Month: November 2020

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

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

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

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

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

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.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

303-26-4, 1-((4-Chlorophenyl)(phenyl)methyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

D. Synthesis of Final Product To a solution of 1-[(4-chloro-phenyl)-phenyl-methyl]-piperazine (0.59 g, 2.08 mmol) in dry CH2Cl2 (40 ml) was added diphenylaminoacetic acid (0.472 g, 2.08 mmol) under nitrogen. To the reaction was added EDC (0.797 g, 4.16 mmol) and DMAP (cat) and the reaction mixture stirred under nitrogen at room temperature overnight. The reaction was then concentrated under reduced pressure. The residue dissolved in ethyl acetate: water (10:1) (150 ml). The organic was washed with water (30 ml, 2*) and 10% NaOH (30 ml) and dried over MgSO4 and evaporated to dryness. The resulting residue was purified by column chromatography using hexane:ethyl acetate (3:1) to give desired product in 76% yield.

303-26-4, The synthetic route of 303-26-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NeuroMed Technologies Inc.; US2005/227999; (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.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

5747-48-8, General procedure: To a solution of isocyanate (1.877mmol) in toluene (2.5mL) was added a solution of a monosubstituted piperazine (1.877mmol) in toluene (1.0mL). The reaction mixture was heated at 40-45C for 30 to 60min. The reaction mixture was then cooled down to room temperature (22-25C) and the resulting solids were filtered and washed with more toluene (2.0mL). The wet solids were then placed in 2.0mL of toluene, stirred at room temperature for about 30min, filtered and washed with toluene (1.0mL) to obtain the crude disubstituted piperazine derivative. Finally, all crude derivatives were purified by silica-gel column chromatography using a mixture of dichloromethane/methanol (9:1) to afford pure piperazines products.

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

Reference£º
Article; Patil, Mahadev; Noonikara Poyil, Anurag; Joshi, Shrinivas D.; Patil, Shivaputra A.; Patil, Siddappa A.; Bugarin, Alejandro; Bioorganic Chemistry; vol. 92; (2019);,
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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

2-Methylpiperazine (0. 5G), 2-AMINO-6-CHLORO-7H-PURINE (0.85g) and Hunigs base (LML) in isopropanol (3ML) and NMP (3ml) was heated at 50 C for 18h. The precipitate was filtered off to give the sub-title compound as a white solid (L. LG). MS (APCI+) 234 [M+H] +, 109-07-9

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; WO2004/74287; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics