Tag: M.W:200-300

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.

EXAMPLE D rac-3-Methyl-4-(4-trifluoromethyl-phenyl)-piperazine-1-carboxylic acid tert-butyl ester To a solution of 3-Methyl-piperazine-1-carboxylic acid tert-butyl ester (1.0 g, 5.3 mmol) and of 1-Bromo-4-trifluoromethyl-benzene (1.0 g, 4.4 mmol) in toluene (10 ml) were added sodium-tert butylate (0.6 g, 6.2 mmol), 2-(dicyclohexylphosphino)biphenyl (31. mg,89 mmol), and tris(dibenzylideneacetone)dipalladium-chloroform complex (23 mg, 22 mmol). The reaction mixture was then stirred for 16 hours at 80¡ã C. After allowing to cool to room temperature the reaction mixture was concentrated in vacuo and purified by column chromatography (SiO2, 70 g, heptane/ethyl acetate 0-30percent) to give the title compound as a light brown solid (0.47 g); MS (m/e): 345.2 (M+H+, 100percent)., 120737-59-9

Big data shows that 120737-59-9 is playing an increasingly important role.

Reference£º
Patent; Alberati-Giani, Daniela; Jolidon, Synese; Narquizian, Robert; Nettekoven, Matthias Heinrich; Norcross, Roger David; Pinard, Emmanuel; Stalder, Henri; US2005/59668; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

77279-24-4,77279-24-4, tert-Butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 63; l-{2-[4-(3,5-dimethoxybenzyl)piperazin-l-yl]ethyl}-3,3-bis(4-fluorophenyl)pyrrolidin-2- one; Example 63A; tert-butyl 4-(2-bromoethyl)piperazine-l-carboxylate; tert-Butyl 4-(2-hydroxyethyl)piperazine-l-carboxylate (5.76 g, 25.0 mmol) was dissolved in dry tetrahydrofuran (100 mL) and carbon tetrabromide (9.12 g, 27.5 mmol). A solution of triphenyl phosphine (6.62 g, 25.3 mmol) in dry tetrahydrofuran (25 mL) was added dropwise, and the mixture was stirred for 20 hours. The reaction was diluted with n- hexane (100 mL) and washed with a saturated NaHCO3 solution, water and brine, dried with MgSO4, filtered and concentrated. Silica gel chromatography eluting with ethyl acetate/hexanes 1 :4 gave the title compound. MS (DCI) m/z 295(M+H)+.

The synthetic route of 77279-24-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ABBOTT LABORATORIES; BHATIA, Pramila, A.; DOHERTY, George, A.; DRIZIN, Irene; MACK, Helmut; PERNER, Richard, J.; STEWART, Andrew, O.; ZHANG, Qing Wei; WO2010/39947; (2010); 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.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

Step A: Preparation of 2a; According to general procedure C, 2a was obtained with 1a (0.25 mL, 5.18 mmol, 1.0 eq.), EDC (324 mg, 10.36 mmol, 2.0 eq.), DMAP (317 mg, 10.36 mmol, 2.0 eq.) and N-methylpyrrole-2-carboxylic acid (329 mg, 10.36 mmol, 2.0 eq.). The mixture was washed first with a saturated solution of ammonium chloride, then with 1 N HCl and at the end with a saturated solution of sodium carbonate. The residue was purified by flash chromatography on silica gel, eluting with cyclohexane-ethyl acetate (8:2 to 1:1) to afford 2a (420 mg, 98percent) as a colorless oil.MS (ESI+) (+0.1percent HCOOH): 328.12 [C18H21N3O3+H]+ (m/z); “General method C” (peptide coupling) consists of adding 1.2 to 2.0 equivalents of EDCl and 1.2 to 2.0 equivalents of HOBt or DMAP and 1.2 to 2.0 equivalents of heteroaryl carboxylic acid, at 0¡ã C., to a 0.2 to 0.6M solution within DMF of protected amino(piperidine) derivative N-Boc or N-CBz. The mixture is maintained under stirring at ambient temperature for 16 to 18 hours, then diluted with ethyl acetate and washed with water. The solution is then dried and concentrated to dryness under reduced pressure, then the residue is purified by chromatography over silica eluting with the cyclohexane-ethyl acetate mixture., 31166-44-6

31166-44-6 1-Cbz-Piperazine 643495, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Vetoquinol SA; US2010/9980; (2010); 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.1030377-21-9,(S)-1-Boc-2-(Hydroxymethyl)piperazine,as a common compound, the synthetic route is as follows.

a) To a solution of (R)-N-(l-(2,4-dichlorophenyl)ethyl)-5-fluoro-2-nitroaniline (prepared from Example 14 step a, 1.6 g, 4.9 mmol) and (5)-2-(hydroxymethyl)piperazine-l- carboxylic acid ?-butyl ester (0.99 g, 4.9 mmol) in anhydrous DMSO (10 mL) was added K2CO3 (1.88 g, 14.6 mmol). The reaction mixture was heated with stirring at 125 C for 2 h. After cooling to room temperature, the mixture was diluted with deionized water (10 mL) and stirred for 30 min. The aqueous layer was extracted with dichloromethane. The organic layer was dried (MgS04), filtered, and concentrated in vacuo. The crude oil was dried under vacuum to give the desired compound (1.9 g, 3.5 mmol, 73%).

1030377-21-9, 1030377-21-9 (S)-1-Boc-2-(Hydroxymethyl)piperazine 22884145, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CHEMOCENTRYX, INC.; LELETI, Manmohan Reddy; LI, Yandong; MALI, Venkat Reddy; POWERS, Jay; YANG, Ju; WO2013/82429; (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.118753-66-5,tert-Butyl 4-aminopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of tert-butyl 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 2-(4-chloro-3-fluorophenoxy)acetic acid (0.201 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), brine solution (30 mL x 2), dried over anhydrous sodium sulfate and concentrated under reduced pressure, to obtain tert-butyl 4-(2-(4-chloro-3-fluorophenoxy)acetamido)piperazine-l -carboxylate (0.150 g, 38 % Yield) as a semi solid. LCMS 388 2 | M H | ; NMR (400MHz, DMSO-de) d 7.57 – 7.36 (m, 1 H), 7.11 – 6.94 (m, 1 H), 6.92 – 6.69 ( m. 1 H), 5.76 (s, 1 H), 5.04 – 4.79 (m, 1 ). 4.48 (s, 1 H), 3.85 (br s, 1 H), 2.92 (br. s., 2 H), 2.70 (d, J= 11.8 Hz, 2 H), 1 40 (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

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.

4-(Thiophen-2-yl)butanoic acid (0.05 ml, 0.34 mmol), HOBt (58 mg, 0.43 mmol), TBTU (140 mg, 0.43 mmol), anhydrous triethylamine (0.1 ml, 0.69 mmol) and dry DMF (2 ml) were placed in an oven-dried Schlenk tube under a nitrogen atmosphere. The resulting solution was stirred at room temperature for 15 minutes. A second Schlenk tube was prepared containing 1-(4-trifluoromethyl phenyl) piperazine (100 mg, 0.43 mmol) and dry DMF (1 ml) under a nitrogen atmosphere. The resulting solution was stirred until complete dissolution of the piperazine had occurred. The piperazine solution was then transferred, via a cannula, to the first Schlenk tube containing the carboxylic acid. The resulting solution was stirred for 24 hrs, under nitrogen, and monitored by TLC. After 24 hrs, the DMF was removed under reduced pressure and the resulting oil was acidified using a 0.1 M hydrochloric acid solution. The aqueous mixture was extracted with dichloromethane (20 ml, followed by 4 x 10 ml) and the organic layer washed with a saturated sodium bicarbonate solution (3 x 20 ml) and brine (3 x 20 ml). The organic layer was dried over magnesium sulphate and evaporated under reduced pressure. The residue was purified using flash chromatography (3:2, EtOAc:n-hexane) to obtain the desired product in an 80% yield. H NMR (300 MHz, CDCI3) ? 7.49 (d, 2H), 7.12 (dd, 1 H), 6.90-6.94 (m, 3H), 6.80-6.82 (m, 1 H), 3.76 (t, 2H), 3.56 (t, 2H), 3.24 (t, 4H), 2.91 (t, 2H), 2.38 (t, 2H), 2.0-2.1 1 (m, 2H). MS (+ESI) calcd for C18 H21 F3 N2 O S m/z: [M + H]+, 382.1329; found 383.1399 [Diff(ppm) = 0.61]., 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; NATIONAL UNIVERSITY OF IRELAND, MAYNOOTH; STEPHENS, John; FINDLAY, John; KINSELLA, Gemma; MARTIN, Darren; DEVINE, Robert; VELASCO-TORRIJOS, Trinidad; WO2013/60860; (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.1214196-85-6,1-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

A 50 mL rb flask equipped with an air condenser, rubber septum and a magnetic stir bar was set under Ar atmosphere and charged with 500 mg of 1 -(/tv7-b utoxy carbonyl)piperazine-2- carboxylic acid (2.17 mmol, 1 equiv.), 80.0 mg of DMAP (0.651 mmol, 0.3 equiv.), 500 mg of EDCI (2.61 mmol, 1.2 equiv.), 10 mL of CH2CI2 and 3 mL of dry methanol. The reaction mixture was stirred at 40 C for 1.5 h and then the reaction was allowed to cool to rt. After stirring for 20 h, the reaction mixture was concentrated and the residue was dissolved in CH2CI2. The CH2CI2 solution was washed with water (3x). The water solutions were combined and the product was back-extracted with CH2CI2 (3x). Then the combined organics were washed with sat. NaHC03 solution, brine and dried over Na2S04. The crude product (661 mg) was purified on silica gel column using 0 to 5 % MeOH in CH2CI2 as eluent affording 419 mg (79 %) of the product 41 as a colorless oil.

1214196-85-6, The synthetic route of 1214196-85-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; EMORY UNIVERSITY; LIOTTA, Dennis C.; JECS, Edgars; ALTAS TAHIROVIC, Yesim; WILSON, Lawrence; PELLY, Stephen Christopher; (102 pag.)WO2019/183133; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8,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.

A 1 liter round bottom flask equipped with stirring rod, thermo pocket, water condenser was charged with solution of 11- piperazinyldibenzo[b,f] [l,4]thiazepine in toluene 350 cc [63.0 g (0.22 moles)] and the mixture was stirred for 15 min 25- 30C, and, to which, was added sodium carbonate [41.0 gm (0.39 moles)], tetra butyl ammonium bromide [16.0 gm (0.05 moles)] 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 absence of compound of formula IV) and was cooled to 25C to 30C. To which, was added 150 cc DM water. Then 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 extracts and the organic layer were combined, and the pH was adjusted to 2-3 using IN HCl solution in DM (demineralized) water, the reaction mixture was then stirred for 30 min at 25-30C. 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 extracted with 125 cc toluene. The extracts and the organic layer were combined, and washed with DM (demineralized) water 300 cc twice. The organic layer was distilled – off under vacuum below 70C to afford 2-(2-(4-dibenzo[b,f]-[l,4] thiazepine- l l-yl-l-piperazinyl)ethoxy)ethanol Purity of 2-(2-(4-dibenzo[b,f]-[l,4] thiazepine- l l-yl-l-piperazinyl)ethoxy)ethanol was 99.0 (area % by HPLC).

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2008/121415; (2008); A2;,
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,129779-30-2

To a stirred solution of compound 1(2.1 g, 1 eq.) and compound 2 (2.3 g, 1 eq.) in ACN (20 mL), potassium carbonate (4.1 g, 3 eq.) was added. The reaction mixture was stirred at room temperature for 16 h. The reaction completion was monitored by TLC. The reaction mixture was diluted with water and extracted with ethyl acetate. The combined organic extracts were washed with water and brine, dried over anhydrous Na2504, filtered and concentrated under reduced pressure to give a crude residue which was purified by silica gel column chromatography to afford compound 3.

The synthetic route of 129779-30-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIOMARIN PHARMACEUTICALS INC.; LUEDTKE, Gregory; BHAGWAT, Shripad; (99 pag.)WO2018/119362; (2018); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

Step 1 4-Benzyl-3-oxo-piperazine-1-carboxylic acid tert-butyl ester Sodium hydride (60%, 18.11 g, 452 mmol) in mineral oil was triturated with 35 hexanes, dried under a stream of nitrogen and taken up in 1500 mL of THF. To the slurry at 0 C. was added 3-oxo-piperazine-1-carboxylic acid tert-butyl ester (75.057 g, 200.4 mmol) in portions over 15 min. After 90 minutes benzyl bromide (71.01 g, 415.1 mmol) was added and the mixture was warmed to room temperature for 18 hours. The solution was quenched with H2O and extracted with Et2O. The combined organic layers were washed with H2O, washed with brine, dried over MgSO4. Concentration in vacuo gave a crude solid which was recrystallized from hexane to afford 4-benzyl-3-oxo-piperazine-1-carboxylic acid tert-butyl ester (83.5 g, 76%) as a white crystalline solid.

76003-29-7 1-Boc-3-Oxopiperazine 3157178, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Roche Palo Alto LLC; US2009/209553; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics