Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.859518-35-7,tert-Butyl 3-cyanopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

859518-35-7, A solution of tert-butyl 3-cyanopiperazine-1-carboxylate, prepared as described in the previous step, (10 g, 0.047 mol) and 2-(2-hydroxyethoxy)acetaldehyde (14.8 g) (see: Bodin, A., Contact Dermatitis, 2001, 44:207) in dichloromethane was treated with formic acid (12.7 g), and the reaction mixture was stirred at room temperature overnight. Sodium cyanoborohydride (7.2 g, 0.118 mol) was added in portions. The reaction mixture was stirred at room temperature for 3 hours followed by the addition of water and extraction with dichloromethane. The organic layer was washed with brine, dried over sodium sulfate, filtered, and concentrated. The crude product was purified by column chromatography to provide the product. 1H NMR: (CDCl3, 400 MHz): delta (ppm) 4.15 (s, 1H), 3.69-3.63 (m, 4H), 3.58 (d, J=4.4 Hz, 2H), 3.47-3.44 (m, 4H), 2.61 (d, J=5.2 Hz, 2H), 2.51-2.48 (m, 4H), 1.43 (s, 9H).

The synthetic route of 859518-35-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Janssen Pharmaceutica NV; Hryhorenko, Eric; Sankaran, Banumathi; DeCory, Thomas R.; Tubbs, Theresa; Colt, Linda; Remmerie, Bart M.; Salter, Rhys; Donahue, Matthew Garrett; Gong, Yong; (53 pag.)US9850318; (2017); B2;,
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

To a stirred solution of 1 -(tert-butyl) 3-methyl piperazine-1 , 3-d icarboxy late (CAS Number 129799-08-2; 0.500 g, 2.05 mmol) in DCM (5 ml) were added phenylboronic acid (0.347 g, 3.07 mmol) and copper acetate (0.1 1 1 g, 0.614 mmol) at rt. The reaction mixture was stirred at rt for 16 h. The resulting reaction mixture was poured into water (50 ml) and extracted with EtOAc (2 x 25 ml). The combined organic phase was collected, dried over Na2S04, filtered and concentrated under reduced pressure. The resulting residue was purified by column chromatography (10% MeOH in DCM) yielding 1 -(tert-butyl) 3-methyl 4-phenylpiperazine-1 ,3- dicarboxylate (0.200 g, 0.625 mmol). LCMS: Method C, 2.385 min, MS: ES+ 321 .53.

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; MISSION THERAPEUTICS LIMITED; STOCKLEY, Martin Lee; KEMP, Mark Ian; MADIN, Andrew; (167 pag.)WO2018/65768; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

278788-66-2, (R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

diisopropylethylamine (156 mL, 894 mmol) was added to a stirred, room temperaturemixture of 3-(2-Bromo-acetyl)-6-fluoro-2-methyl-benzonitrile (176 g, 688 mmol) and (R)-4-N-Boc-2-hydroxymethylpiperazine(149 g, 688 mmol) in THF (3500 mL) and the mixture was stirred at room temperature for 18 h. Thereaction was diluted with 3 L EtOAc, washed twice with 1500 mL 10% NaHCO3 aqueous solution, dried over MgSO4,filtered and concentrated. The residue was purified by column chromatography on silica gel (40-80% EtOAc/Hexanes,linear gradient), to provide the title compound.Step E: 17C and 17D: A 5000-mL, three-necked,, 278788-66-2

As the paragraph descriping shows that 278788-66-2 is playing an increasingly important role.

Reference£º
Patent; Merck Sharp & Dohme Corp.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; (128 pag.)EP2744499; (2016); B1;,
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Piperazines – an overview | ScienceDirect Topics

70261-81-3, 1-Methyl-4-(4-nitrobenzyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

70261-81-3, A mixture of 1-methyl-4-(4-nitro-benzyl)-piperazine (3.09 g, 13.1 mmol), zinc dust (4.29 g, 65.6 mmol) and ammonium chloride (2.81 g, 52.5 mmol) in methanol (100 mL) was refluxed 1h, cooled, filtered through Celite (washing with methanol) and evaporated to provide 4-(4-methyl-piperazin-1-ylmethyl)-phenylamine (2.67 g, 99% yield) as a pale yellow, waxy solid. 1H-NMR (DMSO-d6, 500 MHz) 6.89 (d, 2H), 6.49 (d, 2H), 4.89 (s, 2H), 3.24 (s, 2H), 2.3 (br m, 8H) ppm; MS (FIA) 206.2 (M+H); HPLC (Method A) co-elutes with solvent front.

As the paragraph descriping shows that 70261-81-3 is playing an increasingly important role.

Reference£º
Patent; VERTEX PHARMACEUTICALS INCORPORATED; WO2004/46120; (2004); 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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: To solution of compound 3 (1 equiv) in 20 ml of ACN,NaI (1.2 equiv) was added and the mixture was refluxed for 30 min and cooled to room temperature. Subsequently,K2CO3 (1.2 equiv) and appropriate phenylpiperazine derivative(1.2 equiv) were added. Then the mixture was refluxedfor 4h. At the end of this period, the mixture was evaporatedto dryness then the product was solidified with ice-cold waterand crystallized from appropriate solvent., 30459-17-7

The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Kilic, Burcu; Erdogan, Merve; Gulcan, Hayrettin O.; Aksakal, Fatma; Oruklu, Nihan; Bagriacik, Emin U.; Dogruer, Deniz S.; Medicinal Chemistry; vol. 15; 1; (2019); p. 59 – 76;,
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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

30459-17-7, Example 88 [00202] To a solution of Compound 88a (25 mg, 0.077 mmol) in DMF (0.6 mL) was added DIEA (0.041 mL, 0.23 mmol) followed by l-(4-(trifluoromethyl)phenyl)piperazine (36 mg, 0.16 mmol). To the stirring solution was added BOP reagent (41 mg, 0.093 mmol) then the reaction mixture heated at 80 C for 2 h then 100 C for 2 h. The reaction mixture was allowed to cool to rt, diluted with ACN then purified by prep HPLC (RT = 1 1.0 min using Axia Luna 5u C 18 30x100mm column with flow rate of 40 mL/min over 10 min period. Solvent A = 10/90/0.1% ACN/H20/TFA to solvent B = 90/10/0.1 , 20 to 100% B). The fractions containing product were evaporated to remove the ACN, then lyophilized. This material was chromatographed on silica gel eluting with 0 to 20% EtOAc/DCM to give Example 88 (3.0 mg, 7% yield) as a yellow solid. LCMS = 2.37 min using analytical method (B), 536.2 (M+H). NMR (400MHz, CDC13) delta 8.42 (d, J=8.8 Hz, IH), 8.21 (d, J=1.3 Hz, IH), 7.86 (dd, J=8.8, 1.8 Hz, IH), 7.69 (d, J=7.3 Hz, 2H), 7.55 (d, J=8.5 Hz, 2H), 7.51 (t, J=7.4 Hz, 2H), 7.46 – 7.39 (m, IH), 7.00 (d, J=8.5 Hz, 2H), 3.98 – 3.90 (m, 4H), 3.48 – 3.42 (m, 4H). EL IC50 494nM.

30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; TORA, George O.; FINLAY, Heather; HU, Carol Hui; JIANG, Ji; JOHNSON, James A.; KIM, Soong-Hoon; LLOYD, John; PARKHURST, Brandon; PI, Zulan; QIAO, Jennifer X.; WANG, Tammy C.; WO2014/42939; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

196811-66-2, tert-Butyl 4-carbamothioylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of tert-butyl 4-carbamothioylpiperazine-1-carboxylate (synthesized according to Example 5, Step 1, 1.31 g, 5.36 mmol) in isopropanol (15 mL), tert-butyl 3-bromo-2,4- dioxopiperidine-1-carboxylate obtained in the first step (1 .3 g, 4.46 mmol) was added at rt. The reaction mixture was stirred overnight at 90 C. It was cooled down to rt and evaporated under reduced pressure. Water (10 mL) was added and the desired product was extracted with diethyl ether (2 x 30 mL), dried over Na2SO4 and concentrated, affording the title product. Yield: 74% (1.42 g, yellow solid). LCMS: (Method A) 239.0 (M-Boc+H), Rt. 0.70 min, 48.39% (Max)., 196811-66-2

As the paragraph descriping shows that 196811-66-2 is playing an increasingly important role.

Reference£º
Patent; ASCENEURON SA; QUATTROPANI, Anna; KULKARNI, Santosh S.; GIRI, Awadut Gajendra; (243 pag.)WO2016/30443; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,169447-70-5

To a solution of iodobenzene (2.08 g, 10.19 mmol) in toluene (60 mL) at rt was added (S)-tert-butyl-2-methylpiperazine-l-carboxylate (1.7 g, 8.49 mmol), Pd2(dba)3 (778 mg, 0.85 mmol) , t-BuONa (2.44 g, 25.46 mmol), XantPhos (982 mg, 1.70 mmol) under nitrogen. The reaction mixture was stirred at 100 C for 16 h, then cooled to rt and diluted with EtOAc (60 mL x 3). The combined organic layers were washed with brine, dried over Na2S04, filtered, concentrated, and purified by chromatography (silica, EtOAc/PE = 1/10) to afford (S)-tert-butyl- 2-methyl-4-phenylpiperazine-l-carboxylate (1.8 g , 6.5 mmol, 64%) as an oil. ESI-MS (EI+, m/z): 277.2 [M+H]+.

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NAVITOR PHARMACEUTICALS, INC.; O’NEILL, David John; SAIAH, Eddine; KANG, Seong Woo Anthony; BREARLEY, Andrew; BENTLEY, Jonathan; (184 pag.)WO2018/89493; (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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

[0707] To a mixture of 1-[4-(trifluoromethyl)phenyl]piperazine (600 mg, 2.61 mmol) and triethylamine (660 mg, 6.52 mmol) in dichloromethane (20 ml) was added 2-chloroacetyl chloride (380 mg, 3.36 mmol) dropwise at 0 C. The resulting solution was stirred for 1 hour at room temperature. The reaction mixture was then quenched by water (80 ml) and extracted with dichloromethane (3¡Á30 ml). The organic layers were combined, dried over anhydrous magnesium sulfate, and concentrated under vacuum. The residue was purified by silica gel column chromatography using 1%-10% ethyl acetate in petroleum ether to afford 2-chloro-1-[4-[4-(trifluoromethyl)phenyl]piperazin-1-yl]ethan-1-one as a white solid (479 mg, 60%). (ES, m/z): [M+H]+ 307.1; 1H NMR (300 MHz, CDCl3): delta 7.52 (d, J=8.4 Hz, 2H), 6.97 (d, J=8.7 Hz, 2H), 4.12 (s, 1H), 3.81 (t, J=5.1 Hz, 2H), 3.72 (t, J=5.1 Hz, 2H), 3.36 (t, J=5.1 Hz, 2H), 3.30 (t, J=5.1 Hz, 2H).

30459-17-7, 30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Merial Limited; Meng, Charles Q.; Long, Alan; Huber, Scot; Gurrala, Srinivas Reddy; Wilkinson, Douglas Edward; Pacofsky, Gregory; US2014/142114; (2014); 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

5747-48-8, EXAMPLE 3:PREPARATION OF 1 1 -[4-(2-(2-HYDROXYETHOXY)-ETHYL)- I-PIPERAZINYL] DIBENZO[b,f][l,4]THIAZEPINETo a mixture of 1000 ml of organic layer (obtained from example 2), 100 grams of sodium carbonate (0.944 mol) and 6.25 grams of sodium iodide (0.042 mol), 37.5 ml of chloroethoxyethanol (0.36 mol) and 187.5 ml of N-Methyl pyrrolidone (NMP; 1.95 mol) are added and the reaction mixture is stirred at 1 10-120 degree C for about 8 hours. 1000 ml of water is added to the reaction mass and stirred for 15 min. The organic layer is separated and washed with water (2x1000ml). Organic layer is dried using Dean stark by azeotropic distillation. This organic layer on distillation under reduced pressure yields the title compound (quetiapine free base) as a viscous oil. Yield : 135g (80 % ); Purity (HPLC area%) : 98.5 %.

As the paragraph descriping shows that 5747-48-8 is playing an increasingly important role.

Reference£º
Patent; SANDOZ AG; WO2007/20011; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics