Month: January 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.196811-66-2,tert-Butyl 4-carbamothioylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step e) 4-[2-(4-tert-Butoxycarbonylpiperazin-1-yl)-5-methylthiazol-4-yl]benzoic acid methyl ester All of the alpha-bromoketone above and 4-thionocarbonylpiperazine-1-carboxylic acid tert-butyl ester (J. Med. Chem., 1998, 5037-5054, 917 mg, 3.73 mmol) were refluxed in 36 mL THF at 70 C. for 2 h, under N2. The precipitate was filtered and the filtrate concentrated in vacuo to give a yellow solid. Flash column chromatography (silica, 5/1 petroleum ether-EtOAc) gave 624 mg of light yellow solids. Chromatography of the precipitate (silica, 2/1 petroleum ether-EtOAc) gave a further 32 mg of compound. Total yield is 44%. 1H NMR (CDCl3) delta ppm: 1.46 (s, 9H), 2.43 (s, 3H), 3.42, (m, 4H), 3.54 (m, 4H), 3.90 (s, 3H), 7.68 and 8.04 (ABq, 4H).

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; Nilsson, Magnus; Oden, Lourdes; Kahnberg, Pia; Grabowska, Urszula; US2009/23748; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,59702-07-7

EXAMPLE 160 N-(4-fluorobenzyl)-8-hydroxy-5-(4-methyl-3-oxopiperazin-1-yl)-1,6-naphthyridine-7-carboxamide A solution of 5-bromo-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide (0.20 g, 0.53 mmol), 1-methylpiperazin-2-one (0.21 g, 1.86 mmol) and diisopropylethylamine (0.19 mL, 1.06 mmol) in DMPU (2.0 mL) were heated at 135C for 26 hr. Diisopropylethylamine (0.19 mL, 1.06 mmol) was added and the reaction heated at 135C for a further 24 hr. The reaction was cooled to room temperature, neutralized by the addition of TFA and purified by reverse phase HPLC. (Vydak C18, Gradient elution with Water: Acetonitrile 95:5 to 5:95 with 0.1percent TFA at 30 mL/min over 15 mins). Lyophilization of the pure fractions afforded the title compound as an off white solid. 1H NMR (CDCl3, 400 MHz) delta 12.95 (1H, s), 9.18 (1H, dd, J=1.6 and 4.4 Hz), 8.43 (1H, dd, J=1.7 and 8.4 Hz), 8.21 (1H, m), 7.63(1H, dd, J=4.3 and 8.4 Hz), 7.40(2H, m), 7.05(2H, t, J=8.7 Hz), 4.65 (2H, d, J=6.4 Hz), 4.01 (2H, s), 3.61 (2H, t, J=5.7 Hz), 3.34(2H, t, J=5.7 Hz), 2.95 (3H, s) ppm. FAB MS calcd for C21H20FN5O3 410 (MH+), found 410.

59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Anthony, Neville J.; Gomez, Robert P.; Young, Steven D.; Egbertson, Melissa; Wai, John S.; Zhuang, Linghang; Embrey, Mark; Tran, LeKhanh; Melamed, Jeffrey Y.; Langford, H. Marie; Guare, James P.; Fisher, Thorsten E.; Jolly, Samson M.; Kuo, Michelle S.; Perlow, Debra S.; Bennett, Jennifer J.; Funk, Timothy W.; US2003/55071; (2003); 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.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.

Preparation of 2,4-dihydroxy-5-isopropyl-N-(4-((4-methylpiperazin-l- yl)methyl)phenyl)- benzothioamide (K): [00447] To a stirred solution of 5.0g (21.89mmols) of 2,4-dihydroxy-5- isopropylbenzodithioic acid (J) in 30mL of anhydrous DMF was added 5.9g (70.07mmols) of NaHC03 followed by 2.55g (21.89mmols) of sodium 2-chloroacetate and the mixture was heated at 80 C for lh. 4-((4-methylpiperazin-l-yl)methyl)aniline (4.3g, 20.80mmols) was then added portion wise and the mixture was further heated at 80 C for 2h. The reaction mixture was then cooled, lOOmL of ice-water was added and the pH of the mixture was brought down to approx. 7 using saturated NH4CI solution. The resultant precipitate was then filtered, dried and redissolved in 9:1 ethyl acetate methanol, dried over Na2S04 and concentrated to afford compound K (7.8g) as yellow solid which was carried to next step without purification., 70261-82-4

As the paragraph descriping shows that 70261-82-4 is playing an increasingly important role.

Reference£º
Patent; SYNTA PHARMACEUTICALS CORP.; CHIMMANAMADA, Dinesh, U.; YING, Weiwen; WO2013/152206; (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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.,70261-81-3

A mixture of 1-methyl-4-(4-nitro-benzyl)-piperazine (3.09 g, 13.1 mmol), zinc dust (4.29 g, 65.6 mmol) and ammonium chloride (2.81 g, 52.5 mmol) in methanol (100 mL) was refluxed 1h, cooled, filtered through Celite (washing with methanol) and evaporated to provide 4-(4-methyl-piperazin-1-ylmethyl)-phenylamine (2.67 g, 99% yield) as a pale yellow, waxy solid. 1H-NMR (DMSO-d6, 500 MHz) 6.89 (d, 2H), 6.49 (d, 2H), 4.89 (s, 2H), 3.24 (s, 2H), 2.3 (br m, 8H) ppm; MS (FIA) 206.2 (M+H); HPLC (Method A) co-elutes with solvent front.

The synthetic route of 70261-81-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; VERTEX PHARMACEUTICALS INCORPORATED; WO2004/46120; (2004); A2;,
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.78551-60-7,tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

EXAMPLE 42 4-t-butoxycarbonyl-3-[2-(methylthio)ethyl)-1-(phenylmethyl)piperazinone (XVI) Following the general procedure of Example 47 and making non-critical variations, but substituting 4-t-butoxycarbonyl-1-(phenylmethyl)piperazinone (XV, Example 41) for 1-methyl-4-(phenylmethyl)piperazinone and 1-chloro-2-(methylthio)ethane [Chem. Ber., 84, 911 (1951)] for 1-bromo-2-methylpropane, there is obtained the title compound., 78551-60-7

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

Reference£º
Patent; The Upjohn Company; US4251438; (1981); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 14: Synthesis of XZ-14523 Preparation of tert-butyl 4-((4-(N-(2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4- chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)benzoyl)sulfamoyl)-2- nitrophenylamino)methyl)piperidine-1-carboxylate (52) A mixture of compound 50 (571 mg), 51 (415 mg), DMAP (244 mg), EDCI (250 mg), and TEA (280 muL) in 20 mL DCM was stirred at room temperature overnight. The solvent was removed under reduced pressure and the residue was purified via column chromatography using DCM and methanol as eluents to give 758 mg pure product as yellow solid. Yield 79%. 1H NMR (400 MHz, CDCl3) delta 10.14 (br s, 1H), 9.72 (br s, 1H), 8.89 (d, J = 2.2 Hz, 1H), 8.52 (t, J = 5.4 Hz, 1H), 8.21 (d, J = 2.5 Hz, 1H), 8.16 (dd, J = 9.2, 2.1 Hz, 1H), 7.95 (d, J = 9.1 Hz, 1H), 7.71 (d, J = 2.5 Hz, 1H), 7.53-7.43 (m, 1H), 7.22 (d, J = 8.4 Hz, 2H), 6.94-6.83 (m, 3H), 6.60-6.47 (m, 2H), 5.98 (d, J = 2.1 Hz, 1H), 4.27-4.13 (m, 2H), 3.32-3.20 (m, 2H), 3.13-3.01 (m, 4H), 2.83-2.65 (m, 4H), 2.26-2.10 (m, 6H), 1.96 (s, 2H), 1.92-1.74 (m, 3H), 1.47 (s, 9H), 1.40 (t, J = 6.4 Hz, 2H), 1.25-1.18 (m, 2H), 0.93 (s, 6H) ppm., 1235865-77-6

As the paragraph descriping shows that 1235865-77-6 is playing an increasingly important role.

Reference£º
Patent; BIOVENTURES, LLC; ZHENG, Guangrong; ZHOU, Daohong; ZHANG, Xuan; WANG, Yingying; CHANG, Jianhui; (269 pag.)WO2017/184995; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Synthesis of 6-(4-cyclopentylpiperazin-l-yl)-9H-purin-2-amine (28): Compound 1 (0.5 g, 2.95 mmol) was dissolved in acetonitrile (8 mL) and potassium carbonate (1.63 g, 11.8 mmol) and 1 – cyclopentylpiperazine (0.91 g, 5.9 mmol) were added. The reaction was stirred under the N2 atmospheric condition at 100C for 12 hours. Organic layer was extracted with CHCI3 system and column chromatography was done by using CH3OH and CHCI3 system to give compound 28 (yield 60%) as a off-white solid. 1H NMR (300MHz, DMSO-d6) delta ppm 7.66 (s, 1H), 5.72 (s, -NH2), 4.09 (m, 4H), 2.46 (t, J = 4.2 Hz, 4H), 2.42-2.39 (m, 1H), 1.61 -1.50 (m, 4H), 1.43-1.29 (m, 4H). ESI-MS m/z 288.14 (M+H).

21043-40-3, 21043-40-3 1-Cyclopentylpiperazine 806421, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH; TALUKDAR, Arindam; GANGULY, Dipyaman; MUKHERJEE, Ayan; PAUL, Barnali; RAHAMAN, Oindrila; KUNDU, Biswajit; ROY, Swarnali; DEBLINA, Raychaudhuri; (60 pag.)WO2019/92739; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

54699-92-2, 4-Methyl-1-piperazineacetic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 13; General Method for the Preparation of Active Esters of N-Substituted Piperazine Acetic Acid from Trifluoroacetate Esters; A solution of the trifluoroacetate in THF (0.58 M, 1.2 equiv) was added to a solid sample of N-methyl piperazine acetic acid and mixed in a vortex or shaker until a homogeneous solution was obtained. The reaction of the carboxylic acid with the trifluoroacetate ester was generally complete within 30 min for all cases except N-hydroypyrrolidinone (NHP, 18 h). The progress of conversion to the active ester was monitored by ES-MS. The amount of product and any starting material (N-MPA) could be determined by direct infusion of a sample of the reaction (in ethanol) into the ES-MS. In some cases the active ester product was precipitated as dihydrochloride salt by the addition of a solution by addition of HCl solution in dioxane (4 M, 50% volume of the reaction) followed by washing with THF, ethyl acetate and hexanes. In other cases the product was isolated from the reaction as the mono TFA salt. Addition of TFA could be performed if the bis-TFA salt was desired. Dhbt ester, Calculated MH+ = 304.14 Found = 304.20 NHP ester, Calculated MH+ = 242.15 Found = 242.20 4-NP ester, Calculated MH+ = 280.13 Found = 280.20 1H NMR (400 MHz, CDCl3) d 8.20 (d, 2H, J=9.2 Hz, aromatic protons), 7.25 (d, 2H, J=9.2 Hz, aromatic protons), 3.69-3.40 (broad, 2H, ring protons), 3.57 (s, 2H, -CH2-CO-), 3.15-2.90 (broad, 6H, ring protons), 2.78 (s, 3H, -CH3). Pfp ester, Calculated MH+ = 325.10 Found = 325.10 Pcp ester, Calculated MH+ = 404.95 Found = 405.90 3-NP ester, Calculated MH+ = 280.13 Found = 280.20 NHS ester, Calculated MH+ = 256.13 Found = 256.10, 54699-92-2

As the paragraph descriping shows that 54699-92-2 is playing an increasingly important role.

Reference£º
Patent; Applera Corporation.; US2005/148771; (2005); A1;; ; Patent; Applera Corporation.; US2005/148774; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

57260-71-6, The compound 1-tert-butoxycarbonyl piperazine (0.6g, 3.2mmol) and triethylamine (4.6mL, 32mmol) wasdissolved in dry tetrahydrofuran (10 mL), at room temperature, to this solution was added dropwisetrimethylsilyl isocyanate (4.2mL, 32mmol), stirred at rt for 1.5h, ice Water (10 mL), tetrahydrofuran spin, theaqueous phase with ethyl acetate (30mL ¡Á 3). The organic phase was dried over anhydrous Na 2 SO 4, removeThe solvent was concentrated and solid was washed with ethyl acetate (2mL) ultrasonic cleaning 1min, suctionfiltration, to give 0.3g white solid: 4-carbamoyl-piperazine 1-carboxylate, yield: 40%.

As the paragraph descriping shows that 57260-71-6 is playing an increasingly important role.

Reference£º
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

934-98-5, 2-(4-Methylpiperazin-1-yl)ethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A 250 mL round bottom flask equipped with a stir bar was charged with Example 1U (1.96 g) and anhydrous dichloromethane (160 mL) at room temperature under nitrogen. The mixture was cooled to 0¡ã C. in an ice bath, and 2-(4-methylpiperazin-1-yl)ethanamine (0.395 mL) was added via a syringe. The mixture was stirred for 25 minutes at 0¡ã C., and sodium triacetoxyborohydride (156 mg) was added as a solid. The reaction mixture was stirred for 15 minutes at 0¡ã C., and powdered activated 3 angstrom molecular sieves were added (1.96 g). The reaction mixture was stirred 2 hours at 0¡ã C., and was allowed to stir and warm slowly to room temperature overnight. LC/MS indicated one major peak with a mass that corresponded to desired product. The reaction mixture was quenched with dichloromethane and water. The layers were separated, and aqueous layer was extracted with dichloromethane and 10percent methanol/dichloromethane. The aqueous layer was neutralized with saturated aqueous NaHCO3 mixture, and was extracted one more time with 10percent methanol/dichloromethane. The combined extracts were washed with saturated aqueous NaHCO3 and brine, dried with Na2SO4, filtered, and concentrated. The residue was dissolved in dichloromethane and was purified on a Grace Reveleris X2 MPLC using a Teledyne Isco RediSep? Rf gold 750 g silica gel column eluting with a gradient of 0-20percent of methanol/dichloromethane over 40 minutes. The mixed fractions were purified on a Grace Reveleris X2 MPLC using a Teledyne Isco RediSep? Rf gold 330 g silica gel column eluting with a ramp of 0-15percent of methanol/dichloromethane over 40 minutes to collect additional title compound. The material from both columns was combined to provide the title compound. 1H NMR (501 MHz, dimethyl sulfoxide-d6) delta ppm 8.61 (m, 2H), 7.47 (m, 2H), 7.39 (d, 1H), 7.17 (m, 7H), 7.04 (td, 1H), 6.96 (dd, 1H), 6.67 (d, 1H), 6.51 (d, 1H), 5.84 (dd, 1H), 5.06 (m, 2H), 4.07 (ddq, 2H), 3.90 (d, 1H), 3.75 (s, 3H), 3.68 (dd, 2H), 3.50 (d, 1H), 3.17 (m, 1H), 3.08 (m, 1H), 2.90 (m, 2H), 2.65-2.20 (m, 10H), 2.14 (s, 3H), 1.67 (s, 3H), 1.09 (t, 3H). MS (ESI) m/z 928.4 (M+H)+., 934-98-5

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

Reference£º
Patent; AbbVie Inc.; AbbVie Deutschland GmbH & Co. KG; Brady, Patrick B.; Braje, Wilfried; Dai, Yujia; Doherty, George A.; Gong, Jane; Jantos, Katja; Ji, Cheng; Judd, Andrew S.; Kunzer, Aaron R.; Lai, Chunqiu; Mastracchio, Anthony; Risi, Roberto M.; Song, Xiaohong; Souers, Andrew J.; Sullivan, Gerard M.; Tao, Zhi-Fu; Teske, Jesse A.; Wang, Xilu; Wendt, Michael D.; Yu, Yiyun; Zhu, Guidong; Penning, Thomas D.; (218 pag.)US2019/55264; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics