Tag: M.W:200-300

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

278788-66-2, Step E: tert-butyl (3R)-4-[ 5-cyano-2-fluoro-4-methoxyphenyl)-2-oxoethyl]-3 -(hydroxymethyl)piperazine-1-carboxylate: To a 250 mL flask was added 5-(bromoacetyl)-4-fluoro-2-methoxybenzonitrile (2.00 g, 7.35 mmol), (R)-N-Boc-2-hydroxymethyl-piperazine (3.18 g, 14.7mmol), DIEA (2.57 mL, 14.7 mmol) and THF (50 mL) and stirred at rt for 1 h; LC analysis of the reaction mixture indicated completion of the reaction. The solution was treated with EtOAc(100 mL), washed with brine, dried (Na2S04), filtered and concentrated to dryness. The residuewas then purified over silica gel with the solvent systems of 5% MeOH in DCM to furnish thedesired product. LC/MS: [(M+ l)t =408.

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; WO2013/28474; (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.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

5747-48-8, A 1 liter round bottom flask equipped with stirring rod, thermo pocket, water condenser was charged with solution of l l-piperazinyldibenzo[b,fj [l,4]thiazepine in toluene 350 cc [63.0 g (0.22 moles)] and the mixture was stirred for 15 min 25- 30C, to which, was added sodium carbonate [41.0 gm (0.39 moles)], tetra butyl ammonium bromide [16.0 gm (0.05 mole)] and 2-(2-chloroethoxy) ethanol [32.0 gm ( 0.257 moles)] at room temperature. The reaction mixture was heated to reflux at 110- 112C. The reaction mixture was maintained at reflux for 10-12 hrs. The reaction mixture was analyzed by HPLC (to check for absence of compound IV) and was cooled to at 25C to 30C,and was added 150 cc DM water, the reaction mixture was stirred for 30 min at 25-30C. The layers were separated and the aqueous layer extracted with 50 cc toluene. The extract and the organic layer were combined, and the pH was adjusted to 2-3 using IN HCl solution in DM water, the reaction mixture was stirred for 30 min at 25-3O0C. The layers were separated and the aqueous layer washed with 100 cc toluene twice. To the aqueous layer was added 250 cc toluene, and the pH was adjusted to 8-10 using sodium carbonate, the reaction mixture was stirred for 30 min at 25-30C. The layers were separated and the aqueous layer extract with 125 cc toluene. The extract and the organic layer were combined, and washed with DM water 300 cc twice. The organic layer was distilled off under vacuum below 500C leaving 50-60 cc toluene with product. Purity of 2-(2-(4- dibenzo[b,f]-[l,4] thiazepine- l l-yl-l-piperazinyl)ethoxy) ethanol in toluene was 99.0% (area % by HPLC). To this solution 1000 cc absolute ethanol was added with activated carbon 5.0 gm and heated to reflux for 90 min. The resulting solution was cooled to 50-550C and filtered. The resulting solution was added 12.5 gm (0.5 moles) fumaric acid at 500C. The reaction mixture was heated to reflux for 2 hrs and was slowly cooled to room temperature and maintained for 2 hrs at room temperature. The reaction mass was filtered and washed with 200 cc absolute ethanol. The wet material obtained was dried under vacuum at 50-55C to afford quetiapine fumarate. Dry weight of quetiapine fumarate is 60-65 gm. Purity of quetiapine fumarate was 99.5% (area % by HPLC).

As the paragraph descriping shows that 5747-48-8 is playing an increasingly important role.

Reference£º
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2008/121415; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 0.31 mmol 2-isopropylsulfanyl-5-nitro-benzoic acid in 5 ml tetrahydrofuran were added successively 0.31 mmol TBTU, 0.84 mmol N-ethyldiisopropylamine and 0.22 mmol 1-(4-trifluoromethylphenyl)-piperazine (commercially available, e.g. from Fluorochem). The reaction mixture was stirred at 35 C. for 16 h and then concentrated in vacuo. Chromatography (SiO2, ethyl acetate/heptane) followed by trituration in pentane afforded the title compound as a yellow solid (yield 83%). MS (m/e): 454.4 (M+H+, 100%)., 30459-17-7

The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Jolidon, Synese; Narquizian, Robert; Norcross, Roger David; Pinard, Emmanuel; US2006/149062; (2006); A1;,
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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

Reference Example 32(R)-4-(2-ChIoro-acetyl)-3-hydroxymethyl-piperazine-l-carboxylic acid tert-butyl esterTo a solution of (i?)-3-hydroxymethyl-piperazine-l-carboxylic acid tert-butyl ester (795 mg, 3.68 mmol) in DCM (20 mL) was added triethylamine (1.53 mL, 11.04 mmol). The resulting mixture was cooled to 0 0C before the dropwise addition of chloroacetyl chloride (325 muL, 4.05 mmol). The mixture was warmed to RT and stirred for 5 h. The reaction mixture was partitioned between a saturated aqueous solution OfNaHCO3 and DCM and the aqueous layer extracted with further DCM. The combined organic fractions were dried (Na2SO4) and concentrated in vacuo. The resulting residue was purified by column chromatography to give the title compound as a colourless oil which was a mixture of rotamers (710 mg, 66%).1H NMR (400 MHz, CDCl3): delta 1.48 (s, 9H), 2.80-2.92 (m, IH), 2.95-3.10 (m, 2H), 3.34-3.44 (m, 1AH), 3.60-3.74 (m, 21Z2H), 3.96-4.16 (m, 31AH), 4.22-4.30 (m, ‘/2H)5 4.32-4.40 (m, Y2H) and 4.63 (bs, VzYi)., 278788-66-2

The synthetic route of 278788-66-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; F.HOFFMANN-LA ROCHE AG; WO2009/53716; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

132710-90-8, 1-Boc-4-(3-hydroxypropyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Triphenylphosphine (1.86 g, 7.08 mmol) was charged to a round bottom flask under nitrogen atmosphere and dissolved in dry tetrahydrofuran (40 mL). The solution was cooled to -40 C via an acetonitrile/dry ice bath. After 30 minutes of cooling, DIAD (1.14 g, 7.08 mmol, 1.11 mL) was added dropwise over the course of about 30 minutes. The solution became a slurry of white precipitate and was allowed to stir for 10 minutes at -40 C before 27B (500 mg, 1.42 mmol) and tert-butyl 4-(3- hydroxypropyl)piperazine-l-carboxylate (1.04 g, 4.25 mmol) were added. The reaction continued to stir for 1 hour before the the reaction was pulled from the cooling bath and allowed to warm to room temperature and stir for 3 days. The boc- protected product was precipitated from the reaction with water (150 mL) and isolated by vacuum filtration. The solid was resuspended in TFA (7.45 g, 65.34 mmol, 5 mL) and dichlormethane (5 mL) and stirred overnight. The product was precipitated with MTBE (100 mL) and isolated by filtration to yield 211 mg of Compound 27A (42%) as an off-white solid (2.23m, M+H = 480), 132710-90-8

132710-90-8 1-Boc-4-(3-hydroxypropyl)piperazine 16217800, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; TARVEDA THERAPEUTICS, INC.; CIPRIANI, Tyler; MOREAU, Benoit; BILODEAU, Mark T.; QUINN, James M.; WOOSTER, Richard; CIRELLO, Amanda L.; PERINO, Samantha; WHALEN, Kerry; KADIYALA, Sudhakar; WHITE, Brian H.; (172 pag.)WO2019/118830; (2019); 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.278788-60-6,(R)-1-Boc-Piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

(2R)-l-(fc/^-Butoxycarbonyl)-4-isopropyIpiperazine-2-carboxylic acidTo (2i?)-l-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (4.5 g) and Na2CO3 (8.32 g) was added dry EtOH (135 ml) and isopropyl iodide (2.16 ml) and the mixture heated at reflux for 18 hours under argon. The solvent was then removed under reduced pressure, 5percentMeO?/DCM (50 ml) added, the mixture stirred for 1 hour in a stoppered flask, filtered and washed through with DCM (2 x 10ml). The filtrate was applied directly to a 12Og- silica Redisep cartridge and purified using 10-70percent MeOH/DCM. After evaporation, the product was isolated as a white foam (4.50 g), which was used without further purification. 1H NMR (400.132 MHz, DMSO) 0.95 (m, 6H), 1.40 (2x s, 9H), 2.30 (m, 2H), 2.75 (m, 2H), 2.95 (t, IH), 3.12 (t, IH,), 3.70 (m, IH), 4.48 (d, IH), 12.60 (br. s, IH).

278788-60-6, As the paragraph descriping shows that 278788-60-6 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2007/71952; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

At 0C under nitrogen, 366mg of commercially available 2-chloropyridine-4-carbonyl chloride dissolved in 2ml of dichloromethane were added dropwise to a solution of 530mg of commercially available 4-(1 -piperazinyl)-2-trifluoromethylbenzonitrile in 5ml ofdichloromethane and 630mg of Et3N. The reaction mixture was stirred overnight at room temperature, poured over a stirred mixture of 100ml EtOAc and 40ml of water. The aqueous layer was extracted with EtOAc. The combined organic layers were washed with brine, dried over MgS04, filtered, concentrated under vacuum and purified by column chromatography on silica gel to isolate 620mg of 4-{4-[(2-chloropyridin-4-yl)carbonyl]piperazin-1 -yl}-2- (trifluoromethyl)benzonitrile. 99mg of this material were then added to a degased mixture of 85mg of commercially available 1 -(4-trifluoromethylphenyl)piperazine, 6mg of Pd(OAc)2, 23mg of RuPhos, 163mg of Cs2C03, and 1 .5ml of ie/f-Butanol then, heated to 85 C overnight. The reaction mixture was then poured at room temperature over a stirred mixture of 50ml of EtOAc and 10ml of water. The aqueous layer was extracted with 10ml EtOAc. The combined organic layers were washed with brine, dried over MgS04, filtered, concentrated under vacuum and purified by column chromatography to isolate 60mg of compound No. 32 in Table 2., 30459-17-7

30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS TIERGESUNDHEIT AG; GAUVRY, Noelle; PAUTRAT, Francois; WO2015/71417; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution [OF TERT-BUTYL 3-OXOPIPERAZINE-1-CARBOXYLATE] (0.500 mg, 2. [50] mmol) in 10 mL of DMF at [0 C] was added NaH as a 60% dispersion in mineral oil (2.62 mmol), and the reaction was stirred for 45 minutes. [4-BROMO-1-BUTENE] was added (0.280 mL, 2.75 mmol) dropwise as a solution in 1 mL of THF. The solution was stirred overnight, allowing it to warm to room temperature. The reaction was partitioned between EtOAc and saturated [NAHC03] solution. The organic phase was washed with brine, dried [(NA2S04),] filtered, and concentrated in vacuo to give the titled compound. Proton NMR for the product was consistent with the titled compound. ESI+MS : 255.1 [[M+H]] [+.], 76003-29-7

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

Reference£º
Patent; MERCK & CO., INC.; WO2004/14851; (2004); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step D: tert-butyl (3S)-4-[2-(3-cyano-4-fluoro-2-methylphenyl)-2-hydroxyethyl]-3-(hydroxymethyl)piperazine~1~carboxylate: 6-Fluoro-2-methyl-3-(oxiran-2-yl)benzonitrile (12.0g, 67.7 mmol) and (S)-4-N-BOC-2-hydroxymethylpiperazine (22.0 g. 102 mmol) were suspendedin ethanol (100 mL) then heated in a microwave apparatus for 30 minutes at 150 C. Thereaction mixture was cooled and evaporated dryness. The residue was purified by MPLC chromatography through a 330g Redi-sep column eluting with 5%MeOH/95% EtOAc solventsystem to yield the title compound. LC-MS: M+ 1 = 394., 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

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.

EXAMPLE 46 5-(3,4-Dimethoxybenzylamino)-2-(2-furyl)-8-[4-(4-trifluoromethylphenyl)piperazin-1-ylmethyl][1,2,4]triazolo[1,5-c]pyrimidine (Compound 46) The subject compound (quantitative) was obtained as a pale brown oily matter from 5-(3,4-dimethoxybenzylamino)-8-formyl-2-(2-furyl)[1,2,4]triazolo[1,5-c]pyrimidine and 1-(4-trifluoromethylphenyl)piperazine in a manner similar to that in Example 1. 1H NMR (CDCl3, delta, ppm): 2.75 (t, J=5.0 Hz, 4H), 3.31 (t, J=5.0 Hz, 4H), 3.88 (s, 3H), 3.88 (s, 3H), 3.90 (s, 2H), 4.76 (d, J=5.6 Hz, 2H), 6.44 (t, J=5.6 Hz, 1H), 6.57 (dd, J=1.7, 3.3 Hz, 1H), 6.85 (d, J=8.0 Hz, 1H), 6.90 (d, J=8.9 Hz, 2H), 6.95 (s, 1H), 6.96 (d, J=8.0 Hz, 1H), 7.22 (d, J=3.3 Hz, 1H), 7.45 (d, J=8.9 Hz, 2H), 7.60 (d, J=1.7 Hz, 1H), 7.96 (s, 1H)

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

Reference£º
Patent; Uesaka, Noriaki; Imma, Hironori; Kashima, Hajime; Kurokawa, Masako; Nonaka, Hiromi; Kanda, Tomoyuki; Kuwana, Yoshihisa; Toki, Shinichiro; Shimada, Junichi; US2004/110826; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics