Heterocyclic Building Blocks-piperazine

57260-70-5, tert-Butyl 4-benzylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

57260-70-5, [Referential Example 159] 1-Benzylpiperazine hydrochloride To 1-benzyl-4-tert-butoxycarbonylpiperazine (3.12 g), saturated ethanol hydrochloride was added, followed by stirring for 90 minutes at room temperature. The solvent was distilled off under reduced pressure, followed by drying, whereby the title compound (2.73 g, 97%) was obtained as white powder. 1H-NMR (DMSO-d6) delta: 3.05-3.67(9H,m), 4.38(2H,br), 7.35-7.70(5H,m), 9.61(1H,br). MS (EI) m/z: 176M+. Elementary analysis for C11H16N2·2HCl·0.2H2O Calculated: C, 52.27; H, 7.34; Cl, 28.05; N, 11.27. Found: C, 52.04; H, 7.36; Cl, 27.89; N, 11.24.

57260-70-5 tert-Butyl 4-benzylpiperazine-1-carboxylate 584330, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1104754; (2001); 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.262368-30-9,N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide,as a common compound, the synthetic route is as follows.

Method 2; A suspension of methyl-3-[methoxy(phenyl)methylene]-2-oxoindoline-6- carboxylate (20,0 g; 0,064 mol) and N-(4-aminophenyl)-N-methyl-2-(4- methylpiperazin-1-yl)acetamide (17,1 g; 0,065 mol) in methanol (180 ml) is heated to reflux for 7,5 h. The resulting suspension is cooled down to 10 0C within 1 h and stirring is maintained for 1 h. After filtration, the solid is washed with ice cold methanol (80 ml) and dried to afford 31 ,0 g (89,0 %) of the “anilino” compound as yellow crystals., 262368-30-9

262368-30-9 N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide 21927707, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; WO2009/71523; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

192130-34-0, tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 48; 4-{2-[5-(3-Trifluoromethoxy-phenyl)-imidazo[2,1-b][1 ,3,4]thiadiazol-2- ylamino]-ethyl}-piperazine-1-carboxylic acid tert-butyl ester; A mixture of 2-methanesulfonyl-5-(3-trifluoromethoxy-phenyl)-imidazo[2, 1- b][1 ,3,4]thiadiazole (1 16 mg, 0.319 mmol), 4-N-(2-aminoethyl)-1 -N-boc- piperazine (1 10 mg, 0.479 mmol) and Et3N (0.089 mL, 0.639 mmol) in ‘PrOH (5 mL) was heated in a sealed tube at 1 10°C for 16 hours. On cooling, DCM was added and the mixture was washed with H20. The organic layer was dried (sodium sulfate), filtered and concentrated. The residue was purified by column chromatography (Isolute/Flash, Sill, 0percent to 20percent MeOH in DCM) to give the desired product (4-{2-[5-(3-trifluoromethoxy-phenyl)-imidazo[2, 1 – b][1 ,3,4]thiadiazol-2-ylamino]-ethyl}-piperazine-1 -carboxylic acid tert-butyl ester) (20 mg, 12percent yield).HPLC-MS (method 1): Rt= 3.99 min, [M+1f m/z 513.2.H NMR (300 MHz, MeOD) delta 8.04 (s, 1 H), 7.90 (m, 1 H), 7.52 (s, 1 H), 7.51 (t, J = 8.1 Hz, 1 H), 7.19 (m, 1 H), 3.62 (t, J = 6.4 Hz, 2H), 3.44 (m, 4H), 2.72 (t, J = 6.4 Hz, 2H), 2.54 (m, 4H), 1.46 (s, 9H).

192130-34-0, As the paragraph descriping shows that 192130-34-0 is playing an increasingly important role.

Reference：
Patent; CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS (CNIO); PASTOR FERNANDEZ, Joaquin; GARCIA COLLAZO, Ana, Maria; NOYA MARINO, Beatriz; GONZALEZ CANTALAPIEDRA, Esther; WO2012/20217; (2012); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129722-25-4,7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one,as a common compound, the synthetic route is as follows.

To a solution of dehydro-Aripiprazole (1.0 g, 2.24 mmol) in 2-methyltetrahydroffiran (25 mE) was added silver carbonate (0.864 g, 3.13 mmol) and iodomethyl octanoate (0.764 g, 2.68 mmol) at room temperature. The reaction was stirred for5 days. The reaction was quenched with H20 (30 mE) and filtered through celite. The reaction was extracted with ethyl acetate (3×20 mE), washed with 5% w/v sodium sulfite solution (15 mE), brine (20 mE), dried over MgSO4 and concentrated. The product was purified by column chromatography on silica eluting with 0-70% ethyl acetate in heptane to provide Compound 1206 (0.602 g) as a pale orange oil.?H-NMR (300 MHz, CDC13) oe 7.95 (1H, d), 7.60 (1H, d),7.21 (1H, m), 7.14 (2H, m), 7.07 (1H, dd), 6.95 (1H, m), 6.79(1H, d), 6.24 (2H, s), 4.12 (2H, m), 3.09 (4H, m), 2.68 (4H,m), 2.54 (2H, m), 2.36 (2H, t), 1.90 (2H, m), 1.77 (2H, m),1.61 (4H, m), 1.23 (6H, m), 0.83 (3H, t). [M+H]=602.2

129722-25-4, 129722-25-4 7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one 10114519, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Alkermes Pharma Ireland Limited; Blumberg, Laura Cook; Remenar, Julius F.; Almarsson, Orn; Zeidan, Tarek A.; US9102618; (2015); B2;,
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Piperazines – an overview | ScienceDirect Topics

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

129799-15-1, EXAMPLE 20 Preparation of 1-tert-butyl 2-methyl 4-(4-chlorophthalazin-1-yl)piperazine-1,2-dicarboxylate (JK-16) 1,4-dichlorophthalazine (741 mg, 3.72 mmol), 1-tert-butyl 2-methyl piperazine-1,2-dicarboxylate (1.00 g, 4.09 mmol), N,N-diisopropylethylamine (0.972 mL), and 4-methyl-2-pentanone (6 mL) were heated at 120 for 16 hours. The solvent was removed and the residue purified by chromatography over silica using a gradient of hexanes/0-70% ethyl acetate. The compound was obtained as a white solid. MS (M+H)+=407.1.

129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Amgen Inc.; US2009/48259; (2009); 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.161357-89-7,1-(Methylsulfonyl)piperazine hydrochloride,as a common compound, the synthetic route is as follows.

2-Chloro-4-morpholinofuro[3,2-d]pyrimidine-6-carbaldehyde 39 prepared following Example 20 (65 mg, 1.0 eq) was dissolved in 1 ,2-dichloroethane (9.7 ml) and treated with hydrochloride salt of 1-methanesulfonylpiperazine (69 mg, 1.4 eq), sodium acetate (28 mg, 1.4 eq) and trimethyl orthoformate (0.27 ml, 10 eq). Reaction mixture was stirred at r.t. for 12 h. Sodium triacetoxyborohydride (62 mg, 1.2 eq) was added and reaction mixture was stirred at r.t. for 8 h. Reaction mixture was quenched with saturated aq. NaHCO3 and extracted with dichloromethane. The combined organic layers were dried (Na2SO4) and concentrated. The crude reaction mixture was purified by flash chromatography to yield 2- chloro-6-((4-(methylsulfonyl)piperazin- 1 -yl)methyl)-4-morpholmofuro [3 ,2-d]pyrimidine(70 mg, 68%) : MS (Ql) 416 (M)+., 161357-89-7

161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; PIRAMED LIMITED; GENENTECH, INC.; BAYLISS, Tracy; CHUCKOWREE, Irina; FOLKES, Adrian; OXENFORD, Sally; WAN, Nan, Chi; CASTANEDO, Georgette; GOLDSMITH, Richard; GUNZNER, Janet; HEFFRON, Tim; MATHIEU, Simon; OLIVERO, Alan; STABEN, Steven; SUTHERLIN, Daniel, P.; ZHU, Bing-Yan; WO2008/70740; (2008); A1;,
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Piperazines – an overview | ScienceDirect Topics

934-98-5, 2-(4-Methylpiperazin-1-yl)ethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 58: 2-[2-( 4-methvl-piperazin-1-vl)-ethvlami no l-N-[3-( 5-thiophen-3-vl-pvrimidin-2-vlamino )- phenyl] acetamide; To a stirring solution of U (200 mg, 0.58 mmol) in CH3CN (100 mL) was added J (486 mg, 3.48 mmol) followed by diisopropylethylamine (300 muL, 1.74 mmol). The solution was brought to reflux and monitored by tic analysis. After 13 hours the solvent was removed in vacuo and the residue purified via column chromatography (silica gel, 9:1 CH2CI2/MeOH). The fractions containing product were evaporated to dryness under vacuum to yield compound 58 in 44percent yield as a white crystalline solid. 1H NMR (300 MHz, CDCl3) No. 2.27 (s, 3H), 2.27-2.46 (m, 10H), 2.5-2.54 (m, 2H), 3.39 (s, 2H), 7.2-7.46 (m, 11 H), 8.09 (s, 1 H), 8.67 (s, 2H), 9.42 (s, 1H). MS m/z 452 [M++1]., 934-98-5

934-98-5 2-(4-Methylpiperazin-1-yl)ethanamine 70284, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SUGEN, INC.; WO2005/113548; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 4-(2-hydroxyethyl)piperazine-l-carboxylate (SD038) Benzylchloroformate (4.7 g, 27.6 mmol) in acetonitrile (30 mL) was added dropewise over 30 min to a solution of 1 -(2-hydroxyethyl)piperazine (3 g, 23 mmol) in water (30 mL) via an isobar cylindrical funnel. The pH was maintained around 8-9 by addition of a solution of NaOH 4N. The reaction was stirred overnight at room temperature. The mixture was first extracted with dichloromethane (100 mL) in order to remove the diprotected compound and then acidified with HC1 4N. The acidic aqueous phase was extracted twice with dichloromethane (2 x 100 mL). The organic phase was washed with brine and dried over anhydrous Na2S04. The solvent was removed under vacuum and the crude was purified by flash chromatography with the gradient of methanol in dichloromethane (0-8%) to yield 5.41 g (90%) of product SD038 as a colorless oil.

103-76-4, The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; PRESIDENT AND FELLOWS OF HARVARD COLLEGE; HALPERIN, Jose A.; CHOREV, Michael; AKTAS, Bertal Huseyin; WO2014/47437; (2014); 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.55121-99-8,(4-Aminophenyl)(4-methylpiperazin-1-yl)methanone,as a common compound, the synthetic route is as follows.,55121-99-8

Step 3: l-(4-Bromo-phenyl)-3-[4-(4-methyl-piperazine-l-carbonyl)-phenyl]-urea rTo a solution of (4-amino-phenyl)-(4-methyl-piperazine-l-yl)-methanone (10.0 g, 0.0456 mol) and TEA (4.7 g, 0.0456 mol) in DCM (150 mL) was added 4-bromophenyl isocyanate (10.9 g, 0.0547 mol). The reaction mixture was stirred at room temperature for 12 h. The white solid was obtained and was filtered and dried to afford the title compound [15.0 g, 79%]; LC-MS (ESI): Calculated mass: 416.1; Observed mass: 417.1 [M+H]+ (RT: 0.23 min).

As the paragraph descriping shows that 55121-99-8 is playing an increasingly important role.

Reference：
Patent; ENDO PHARMACEUTICALS INC.; SMITH, Roger, Astbury; THOMPSON, Scott, Kevin; HOSAHALLI, Subramanya; BEJUGAM, Mallesham; NANDURI, Srinivas; PANIGRAHI, Sunil, Kumar; MAHALINGAM, Natarajan; WO2012/58671; (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.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: A mixture of 4-chloro-3-methyl-5-phenyl-1,1-pyrazolo[3,4-c]pyridazine (0.33 mmol), the alcohol (0.65 mmol), diethyl azodicarboxylate (114 mg, 0.65 mmol) and triphenyl phosphine (171 mg, 0.65 mmol) in 1,4-dioxane (2 mL) was heated using microwave irradiation to a temperature between 85 and 120° C. for a 30 to 90 min period. The reaction mixture was concentrated in vacuo and the residue was purified by preparative HPLC to provide the title compound.4-chloro-3-methyl-1-[2-(4-methylpiperazin-1-yl)ethyl]-5-phenyl-pyrazolo[3,4-c]pyridazine (Compound Iv) Compound Iv was synthesized from 4-chloro-3-methyl-5-phenyl-1H-pyrazolo[3,4-c]pyridazine and 2-(4-methylpiperazin-1-yl)ethanol following the general procedure for the Mitsunobu reaction described above. 1H NMR delta (ppm) (CHCl3-d): 7.80-7.77 (2H, m), 7.56-7.48 (3H, m), 4.80 (2 t), 2.99 (2H, t), 2.80 (3H, s), 2.64 (4H, br s), 2.40 (4H, br s), 2.26 (3H, s). LCMS (10 cm_ESCI_Formic_MeCN) Rt 2.53 min; m/z 371 [M+H] 99.25percent purity., 5464-12-0

As the paragraph descriping shows that 5464-12-0 is playing an increasingly important role.

Reference：
Patent; BUeRLI, Roland Werner; ESMIEU, William Rameshchandra Krishna; LOCK, Christopher James; MALAGU, Karine Fabienne; OWENS, Andrew Pate; HARTE, William E.; US2014/121197; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics