Month: October 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1228780-72-0,1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine,as a common compound, the synthetic route is as follows.

1228780-72-0, To a solution of 1 – ((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro- [1,1′-biphenyl] -2-yl)Methyl) piperazine (1.62 g, 5.08 mmol, 1.12 eq)Compound 7 (1.30 g, 4.54 mmol, 1.0 eq)And dipotassium hydrogen phosphate(2.0 g, 13.0 mmol, 2.8 eq) and reacted at 140 C overnight under nitrogen. The reaction solution was poured into 100 mL of water and EA (40 mL x 3) was extracted. The organic phase was dried over anhydrous sodium sulfate, dried over the column, and the eluent was dried with PE / EA (v / v) = 3/1 The yellow oil was 1.4 g, yield 51.0%.

The synthetic route of 1228780-72-0 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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,109-07-9

Reference Example 10 Benzyl 3-methylpiperazine-1-carboxylate A 4 g portion of 2-methylpiperazine was dissolved in 40 ml of dichloromethane, and 1.71 g of benzyl chloroformate was added dropwise thereto at -78C. After 1 hour of stirring, the mixture was washed by adding water and dried and then the solvent was evaporated to obtain 2.0 g of the title compound.

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

Reference£º
Patent; YAMANOUCHI PHARMACEUTICAL CO. LTD.; EP1122242; (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.438049-35-5,N-Boc-3-Ethylpiperazine,as a common compound, the synthetic route is as follows.

(RS) 1-Chlorocarbonyl-2-ethyl-4-tert-butoxycarbonylpiperazine a solution of (RS)4-tert-butoxycarbonyl-2-ethylpiperazine (3.95 g) and pyridine (1.64 ml) in DCM (35 ml) was added dropwise to a stirred solution of triphosgene (2.1 g) in DCM (100 ml) at 0 C. under Ar. The mixture was warmed to room temperature, stirred for 30 min then washed with water (100 ml) and brine (100 ml). The organic solution was dried (sodium sulfate) and concentrated in vacuo. The residue was dissolved in isohexane, filtered and concentrated in vacuo to give the product as a clear oil (3.73 g) which was used without further purification; deltaH (400 MHz, CDCl3) 4.39-3.80 (4H, m), 3.39-2.69 (3H, m), 1.66 (2H, m), 1.47 (9H, s), 0.96 (2.7H, d, J 7 Hz) and 0.89 (0.3H, d, J 7 Hz); GC (150 C. -10 min-320 C.) 83%, 8.72 min. (+/-)4-Difluoromethoxybenzyl-2-ethyl-4-tert-butoxycarbonylpiperazine-1-carboxylate:

438049-35-5, The synthetic route of 438049-35-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Adams, David Reginald; Bentley, Jonathan Mark; Davidson, James Edward Paul; Dawson, Claire Elizabeth; George, Ashley Roger; Mansell, Howard Langham; Mattei, Patrizio; Mizrahi, Jacques; Nettekoven, Matthias Heinrich; Pratt, Robert Mark; Roever, Stephan; Roffey, Jonathan Richard Anthony; Specklin, Jean-Luc; Stalder, Henri; Wilkinson, Kerry; US2002/143020; (2002); 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.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Step 1 3-(R)-Methyl-piperazine-1-carboxylic acid tert-butyl ester Triethylamine (3 g, 4.2 mL, 30 mmol) was added to a solution of (R)-2-methyl piperazine (2 g, 20 mmol) in dichloromethane (40 mL) followed by di-tert-butyl-dicarbonate (4.8 g, 22 mmol). The reaction mixture was stirred at room temperature for 20 h. The mixture was diluted with dichloromethane and washed with saturated aqueous sodium bicarbonate and brine and dried over sodium sulfate. The crude product was purified using a short plug of silica gel using hexane/ethyl acetate (1:1). 1H-NMR (CDCl3) delta: 1.05 (3H, d), 1.45 (9H, s), 2.11 (1H, s), 2.37-2.44 (1H, m), 2.66-2.79 (3H, m), 2.93-2.96 (1H, m), 3.93 (2H, br s). ESI-MS m/z: 201 (M+1)., 75336-86-6

As the paragraph descriping shows that 75336-86-6 is playing an increasingly important role.

Reference£º
Patent; Millennium Pharmaceuticals, Inc.; Kyowa Hakko Kirin Co., Ltd.; LULY, Jay R.; NAKASATO, Yoshisuke; OHSHIMA, Etsuo; HARRIMAN, Geraldine C.B.; CARSON, Kenneth G.; GHOSH, Shomir; ELDER, Amy M.; MATTIA, Karen M.; (190 pag.)US2016/31908; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

216144-45-5, 4-(4-Methylpiperazin-1-yl)benzylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The product (O from step 1 (190.00 mg, 369.21 muiotaetaomicronIota, 1.5 eq.) was taken in a flask along with DMF as a solvent. (4-(4-methylpiperazin-l-yl)phenyl)methanamine (50.53 mg, 246.14 muiotatauiotaomicronIota, 1 eq.), HOBT (66.52 mg, 492.28 muiotaetaomicronIota, 2 eq.), and DIC (66.70 muIota_, 430.75 muiotatauiotaomicronIota, 1.75 eq.) were added respectively at room temperature and stirred under N2. After 5 hours, the reaction was finished. The solution was quenched with water and then extracted with ethyl acetate. The organic layer was combined and dried with anhydrous MgS04 and concentrated in vacuo. The crude solid was purified through column chromatography using silica gel and dichloromethane: methanol (upto 3%) as an eluent. The product, 17, was a yellow solid with 80% yield. (0277) FT-IR (Neat) : v (cm”1) = 2930, 2849, 1736, 1698, 1693, 1655, 1650, 1632, 1603, 1561, 1537, 1503, 1440, 1380, 1349, 1327, 1239, 1177; 1H-NMR (400 MHz, CDCI3) : delta ppm 7.76 -7.83 (m, 2H), 7.58 – 7.61 (m, 1H), 7.21 – 7.31 (m, 4H), 6.95 – 7.01 (m, 2H), 6.91 (d, J = 8.56 Hz, 2H), 6.71 – 6.77 (m, 2H), 6.32 (br. s., NH), 4.50 (d, J = 5.54 Hz, 2H), 3.90 (s, 3H), 3.17 – 3.26 (m, 8H), 2.98 (s, 3H), 2.56 – 2.62 (m, 4H), 2.34 – 2.38 (m, 3H), 1.58 – 1.73 (m, 6H); 13C-NMR (100 MHz, CDCI3) : delta 166.25, 160.35, 153.25, 152.58 (2C), 150.88, 145.07, 136.15, 131.63, 131.11, 130.06 (2C), 129.31, 129.15, 128.26, 127.36, 125.91, 124.15, 119.52 (2C), 116.16 (2C), 114.38 (2C), 54.94 (2C), 52.12 (2C), 49.13, 48.86, 46.02, 43.67, 37.47, 31.72, 25.46 (2C), 24.25; HRMS-ESI (m/z) : calcd. for C37H43N505S2 = 701.2706, found = 701.2772., 216144-45-5

The synthetic route of 216144-45-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; KING’S COLLEGE LONDON; THURSTON, David Edwin; KHONDAKER, Mirazur Rahman; JAMSHIDI, Shirin; NAHAR, Kazi Sharmin; (77 pag.)WO2019/30538; (2019); 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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

In a sealed tube, 2- (2, 8-dimethylimidazo [1 ,2-b]pyridazin-6-yl)-7-fluoro-pyrido [1,2- a]pyrimidin-4-one (Intermediate 2; 50 mg, 0.162 mmol), and cis-2,6-dimethylpiperazine (74 mg, 0.647 mmol, 4.0 eq.) were stirred in DMSO (1.5 mL) at 110C overnight. The solvent wasremoved under high vacuum. The residue was taken up in CH2C12 and washed with an aqueous saturated solution of NaHCO3. The organic layer was separated and dried over Na2504 and concentrated in vacuo. The crude was purified by column chromatography (5i02, CH2C12/MeOH=95/5 to 90/10) to afford the title product (32 mg, 49%) as a light yellow solid. MS m/z 404.4 [M+Hi.

21655-48-1, The synthetic route of 21655-48-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; ALSENZ, Jochem; GRASSMANN, Olaf; KUEHL, Peter; METZGER, Friedrich; MCCARTHY, Kathleen Dorothy; MORAWSKI VIANNA, Eduardo Paulo; WOODHOUSE, Marvin Lloyd; (130 pag.)WO2017/80967; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

373608-48-1, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 1662-[5-Methyl-2-(3-piperazin-1-ylpropylamino)-pyrimidin-4-yl]-benzo[b]thiophene-6-carboxylic acid methylamide tri-hydrochloride; A mixture of 2-(2-chloro-5-methylpyrimidin-4-yl)-benzo[b]thiophene-6-carboxylic acid methylamide (263 mg, 0.830 mmol), 4-(3-aminopropyl)-piperazine-1-carboxylic acid tert-butyl ester (358 mg, 1.47 mmol) and diisopropylethylamine (0.44 mL) in 1,4-dioxane (10 mL) is heated at 95 C. for 20 hours. The solvent is removed after cooling and the residue is subjected to chromatography on silica gel, eluting with 2.0 M NH3/MeOH in dichloromethane 0-10%, to give 4-{3-[5-methyl-4-(6-methylcarbamoyl-benzo[b]thiophen-2-yl)-pyrimidin-2-ylamino]-propyl}-piperazine-1-carboxylic acid tert-butyl ester (191 mg, 44% yield). The intermediate is dissolved in THF (8 mL) and 5 N hydrochloric acid (5 mL) is added. The solution is heated at 70 C. for 4.5 hours and then cooled before evaporating the solvent. Methanol is added to the residue and the mixture is sonicated for 30 minutes. The solid is filtered and washed with diethyl ether, then dried in a vacuum oven at 50 C. for 18 hours to give the title compound (129 mg, 66% yield). ES+(m/z) 425 [M(free base)+H].

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

Reference£º
Patent; Dahnke, Karl Robert; Lin, Ho-Shen; Richett, Michael Enrico; Shih, Chuan; Wang, Q May; Zhang, Bo; US2008/306082; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

196811-66-2, tert-Butyl 4-carbamothioylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of tert-butyl 4-carbamothioylpiperazine-1-carboxylate (synthesized according to Example 5, Step 1, 3.0 g, 12 mmol) in dioxane (10 mL), TEA (2.6 mL, 16 mmol) and 3-bromo-ethyl pyruvate (2.1 mL, 16 mmol) were added at rt and the mixture was stirred at 90 C for 16 h. The completion of the reaction was monitored by TLC. The reaction mixture was quenched with water and extracted with EtOAc. The organiclayer was dried over anhydrous Na2504, concentrated under vacuum and the resulting crude product was taken as such for next step. Yield: 95% (4 g, black solid)., 196811-66-2

The synthetic route of 196811-66-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASCENEURON S. A.; QUATTROPANI, Anna; KULKARNI, Santosh, S.; GIRI, Awadut Gajendra; TORONTO, Dawn, V.; CROWE, David, Malcolm; (150 pag.)WO2017/144637; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

170911-92-9, tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

tert -Butyl 4-(4-Phenoxycarbonylaminophenyl)piperazine-1-carboxylate (XIX; X=H): To a solution of tert-butyl 4-(4-aminophenyl)piperazine-1-carboxylate (50 g, 0.18 mol) and triethylamine (39 ml, 0.27 mol) in dichloromethane (400 ml) was added dropwise a solution of phenyl chloroformate (36.65 g, 0.23 mol) in dichloromethane (100 ml) at 0 oC. The resulting reaction mixture was stirred for 2 h at 0 C and additional 3 h at room temperature. Then diluted with chloroform (100 ml), washed with water, brine and dried over sodium sulphate. The solvent was removed under reduced pressure, the crude product was purified on a column of silica gel (hexane/EtOAc, 1:1) to give the tiltle compound as colorless solid (60 g, 84%). m.p.: 158-160 C. 1H NMR (CDCl3) delta: 1.48 (s, 9H, 3XCH3), 3.0-3.2 (m, 4H, 2XCH2), 3.6 (m, 4H, 2XCH2), 6.8 (brs, 1H, NH), 6.92 (d, 2H, Ar-H), 7.1-7.5 (complex, 7H, Ar-H).

170911-92-9, 170911-92-9 tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate 11011301, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Naeja Pharmaceutical Inc.; TAIHO PHARMACEUTICAL CO., LTD.; EP889881; (2003); B1;,
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.278788-66-2,(R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of (R)-tert-butyl 3-(hydroxymethyl)piperazine-1-carboxylate (231 mg, 1.07mmol), 2-(4-(bromomethyl)phenyl)-1 ,1 ,1 ,3,3,3-hexafluoropropan-2-ol (400mg, 1.19mmol) and sodium iodide (18mg, 0.12mmol) in acetonitrile (1 OmL) was added potassium carbonate (655mg, 4.75mmol). The reaction mixture was stirred at room temperature for 3 days, before being diluted with dichloromethane (1 OmL), filtered through cotton wool and concentrated under reduced pressure. The residue was purified by flash column chromatography (eluting with dichloromethane to 10% methanol in dichloromethane) to afford the intermediate (R)-tert-butyl 4-(4-(1 ,1 ,1 ,3,3,3-hexafluoro-2- hydroxypropan-2-yl)benzyl)-3-(hydroxymethyl)piperazine-1-carboxylate (250mg, 0.53mmol). To a stirred solution of (R)-tert-butyl 4-(4-(1 ,1 ,1 ,3,3,3-hexafluoro-2- hydroxypropan-2-yl)benzyl)-3-(hydroxymethyl)piperazine-1-carboxylate (220mg, 0.466mmol) in dichloromethane (3mL), was added trifluoroacetic acid (3mL, 38.3mmol). The reaction mixture was stirred at room temperature for 5 hours before being purified directly by SCX chromatography, eluting with 2N ammonia in methanol solution to afford the title compound (165mg). MS (ESI) m/z 373.3 [M+H]+, 278788-66-2

278788-66-2 (R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820286, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; N.V. ORGANON; WO2009/138438; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics