Tag: M.W:100-200

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

N-(4-(2-(Chloromethyl)-5-methyl-4-oxo-4,5-dihydrofuro[3,2-c]pyridin-7-yl)p (for a preparation see Intermediate 82, 50 mg, 0.151 mmol) was dissolved in DMF (5 mL), potassium carbonate (62.5 mg, 0.452 mmol) was added, followed by 1-methylpiperazin-2-one (17.20 mg, 0.151 mmol). The mixture was stirred for 3 h at room temperature. The mixture was diluted with water (10 mL) and extracted with a mixture of methanol (3 mL) and DCM (15 mL), the organic layer was dried, 59702-07-7

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED; AMANS, Dominique; BAMBOROUGH, Paul; BARKER, Michael David; BIT, Rino Antonio; BROWN, John Alexander; CAMPBELL, Matthew; GARTON, Neil Stuart; LINDON, Matthew J; SHIPLEY, Tracy Jane; THEODOULOU, Natalie Hope; WELLAWAY, Christopher Roland; WESTAWAY, Susan Marie; WO2014/140077; (2014); A1;,
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Piperazines – an overview | ScienceDirect Topics

13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1-{4-[3-(6-Bromo-quinazolin-4-yl)-5-fluoro-benzoyl]-piperazin-1-yl}-ethanone To a mixture of 3-(6-bromo-quinazolin-4-yl)-5-fluoro-benzoic acid (1.36 g, 3.72 mmol) in CH2Cl2 (15 mL) was added DIPEA (1.30 mL, 7.44 mmol) and HBTU (1.694 g, 4.47 mmol) at rt. The reaction mixture was stirred at rt for 20 min. To the mixture was then added 1-(piperazin-1-yl)ethanone (0.572 g, 4.47 mmol) and the reaction mixture was stirred at rt for 1 h. The reaction was quenched with a saturated aqueous solution of NaHCO3 and extracted with CH2Cl2. The organic layer was washed twice with brine, dried by passing through a phase separating cartridge and evaporated. Purification by Flash chromatography using Biotage Isolera system (amine functionalized silica KP-NH, eluting with Cyclohexane/EtOAc 0 to 100%) gave the title compound (1.20 g, 68% yield) as a beige foam. MS: 457.4-459.3 [M+1]+, Rt(2′)=1.03 min., 13889-98-0

The synthetic route of 13889-98-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NOVARTIS AG; COOKE, Nigel Graham; FERNANDES GOMES DOS SANTOS, Paulo Antonio; FURET, Pascal; HEBACH, Christina; HOGENAUER, Klemens; HOLLINGWORTH, Gregory; KALIS, Christoph; LEWIS, Ian; SMITH, Alexander Baxter; SOLDERMANN, Nicolas; STAUFFER, Frederic; STRANG, Ross; STOWASSER, Frank; TUFFILLI, Nicola; VON MATT, Anette; WOLF, Romain; ZECRI, Frederic; US2015/342951; (2015); A1;,
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Piperazines – an overview | ScienceDirect Topics

52385-79-2, 2-(3-Chlorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 300 3-[1-(ethylsulfonyl)-4-piperidinyl]-5-[3-(2-piperazinyl)phenyl]-1H-indole-7-carboxamide trifluoroacetate To a solution of 3-[1-(ethylsulfonyl)-4-piperidinyl]-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole-7-carboxamide (60 mg, 0.13 mmol) in dioxane (1.5 mL) and water (0.5 mL) was added 2-(3-chlorophenyl)piperazine (63.7 mg, 0.325 mmol) and potassium carbonate (90 mg, 0.650 mmol). This mixture was degassed for 5 min then tetrakis(triphenylphosphine)palladium(0) (12 mg, 0.011 mmol) was added. The resulting mixture was reacted in a microwave for 30 min at 160 C. The solid was filtered off and all solvents were evaporated. The resulting solution was re-dissolved in dichloromethane and separator was used to remove water. The mixture was concentrated to give organic solvent and then purified by Gilson Preparatory HPLC to give 21.7 mg of the title compound (27.4%). LC/MS=m/z 496.4 [M+H] Ret. Time: 1.28 min., 52385-79-2

As the paragraph descriping shows that 52385-79-2 is playing an increasingly important role.

Reference：
Patent; Deng, Jianghe; Kerns, Jeffrey K.; Jin, Qi; Lin, Guoliang; Lin, Xichen; Lindenmuth, Michael; Neipp, Christopher; Nie, Hong; Thomas, Sonia M.; Widdowson, Katherine L.; US2009/143372; (2009); 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.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.,109384-27-2

EXAMPLE 21b (4-methyl-3-oxopiperazin-1-yl)acetic acid The compound can be prepared in the following way: A solution of 0.61 g of 2-bromoacetic acid, 10 ml of water, 0.74 g of 1-methyl-piperazin-2-one hydrochloride (commercially available product) and 0.61 g of potassium carbonate is kept stirred at a temperature in the vicinity of 20 C. for 18 hours. 0.31 g of potassium carbonate is then added and stirring is maintained for one hour. The reaction medium is acidified (pH~1) by addition of an aqueous hydrochloric acid solution (1N) and then concentrated by evaporation under reduced pressure. The residue obtained is taken up in 2 times 30 ml of toluene and then concentrated. The yellow solid obtained is taken up in 5 ml of ethanol, filtered off on a sintered glass funnel and washed with 2 times 5 ml of ethanol. The filtrate is concentrated by evaporation under reduced pressure and 1.03 g of (4-methyl-3-oxopiperazin-1-yl)acetic acid hydrochloride are thus obtained in the form of a yellow foam. MS: method A; [M+H]+: m/z=173; [M-H]-: m/z=171; Tr=0.11 min.

The synthetic route of 109384-27-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; sanofi-aventis; US2011/263593; (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.13754-38-6,1-Benzoylpiperazine,as a common compound, the synthetic route is as follows.

13754-38-6, General procedure: A solution of 2-chloroalkyl/aryl substitutedwith or without N-substitution as well as with or without 5 and/or 6-substituted benzimidazole derivative (1.75g,0.01051mol) and 1-[(4-phenyl)carbonyl]piperazine (3g,0.0105mol) in N, N dimethylformamide was taken in a RBF.K2CO3(2gm,) was added to the reaction mixture. The reaction mixture was stirred for 8h at 80C on a magnetic stirrer (heat + stirring). The progress of the reaction was monitored by thin layer chromatography (TLC).Upon completion of the reaction, water was added to the reaction mixture and the product extracted by shaking the reaction mixture with dichloromethane in a separating funnel.The dichloromethane layer was washed successively with water and brine, dried over anhydrous sodium sulfate. Evaporation of the solvent gave theproduct. 11a-l Recrystallized with various solvent like chloroform, ethanol, methanol.(4-((1H-benzo[d]imidazol-2-yl) methyl) piperazin-1-yl)(Phenyl) methanone (11a) Compound 11a was obtained as a white solid (yield: 74.35%; MP:224-226; IR (KBr): 3220(N-H), 2365 (C-H), 1670(C=O),1604(C=N),1556(C=C), 1232 (C-N) cm-1; 1H NMR (300 MHz,CDCl3)ppm: 3.45-3.51(m, 4H,PIP-H), 4.34(s, 2H,-CH2-), 4.79(s, 1H, N-H), 7.30-7.45 (m, 4H, Ar -H of Benzim) 7.89-8.07 (4H, Ar -H of benzoyl) ; 13C-NMR(400 MHz, CDCl3, TMS): 52.14 (CH2), 55.4(CH2),61.7 (CH2), 117(arom. CH), 124 (arom. CH),129(arom. CH), 133.5 (quat. C), 139.8 (quat. C), 145.6(quat. C),171.6 (carbonyl C).ESI-MS m/z:320,243,189,131.Anal. Calcd. for C19H20N4O(320): C, 71.23; H, 6.29; N, 17.49; O, 4.99. Found: C,71.10; H, 6.23; N, 17.43; O, 4.91

The synthetic route of 13754-38-6 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Kankate, Rani S.; Gide, Parag S.; Belsare, Deepak P.; Oriental Journal of Chemistry; vol. 30; 4; (2014); p. 1855 – 1863;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred suspension of 1-fluoro-4-nitrobenzene (2 g,14.17 mmol) and potassium carbonate (3.92 g, 28.3 mmol) in anhydrous dimethyl sulfoxide (10 mL) was added 2- (piperazin-1-yl)ethanol (2.089 mL, 17.01 mmol) and the mixture was heated at 80 C for 16 hours. After coolingthe mixture was partitioned between water (100 mL) and ethyl acetate (30 mL) . The aqueous layer was separated and extracted with ethyl acetate (2 x 30 mL) . The combined organic fractions were reduced in vacuo. The residue was triturated in water (100 mL) . The solid wascollected by filtration under vacuum and dried for 16 hours under vacuum and flowing nitrogen to give the title compound (3.45 g, 97 %) . ?H NMR (400 MHz, CDC13) : 3 8.11 (d, 2H), 6.82 (d, 2H), 3.68 (t, 2H), 3.44 (t, 4H), 2.67 (t, 4H), 2.62 (t, 2H), 2.55 (br s, 1H) . LCMS (Method C):RT = 0.45 mi m/z = 252 [M+H]., 103-76-4

103-76-4 N-(2-Hydroxyethyl)piperazine 7677, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ALMAC DISCOVERY LIMITED; HARRISON, Timothy; TREVITT, Graham; HEWITT, Peter Robin; O’DOWD, Colin Roderick; BURKAMP, Frank; WILKINSON, Andrew John; SHEPHERD, Steven D.; MIEL, Hugues; WO2015/92431; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

74879-18-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

c) A mixture of (R)-6-bromo-l-(l-(4-chloro-2-(trifluoromethyl)phenyl)ethyl)-lH- benzo[i/]imidazole (0.25 g, 0.62 mmol), (5)-(+)-2-methylpiperazine (0.13 g, 1.3 mmol), Pd2(dba)3 (0.028 g, 0.031 mmol), BetaGammaNuAlphaRho (0.057 g, 0.093 mmol), and Cs2C03 (0.60 g, 1.9 mmol) in toluene (10 mL) was purged with nitrogen for 5 min, and then heated at 100 C for 16 h. After cooling to room temperature, the mixture was filtered and washed with EtOAc (10 mL). The filtrate was concentrated in vacuo. The resulting crude mixture was diluted with ethyl acetate (20 mL), washed with deionized water and brine, dried ( a2S04), and concentrated in vacuo. The resulting crude material was purified by flash chromatography (Si02, 0-20% methanol in dichloromethane) to afford the coupled product (0.13 g, 0.24 mmol, 39%).

As the paragraph descriping shows that 74879-18-8 is playing an increasingly important role.

Reference：
Patent; CHEMOCENTRYX, INC.; LELETI, Manmohan Reddy; LI, Yandong; MALI, Venkat Reddy; POWERS, Jay; YANG, Ju; WO2013/82429; (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.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

A solution of 5-chloro-3-(1-methyl-1H-pyrazol-4-yl)-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-pyrazolo[4,3-d]pyrimidine (40 mg, 0.110 mmol), 1-methylpiperazin-2-one hydrochloride (33.0 mg, 0.219 mmol), and N,N-diisopropylethylamine (56.7 mg, 0.438 mmol) in dioxane (1 mL) was heated to 100 C. After 20 hrs, the reaction was cooled to r.t., diluted with water and extracted with EtOAc. The organic layer was washed with brine, dried with Na2SO4 and concentrated. The crude was taken up in 1 mL MeOH and 1 mL HCl (4 M solution in dioxane) and stirred at 60 C. for 2 hrs. The resulting mixture was purified with prep-LCMS (XBridge C18 column, eluting with a gradient of acetonitrile/water containing 0.1% TFA, at flow rate of 60 mL/min). LCMS calculated for C14H17N8O (M+H)+: m/z=313.1; found 313.1. The product was isolated as the TFA salt., 109384-27-2

As the paragraph descriping shows that 109384-27-2 is playing an increasingly important role.

Reference：
Patent; Incyte Corporation; Vechorkin, Oleg; Nguyen, Minh; Qi, Chao; Wang, Anlai; Wu, Liangxing; Yao, Wenqing; Zhao, Peng; (82 pag.)US2020/95250; (2020); 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.

A vial was charged with 5-amino-3,6-dichloro-l ,2,4-triazine (495.1 mg, 4.25 mmol) and triethylamine (1.5 mL, 10.76 mmol), 2,6-dimethylpiperazine (0.7054 g, 4.28 mmol) in dioxane (11 mL). The mixture was heated at 95 C for 1.5 h using microwave. The mixture was cooled to room temperature, filtered and the white solid was washed with dichloromethane. The organic solution was concentrated. The residue was dissolved in dichloromethane, washed with saturated potassium carbonate, dried over anhydrous sodium sulfate, concentrated. The residue was purified with flash column chromatography on silica gel using ethyl acetate and 0-10% methanol/ethyl acetate to afford product as solid (0.8916 g, yield: 86%). NMR (500 MHz, Chloroform-i/) delta 5.168 (br, 2H), 4.550 (d, J = 12.5 Hz, 2H), 2.859-2.800 (m, 2H), 2.432 (d, – J= 13.2 Hz, 1 H), 2.406 (d, J= 10.5 Hz, 1H), 1.094 (d, J = 6.5 Hz, 6H). LC-MS: 243.0 (MH+/z).

21655-48-1, As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

Reference：
Patent; NEKTAR THERAPEUTICS (INDIA) PVT. LTD.; NEKTAR THERAPEUTICS; SHARMA, PANKAJ; KHATRI, VIJAY KUMAR; GU, XUYUAN; SONG, YUAN; SHEN, MICHAEL LIXIN; SAUTHIER, JENNIFER RIGGS; ANAND, NEEL K.; KOZLOWSKI, ANTONI; ODINECS, ALEKSANDRS; RILEY, TIMOTHY A.; REN, ZHONGXU; MU. YONGQI; SHEN, XIAOMING; YUAN. XUEJUN; AURRECOECHEA, NATALIA; O’MAHONY, DONOGH JOHN ROGER; WO2015/92819; (2015); 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.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: To a solution of 6 or 7 (0.68-0.74 mmol) in 3 mL of n-BuOH kept in a PV with stirring, cyclic amines (1.02-1.11 mmol) was added. The sealed PV was placed in an oil bath at 145-150 C and stirred for 50-60 min. The solvent was evaporated in vacuo with the aid of DCM and the residue was re-dissolved in 2:1 EtOAc/DCM and washed successively with saturated NaHCO3 and NaCl solution (1 x 15 mL), respectively. The aqueous layer was washed with EtOAc (3 x 5 mL) and the organic layer was dried over anhydrous MgSO4 then filtered. The solution was evaporated in vacuo and purified using silica gel column chromatography with appropriate eluents (EtOAc/hexanes 3:1 and 1:3 v/v, respectively or 9:1 DCM/EtOAc) to afford either solid or semisolid products., 13484-40-7

As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

Reference：
Article; Mohamed, Tarek; Yeung, Jacky C.K.; Rao, Praveen P.N.; Bioorganic and Medicinal Chemistry Letters; vol. 21; 19; (2011); p. 5881 – 5887;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics