Month: March 2021

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 7-bromo-2-(chloromethyl)-5-cyclopropyl-6-methyl-oxazolo[4, 5-c]qui nol in-4-one (Intermediate 2) (150 mg, 0.41 mmol) and potassium phosphate tribasic (173 mg, 0.82 mmol) in dry (mol. sieves) and degassed DMF (5 mL) under N2 was added methyl 4-Boc- piperazine-2-carboxylate (199 mg, 0.82 mmol). The reaction mixture was heated to 80C under microwave irradiation for 1 h. On cooling H20 (20 mL) was added to the reaction mixture followed by EtOAc (30 mL) and the layers were separated. The organic layer was washed with H20 (3 x 20 mL) and the solvent was removed in vacuo. The crude reaction product was purified by flash silica chromatography using a gradient of 0-50% EtOAc in DCM as the eluent. The solvent was removed from fractions containing the desired product to give 1 -tert-butyl 3-methyl 4-[(7-bromo-5-cyclopropyl-6-methyl-4-oxo-oxazolo[4, 5- c]quinolin-2-yl)methyl]piperazine-1 ,3-dicarboxylate (132 mg, 56 % yield).LC-MS (Method F) 575.3/577.3 [M+H] RT 3.50 mm, 129799-08-2

The synthetic route of 129799-08-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; REDX PHARMA PLC; HUXLEY, Anthony; KIRK, Ralph; NOONAN, Gary; UOSIS-MARTIN, Mario; BARDELL-COX, Oliver; STOKES, Neil; (276 pag.)WO2017/46606; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

Piperazine-1,2-dicarboxylic acid, 1-tert-butyl ester, 2-methyl ester (250 mg, 1.03 mmol) was added dropwise to a stirred solution of 4-bromobenzoyl chloride (250 mg, 1.14 mmol), triethylamine (0.43 mL, 3.09 mmol) and DMAP (5 mg) in anhydrous 1,2-dichloroethane (10 mL) at room temperature. The reaction mixture was stirred for 2 hrs (TLC control) and then poured into water (25 mL) and extracted with diethyl ether (3¡Á25 mL). The combined extract was washed with water (2¡Á10 mL), brine (3¡Á10 mL), dried over anhydrous MgSO4, filtered and concentrated in vacuo. Purification of the product by flash column chromatography, using 40% ethyl acetate/hexane as eluent, afforded the title compound as a white foam (310 mg, 71%), 129799-15-1

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference£º
Patent; The Institutes for Pharmaceutical Discovery, LLC; US2006/122222; (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.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,as a common compound, the synthetic route is as follows.

EXAMPLE 1 J (3.39 g), EXAMPLE 2A (1.87 g), l-ethyl-3-[3-(dimethylamino)propyl]- carbodiimide hydrochloride (2.39 g), and 4-dimethylaminopyridine (1.09 g) were stirred in CH2C12 (40 mL) for 24 hours. The residue was purified by flash chromatography, eluting with 25-100%o ethyl acetate in hexanes, then 10% methanol in ethyl acetate with 1% acetic acid to give the product as a white solid. .H NMR (300MHz, dimethylsulfoxide-d6) 11.65 (brs, 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).

1235865-77-6, The synthetic route of 1235865-77-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ABBOTT LABORATORIES; TAO, Zhi-Fu; WANG, Xilu; SOUERS, Andrew J.; CATRON, Nathaniel D.; SULLIVAN, Gerard; WO2011/150016; (2011); 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.109-01-3,1-Methylpiperazine,as a common compound, the synthetic route is as follows.

To a mixture of 4-aminobenzoic acid (5g, 36.5 mmol), 1-methylpiperazine (3.7 mL, 32.8 mmol) and TEA (16.0 mL, 114.8 mmol) in DCM (100 mL) was added EDC.HCl (10.5 g, 54.8 mmol) and the mixture was stirred at room temperature overnight. The sovent was removed and the residue was purified by silica flash chromatography with 0 to 10% MeOH in DCM. The light yellow oil obtained was dissolved in DCM and filtered. The yellow solid obtained was dissolved in DCM washed with brine then with Na2CO32M. The organic phase was dried and evaporated to give 4-(4-methylpiperazine-1-carbonyl)aniline (3 g, 42% yield). MS found for C12H17N3O as (M+H)+ 220.2., 109-01-3

109-01-3 1-Methylpiperazine 53167, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; PHARMACYCLICS LLC.; ATALLAH, Gordana, Babic; CHEN, Wei; JIA, Zhaozhong, J.; POZZAN, Alfonso; RAVEGLIA, Lucal, Francesco; ZANALETTI, Riccardo; (815 pag.)WO2016/196776; (2016); 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.76003-29-7,1-Boc-3-Oxopiperazine,as a common compound, the synthetic route is as follows.

Step 1: ferf-Butyl 3-oxo-4-(3-thienyl)piperazine-l-carboxylate (Hl)A mixture of l-Boc-3-oxopiperazine (1.0 eq.), 3-bromothiophene (1.5 eq.), K3PO4 (2.0 eq.), CuI (0.4 eq.) and lambda^-dimethylethylendiamine (0.8 eq.) in 1,4-dioxane (0.5M) was put in a sealed vial and stirred at 1100C for 18 hr. Reaction mixture was diluted with EtOAc and filtered through a pad of SolcaFloc 200 FCC. After removal of the solvent, the crude product was purified by flash column chromatography on silica gel using 10- 40% EtO Ac/Petroleum ether as eluent to afford the desired product Hl as pink solid (80% yield). 1H NMR (400 MHz, CDCl3, 300K) delta 7.32-7.28 (3H, m), 4.25 (2H, s), 3.82-3.75 (4H, m), 1.49 (9H, s). MS (ES) CnHi8N2 O3S requires: 282, found: 283 (M+H)+.

76003-29-7, The synthetic route of 76003-29-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A.; WO2009/63244; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

112257-12-2, tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound D_1 (477 mg, 3 mmol), compound G_1 (1 ¡¤ 38 g, 4.5 mmol), 15 mL of acetonitrile was added to a 50 mL single-mouth flask, and the mixture was heated under argon atmosphere. The mixture was heated under reflux, followed by TLC. Acetonitrile, the residue was dissolved with as little CH2CI2 as possible. A large amount of ether was added to precipitate a solid. The solid was carefully sucked out into an Erlenmeyer flask. It was necessary to allow ether to remain on the surface. The ether was immediately blown dry with argon, and the cone was dried. The bottle is sealed with a sealing membrane and kept out of the air. The product was a pink solid 700 mg (compound H-1) with a yield of 50%., 112257-12-2

112257-12-2 tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate 15829155, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; East China University of Science and Technology; Qian Xuhong; Xu Yufang; Jia Xiaotong; Zhu Weiping; Yang Youjun; (14 pag.)CN107619397; (2018); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59702-31-7, 1-Ethylpiperazine-2,3-dione is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

59702-31-7, 650 L of dichloromethane was pumped into a 1000 L No. 2 dissolution tank, and 89 kg of ethyl-dioxypiperazine was added to the feed port under vacuum to cool to 5 C. 91 kg of trimethylchlorosilane was vacuumed in, stirred for 30 min, and the temperature was further lowered to 0 C to obtain a first intermediate.

The synthetic route of 59702-31-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Changzhou Hong Sun Pharmaceutical Co., Ltd.; Chen Jianlin; Zhang Xuejiao; (17 pag.)CN109438476; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2-fluoro-4- (4 4 5 5-tetramethyl-1 3 2-dioxaborolan-2-yl) aniline (500 mg 2.109 mmol) in THF (50 mL) was added triphosgene (219 mg 0.738 mmol) . The resulting miature was stirred at 70 . After 30min LCMS analysis showed the starting material was disappeared. The solvent was removed in vacuo to give 2- (3-fluoro-4-isocyanatophenyl) -4 4 5 5-tetramethyl-1 3 2-dioxaborolane (520 mg 1.977 mmol 94yield) . To a solution of 4- ( (4-ethylpiperazin-1-yl) methyl) -3- (trifluoromethyl) aniline (568 mg 1.977 mmol) Et3N (0.827 mL 5.93 mmol) and DMAP (24.15 mg 0.198 mmol) in THF (50 mL) was added a solution of 2- (3-fluoro-4-isocyanatophenyl) -4 4 5 5-tetramethyl-1 3 2-dioxaborolane (520 mg 1.977 mmol) at 70 . The resulting mixture was stirred at 70 . After LCMS analysis showed the starting material was disappeared. The solvent was removed in vacuo. The residue was dissolved in DCM (100 mL) and washed with H2O (30 mL) and brine (30 mL) . The organic layer was dried over Na2SO4 filtered and concentrated. The residue was purified by column chromatography (DCM/MeOH 20/1) to yiled 1- (4- ( (4-ethylpiperazin-1-yl) methyl) -3- (trifluoromethyl) phenyl) -3- (2-fluoro-4- (4 4 5 5-tetramethyl-1 3 2-dioxaborolan-2-yl) phenyl) urea (0.67 g 0.851 mmol 43.0yield) 1HNMR(400 MHz CD3OD) delta 8.17-8.14 (m 1H) 7.86 (s 1H) 7.69-7.67 (m 1H) 7.60 (d J 8.4 Hz 1H) 7.49 (d J 8.0 Hz 1H) 7.41 (d J 11.2 Hz 1H) 4.59 (s 2H) 3.60 (s 2H) 2.52-2.47 (m 8H) 1.33 (s 12H) 1.10 (t J 7.2 Hz 3H) ES-LCMS m/z m/z 551.2 (M+H), 630125-91-6

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

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXOSMITHKLINE (CHINA) R & D COMPANY LIMITED; CHEUNG, Mui; DEMARTINO, Michael P.; EIDAM, Hilary Schenck; GUAN, Huiping Amy; QIN, Donghui; WU, Chengde; GONG, Zhen; YANG, Haiying; YU, Haiyu; ZHANG, Zhiliu; (391 pag.)WO2016/37578; (2016); 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.

(1) 1-(2-Hydroxyethyl)-4-methylpiperazine A mixture of 1-(2-hydroxyethyl)piperazine (10.0 g, 76.8 mmol), 37percent aqueous formaldehyde solution (11.5 ml, 154 mmol), 10percent palladium carbon catalyst (1.0 g) and methanol (100 ml) was stirred for 13 hr at room temperature in a hydrogen atmosphere. The reaction mixture was filtrated and the filtrate was concentrated. To the obtained residue was added 2N hydrochloric acid, and the mixture was washed with diethyl ether (200 ml). Sodium hydroxide (16 g) was added to the aqueous layer to make the layer alkaline, and the mixture was extracted with chloroform (4*200 ml). The organic layer was dried over anhydrous sodium sulfate and concentrated to give the title compound (9.3 g, 84percent) as a pale-yellow liquid. 1H-NMR (300 MHz, CDCl3) delta 3.61 (t, J=5.4 Hz, 2H), 2.90-2.30 (m, 8H), 2.55 (t, J=5.4 Hz, 2H), 2.29 (s, 3H).

103-76-4, 103-76-4 N-(2-Hydroxyethyl)piperazine 7677, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Mitsubishi Pharma Corporation; US6610729; (2003); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

51.1: 2-Methyl-4-(1-m-tolyl-1H-[1,2,4]triazole-3-carbonyl)-piperazine-1-carboxylic acid tert-butyl ester 2.00 g (9.84 mmol) 1-m-tolyl-1H-[1,2,4]-triazole-3-carboxylic acid was stirred with 3.30 g (10.3 mmol) TBTU and 2.50 mL (14.6 mmol) DIPEA in 30 mL DCM at RT. After 10 min, 2.05 g (9.84 mmol) 2-methyl-piperazine-1-carboxylic acid tert-butyl ester was added and the reaction mixture was stirred at RT for 12 h. The solvent was removed by distillation. The residue was taken up in water and extracted with EtOAc. The combined organic phases were dried over sodium sulfate, filtered and concentrated in vacuo. The crude material was purified by flash chromatography (EtOAc). Yield: 4.00 g (95%), purity: 90% ESI-MS: m/z=386 (M+H)+ Rt(HPLC): 1.48 min (method 8), 120737-78-2

The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; HEIMANN, Annekatrin; DAHMANN, Georg; GRUNDL, Marc; MUELLER, Stephan Georg; WELLENZOHN, Bernd; US2013/158042; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics