Month: September 2020

34770-60-0, 4-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(iii) (S)- 1 -(4- 1 [2-Amino-4-( 1 -hvdroxyhexan-3-ylamino)-6-methylpyrimidin-5-yl]methyl } -3- methoxyphenyl)-4-methylpiperazin-2-one To a solution of the product from step (ii) (126 mg, 0.240 mmol) in 1 ,4-dioxane (1 mL) was added Cul (46.0 mg, 0.240 mmol), N,N ‘-dimethyldiaminoethane (52.0 mu, 0.480 mmol), 4-methylpiperazin-2-one (55.0 mg, 0.480 mmol), and Cs2C03 (234 mg, 0.720 mmol). The mixture was heated to 100C and stirred for 1 Oh. After cooling, water was added and the resulting mixture was extracted with EtOAc. The combined organic solutions were washed with brine, and then dried (Na2S04). After removal of the solvent in vacuo, the crude residue was used for the next reaction without further purification. To the crude residue in THF (1.0 mL) was added tetra-rc-butylammonium fluoride (1.0 mL, 1M solution in THF) and the mixture was stirred at r.t.. After 5h, water was added and the resulting mixture was extracted with EtOAc. The combined organic solutions were washed with brine, and then dried(Na2S04). After removal of the solvent in vacuo, the crude residue was purified by silica gel column chromatography to give the title compound as a white amorphous solid (19.6 mg, 0.0430 mmol, 18%); NMR: 6.94 (1H , d), 6.86 (1 H, d), 6.75 (1H, dd), 5.07 (2H, br s), 4.90 (1H, d), 4.51 (1H, br s), 4.13 (1 H, m), 3.88 (3H, s), 3.69-3.65 (2H, m), 3.67 (2H, s,),3.31-3.26 (2H, m), 3.25 (2H, s), 2.78-2.76 (2H, m), 2.40 (3H, s), 2.35 (3H, s), 1.80-1.76 (1H, m), 1.44-1.1 1 (5H, m), 0.81 (3H, t); LC-MS: m/z = 457 [MH+] (T = 1.48).

34770-60-0, As the paragraph descriping shows that 34770-60-0 is playing an increasingly important role.

Reference£º
Patent; Dainippon Sumitomo Pharma Co., Ltd.; ASTRAZENECA AKTIEBOLAG; TOSAKI, Shinya; HORI, Seiji; WO2012/67268; (2012); A1;,
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1228780-72-0, 1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(0085) A mixture of Compound 3H (1.55 g), Compound 3E (2.42 g), and HK2PO4 (1.42 g) in dimethylsulfoxide (20 ml) at 135 C. was stirred for 24 hours. The reaction was cooled, diluted with ether (400 ml), and washed with 3¡Á1M NaOH, and brine, and concentrated. The crude product was chromatographed on silica gel with 10-50% ethyl acetate/hexanes.

1228780-72-0, 1228780-72-0 1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine 66713599, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; AbbVie Inc.; Catron, Nathaniel; Lindley, David; Miller, Jonathan M.; Schmitt, Eric A.; Tong, Ping; US10213433; (2019); B2;,
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674792-05-3,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.674792-05-3,(S)-1-Boc-2-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

1-Propanephosphonic acid cyclic anhydride (1.752 mmol. 1.043 ml, 1115 mg) was added to a solution of (S)-tert-butyl 2-isopropylpiperazine-1-carboxylate (0.876 mmol, 200 mg), 4-amino-3-fluorobenzoic acid (0.876 mmol, 136 mg) and triethylamine (1.752 mmol, 0.244 ml, 177 mg) in dichloromethane and stirred at room temperature for 2 hours. After this time, ethyl acetate (100 mL) was then added to the reaction. The organic mixture was washed with saturated sodium hydrogen carbonate, water, dried over sodium sulphate and concentrated under vacuum. The residue was then dissolved in dichloromethane (5 ml) and trifluoroacetic acid (17.52 mmol, 1997 mg) added. The resultant solution was allowed to stand at room temperature overnight. The reaction was concentrated under vacuum and purified by strong cation exchange chromatography to give the title compound (200 mg) as a clear oil. MS (ESI) m/z 266.3 [M+H]+

674792-05-3 (S)-1-Boc-2-Isopropylpiperazine 17750439, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; N.V. Organon and pharmacopeia, Inc.; US2009/264416; (2009); A1;,
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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.

Description 149(S)-tert-butyl 4-(5-fluoro-2-methyl-3-nitrobenzyl)-2-methylpiperazine-1-carboxylate (D149)To a solution of 5-fluoro-2-methyl-3 -nitrobenrzaldehyde (D142, 10 g) and (S)-tert-butyl 2-methylpiperazine-l-carboxylate (12.03 g) in DCM (120 mL) was added drops of acetic acid (3.28 g) and the mixture was stirred at RT for 1 hour. Sodium triacetoxyhydroborate (23.15 g) was added to the mixture in ice-bath and the mixture was stirred at RT overnight and quenched with saturated NaHCO3 solution. The organic layer was dried with anhydrous Na2SO4, filtered and the filtrate evaporated in vacuo to give the title compound (22.17 g) as a syrup. MS (ESI): C18H26FN304requires 367; found 368 {M+H]., 169447-70-5

The synthetic route of 169447-70-5 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; DENG, Jing; LEI, Hui; MA, Xin; LIN, Xichen; WO2015/180612; (2015); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.149057-19-2,4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

Example 52 – Preparation of Intermediate 17 The synthesis of Intermediate 17 followed the procedure of General Procedure 13 following: Intermediate 16 Intermediate 17 To a cooled solution (0C) of 4-(benzyloxycarbonyl)-1-(tert- butoxycarbonyl)piperazine-2-carboxylic acid (Intermediate 16, 20 g, 54.9 mmol) in dry DMF (200 mL) was added cesium carbonate (Cs2CO3, 35.8 g, 109.9 mmol) followed by methyl iodide (10.26 mL, 164.83 mmol). The reaction mixture was stirred at room temperature for 4 hours. After cooling to 0 C the mixture was quenched with ice-cold water (90 mL), and extracted with EtOAc (2 x 100 mL). The combined organic layers were dried over sodium sulfate, filtered and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (100-200 mesh), eluting with 20% EtOAc/n-hexane, to afford 4- benzyl 1-tert-butyl 2-methyl piperazine-1,2,4-tricarboxylate (Intermediate 17, 25 g, yield-55%) as an off-white solid. TLC: 30% ethyl acetate in hexane. Rf: 0.5.

149057-19-2, As the paragraph descriping shows that 149057-19-2 is playing an increasingly important role.

Reference£º
Patent; VERSEON CORPORATION; SHORT, Kevin Michael; ESTIARTE-MARTINEZ, Maria de los Angeles; KITA, David Ben; SHIAU, Timothy Philip; (340 pag.)WO2016/138532; (2016); A1;,
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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 a stirred solution of compound 5a-b (2 mmol) in dry DCM (10 mL) was added K2CO3 (1.1 equiv, 2.2 mmol, 304 mg). The mixture was cooled with a bath of ice/water, and then the appropriate N-substituted piperazine (2 equiv, 4 mmol), dissolved in DCM (2 mL), was added slowly over 30 min. The mixture was then stirred at room temperature for two hours, diluted with DCM (10 mL), washed with water (10 mL) and then with brine (10 mL). The organic layer was dried (Na2SO4), filtered and concentrated in vacuo to give a brown residue that was purified by column chromatography to furnish the derivatives 6a-aq.

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

Reference£º
Article; Romagnoli, Romeo; Baraldi, Pier Giovanni; Carrion, Maria Dora; Cara, Carlota Lopez; Cruz-Lopez, Olga; Salvador, Maria Kimatrai; Preti, Delia; Tabrizi, Mojgan Aghazadeh; Shryock, John C.; Moorman, Allan R.; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Bioorganic and Medicinal Chemistry; vol. 20; 2; (2012); p. 996 – 1007;,
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.2031-23-4,1-(3-Chloropropyl)-4-methylpiperazine dihydrochloride,as a common compound, the synthetic route is as follows.

EXAMPLE 183 4-Anilino-5-bromo-2-{4-[3-(4-methylpiperazin-1-yl)propoxy]anilino}pyrimidine A mixture of potassium carbonate (180 mg, 1.3 mmol), 4-anilino-5-bromo-2-(4-hydroxyanilino)pyrimidine (Method 4, 150 mg, 0.42 mmol) and 3-(4-methyl-1-piperazinyl)propyl chloride dihydrochloride (120 mg, 0.48 mmol) in DMSO (2 ml) was heated at 100 C. for 12 hours. Silica (1 g) was added and volatile material was removed by evaporation. The residue was loaded onto a Varian Mega Bond Elut column and the column was eluted with 50:50 iso-hexane: DCM (2*20 ml), DCM (2*20 ml), 2% 2M NH3/MeOH/DCM (2*20 ml), 4% 2M NH3/MeOH/DCM (2*20 ml), 6% 2M NH3/MeOH/DCM (2*20 ml) and 10% 2M NH3/MeOH/DCM (8*20 ml). Concentration of the appropriate fractions gave the product as a yellow solid (35 mg, 17%). MS (MH+): 497, 499; HPLC (RT): 2.74.

2031-23-4, As the paragraph descriping shows that 2031-23-4 is playing an increasingly important role.

Reference£º
Patent; AstraZeneca AB; US6593326; (2003); B1;,
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13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate (c) (1.82 g, 4.8 mmol), palladium acetate (52 mg, 0.24 mmol), 2-dicyclohexylphosphino-2′,6′-dimethoxybiphenyl (240 mg, 0.48 mmol), cesium carbonate (2.32 g, 7.2 mmol) is dissolved in dioxane (15 ml), add 1-acetylpiperazine (0.92 g, 7.2 mmol), nitrogen protection, 100 C reflux stirring 6 hr, the reaction liquor is brown clear liquid. To the reaction solution to room temperature, add 15 ml water, ethyl acetate (10 ml ¡Á 3) extraction, the combined organic phase, dried with anhydrous sodium sulfate, filtered concentrated by reduced pressure distillation, column chromatography (PE: EtOAc=1:1), to obtain white solid 1.5 g, yield 75%.

13889-98-0, 13889-98-0 1-Acetylpiperazine 83795, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Fudan University; Fu Wei; Sun Nannan; (18 pag.)CN108503584; (2018); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.314741-39-4,(S)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

(d) [2S]-4-t-Butoxycarbonyl-2-hydroxymethylpiperazine A solution of Example 1(c) in dry tetrahydrofuran (40 ml) at 0 C. was treated with lithium aluminum hydride (0.50 g) and the mixture was stirred at 0 C. for 1.5 hours. The cooled solution was treated dropwise with a solution of 2M sodium hydroxide until a white precipitate had formed. Dichloromethane and anhydrous sodium sulfate were added and the solution was filtered and evaporated to give a pale yellow oil (3.0 g). MS (+ve ion electrospray) m/z 217 (MH+).

314741-39-4, As the paragraph descriping shows that 314741-39-4 is playing an increasingly important role.

Reference£º
Patent; SmithKline Beecham Corporation and SmithKline Beecham p.l.c.; US2003/203917; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step L: 2, 6-Dichloro-4-[ 4-chloro-6- ( 4-fluorophenyl) thienof 2, 3-dJpyrimidin-5-ylJ-3, 5- dimethyl-phenol and 4-f 4-bromo-6-(4-fluorophenyl)thieno[2,3-d]pyrimidin-5-yl]-2, 6- dichloro-3, 5 -dimethyl-phenol (0234) To a stirred solution of 700 mg compound of Step K above (1.50 mmol, 1.0 eq.) in 15 mL dichloromethane, 3.0 mL boron tribromide (1M in dichloromethane) (3.0 mmol, 2.0 eq.) was added at 0 ¡ãC and the mixture was allowed to warm up to room temperature and it was stirred until no further conversion was observed. The mixture was quenched with saturated aqueous NH4C1 and extracted with dichloromethane. The combined organic phases were dried over Na2S04 and concentrated under reduced pressure. The residue was purified via flash chromatography using heptane and ethyl acetate as eluents to obtain 2,6-dichloro-4- [4-chloro-6-(4-fluorophenyl)thieno[2,3-(i]pyrimidin-5-yl]-3,5-dimethyl-phenol and 4-[4- bromo-6-(4-fluorophenyl)thieno[2,3- ]pyrimidin-5-yl]-2,6-dichloro-3,5-dimethyl-phenol as a 37:63 mixture of products. (0235) 1H NMR (400 MHz, DMSO-d6): 10.14 (br s, 1H), 9.01 (s, 1H), 7.40-7.23 (m, 4H), 1.95 (s, 6H) and 10.14 (br s, 1H), 8.93 (s, 1H), 7.40-7.23 (m, 4H), 1.93 (s, 6H) (0236) HRMS (M+H)+ = 452.9800 and 496.9287 Step M: 4-Chloro-5-[3,5-dichloro-2,6-dimethyl-4-[2-(4-methylpiperazin-l- yl) ethoxy] phenyl] -6- ( 4-fluorophenyl) thienof 2, 3-dJpyrimidine and 4-bromo-5-[ 3, 5- dichloro-2, 6-dimethyl-4-[ 2- ( 4-methylpiperazin-l-yl) ethoxy] phenyl] -6- ( 4- fluorophenyl) thienof 2, 3-d]pyrimidine (0238) 300 mg mixture of 2,6-dichloro-4-[4-chloro-6-(4-fluorophenyl)thieno[2,3-5464-12-0, Big data shows that 5464-12-0 is playing an increasingly important role.

Reference£º
Patent; LES LABORATOIRES SERVIER; VERNALIS (R&D) LIMITED; PACZAL, Attila; SZLAVIK, Zoltan; KOTSCHY, Andras; CHANRION, Maia; MARAGNO, Ana Leticia; GENESTE, Olivier; DEMARLES, Didier; BALINT, Balazs; SIPOS, Szabolcs; (81 pag.)WO2017/125224; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics