Month: May 2021

3022-15-9, Piperazine-2-carboxylic acid dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of di-tert-butyldicarbonate (63 g, 290 mmol) in MeOH (100 mL) was added portionwise to a solution of piperazine-2-carboxyilic acid dihydrochloride (25.0 g, 123 mmol) and triethylamine (48 mL, 340 mmol) in MeOH (150 mL) over 30 minutes. Upon complete addition, the reaction mixture was heated to 50 0C for 2 h. Upon cooling to rt, the reaction mixture was concentrated under reduced pressure. The material was dissolved in water (300 mL) and the solution was brought to pH 2 with 1 M aqueous HCl. This was extracted with EtOAc (4 x 200 mL), and the combined extracts were dried over Na2SO4, filtered, and concentrated under reduced pressure until -100 mL EtOAc remained. The solution was diluted with hexanes (150 mL) and cooled to 0 0C. The resulting solid was collected by filtration, washed with hexanes (2 x) and air- dried. This gave 38.9 g (96%) of the title compound as a white solid. Analytical data: 1H NMR (400 MHz, DMSO-J6) delta 13.02-12.80 (br, IH), 4.50-4.24 (m, 2H)5 3.94-3.72 (br, IH), 3.66 (d, J= 12.8 Hz, IH), 3.22-2.92 (m, 2H), 2.90-2.68 (brs IH), 1.42-1.34, (m, 18H).

3022-15-9, As the paragraph descriping shows that 3022-15-9 is playing an increasingly important role.

Reference£º
Patent; CRITICAL THERAPEUTICS, INC.; WO2007/146066; (2007); 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.162046-66-4,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

116a) tert-butyl 4-{4-[(dimethylamino)carbonyl]phenyl}piperazine-1-carboxylate; After 1,1′-carbonyldiimidazole (0.58 g, 3.6 mmol) was added to tetrahydrofuran (10 mL) solution of 4-[4-(tert-butoxycarbonyl)piperazin-1-yl]benzoic acid (1.00 g, 3.3 mmol) and the mixture was stirred at room temperature for 30 minutes, 50% dimethylamine aqueous solution (0.45 mL) was added. The reaction liquid was stirred at room temperature for four hours and a saturated saline solution (100 mL) and ethyl acetate (100 mL) were added and partitioned. The organic layer was washed with a saturated sodium carbonate aqueous solution (30 mL) and the solvent was evaporated under reduced pressure after drying over sodium sulfate. The residue was purified by silica gel column chromatography (100% ethyl acetate) and 1.00 g of the title compound was obtained (yield 92%). Mp 126-128C; IR (KBr) numax 1689, 1628, 1241, 1165, 835, 769 cm-1; 1H NMR (CDCl3, 400MHz) delta 1.49 (9H, s), 3.06 (6H, brs), 3.20 (4H, t, J = 5.1 Hz), 3.58 (4H, t, J = 5.1 Hz), 6.89 (2H, d, J = 8.6 Hz), 7.38 (2H, d, J = 8.6); MS (FAB) m/z: 333 [M+]; Anal. Calcd for C18H27N3O3: C, 64.84; H, 8.16; N, 12.60. Found: C, 64.82; H, 8.41; N, 12.59., 162046-66-4

162046-66-4 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid 2795508, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Sankyo Company, Limited; EP1764367; (2007); 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.76003-29-7,1-Boc-3-Oxopiperazine,as a common compound, the synthetic route is as follows.,76003-29-7

This compound was prepared as set out in step 1 of the scheme for example 4. NMR (300 MHz, CDC13) delta 9.09 (d, J= 2.1 Hz, 1H), 7.73 (d, J = 2.1 Hz, 1H), 7.53- 7.43 (m, 2H), 7.42-7.31 (m, 3H), 5.33 (s, 2H), 4.30 (s, 2H), 3.93-3.72(m, 7H), 1.51 (s, 9H)MS (ESI+) m/z 587 (M[Br79]+l), 589 (M[Br81]+l)

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

Reference£º
Patent; AVEXA LIMITED; SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY (SIOC); RHODES, David, Ian; DEADMAN, John, Joseph; LE, Giang, Thanh; VAN DE GRAFF, Nicholas, Andrew; LONG, Lu; XINMING, Li; XIAO, Feng; CHANGJIANG, Yu; WO2012/6680; (2012); 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.187669-60-9,1-(4-(Methylsulfonyl)phenyl)piperazine,as a common compound, the synthetic route is as follows.

Example 80; 4-{2-[4-(4-Mcthancsulfonylphcnyl)pipcrazin-l-yl]-2-oxocthyl}pipcridinc-l- carboxylic acid ferf-butyl ester; To a solution of l-(4-methanesulfonylphenyl)piperazine (0.22 g, 0.91 mmol), 4-carboxy methylpiperidine-1-carboxylic acid tert-butyl ester (0.20 g, 0.80 mmol), HOBT.H2O (0.14 g, 0.91 mmol) and DIPEA (0.47 mL, 2.72 mmol) in DMF (5mL) was added EDCI (0.19 g, 0.99 mmol) and the mixture was stirred for 18h. The solvent was removed under vacuum and the resulting residue was partitioned between EtOAc and saturated NaHCO3 solution. The aqueous phase was re-extracted with EtOAc, the organic extracts were combined, washed with brine, dried (MgSO4) and adsorbed onto SiO2. The adsorbed sample was purified by flash chromatography eluting with 50:50 EtOAc:hexane to afford the title compound: RT = 3.26 min; m/z (ES+) = 466.33 [M+H]+., 187669-60-9

The synthetic route of 187669-60-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PROSIDION LIMITED; WO2007/3964; (2007); 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.59702-31-7,1-Ethylpiperazine-2,3-dione,as a common compound, the synthetic route is as follows.

To Boc-Asp-OBzl 5 g (15.5 mmol) in dichloromethane (50 mL) was added triethylamine 6.43 mL (46.4 mmol), followed by HATU 7 g (18.6 mmol) and the mixture was stirred at RT for 30 min.1-Ethylpiperazine-2,3-dione 2.6 g (18.6 mmol) was added to the reaction in one portion, stirred at RT for 1 h and diluted with dichloromethane. The solution was washed with water/brine, dried over sodium sulfate, concentrated and purified using silica gel chromatography (70-80% ethyl acetate/hexanes) to give the desired compound, 5.64 g. ESI-MS m/z 448 (MH)+.

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

Reference£º
Patent; VENATORX PHARMACEUTICALS, INC.; BURNS, Christopher J.; DAIGLE, Denis; CHU, Guo-Hua; HAMRICK, Jodie; BOYD, Steven A.; ZULLI, Allison L.; MESAROS, Eugen F.; CONDON, Stephen M.; TROUT, Robert E. Lee; MYERS, Cullen L.; XU, Zhenrong; (327 pag.)WO2019/226931; (2019); 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

6-Fluoro-2-methyl-3-(oxiran-2-yl)benzonitrile (prepared as described above for I-17A and I-17B, Method1, Steps A-C) (4.80 g, 27.1 mmol) and (R)-4-N-BOC-2-hydroxymethyl-piperazine (commercially available, e.g. fromAcesys Pharmatech, catalog A1612R; and also described in J. Org. Chem, 2007, 72(22), p. 8591-8592) (8.79g.40.6 mmol) were suspended in EtOH (30mL) and heated in a microwave apparatus at 150 C for 1 h. The reactionmixture was cooled and evaporated to dryness. The residue was purified by chromatography through a 330 g ISCORedi-sep column eluting with ethyl acetate to 5% MeOH/ ethyl acetate gradient to yield the title compound. LC-MS:M+1 = 394;

278788-66-2, 278788-66-2 (R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820286, 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; (128 pag.)EP2744499; (2016); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

118753-66-5, tert-Butyl 4-aminopiperazine-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-hutyl 4-aminopiperazine-l-carboxylate (0.200 g, 0.99 mmol, 1.0 equiv) in DMF (05 mL) was added HATU (0.753 g, 1.98 mmol, 2.0 equiv) at RT and stirred for 10 minutes. Then 6-chloroquinoline-2-carboxylic acid (0.206 g, 0.99 mmol, 1.0 equiv) was added followed by the addition of DIPEA (0.6 mL, 2.97 mmol, 3.0 equiv). The resulting reaction mixture was allowed to stir at RT for overnight. Product formation was confirmed by LCMS The reaction mixture was diluted with water (50 mL) and extracted with EtOAc (50 mL * 2). The combined organic layer was washed with water (30mL x 3), brine solution (30 ml, c 2), dried over anhydrous sodium sulfate and concentrated under reduced pressure, to obtain tert-butyl 4-(6-chloroquinoline-2-carboxamido)piperazine-l-carboxylate (0.140 g, 36 % Yield) as a brown solid. LCMS 390 ] M 1 1 | : NMR (400MHz, DMSO-de) d 9.95 (br. s., 1 H), 8.53 (d, ./ 8.3 Hz, 1 H), 8.24 (br. s., 1 H), 8.15 (d, J= 5.3 Hz, 2 H), 7.88 (d, J = 7.5 Hz, 1 H), 3 45 (br. s., 4 H), 2.90 (d, J= 1 1.0 Hz, 4 H), 1.42 (s, 9 H).

118753-66-5, The synthetic route of 118753-66-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PRAXIS BIOTECH LLC; DELGADO OYARZO, Luz Marina; URETA DIAZ, Gonzalo Andres; PUJALA, Brahmam; PANPATIL, Dayanand; BERNALES, Sebastian; CHAKRAVARTY, Sarvajit; (0 pag.)WO2019/236710; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

55276-43-2, 1-Methanesulfonylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

55276-43-2, (S)-Epichlorohydrin (48.0 mL, 0.612 mol) was added to a stirred solution of piperazine N-methylsulfonamide (87.3 g, 0.532 mol) in ethanol (1.33 L) at room temperature. The reaction mixture was stirred for 18 h and the white solid precipitate which formed was collected by filtration and washed with ethanol to afford (S)-1-chloro-3-(4-methylsulfonyl-1-piperazinyl)-2-propanol (107.76 g) as a white solid which was used without further purification. (m/z): [M+H]+ calcd for C8H17ClN2O3S, 257.07; found, 257.2. 1H-NMR (DMSO): delta (ppm) 2.37 (dd, 1H), 2.45 (dd, 1H), 2.50-2.58 (m, 4H), 2.86 (s, 3H), 3.09 (m, 4H), 3.55 (dd, 1H), 3.65 (dd, 1H), 3.84 (m, 1H), 5.09 (d, 1H).

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

Reference£º
Patent; THERAVANCE, INC.; US2006/100426; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

611225-86-6, 4-(4-Ethylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

611225-86-6, 104 mg (0.35 mMol) triphosgene are ^j-n’ ^ dissolved in13 ml ice-cooled CH2CI2. ^-/ ~~” Then a solution of 230 mg (1.05mMol) 4-(4-ethylpiperazin-1-O Hylmethyl)~aniline and 209 i (1.50 mMol) Et3N in 6 ml CH2CI2 is added during 8 min. After 3 additional minutes, the mixture is warmed up to rt by a water bath and then a solution of 1.0 mMol 5-(6-chloro-pyrimidin-4-yioxy)-2,3-dihydro-1H-indole (Step 14.1) and 139 jll. (1.00 mMol) Et3N in 6 ml CH2CI2 is added during 8 min. After 2 h at rt, the mixture is diluted with sat. Na2C03 solution / water 1:1 and EtOAc, the aqueous phase separated off and extracted twice with EtOAc. The organic layers are washed with water and brine, dried (Na2S04) and concentrated. Crystallization from DIPE gives the title compound: MS: [M+1]+= 493 / 495; TLC(CH2CI2/MeOH/NH3conc- 90:10:1): Rf = 0.24; HPLC: et_ = 10.5.

The synthetic route of 611225-86-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2006/34833; (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.112257-12-2,tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

4-(2-bromoacetyl)piperazine-1-carboxylate (9.77 mmol, 1 eq.) in methanol (26 ml) at 0C. The reaction vial was sealed and the mixture stirred vigorously overnight at room temperature. The solvent was subsequently evaporated, the residue dissolved in hydrogen chloride (aqueous soln., 0.1 N, 100 ml) and extracted with ethyl acetate (3 x 100 ml). The pH of the recovered aqueous layer was adjusted to 10 by addition of sodium hydroxide (aqueous soln., 1 N), then the organics extracted with ethyl acetate (3 x 100 ml). The combined organic layers were dried over magnesium sulfate, filtered and the solvent evaporated under vacuum to give a light yellow crude product. Further trituration in diethyl ether conducted to the desired amine as a white solid used for the next step without additional purification. C11 H21N3O3; yield 58%; white solid; m.p. 159-160 C; M = 243.30 g/mol; IR (ATR): v = 2974 (w), 1675 (s), 1627 (s), 1417 (m), 1360 (m), 1235 (m), 1172 (m), 1123 (m), 990 (m), 759 (m) cm – ; H NMR (250 MHz, CDCI 3) delta 3.71-3.41 (m, 10H), 1.46 (s, 9H); C NMR (63 MHz, CDCI 3) delta 169.5 (C q), 154.6 (C q), 80.5 (C q), 50.4 (CH 2), 44.6 (2CH 2), 41.7 (2CH 2); HRMS: calcd. for CHH21 3O3 244.1661 , found. 244.1657;, 112257-12-2

The synthetic route of 112257-12-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTON UNIVERSITY; GRIFFIN, Martin; RATHBONE, Daniel; BADARAU, Leonas Eduard; WO2014/57266; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics