Heterocyclic Building Blocks-piperazine

109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A 100 mL 3-necked flask was equipped with a magnetic stirrer bar, nitrogen in- and outlet and septum. The setup was thoroughly dried using a heat gun and allowed to cool to room temperature under a nitrogen flow. Then, 4-nitrobenzoyl chloride (4.64 g, 25.0 mmol) was dissolved in dry dichloromethane (50 mL) and the solution was 10 minutes in an ice-water bath. N-methylpiperazine (2.58 g, 25.8 mmol, 1.03 eq) was added drop wise over a 10 minute time interval while stirring vigorously. The resulting suspension was stirred for 1 hour at 0 C., after which triethylamine (5.01 g, 50.0 mmol, 2.0 eq) was added and stirrring was continued at r.t. for 1 h. The reaction mixture was transferred into a separatory funnel and washed with demineralized water (3×50 mL). The organic layer was dried over Na2SO4, filtered over a paper filter and all volatiles were removed under reduced pressure using a rotary evaporator to give the desired product as a pale orange solid (5.77 g 23.1 mmol, 92%)., 109-01-3

The synthetic route of 109-01-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TEIJIN ARAMID B.V.; VAN DEN HEUVEL, Christiaan J.M.; VELD, Martijn Arnoldus Johannes; QUAIJTAAL, Joannes H.M.; VERHOEF, Rene P.; DE JONG, Jorrit; NIJENHUIS, Wido; (12 pag.)US2018/223077; (2018); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.215309-01-6,3-(4-Methylpiperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

General procedure: A solution of 2-(2-methyl-1H-indol-1-yl)ethanamine (4a) (65 mg, 0.373 mmol) and 4-(piperidin-1-yl)benzoic acid (5) (76 mg, 1 eq.), and dimethylaminopyridine (catalytic, ?5 mg) in dichloromethane (6 mL) was added 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide.hydrochloride (EDCI) (92 mg, 1.3 eq.) at room temperature. The resulting reaction mixture was stirred for 6h. At the conclusion of the reaction (TLC), water (15 mL) was added to quench the reaction. The product was extracted with ethyl acetate (20mL×3). Organics were washed with dilute HCl (10 mL), saturated NaHCO3 solution (10 mL), water (10 mL) and brine solution (10 mL) and dried over Na2SO4 and concentrated. The resulting crude product was subjected to silica gel chromatography eluting with 0-40% ethyl acetate in hexane to furnish 7k (TG7-152) (100mg, 74% yield). 1H NMR (CDCl3): delta 7.52 (d, J=5.6Hz, 1H), 7.49 (d, J=8.8Hz, 2H), 7.30 (d, J=8Hz, 1H), 7.07 (m, 2H), 6.80 (d, J=8.2Hz, 2H), 6.23 (s, 1H), 5.98 (t, J=5.4Hz, 1H), 4.33 (t, J=6Hz, 2H), 3.76 (q, J=6Hz, 2H), 3.25 (t, J=4.8Hz, 4H), 2.37 (s, 3H), 1.6 (m, 6H). LCMS (ESI): >97% purity at lambda 254, MS; m/z, 362 [M+H]+. Anal. Calcd. for C23H27N3O: C, 76.42; H, 7.53; N, 11.62; found; C, 76.48; H, 7.55; N, 11.59.

215309-01-6, As the paragraph descriping shows that 215309-01-6 is playing an increasingly important role.

Reference：
Article; Ganesh, Thota; Jiang, Jianxiong; Dingledine, Ray; European Journal of Medicinal Chemistry; vol. 82; (2014); p. 521 – 535;,
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55121-99-8,55121-99-8, (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 257Preparation of 1-{4-[3-(1-methylethyl)-7-morpholin-4-yl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl]phenyl}-3-{4-[(4-methylpiperazin-1-yl)carbonyl]phenyl}urea. To a stirred solution of triphosgene (35 mg, 0.12 mmol) in CH2Cl2 (4 mL) was added 4-(3-isopropyl-7-morpholino-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl)aniline (50 mg, 0.14 mmol) at 25 C. The reaction mixture was stirred for 15 min and NEt3 (20 muL, 0.14 mmol) was added. Stirring was continued for 1 h and (4-aminophenyl)(4-methylpiperazin-1-yl)methanone (103 mg, 0.43 mmol) and NEt3 (200 muL, 1.4 mmol) were added and the reaction mixture was stirred for additional 1 hr. The solvents were removed in a N2 stream and the crude mixture was purified by semi-prep-HPLC (NH3-method) to give 1-{4-[3-(1-methylethyl)-7-morpholin-4-yl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl]phenyl}-3-{4-[(4-methylpiperazin-1-yl)carbonyl]phenyl}urea (43 mg, 39% yield), MS (ESI) m/z 585.4.

55121-99-8 (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone 231408, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Wyeth; US2009/181963; (2009); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5521-38-0,2-(4-(4-Nitrophenyl)piperazin-1-yl)ethanol,as a common compound, the synthetic route is as follows.

REFERENCE EXAMPLE 19b 2-[4-(4-amino-phenyl)-piperazin-1-yl]-ethanol. 2-[4-(4-amino-phenyl)-piperazin-1-yl]-ethanol is prepared by catalytic hydrogenation of 2[4-(4-nitrophenyl)piperazine-1-yl]-ethanol (prepared as in Reference Example 19a) as described in Reference Example 13b, 5521-38-0

The synthetic route of 5521-38-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Chapdelaine, Marc; Davenport, Timothy; Haeberlein, Markus; Horchler, Carey; McCauley, John; Pierson, Edward; Sohn, Daniel; US2004/87575; (2004); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.373608-48-1,tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A solution of intermediate compound E1 (1 .1 g), triethylamine (0.674 ml_) and 2-oxo-2H-chromen-4-yl trifluoromethanesulfonate (1 .2 g), prepared as described in step 5 of the preparation of compound 51 , in acetonitrile (20 ml_) was heated to 705C for 1 hour. The reaction mixture was concentrated under reduced pressure and the residue was partitioned between dichloromethane and a brine/sodium bicarbonate mixture (1 :1 ). The mixture was filtered through a hydrophobic frit (Phase Separator) washing with dichloromethane. The organic phase was evaporated under reduced pressure and the residue was chromatographed on silica gel (SNAP50) eluting with a gradient of EtOAc in cyclohexane to give 700 mg of tert-butyl 4-{3-[(2-oxo-2H-chromen- 4-yl)amino]propyl}piperazine-1 -carboxylate intermediate compound E2 (700 mg, Y=44%). LC-MS (M-H+) = 388.3, 373608-48-1

As the paragraph descriping shows that 373608-48-1 is playing an increasingly important role.

Reference：
Patent; AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.; OMBRATO, Rosella; GAROFALO, Barbara; MANGANO, Giorgina; CAPEZZONE DE JOANNON, Alessandra; CORSO, Gaia; CAVARISCHIA, Claudia; FURLOTTI, Guido; IACOANGELI, Tommaso; (161 pag.)WO2016/96686; (2016); A1;,
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109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 2,3-dichloropyrazine (2.80 g, 18.8 mmol), racemic 2- methylpiperazine (1.88 g, 18.8 mmol) and K2CO3 (3.90 g, 28.2 mmol) in acetonitrile (25 mL) was heated at 65 C for 15 h with stirring. The reaction mixture was filtered and concentrated. The crude product was purified by flash chromatography on silica gel using CHCl3/MeOH (15: 1) as eluent to give 3.2 g (79%) of the title compound. MS m/z 213 (M+H) +., 109-07-9

As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference：
Patent; BIOVITRUM AB; WO2004/9586; (2004); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

a) 1,4-Bis(tert-butoxycarbonyl)-2-piperazinecarboxylic acid To a solution of piperazine-2-carboxylic acid dihydrochloride (5 g, 24.6 mmol) in 2M sodium hydroxide (40 mL) and ethanol (40 mL) was added di-tert-butyl dicarbonate (11.82 g, 54.1 mmol) and the reaction mixture stirred for 3 days. The organic solvent was removed in vacuo, the aqueous phase basified with 2M sodium hydroxide and extracted with diethyl ether to remove excess di-tert-butyl dicarbonate. The aqueous layer was adjusted to pH 3-4 and extracted with ethyl acetate. The combined organic extracts were dried (MgSO4), filtered and evaporated to yield 1,4-bis(tert-butoxycarbonyl)-2-piperazinecarboxylic acid as a white solid., 3022-15-9

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

Reference：
Patent; Agejas-Chicharro, Javier; Belen Bueno Melendo, Ana; Camp, Nicholas Paul; Gilmore, Jeremy; Jimenez-Aguado, Alma Maria; Lamas-Peteira, Carlos; Marcos-Llorente, Alicia; Mazanetz, Michael Philip; Montero Salgado, Carlos; Timms, Graham Henry; Williams, Andrew Caerwyn; US2004/122001; (2004); A1;,
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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.,118753-66-5

The compound 4-chloro-5-nitro-1-p-toluenesulfonyl-1H-pyrrolo [2,3-b] pyridine (1.18 g, 5.87 mmol), N, N-diisopropylethylamine (7.10 g, 55mmol)And 1-Boc-4-aminopiperazine (1.18 g, 5.87 mmol) were added to 60 mL of isopropanol (suspension), and the temperature was raised to 100 C. with stirring under nitrogen for 16 hours.After the reaction was completed, the mixture was cooled to room temperature, ether was added, and a large amount of a yellow solid precipitated.Filtration, collection of solids and drying1-Boc-4-((5-nitro-1-p-toluenesulfonyl-1H-pyrrolo [2,3-b] pyridin-4-yl) amino) piperazine (2.16 g, yield 76%) .

As the paragraph descriping shows that 118753-66-5 is playing an increasingly important role.

Reference：
Patent; Weimou Bio-technology (Shanghai) Co., Ltd.; Shen Wang; Liu Pengfei; Bai Rujun; Liu Yufei; Luo Qiuping; Ke Pingbo; Gong Yanchuan; (71 pag.)CN110483514; (2019); A;,
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112984-60-8, 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

28 grams of ulifloxacin dissolved at room temperatureIn a 14 ml volume ratio of 5:1 acetic acid in acetonitrile,Dissolve and filter at 10CThen add 16ml of 10M hydrochloric acid to the filtrate.And stirred at 10 C for 4 hours to complete the reaction.After filtration, the precipitate was collected and washed with acetonitrile and dried under vacuum at 20C.The collected crystals were dissolved in methanol,After heating and stirring, cool in an ice bath and stir to crystallize.Precipitated crystals were collected and vacuum dried at 20C.That is, ulifloxacin hydrochloride crystal A is obtained.

112984-60-8, As the paragraph descriping shows that 112984-60-8 is playing an increasingly important role.

Reference：
Patent; Zhaoke Pharmaceutical (Hefei) Co., Ltd.; Li Xiaoyi; Dai Xiangrong; Zhou Guanqun; (18 pag.)CN107501298; (2017); A;,
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169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(a) Step 1 The 7-(bromomethyl)-6-methoxybenzofuran-3(2H)-one (0.514 g, 2.00 mmol) described in [WO2011/136319] and potassium carbonate (0.276 g, 2.00 mmol) were added to 8 mL of methylene chloride and stirred at room temperature. Two milliliters of a methylene chloride solution of tert-butyl (S)-2-methylpiperazine-1-carboxylate (0.401 g, 2.00 mmol) was added dropwise, and stirring was continued for 24 hours at room temperature. The reaction solution was filtered, and the residue obtained by concentrating the filtrate was purified by silica gel chromatography (ethyl acetate/hexane) to obtain tert-butyl (S)-4-[(6-methoxy-3-oxo-2,3-dihydrobenzofuran-7-yl)methyl]-2-methylpiperazine-1-carboxylate (0.531 g, 70%). 1H NMR (300 MHz, CDCl3) delta 1.12 (d, J=6.6 Hz, 3H), 1.36 (s, 9H), 1.98 (dt, J=0.6, 11.7 Hz, 1H), 2.17 (dd, J=4.2, 10.8 Hz, 1H), 2.57 (d, J=10.8 Hz, 1H), 2.72 (d, J=10.8 Hz, 1H), 2.97 (dt, J=3.9, 12.3 Hz, 1H), 3.60 (d, J=2.4 Hz, 2H), 3.69 (d, J=12.3 Hz, 1H), 3.85 (s, 3H), 4.09-4.14 (m, 1H), 4.55 (s, 2H), 6.62 (d, J=8.7 Hz, 1H), 7.54 (d, J=8.7 Hz, 1H).

169447-70-5, The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; THE UNIVERSITY OF TOKYO; NAGANO, Tetsuo; NAKANO, Hirofumi; HASEGAWA, Tsukasa; SAITO, Nae; KOJIMA, Hirotatsu; OKABE, Takayoshi; MUKAIDA, Naofumi; (42 pag.)US2017/145005; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics