Month: September 2021

103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Benzyl chloroformate (3.40 ml, 24.00 mmol) was slowly added to an ice-cold stirred solution of 1-(2-hydroxyethyl)piperazine (2.60 g, 20.00 mmol) and DIEA (7.0 ml, 40.0 mmol) in dichloromethane (75 ml). The mixture was allowed to warm to room temperature and stirred for 24 h then concentrated in vacuo. The residue was purified by (eluant 6% methanol/chloroform) to give a colourless gum identified as benzyl 4-(2-hydroxyethyl)piperazine-1-carboxylate (4.80 g, 91%).

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

Reference：
Patent; Ferring B.V.; EP1449844; (2004); A1;,
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, A mixture of ethyl 3-{[(benzyloxy)carbonyl]amino}-7-bromoquinoline-2-carboxylate (250 mg, 0.58 mmol), 1-methylpiperazin-2-one (130 mg, 1.2 mmol), Pd(OAc)2 (20 mg), dicyclohexyl(2′,6′-diisopropoxybiphenyl-2-yl)phosphine (41 mg, 0.087 mmol), and K3PO4 (490 mg, 2.3 mmol) in tert-butyl alcohol (8 mL) was purged with nitrogen then heated at 100° C. in a sealed vial for 3 h. The mixture was then allowed to cool and EtOAc and water were added. The resulting layers were separated and organic layer was concentrated under reduced pressure. To the resulting bright-yellow solid, 2 mL of dioxane, 2 mL of 2 M NaOH were added. The mixture was heated in 80° C. oil bath with stirring for 0.5 h, then allowed to cooled and neutralized with 4 mL of with 1 M Cl. The red solid formed was collected by filtration and air-dried overnight to give the sub-title compound (24 mg, 9.5percent). LCMS calc. for C26H33N8O2 [M+H]+: m/z=489.3. found: 435.2

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

Reference：
Patent; INCYTE CORPORATION; Li, Yun-Long; Burns, David M.; Feng, Hao; Xue, Chu-Biao; Wang, Anlai; Pan, Jun; US2014/200216; (2014); 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

Example 3-4-3 Preparation of 2-[3-fluoro-4-(BOC-piperazino)]phenylamino-6-chloro-3-nitropyridine To 100ml of methanol were added 2.75g (14.2mmol) of 2,6-dichloronitropyridine and 2.38ml (17.0mmol) of triethylamine and 4.2g (14.2mmol) of [3-fluoro-4-(BOC-piperazino)]aniline obtained in Preparation Example 3-4-2 was then added thereto, followed by reaction at room temperature (20 to 30C) for about 24 hours. After the reaction was complete, the reactant was filtered, washed with 20ml of methanol and then dried under vacuum at about 40C to afford 4.47g (yield: 70%) of the desired compound. Mass (M+): 452.0 1H-NMR (DMSO-d6): 1.42(s, 9H), 2.96(t, 4H), 3.48(m, 4H), 7.01(d, 1H), 7.07(t, 1H), 7.34(d, 1H), 7.53(d, 1H), 8.53(d, 1H), 10.08(s, 1H)., 154590-35-9

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：
Patent; Dong Wha Pharm. Co., Ltd.; EP2394993; (2011); 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.4318-42-7,1-Isopropylpiperazine,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.

4318-42-7, The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference：
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
Piperazines – an overview | ScienceDirect Topics

169448-87-7, (R)-tert-Butyl 2-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 6-bromo-4-(bromomethyl)-2-(phenylsulfonyl)isoquinolin-1 (2H)-one (Examplei 1d, 1.75 g) in THF (20 mL) was treated with (f?)-tert-butyl ethyl(1-hydroxy-3- (methylamino)propan-2-yl)carbamate (0.98 g) and /V,Lambda/-diisopropylethylamine (0.80 mL) under nitrogen. The resulting solution was stirred at 50 C for 1 h. The reaction mixture20 was diluted with water (300 mL), and extracted with ethyl acetate (250 mL x 2). The combined organics were dried (MgSO4), filtered and evaporated. Triturated with diethyl ether / isohexane (1 :1) afforded the subtitle compound (2.30 g) as a solid. 1H NMR delta (CDCI3) 8.16 – 8.10 (m, 3H), 8.06 (s, 1H), 7.90 (s, 1H), 7.71 – 7.65 (m, 1H), 7.60 – 7.54 (m, 3H), 4.23 – 4.16 (m, 1 H), 3.84 (d, 2H), 3.59 – 3.45 (m, 2H), 3.21 – 3.02 (m, 2H),2S 2.89 – 2.79 (m, 1 H), 2.33 – 2.09 (m, 3H), 1.51 (s, 9H)

169448-87-7, 169448-87-7 (R)-tert-Butyl 2-(hydroxymethyl)piperazine-1-carboxylate 24820219, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ASTRAZENECA AB; BROUGH, Stephen, John; LUKER, Timothy, Jon; ROBERTS, Bryan, Glyn; ST-GALLAY, Stephen, Anthony; WO2010/39079; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

113028-17-4, Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,113028-17-4

Example 10: Preparation of prulifloxacin hydrochloride; Method A: To the mixture of dimethylformamide (1.5 It) and 6-fluoro-l-methyl-4-oxo-7-(l- piperazinyl)-lH,4H-[l,3]thiazeto[3,2-a]quinoline-3-carboxylic acid (0.3kg), 4-bromomethyl-5- methyl- 1, 3 -dioxolen-2-one, obtained above was added and cooled to 0-50C. Triethylamine (0.87kg) in dimethylformamide (0.3 It) was added slowly in 1-2 hours. After completion of the reaction (monitored by TLC), dichloromethane (3.0 It) and water (1.5 It) were added to the reaction mixture. The layers were separated and aqueous layer was extracted twice with dichloromethane (1.5 It). All organic layers were combined, dried over sodium sulfate followed by distillation. Methanolic hydrochloride (20-25 % w/w, 0.24 It) was added to organic layer at 0- 5C and stirred. The solid, thus precipitated out was filtered, washed with dichloromethane and dried to obtain 0.36kg of the title compound having purity 92.73 % by HPLC. Example 11: Purification of prulifloxacin hydrochlorideDimethylformamide (1.34 It) was added to prulifloxacin hydrochloride (67g) and reaction mass was heated to 110-112C for 1 hour. The reaction mixture was cooled to 25-300C and stirred for 2 hours, filtered, washed with N,iV-dimethylforamide. The product was slurry washed with isopropanol (0.670 It) and dried to obtain 48.8g of title compound having purity 99.30 % by HPLC.

113028-17-4 Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate 10249018, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; IND-SWIFT LABORATORIES LIMITED; WO2009/93268; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

208167-83-3, tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0384] To a solution of l-Boc-4-(2-chloroethyl)piperazine (6.85 g, 27.62 mmol) in methanol (50 ml) was added thiourea (4.12 g, 55.24 mmol). The mixture was heated to reflux for 2 hours. A solution of sodium hydroxide (1.66 g, 41.43 mmol) in water (10 ml) was added, and the mixture was continued to reflux for another hour. Then most solvent was evaporated under reduced pressure. The residue was mixed with ethyl acetate (50 ml) and brine (30 ml) and separated. The ethyl acetate was dried over magnesium sulfate and evaporated under reduced pressure. The residue was dissolved in methanol (20 ml). 4 M hydrochloric acid in dioxane (10 ml) was added. The mixture was stirred at room temperature overnight and most of solvent was evaporated under reduced pressure. The residue was used for the addition reaction without further purification.

208167-83-3, The synthetic route of 208167-83-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SU, Zhuang; LONG, Zhengyu; YANG, Suizhou; WO2014/145686; (2014); A2;,
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

Example 16. Preparation of Compound Nos. 136. 136a and 136b To a solution of l-[4-[(3-cyclopentyl-lH-pyrazol-5-yl)amino]-6,7-dihydro-5H- cyclopenta[d]pyrimidin-2-yl]pyrrolidine-2-carboxylic acid hydrochloride (500 mg, 1.19 mmol) in DMF (6 mL) was added l-methylpiperazin-2-one (205 mg, 1.79 mmol), HOBt (16 mg, 0.11 mmol), EDC’HCl (320 mg , 1.67 mmol), and DIPEA (618 mg, 4.79 mmol), and the reaction mixture was stirred at RT for 18 h. The reaction mixture was diluted with water (50 mL) and extracted with EtOAc (2×50 mL). The combined organic layers were washed with water (8×50 mL) and dried over anhydrous sodium sulfate. Removal of solvent under reduced pressure gave a crude product that was purified by reverse phase HPLC followed by chiral HPLC to afford 20 mg of 4-[(2R)-l-[4-[(3-cyclopentyl-lH-pyrazol-5-yl)amino]-6,7- dihydro-5H-cyclopenta[d]pyrirmdin-2-yl]pyrrolidine-2-carbonyl]-l-methyl-piperazin-2-one (Compound No. 136a). 1H NMR (CD3OD, 400 MHz) 1.60-1.90 (m, 8H), 1.92-2.20 (m, 8H), 2.30-2.42 (m, 1H), 2.60-2.80 (m, 6H), 2.97-3.12 (m, 1H), 3.22-3.56 (m, 3.61-4.30 (m, 4H), 5.02 (brs, 1H), 5.75 (bra, 1H).

59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; MEDIVATION TECHNOLOGIES, INC.; CHAKRAVARTY, Sarvajit; RAI, Roopa; GREEN, Michael, John; ANSARI, Amantullah; AGARWAL, Anil, Kumar; (216 pag.)WO2016/3827; (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 A1, 1-dimethylethyl 4-(2-fIuoro-4-methylphenyl)-3-oxo-1-piporazinecarboxylate A mixture of 1 ,1-dimethylethyl 3-oxo-1 -piperazinecarboxylate (0.326 g, 0.00163 mol), 1-bromo-2-fluoro-4-methylbenzene (0.308 g, 0.0163 mol), (1 R,2R)-N,N’-dimethyl~ 1 ,2-cyclohexanediamine (0.026 mL, 0.163 mmol), copper(l) iodide (3.10 mg, 0.016 mmol) and potassium carbonate (450 mg, 3.26 mmol) in 1 ,4-dioxane (6 mL) in a septum-sealed vial was heated in an oil bath at 120 C overnight. The reaction mixture was cooled to room temperature and filtered through Celite washing with ethyl acetate. The filtrate was washed with saturated aqueous ammonium chloride, water and brine, dried over sodium sulfate and concentrated. The residue was purified by chromatography on silica gel to give the title compound (0. 253 g, 50%). MS (ESI) m/z: 309 (M+1 )., 76003-29-7

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference：
Patent; GLAXOSMITHKLINE LLC; BANKA, Anna; CATALANO, John, G.; CHONG, Pek, Yoke; FANG, Jing; GARRIDO, Dulce, Maria; MAYNARD, Andy; MILLER, John; PATTERSON, Dan; PEAT, Andrew, James; POWERS, Jeremiah; PRICE, Daniel, J.; ROBERTS, Chris; TAI, Vincent; YOUNGMAN, Michael; WO2011/50284; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics