Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.77279-24-4,tert-Butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 4-(2-hydroxy-ethyl)-piperazine-l-carboxylic acid tert-butyl ester (231 mg, 1.0 mmol) in CH2Cl2 (2 mL) at 0 0C was added dropwise SOCl2 (0.15 mL, 2.0 mmol). The mixture was allowed to warm up to ambient temperature and stirred for 14 h. Volatiles were removed in vacuo and the residue partitioned between CH2Cl2 (20 mL) and saturated NaHCO3 (10 mL). The CH2Cl2 phase was dried over Na2SO4 and concentrated in vacuo to afford 4-(2-chloro-ethyl)-piperazine-l-carboxylic acid t¡ãY-butyl ester as a white solid (130 mg, 52%): ESI MS m/z 249 [Ci 1H21ClN2O2 + H

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

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG; WO2006/107923; (2006); 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

30459-17-7, Methyl hydrogen azelate (479 mg, 2.3 mmol), BOP (1 .14 g, 2.6 mmol), anhydrous triethylamine (512 [it, 3.6 mmol) and anhydrous DCM (40 mL) were placed in an oven-dried three neck flask under a nitrogen atmosphere. The resulting solution was stirred at room temperature for 15 minutes. 1-(4- (Trifluoromethyl)phenyl)piperazine (600 mg, 2.6 mmol) was added and the reaction mixture stirred under nitrogen and monitored by TLC. After 16 hours, the DCM was removed under reduced pressure and the resulting oil was acidified using a 0.1 M HCI. The aqueous mixture was extracted with DCM (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 the solvent removed in vacuo. The residue was purified using flash chromatography (3:2, EtOAc et. Ether) to obtain the desired product as an off white solid in a 98% yield. H NMR (300 MHz, CDCI3) ? 7.41 (d, J = 8.7 Hz, 2H), 6.85 (d, J = 8.7 Hz, 2H), 3.73-3.69 (m, 2H), 3.58 (overlapping -OCH3 and piperazine -CH2 signal, m, 5H), 3.23-3.19 (m, 4H), 2.28 (t, J = 7.8 Hz, 2H), 2.21 (t, J = 7.8 Hz, 2H), 1.58-1.56 (m, 4H), 1.30-1.26 (m, 6H). 3C NMR (75 MHz, CDCI3) 174.2, 171 .7, 152.9, 126.4 (q, J = 3.75 Hz), 120.6 (q, J = 33 Hz), 1 19.2 (q, J = 271.5 Hz), 1 14.9, 51.4, 48.4, 48.1 , 45.1 , 41.1 , 34.0, 33.2, 29.2, 29.0, 28.9, 25.1 , 24.8. MS (+ESI) calcd for C2i H29 F3 N2 03 m/z: [M + H]+, 415.2203; found 415.219 [Diff(ppm) = -3.14].

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

Example II. Synthesis of quetiapine by reductive alkilation of 11-piperazindibenz[b,f][1,4]thioazepine with (2-hydroxyethoxy)acetaldehyde in the presence of magnesium borohydride. The mixture of 11-piperazindibenz[b,f][1,4]thioazepine (1 g, 0,0034 mol), sodium acetate (0,8 g, 0,01 mol), glacial acetic acid (4 cm3), (2-hydroxyethoksy)acetaldehyde (0,35g, 0,0034 mol) and water (50 cm3) is cooled to 0C. Next sodium borohydride was slowly (40 min) added (7 g, 0,13 mol) in temperature 0C. After this time the mixture was stirred for 1 h in temperature 10C and 10% aq NaOH was added (to pH about 8-9). The mixture was extracted with diethyl ether (3×30 cm3), organic faze was dried by sodium sulfate. The product (1.09g) was obtain with purity about 90% (HPLC), 5747-48-8

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

Reference£º
Patent; Celon Pharma Sp. z o.o.; EP1602650; (2005); 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.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 mixture of dehydro-aripiprazole (1.5 g, 3.4 mmol), potassium tert-butoxide (0.75 g, 6.7 mmol) and 2-methyltetrahydrofuran (30 mL) at 0 C. was added hexyl chloroformate (1.32 mL, 8.1 mmol). The reaction mixture was stirred for 2 h, allowed to self warm to room temperature and stirred for a further 4 h. The reaction mixture was then diluted with water and extracted with ethyl acetate. The organic phase was dried over MgSO4, filtered and evaporated. The residue was further purified on silica eluting with ethyl acetate/tetrahydrofuran and the major product containing fractions evaporated to give a yellow solid. This was triturated in heptane (30 mL) for 2.5 h, filtered and dried to give Compound 328 (1.55 g) as a white solid.1H-NMR (300 MHz, CDCl3) delta 8.15 (d, 1H), 7.71 (d, 1H), 7.32 (d, 1H), 7.21-7.12 (m, 3H), 7.09 (d, 1H), 6.97-6.91 (m, 1H), 4.29 (t, 1H), 4.13 (t, 1H), 3.12-3.01 (m, 4H), 2.73-2.55 (m, 4H), 2.50 (t, 2H), 1.95-1.85 (m, 2H), 1.82-1.70 (m, 4H), 1.50-1.28 (m, 6H), 0.94-0.86 (m, 3H). [M+H]+=574.2.

129722-25-4, As the paragraph descriping shows that 129722-25-4 is playing an increasingly important role.

Reference£º
Patent; Alkermes, Inc.; US2011/319422; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-82-4,70261-82-4, 4-(4-Methylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-((4-methylpiperazin-1-yl)methyl)phenylamine(4.7g) was added to a solution of Compound 2-5(5.28g) in n-butanol(130ml). The mixture was reacted at 90C for 4.0 hours, cooled to room temperature, filtered, washed and dried to obtain a red solid in a yield of 85.7%. MS m/z(ESI): 412[M+H]+.

70261-82-4 4-(4-Methylpiperazin-1-ylmethyl)phenylamine 3153996, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Si Chuan University; CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd.; YANG, Shengyong; WEI, Yuquan; EP2578584; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 mixture of 1-34 (10 g, 50 mmol), 1 , 4-dibromobenzene (29.4 g, 125 mmol), cesium carbonate (24.3 g, 75 mmol) and BINAP (1.5 g, 2.5 mmol) in 1,4-dioxane (250 mL) was degassed in a stream of argon for 15 minutes. To the mixture was added tris (dibenzylideneacetone) dipalladium(O) (0.900 g, 2.5 mmol), and the reaction mixture was again degassed for additional 15 minutes. After stirring at 90C for 18 hours, the. volatiles were removed by evaporation, and the obtained residue was diluted with water (250 mL) , followed by extraction with ethyl acetate (250 mL x 3) . The combined organic layers were washed with brine (50 mL) , dried over anhydrous Na2S04 and concentrated under reduced pressure. The obtained residue was purified by silica gel column chromatography (60-120 mesh) using 10% EtOAc in hexanes to give the desired product 1-35 as a white solid (5.5 g, 31%); LCMS : m/z 357.1 [M+l] , 359.1, 169447-70-5

As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference£º
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; KOUL, Summon; KURHADE, Suresh; BHOSALE, Sandeep; NAIK, Keshav; SALUNKHE, Videsh; MUNOT, Yogesh; BHUNIYA, Debnath; (284 pag.)WO2015/88045; (2015); 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.

To (S)-2-hydroxymethylpiperazine-1-carboxylic acid tert-butyl ester (950 mg) were added tetrahydrofuran (17 mL),3,5-dimethylpyridine-N-oxide (515 mg),N,N-diisopropylethylamine (2.8 mL) and bromotris(pyrrolidino)phosphonium hexafluorophosphate (2.67 g) and the mixture was stirred at room temperature for 5.5 hr. Water was added to the reaction mixture and the mixture was extracted with ethyl acetate. The solvent was evaporated and the obtained residue was purified by column chromatography (ethyl acetate:hexane)to give the title compound (640 mg). MS(ESI)m/z:322 (M+H)+

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; Mitsubishi Tanabe Pharma Corporation; ISHIBUCHI, Seigo; SARUTA, Kunio; HAMADA, Maiko; MATOBA, Nobuatsu; MATSUDAIRA, Tetsuji; SEKI, Maki; TARAO, Akiko; HONJO, Takashi; OGATA, Shingo; KAWATA, Atsushi; MOROKUMA, Kenji; FUJIE, Naoto; AOYAMA, Yukio; (251 pag.)EP3321256; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

150407-69-5, (S)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,150407-69-5

Step 2: 1 -Benzyl 4-fert-butyl 2-methyl (2,SV1.2.4-piperazinetricarboxylate (AA2); A solution of TMS-diazomethane (2.0 M in Et2O, 4.0 eq.) was added to a stirred 0.16 M solution of AAl in a toluene-MeOH mixture (2:1). The reaction mixture was stirred overnight at RT. Solvents were removed under reduced pressure. The residue was purified by column chromatography on silica gel, eluting with 20 to 100% EtO Ac/petroleum ether to give the title compound in 92 % yield. 97% ee by SFC. [CC]D20 -10.6 (c 1.00, CHCl3). 1H NMR (300 MHz, CDCl3, 300K) delta 7.37 (5H, m), 5.18 (2H, m), 4.79-4.57 (2H, m), 4.10-3.90 (2H, m), 3.75 (1.5H, s), 3.70 (1.5H, s), 3.34-3.30 (IH, m), 3.10 (IH, dd, J = 13.6, 4.4 Hz), 2.86 (IH, m), 1.45 (9H, s). MS (ES+) Ci9H26N2O6 requires 378, found: 401 (M+Na)+.

150407-69-5 (S)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid 1512536, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A.; BRANCA, Danila; FERRIGNO, Federica; HERNANDO, Jose, Ignacio, Martin; JONES, Philip; KINZEL, Olaf; MALANCONA, Savina; MURAGLIA, Ester; PALUMBI, Maria, Cecilia; PESCATORE, Giovanna; SCARPELLI, Rita; WO2010/23480; (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.142-64-3,Piperazine Dihydrochloride,as a common compound, the synthetic route is as follows.

EXAMPLE 26 In a 300-ml. three necked flask was placed 4.9 g. of sodium cyanide and 10 ml. of water to obtain a homogeneous solution. To the resuting solution was added 16.6 g. of 3,4-dimethoxybenzaldehyde dissolved in 40 ml. of methanol and then a solution of 9.7 g. of piperazine hexahydrate and 7.95 g. of piperazine dihydrochloride in 30 ml. of water. The reaction mixture, from which crystalline precipitate separated upon heating, was stirred for about 1 hour at 60C. After the mixture was cooled, crystal to separate was collected by filtration, washed with water and methanol, and dried. There was obtained 22.8 g. of crystal having a melting point of 216 -218.5C. Recrystallization from chloroform-methanol afforded N,N’-bis-(alpha-cyano-3,4-dimethoxybenzyl)piperazine as a crystalline product melting at 216 -218C., 142-64-3

As the paragraph descriping shows that 142-64-3 is playing an increasingly important role.

Reference£º
Patent; Fuji Chemical Industry Co., Ltd.; Nippon Chemiphar Co., Ltd.; US3962247; (1976); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

694499-26-8, General procedure: Step 3: General protocol for the preparation of 5-{3-(phenylcarbamoyl)-benzylamino}-lH- pyrrolo[2,3-b]pyridine-2-carboxylic acid methyl ester 5-amino-iH-pyrrolo[2,3-b]pyridine-2-carboxylic acid methyl ester (1 eq) and 3-formyl- benzamide compound (1.1 eq) were stirred in a mixture of MeOH/AcOH (10/1; 0.06M) for 2h. Then NaBH3CN (1.2eq) was slowly added and the mixture was stirred under argon at RT overnight. The reaction was quenched by addition of saturated NaHC03 solution until neutrality. MeOH and acetic acid were evaporated. The crude was filtered and washed with water and Et20 before being purified on reverse phase (H20 l%TFA/MeCN 1%TFA 100/0, 0/100). MeCN was evaporated. The product was suspended in H20 and basified with saturated NaHC03 solution until pH = 8-9. The aqueous layer was extracted three times with AcOEt. The organic layer was dried over Na2S04, filtered and concentrated to give the expected product.

As the paragraph descriping shows that 694499-26-8 is playing an increasingly important role.

Reference£º
Patent; ORIBASE PHARMA; CHEVE, Gwenael; DAYDE-CAZALS, Benedicte; FAUVEL, Benedicte; BORIES, Cedric; YASRI, Abdelaziz; WO2014/102378; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics