Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5521-39-1,2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol,as a common compound, the synthetic route is as follows.,5521-39-1

30 mg of the 7-chloro-3-(2,4-dichloropyridin-3-yl)-4-imino-l-methyl-3,4- dihydropyrimido[4,5-rf]pyrimidin-2(lH)-one obtained in Production Example 2, and 16 mg of TsOH monohydrate were added to a 5-ml n-butanol solution containing 18.6 mg of 2-[4-(4- aminophenyl)piperazin-l-yl]ethanol, and the mixture was heat stirred for 15 minutes at 100C. The reaction mixture was concentrated under reduced pressure, and purified by basic column chromatography. As a result, 21 mg of a white solid was obtained as a subject compound. iH-NMR (400 MHz, CD3OD) delta: 8.97 (IH, s), 7.60-7.46 (5H, m), 7.00 (2H, d, J = 8.8 Hz), 3.76(2H, br s), 3.61 (3H, s), 3.24 (4H, br), 2.76 (4H, br s), 2.64 (2H, br). ESI-MS Found: m/z[M+H] 542

5521-39-1 2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol 767100, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BANYU PHARMACEUTICAL CO.,LTD.; BAMBA, Makoto; FURUYAMA, Hidetomo; SAKAMOTO, Toshihiro; SUNAMI, Satoshi; TAKAHASHI, Keiji; YAMAMOTO, Fuyuki; YOSHIZUMI, Takashi; WO2010/67886; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

848482-93-9, (S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

848482-93-9, To a stirred suspension of (5)-4-(tert-butoxycarbonyl) piperazine-2-carboxylic acid (1.0 g, 4.34 mmol) in water (5 rnL) was added solid NaHC03 (0.73 g, 8.68 mmol) at room temperature. The reaction mixture was stirred at room temperature to get clear solution. Solution of CBZ-CI (1.22 mL, 8.68 mmol) in 1,4-dioxane (10 mL) was added dropwise and the reaction mixture was stirred at room temperature for 16 h. The reaction mixture was diluted with water (20 mL) and extracted with EtOAc (2×20 mL). The aqueous layer was acidified with 0.5M aqueous HC1 to pH 5 and extracted with EtOAc (2×50 mL). The combined organic layers were dried over anhydrous a2S04, filtered, and concentrated under reduced pressure to afford the title compound (1.30 g) as white solid.

848482-93-9 (S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid 1501850, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; BLIZZARD, Timothy Allen; BIFTU, Tesfaye; WO2013/148478; (2013); 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.120737-59-9,tert-Butyl 3-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

(a) te?^-Butyl 4-(3-cyano-5-(ethoxycarbonyl>6-methylpyridin-2-yl)-3-methylpiperazine- 1-carboxylate; Ethyl 6-chloro-5-cyanonicotinate (0.500 g, 2.4 mmol), tert-butyl 3-methylpiperazine-1- carboxylate (0.480 g, 2.40 mmol), and DIPEA (0.41 mL, 2.40 mmol) were dissolved in DMF (4 mL) and heated at 100 ¡ãC for 8 h. The reaction mixture was cooled to room temperature and the solvent concentrated under reduced pressure. The material was partitioned between EtOAc (50 mL) and saturated aqueous NaHCO3 (2 x 30 mL). The organics were washed with EPO brine (30 mL), dried (Mg5O4) and concentrated under reduced pressure to afford the crude product. No purification was done., 120737-59-9

The synthetic route of 120737-59-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; WO2006/73361; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

154590-35-9, To a solution of 4-(4-Amino-2-fluoro-phenyl)-piperazine-1 -carboxylic acid te/t-butyl ester (1.00 g, 3.4 mmol) and 2-pyhd-3-yl benzoic acid (0.70 g, 3.7 mmol) in DMF (10 ml_) was added HATU (1.42 g, 3.7 mmol) and diisopropylamine (0.65 ml_, 3.7 mmol). After stirring at room tempertaure for 18 h, the reaction mixture was diluted with EtOAc (100 ml_) and washed with H2O (4×50 ml_). The organic extracts were combined, dried (Na2SO4), and the solvent was evaporated under reduced pressure. Chromatography of the resulting residue (SiO2: EtOAc:Hex) yielded 4-[2-fluoro-4-(2-pyridin-3-yl- benzoylamino)-phenyl]-piperazine-1 -carboxylic acid te/t-butyl ester which was further dissolved in MeOH (20 ml_) and 4N HCI in dioxanes. After stirring for 5 h, the reaction mixture was concentrated down, neutralized with 1 N NaOH, and extracted with EtOAc (3x75ml_). The organic extracts were combined, dried (Na2SO4), and the solvent was evaporated under reduced pressure to yield the title compound.MS: mass calcd. for C22H21FN4O, 376.17; m/z found, 378.4 [M+H]+

154590-35-9 tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate 16203630, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; JANSSEN PHARMACEUTICA, N.V.; WO2009/6185; (2009); 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

tert-butyl 4-(4-aminophenyl)piperazine-1-carboxylate (1.12 g, 4.03 mmol) was added to a stirred solution of ethyl 2-chloro-8-methyl-5-oxo-5,8-dihydropyrido [2, 3-d]pyrimidine-6-carboxylate (1.08 g, 4.03 mmol) in DMF (10.0 mL) in a 50mL RB flask. The reaction mixture was heated at 100 C. After 1 h, the reaction mixture was allowed to cool to RT and a precipitate formed that was collected by filtration and washed with methanol to give the title compound (1.75 g, 85%) as a bright yellow solid. LCMS (Method A) : RT =1.25 mi m/z = 509 [M+H].

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

Reference£º
Patent; ALMAC DISCOVERY LIMITED; ROUNTREE, James Samuel Shane; O’DOWD, Colin Roderick; BURKAMP, Frank; BELL, Mark Peter; WO2015/19037; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step D: tert-butyl (38)-4-[2-(3 -cyano-4-fluoro-2-methoxyphenyl)-2-hydroxyethyl]-3-(hydroxymethyl)piperazine-1-carboxylate; 6-Fluoro-2-methoxy-3-( oxiran-2-yl)benzonitrile (1.4g, 7.3 mmol) and (S)-4-N-BOC-2-hydroxymethylpiperazine (3.13 g, 14.5 mmol) were suspendedin ethanol (15 mL) then heated in a microwave apparatus for 60 min at 150 C. The reactionmixture was cooled and evaporated to dryness. The residue was purified by chromatographythrough a 40g Redi-sep column and eluting with 5%MeOH/95% EtOAc to yield the titlecompound: LC-MS: M+1 =410, 314741-40-7

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

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; WO2013/28474; (2013); 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

4-propionylbenzoic acid (890 mg, 5 mmol), NaHCO3 (1.26 g, 15 mmol), and iodomethane (935 uL, 15 mmol) in DMF (10 ml_) were stirred at RT overnight. The mixture was diluted with saturated aqueous NaCI (50 ml_) and extracted with ether (3 x50 ml_). The organic phase was washed with water (50 ml_), dried, and evaporated.Flash chromatography (90 g silica, 2/1 petroleum ether – EtOAc) gave white solids of 4-Propionyl-benzoic acid methyl ester (744 mg, 77%).1 H NMR (CDCI3, 400MHz) delta 1.24 (t, 3H, J = 7 Hz), 3.03 (q, 2H, J = 7 Hz), 3.95 (s, 3H),8.0 and 8.12 (ABq, 4H)4-Propionyl-benzoic acid methyl ester (744 mg, 3.87 mmol), pyrrolidone hydrotribromide (1.98 g), and 2-pyrrolidinone (380 mg, 4.5 mmol) in THF (38 ml_) were heated at 50 0C under nitrogen for 3 h. The mixture was cooled, filtered, concentrated, and then redissolved in ether (50 ml_). The ether solution was washed successively with water (20 ml_), saturated aqueous sodium thiosulphate (20 ml_), saturated aqueous NaCI (20 ml_), and water (2OmL), dried and evaporated to give crude 4-(2-Bromo- EPO propionyl)-benzoic acid methyl ester as a yellow oil (1.025 g) that was used directly in the Hantzsch coupling. This material contained 91% of the desired bromoketone, 5% starting material, and 4% 4-bromo-1-butanol, as determined by 1 H NMR.1 H NMR (CDCI3, 400MHz) delta 1.92 (d, 3H, J = 7 Hz), 3.96 (s, 3H), 5.28 (q, 1 H, J = 7 Hz), 8.07 and 8.14 (ABq, 4H)All of the 4-(2-Bromo-propionyl)-benzoic acid methyl ester above and piperazine-1- carboxylic acid terf-butyl ester (J. Med. Chem., 1998, 5037-5054, 917 mg, 3.73 mmol) were refluxed in 36 ml_ THF at 70 0C for 2 h, under N2. The precipitate was filtered and the filtrate evaporated to give yellow solids. Flash column chromatography (silica, 5/1 petroleum ether – EtOAc) gave 624 mg of 4-[4-(4-Methoxycarbonyl-phenyl)-5-methyl- thiazol-2-yl]-piperazine-1 -ca rboxylic acid tert-butyl ester as a light yellow solid. Chromatography of the precipitate (silica, 2/1 petroleum ether – EtOAc) gave 32 mg more of compound. Total yield is 44%.1 H NMR (CDCI3, 400MHz) delta 1.46 (s, 9H), 2.43 (s, 3H), 3.42, (m, 4H), 3.54 (m, 4H), 3.90 (s, 3H), 7.68 and 8.04 (ABq, 4H).The above methyl ester (564 mg, 1.35 mmol) was heated with 1.35 ml_ 2N NaOH, 5 ml_ THF, and 3.65 ml_ water at 60 0C for 4 h. The reaction mixture was evaporated, poured into 20 ml_ saturated aqueous NaCI and 20 ml_ CH2CI2, and then acidified to pH 3 with 5% citric acid, in an ice bath. The layers were separated and the organic phase was extracted further with 2 x 10 ml_ CH2CI2. The organic phases were combined, washed with water (10 ml_), dried, and evaporated to give 4-[4-(4-Carboxy-phenyl)-5-methyl- thiazol-2-yl]-piperazine-1-carboxylic acid tert-butyl ester as a light yellow solid (537 mg, 98%).1 H NMR (CDCI3, 400MHz) delta 1.48 (s, 9H), 2.47 (s, 3H), 3.47 (m, 4H), 3.57 (m, 4H), 7.74 and 8.12 (ABq, 4H).13C NMR (CDCI3, 100MHz) delta ppm: 12.6, 28.3, 42.8, 48.1 , 80.3, 119.1 , 127.8, 128.2, 130.1 , 140.5, 145.6, 154.6, 167.2, 171.4. LCMS: (M + H)+ 404, (M – H)” 402. EPO 4-[4-(4-Carboxy-phenyl)-5-methyl-thiazol-2-yl]-piperazine-1-carboxylic acid tert-butyl ester (0.421 mmol) was dissolved in 4M HCI in 1 ,4-dioxane, and stirred at room temperature for 1 h. The solvent was then removed under vacuum, and the residue 4-(5-Methyl-2-piperazin-1-yl-thiazol-4-yl)-benzoic acid was suspended in methanol (10 ml) and treated with AcOH/AcONa buffer (pH ~5.5, 5 ml), and formaldehyde (0.547 mmol). The reaction mixture was stirred at room temperature for 1 h, then treated with NaCNBH3 (0.547 mmol) and stirred at room temperature overnight. The solvent was then removed under vacuum, and the residue was purified by column chromatography to afford the title compound (0.403 mmol, 95%). MS(ES) m/z 318 (100%, [M+H]+).

196811-66-2, 196811-66-2 tert-Butyl 4-carbamothioylpiperazine-1-carboxylate 12093220, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MEDIVIR AB; WO2007/6714; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129779-30-2, (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

At 100mLAdd in three bottlescis-3,5-Dimethylpiperazine-1-carboxylic acid tert-butyl ester (2 g, 9.34 mmol),Pyridine (1.47 g, 18.6 mmol) and DCM (10 mL), cooled to 0 C,A solution of allyl chloroformate (1.68 g, 14 mmol) in DCM was added dropwise.The reaction was allowed to warm to room temperature overnight.The reaction system was added with water (20 mL) and allowed to stand for stratification.The organic phase was concentrated to give a crude product. The crude product was purified by column chromatography.Eluent: PE/EA=5/1, collect product,Concentrated under reduced pressure to give 1.2 g of colorless oil.Yield: 43.2%.

129779-30-2, As the paragraph descriping shows that 129779-30-2 is playing an increasingly important role.

Reference£º
Patent; Beijing Purunao Bio-technology Co., Ltd.; Zhang Peilong; Shi Hepeng; Lan Wenli; Song Zhitao; (250 pag.)CN108707139; (2018); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

548762-66-9, (2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

548762-66-9, The solid from the previous step was dissolved in a mixture of N,N-diisopropylethylamine (0.7 mL, 4 mmol) and DMSO (0.7 mL, 10 mmol) and (2S,5R)-2,5-dimethyl-piperazine-1-carboxylic acid tert-butyl ester (590 mg, 2.7 mmol) was added and the reaction mixture heated at 120 C overnight, concentrated by rotary evaporation, dissolved in a small amount of DCM and purified by silica gel chromatography (0-40% ethyl acetate:hexanes) to produce the title intermediate (613 mg, 57 % yield) as a white solid. (m/z): [M+H]+ calcd for C24H27F4N4O4 591.12 found 591.4.

The synthetic route of 548762-66-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Theravance Biopharma R&D IP, LLC; MCKINNELL, Robert Murray; LONG, Daniel D.; VAN ORDEN, Lori Jean; JIANG, Lan; LOO, Mandy; SAITO, Daisuke Roland; ZIPFEL, Sheila; STANGELAND, Eric L.; LEPACK, Kassandra; OGAWA, Gavin; HUANG, Xiaojun; ZHANG, Weijiang; EP2635571; (2015); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step B: tert -butyl(9aS)-3-hydroxy-3 -(1-oxo-3 ,4-dihydro-1 H-isochromen-6-yl)hexahydropyrazino[2, 1-c] [ 1 ,4 ]oxazine-8(1H)-carboxylate:6-(Bromoacetyl)-3 ,4-dihydro-1 Hisochromen-1-one ( -1.54 g, -5.72 mmol, presence of a-chloroketone was noted, -10%) andcommercially available (S)-4-N-BOC-2-hydroxymethylpiperazine (1.24 g, 5.72 mmol) were added to a round bottom flask and diluted with THF (50 mL). Diisopropylethylamine (1.30 mL,7.44 mmol) was then introduced and the mixture left stirring for 14 hat RT during which time aconsiderable amount of solid had formed (presumably HBr salt ofDIPEA). The reaction mixturewas diluted with EtOAc, then washed with saturated NH4Claq followed by H20. Both aqueouslayers were sequentially back extracted once with another portion ofEtOAc, the organics were then combined, dried with MgS04, filtered, and concentrated in vacuo. The recovered crudeproduct was subjected to purification by flash chromatography (Biotage, 50% EtOAc/Hex) toafford the title compound.

314741-40-7, As the paragraph descriping shows that 314741-40-7 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; WO2013/28474; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics