Heterocyclic Building Blocks-piperazine

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a 25 mL flask was added TEA (177 mg, 244 ).ll, 1.75 mmol), tert-butyl piperazine-1-carboxylate (240 mg, 1.29 mmol), (bromomethyl)benzene (200 mg, 139 ).ll, 1.17 mmol) andDCM (4 mL). The colorless solution was stirred at rt for 3 hrs. The reaction mixture wasconcentrated to give a white solid. Then it was purified by silica gel column chromatography(eluted with EA/PE=15- 30% ), about 177 mg tert-butyl4-benzylpiperazine-1-carboxylate20 (Compound lOA) was obtained as a colorless oil. MS: calc’d 277 (M+Ht, measured 277(M+Ht, 57260-71-6

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; WANG, Lisha; YUN, Hongying; ZHANG, Weixing; ZHU, Wei; ZHANG, Zhiwei; (69 pag.)WO2017/202704; (2017); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.170911-92-9,tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate 4d (4 g,14.44 mmol) was dissolved in 40 ml of dry pyridine and stirred at0 C under inert atmosphere. Cinnamoyl chloride 6b (4.45 g,17.33 mmol) was dissolved in 20 ml dry DCM and added dropwiseto above stirred solution at 0 C. The reaction mixture was stirredfor 3 h. After completion of the reaction, the reaction mixture wasdiluted with 40 ml water and 60 ml ethyl acetate followed by 2 NHCl to make it acidic. The organic layer was separated and againwashed with 2 N HCl followed by saturated bicarbonate solution(2 50 ml) and brine solution. The organic layer was dried overanhydrous sodium sulfate and was evaporated under reducedpressure. The crude product was recrystallized from ethyl acetateand hexane to afford 4.52 g of 7l. Light yellow solid; Yield 69.33%;216e218 C (charred); IR (KBr pellets, cm1): 3425, 3105, 1666,1604, 1544, 1514, 1427, 1342, 1220, 1141, 991, 844; 1H NMR(400 MHz, CDCl3) d (ppm): 1.43 (9H, s, CH3), 3.10 (4H, t, J 3.79 Hz),3.62 (4H, t, J 3.76 Hz), 6.71 (1H, d, J 16.5 Hz, PheCH]CHe), 6.98(2H, d, J 7.2 Hz, AreH), 7.29e7.87 (4H, m, AreH), 7.89 (1H, d,J 16.5 Hz, PheCH]CHe), 8.23 (2H, d, J 7.0 Hz, AreH), 9.24 (1H,s, CONH); 13C NMR (100 MHz, CDCl3) d (ppm): 28.76, 49.41, 51.48,78.50, 112.10, 118.03, 121.31, 123.72, 126.08, 129.45, 141.79, 142.11,145.21, 147.29, 157.22, 167.52; HReMS m/z: 453.2067 (M 1)., 170911-92-9

The synthetic route of 170911-92-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Patel, Kavitkumar N.; Telvekar, Vikas N.; European Journal of Medicinal Chemistry; vol. 75; (2014); p. 43 – 56;,
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5464-12-0,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.

1-(2-(4-bromo-3-fluorophenoxy)ethyl)-4-methylpiperazine: A flask was charged with 4-bromo-3-fluorophenol (5.00 g, 26 mmol) and triphenylphosphine (10.30 g, 39 mmol). Methylene chloride (120 mL) was added followed by 2-(4-methylpiperazin-1-yl)ethanol (4.61 g, 32 mmol) and the solution was stirred on an ice water bath to cool. After 5 minutes, diisopropyl azodicarboxylate (7.6 ml, 39.1 mmol) was added over 6 to 8 minutes. The reaction was left stirring on the cold bath to slowly warm to room temperature overnight. The reaction was concentrated and the residue purified by flash chromatography (25percent to 100percent EtOAc in hexanes) to provide the product as a colorless oil (2.62 g, 33percent).

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

Reference£º
Patent; Hangauer, David G.; US2006/160800; (2006); A1;,
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78551-60-7, tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,78551-60-7

4 M HC1 in l,4-dioxane (150 mL, 600 mmol, 12 equiv) was added at room temperature to compound (14.5 g, 50 mmol, 1 equiv) and the mixture was stirred at room temperature for 2 hours, at which time LCMS indicated that the reaction was complete. The mixture was concentrated under reduced pressure and azeotroped with toluene (3 x 200 mL) to give l-benzylpiperazin-2-one hydrochloride (15.1 g, quantitative yield) as a viscous pale-yellow oil

As the paragraph descriping shows that 78551-60-7 is playing an increasingly important role.

Reference£º
Patent; CONATUS PHARMACEUTICALS, INC.; SPADA, Alfred, P.; TERNANSKY, Robert, J.; (0 pag.)WO2020/6341; (2020); A1;,
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103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,103-76-4

A solution of 3,7-dichloro-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one (200 mg, 0.66 mmol), 1-(2-hydroxyethyl)piperazine (117 mg, 0.90 mmol, Aldrich) and triethylamine (0.27 mL, 1.94 mmol) in THF (3 mL) was stirred at room temperature for one hour. The reaction was partitioned between ethyl acetate and water. The layers were separated and the aqueous layer was extracted with ethyl acetate. The combined organic layers were washed with brine, dried over magnesium sulfate, and solvent was removed at reduced pressure to give 7-chloro-3-[4-(2-hydroxyethyl)piperazin-1-yl]-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one. (218 mg, 83% yield). 1H NMR (CDCl3) delta 8.48 (1H), 7.34 (1H), 4.33-4.30 (2H), 4.04-4.00 (4H), 3.76-3.72 (2H), 3.69-3.65 (2H), 3.38-3.34 (2H), 2.67-2.64 (4H), 2.62-2.58 (2H), 1.55-1.48 (2H), 0.87-0.82 (3H).

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

Reference£º
Patent; Pfizer Inc; US2007/249615; (2007); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.,934-98-5

Preparation of Compound 177 (Method D) 2-[2,7-bis[2-[(2R,3S,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydropyran-2- yl]ethynyl]carbazol-9-yl]-N-[2-(4-methylpiperazin-l-yl)ethyl]acetamide To a stirred solution of 2-(4-methylpiperazin-l-yl)ethanamine (7.7 mg, 0.054 mmol) and Et3N (20 mu) in DMF (0.3 mL) is added a premixed solution of Compound 176 and HATU (23 mg, 0.061 mmol) in DMF (0.4 mL). Reaction mixture is stirred at RT for 3 h and the mixture is purified directly by reverse phase HPLC to afford the title compound (16 mg, 40percent yield). NMR (400 MHz, CD3OD) delta 8.38 (brs, 1H), 8.11 (d, J = 8.1 Hz, 2H), 7.63 (s, 2H), 7.36 (dd, J = 8.1, 1.2 Hz, 2H), 5.04 (s, 2H), 4.90 (d, J = 2.1 Hz, 2H), 4.03 (dd, J = 3.2, 2.2 Hz, 2H), 3.96 (dd, J = 9.3, 3.3 Hz, 2H), 3.91 – 3.81 (m, 4H), 3.73 (dd, J = 11.3, 5.8 Hz, 2H), 3.63 (t, J = 9.4 Hz, 2H), 2.64 (s, 3H), 2.46 (t, J = 6.0 Hz, 2H). XH NMR (400 MHz, DMSO-D6) delta 8.17 (d, J = 8.1 Hz, 2H), 8.08 (t, J = 5.6 Hz, 1H), 7.64 (s, 2H), 7.30 – 7.25 (m, 2H), 5.06 (s, 2H), 4.76 (d, J = 2.0 Hz, 2H), 3.83 (s, 2H), 3.77 – 3.65 (m, 4H), 3.63 – 3.55 (m, 2H), 3.46 (dd, J = 11.7, 6.2 Hz, 2H), 3.39 (t, J = 9.3 Hz, 2H), 3.16 (dd, J = 12.1, 6.2 Hz, 2H), 2.40 – 2.16 (m, 10H), 2.11 (s, 3H). ESI-MS m/z calc. 722.3163, found 723.71 (M+l)+.

The synthetic route of 934-98-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; VERTEX PHARMACEUTICALS INCORPORATED; RAMTOHUL, Yeeman, K.; DAS, Sanjoy, Kumar; CADILHAC, Caroline; REDDY, Thumkunta, Jagadeeswar; VAILLANCOURT, Louis; GALLANT, Michel; LIU, Bingcan; DIETRICH, Evelyne; VALLEE, Frederic; MARTEL, Julien; POISSON, Carl; WO2014/100158; (2014); A1;,
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120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2-Methyl-4-pyrimidin-2-yl-piperazine- 1 -carboxylic acid tert-butyl ester 100 mg 2-chloro-pyrimidine was added to 175 mg 2-Methyl-piperazine-l -carboxylic acid tert- butyl ester and this mixture was stirred for 2 h at 120 C to give 240 mg of the desired compound. Rt: 1.31 min (method B), (M+H)+: 279, 120737-78-2

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; GRAUERT, Matthias; BISCHOFF, Daniel; DAHMANN, Georg; KUELZER, Raimund; RUDOLF, Klaus; WELLENZOHN, Bernd; WO2013/83741; (2013); A1;,
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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,132710-90-8

The 6- {4-[4-(3-piperazin- 1 -ylpropoxy)phenyl]piperazin- 1 -yl} -3-(trifluoromethyl)-7,8- dihydro[l,2,4]triazolo[4,3-b]pyridazine used as starting material was prepared as follows:-; Preparation of tert-butyl 4-[3-(4-{4-[3-(trifluoromethyl)[l,2,4]triazolo[4,3- b]pyridazin-6-yl]piperazin-l-yl}phenoxy)propyl]piperazine-l-carboxylate; DIAD (3.24 mL, 16.47 mmol) was added dropwise to 4-{4-[3- (trifluoromethyl)[ 1 ,2,4]triazolo[4,3-b]pyridazin-6-yl]piperazin- 1 -yl}phenol (obtained as described in Example 16, preparation of starting materials) (5 g, 13.72 mmol), tert-butyl 4- (3-hydroxypropyl)piperazine-l-carboxylate (CAS 132710-90-8, 5.03 g, 20.59 mmol) and triphenylphosphine (5.40 g, 20.59 mmol) in THF (50 mL) at 00C under nitrogen. The resulting solution was stirred at ambient temperature for 16 hours. The reaction mixture was evaporated to dryness and redissolved in DCM (100 mL), and washed sequentially with 2M NaOH (100 mL) and saturated brine (100 mL). The organic layer was dried over MgSO4, filtered and evaporated to afford crude product. The crude product was purified by flash silica chromatography, eluting with EtOAc. Pure fractions were evaporated to dryness to give tert-butyl 4-[3-(4-{4-[3-(trifluoromethyl)[l,2,4]t?azolo[4,3-b]pyridazin-6- yl]piperazin-l-yl}phenoxy)propyl]piperazine-l-carboxylate (3.66 g, 45%). IH NMR (399.9 MHz, CDC13) delta 1.46 (9H, s), 1.95 (2H, m), 2.40 (4H, m), 2.52 (2H, t), 3.21 (4H, m), 3.43 (4H, m), 3.78 (4H, m), 3.99 (2H, t), 6.87 (2H, d), 6.93 (2H, d), 7.11 (IH, d), 7.96 (IH, d); m/z = 591 [M+H]+.

As the paragraph descriping shows that 132710-90-8 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; BRADBURY, Robert, Hugh; CARR, Gregory, Richard; RABOW, Alfred, Arthur; RAO KORUPOJU, Srinivasa; TUMMA, Harikrishna; WO2010/92371; (2010); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.140447-78-5,1-(2-N-Boc-Aminoethyl)piperazine,as a common compound, the synthetic route is as follows.

In a sealed tube, 8-bromo-7-fluoro-2-(methyloxy)-1 ,5-naphthyridine (1.1 g, 4.3 mmol), 1 ,1 -dimethylethyl [2-(1-piperazinyl)ethyl]carbamate (1 g, 4.3 mmol), Pd2dba3 (271 mg, 0.262 mmol), rac-Binap (163 mg, 0.262 mmol), Cs2CO3 (2.98 mg, 9.2 mmol) and 18- C-6 (115 mg, 0.436 mmol) in dioxane (22 ml_) were combined and flushed with N2. After 15min, the tube was sealed and heated to 1000C while stirring rapidly. After 12h, the solution was filtered, concentrated and the residue purified via column chromatography (silica,.1% MeOH in DCM (1% NH4OH)) yielding the title compound (725 mg, 41%) as an orange oil: LCMS (ES) m/e 406 (M+H)+., 140447-78-5

The synthetic route of 140447-78-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXO GROUP LIMITED; WO2006/81289; (2006); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1235865-77-6,2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

A solution of 2 – ((lH-pyrrolo [2,3-b] pyridin-5-yl) oxy) -4- (4 – ((4′-chloro-5,5-dimethyl- 5,6-tetrahydro- [1,1′-biphenyl] -2-yl) methyl) piperazin-1-yl) benzoic acid (see Example 1, step 14) (60 mg, 0.105 mmol, 1.0 eq) (40 mg, 0.114 mmol, 1.09 eq) was added to DCM (10 mL) followed by EDCI (40 mg, 0.209 mmol, 1.99 eq) and 4 (4 mL), 2-nitro-4-sulfamoylphenyl trifluoromethanesulfonate (26mg, 0.213mmol, 2.03eq), room temperature reaction 3h, TLC point plate analysis, the basic reaction of acid raw materials, directly to the reaction liquid spin dry, column, PE / EA (v / v) = 1/1 Eluting with a pale yellow solid product 52 mg, yield 53.9%, 1235865-77-6

The synthetic route of 1235865-77-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Sunshine Lake Pharma Co.,Ltd.; Kou, Yuhui; Hu, Bolin; Jiang, Haigang; Ye, Jiuyong; Liu, Zhiqiang; Xie, Hongming; Zhang, Yingjun; (42 pag.)CN106565706; (2017); A;,
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