1 x 60 mL), dried over magnesium sulfate, and concentrated in vacuo. The residue is’ chromatographed over silica gel, eluting with ethyl acetate, to give 4- [4- (6-bromo- imidazo [1, 2-a] pyrazin-8-ylamino)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester (13) as a light brown foam.

As the paragraph descriping shows that 170911-92-9 is playing an increasingly important role.

Reference：
Patent; CELLULAR GENOMICS, INC.; WO2005/14599; (2005); 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.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

To a stirred solution of 4-((4-ethylpiperazin- 1 -yl)methyl)-3-(trifluoromethyl)aniline (Intermediate Cl) (150 mg, 0.52 mmol) in THF (20 mL) was added triphosgene (54 mg, 0.18 mmol) and the resulting mixture was stirred at 70 C. After 1 h of heating the mixture wasconcentrated under reduced pressure and the residue was dissolved in THF (20 mL). That solution was added dropwise to a stirred mixture of tert-butyl 4-(5-amino-2-chlorophenoxy)- 6H-pyrimido [5,4-b] [1 ,4]oxazine-8(7H-carboxylate (step 1 intermediate) (150 mg, 0.40 mmol) and triethylamine (172 jiL, 1.19 mmol) in THF (20 mL) at RT. The resultant mixture was stirred for 2 h at 70 C. The mixture was cooled to RT and quenched with water. Theaqueous mixture was extracted twice with ethyl acetate. The combined organic layers were washed with water followed by brine. The solution was dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure. The residue thus obtained was purified by silica gel column chromatography to yield 100 mg of the desired product. ?H NMR (400 MHz, DMSO-d6) oe 1.09 (t, J= 7.2 Hz, 3H), 1.50 (s, 9H), 2.42-2.5 1 (m, 1OH), 3.54 (br s, 2H),3.94 (t, J= 8.4 Hz, 2H), 4.40 (t, J= 7.6 Hz, 2H), 7.29 (dd, J, = 2.4 Hz, J2 = 8.0 Hz, 1H), 7.48(d, J 8.8 Hz, 1H), 7.55-7.94 (m, 3H), 7.95 (s, 1H), 8.05 (s, 1H), 9.15 (s, 1H), 9.20 (s, 1H)., 630125-91-6

The synthetic route of 630125-91-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLENMARK PHARMACEUTICALS S.A.; PATEL, Vinod; REDDY, Venkateshwar; GHARAT, Laxmikant Atmaram; CHAUDHARI, Sachin Sundarlal; DAS, Sanjib; VELGALETI, Ranganadh; SHAH, Daisy Manish; BAJPAI, Malini; (262 pag.)WO2018/215668; (2018); 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.655225-01-7,tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1. 5-Bromo-4-(cyclobutylmethoxy)-1-methyl-3-(2-piperazin-1-ylethyl)-1,3-dihydro-2H-benzimidazol-2-one A solution of 5-bromo-4-(cyclobutylmethoxy)-1-methyl-1,3-dihydro-2H-benzimidazol-2-one (250 mg, 0.803 mmol) in N,N-dimethylformamide (7.96 mL) was treated with cesium carbonate (1.31 g, 4.02 mmol) followed by the addition of tert-butyl 4-(2-bromoethyl)piperazine-1-carboxylate (471 mg, 1.61 mmol), and the resultant reaction mixture was stirred at 60° C. overnight, after which time the LCMS analysis of the reaction mixture indicated complete conversion of the starting materials. The reaction mixture was diluted with ethyl acetate and water. Layers were separated and the organic layer was washed with brine, dried with magnesium sulfate, filtered, and concentrated in vacuo to give the crude intermediate tert-butyl carboxylate, which was used in further step without purification., 655225-01-7

The synthetic route of 655225-01-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; INCYTE CORPORATION; Yue, Eddy W.; Combs, Andrew P.; Douty, Brent; US2015/148342; (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.303-26-4,1-((4-Chlorophenyl)(phenyl)methyl)piperazine,as a common compound, the synthetic route is as follows.

Example 29 : Preparation of N-(4-methylbenzyl)-5-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-l-yl)-3,3-dimet hyl-5-oxopentanamide; [409][410] 0.5 mmol of 4-(4-methylbenzylcarbamoyl)-3,3-dimethylbutanoic acid prepared inPreparative Example 14, 0.55 mmol of l-(4-chlorobenzhydryl)piperazine, and ben- zotriazol-1-yloxytripyrrolidino phosphonium hexafluorophosphate (PyBOP) were added to 3 mL of dimethylformamide (DMF) to dissolve. Then, 1.0 mmol of N,N-diisopropylethylamine (DIEA) was added thereto, and stirred at room temperature for 16 hours. 20 mL of 10% HCl was put into the reaction solution, and extracted with 30 mL of EtOAc. The organic layer was washed with 20 mL of 10% HCl, and then washed with 20 mL of a saturated NaHCO 3 solution twice and with 20 mL of a saturated NaCl solution twice. The organic layer was collected, dried over anhydrousMgSO , and filtered under reduced pressure. The organic solvent in the filtrate was4 removed under reduced pressure. The residue was purified by column chromatography with a mixed solvent of EtOAc and methanol (20:1), so as to obtain the title compound (light yellow solid, yield: 70%). [411] mp 63-64C;[412] 1U NMR (CDCl ) delta 8.05 (t, J=5.8 Hz, NH), 7.35 (d, J=8.0 Hz, 4CH), 7.30 (d, J=7.2Hz, 3CH), 7.26 (t, J=8.4 Hz, 2CH), 7.18 (d, J=8.0 Hz, 2CH), 7.10 (d, J=8.0 Hz, 2CH), 4.38 (d, J=5.6 Hz, CH2), 4.20 (s, CH), 3.56-3.66 (m, CH2), 3.51 (t, J=5.0 Hz, CH2),2.34-2.37 (m, 2CH ), 2.33 (s, CH ), 2.32 (s, 2CH ), 1.02 (s, 2CH ); [413] HR-FABMS Calcd for C 32 H 38 ClN 3 O 2 : (M++l): 532.2731, Found: 532.2719.

303-26-4, As the paragraph descriping shows that 303-26-4 is playing an increasingly important role.

Reference：
Patent; PARK CHOO, Hea-Young; WO2007/142431; (2007); 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.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

57260-71-6, 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).

As the paragraph descriping shows that 57260-71-6 is playing an increasingly important role.

Reference：
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.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

In a three-neck round-bottomed flask, 1-(2-hydroxyethyl)piperazine (3.00 g, 23.05 mmol) was dissolved in 15 mL of water. A solution of benzylchloroformate (3.95 mL, 27.66 mmol) in 15 mL of acetonitrile was added dropwise via isobar cylindrical funnel. In order to maintain the pH around 9, a solution of 4N NaOH was added dropwise via a second isobar cylindrical funnel. The reaction mixture was stirred overnight at RT and then extracted with DCM (2 x 75 mL). The aqueous phase containing the final compound was acidified with 3N HCl and extracted with DCM (3 x 75 mL). Organic extracts were combined, washed with brine (150 mL), dried over anhyd. sodium sulfate and concentrated under vacuum. The crude was purified by flash chromatography (0 to 2% of MeOH in DCM) to afford 18 (5.41g, 90%) as a colorless oil. 1H-NMR (500 MHz, DMSO, delta): 7.37-7.29 (m, 5H, CH arom.), 5.05 (s, 2H, CH2Phi), 4.41 (s, 1H, OH), 3.49 (m, 2H, CH2OH), 3.35 (m, 4H, (CH2)2N(Z)), 2.36 (m, 6H, CH2N, CH2NCH2). 13C-NMR (100.6 MHz, DMSO, delta): 115.04, 137.59, 129.09, 128.49, 128.22, 66.81, 60.83, 59.14, 53.51, 44.16. MS (ESI) m/z 265.00 (M + H)+., 103-76-4

As the paragraph descriping shows that 103-76-4 is playing an increasingly important role.

Reference：
Article; Denoyelle, Severine; Chen, Ting; Chen, Limo; Wang, Yibo; Klosi, Edvin; Halperin, Jose A.; Aktas, Bertal H.; Chorev, Michael; Bioorganic and Medicinal Chemistry Letters; vol. 22; 1; (2012); p. 402 – 409;,
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.502649-32-3,1-Boc-3-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

502649-32-3, A mixture of 10- hydroxy-10-((6-oxo-4-phenylpyrimidin-1 (6/-/)-yl)methyl)-7-azaspiro[4.5]decane-7-carbonyl chloride (10 mg, 0.0249 mmol), tert- butyl 3-isopropylpiperazine-1-carboxylate (8.5 mg, 0.0373 mmol) and DIPEA (13 mI_, 0.0746 mmol) in DCM (0.5 mL) was stirred at rt for 2 h 30 min before tert- butyl 3-isopropylpiperazine-1-carboxylate (8.5 mg, 0.0373 mmol) and DIPEA (13 pL, 0.0746 mmol) were added. The reaction was stirred for further 18 h 45 min before DMF (0.5 mL) was added and the reaction stirred for a further 6 days. The reaction mixture was diluted with saturated NaHC03(aq) (15 mL) and the resulting mixture was extracted with DCM (3 x 10 mL) using a phase separator. The combined organic phases were concentrated under reduced pressure and the residue was purified by flash (1504) chromatography (0-100% EtOAc in cyclohexane) to give the title compound (7.7 mg, 52%) as colourless glass. LCMS (Method A): RT = 1.70 min, m/z = 594 [M+H]+.

502649-32-3 1-Boc-3-Isopropylpiperazine 44558596, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ALMAC DISCOVERY LIMITED; ROUNTREE, James Samuel Shane; WHITEHEAD, Steven Kristopher; TREDER, Adam Piotr; PROCTOR, Lauren Emma; SHEPHERD, Steven David; BURKAMP, Frank; COSTA, Joana Rita Castro; O’DOWD, Colin; HARRISON, Timonthy; (333 pag.)WO2019/150119; (2019); 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.

Step C: tert-butyl(3S)-3-(hydroxymethyl)-4-[2-hydroxy-2-( 1-oxo- 1 ,3-dihydro-2-benzofuran-5-yl)ethyll piperazine- 1 -carboxylate: 5- (Oxiran-2-yl)-2-benzofuran- 1 (3H)-one (1.5 g, 8.5 mmol)and commercially available (S)-4-N-BOC-2-hydroxymethyl piperazine (2.394 g, 11.07 mmol)were combined in ethanol (10 mL) in a microwave tube. The mixture was degas sed then heated for 60 mm at 150 C. LC-MS showed the product peak. The reaction was worked up by adding ethyl acetate and washing once with brine. The organic layer was separated, dried, andconcentrated to dryness. The crude product was purified by MPLC using an 80g Redi-sep column and eluted with 50%-i 00% EtOAc hexane yielding the title compound.

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

Reference：
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DEJESUS, Reynalda, Keh; FRIE, Jessica, L.; PIO, Barbara; TANG, Haifeng; WALSH, Shawn, P.; WO2014/99633; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics