Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,314741-40-7

Step E: tert-butyl(3S)-4-[2-(5-cyano-4-methylthiophen-3-yl)-2-hydroxyethyl]-3-(hydroxymethyl)piperazine-1-carboxylate: A mixture of 3-methyl-4-(oxiran-2-yl) thiophene-2-carbonitrile (1.3 g, 7.9 mmol) and tert-butyl (3S)-3-(hydroxymethyl)piperazine-1-carboxylate(2.0 g, 9.5 mmol) in 5 mL ofEtOH was heated in a microwave apparatus at 140 C for 90 minutes and then cooled down. The reaction mixture was concentrated, and the residue waspurified by column chromatography (DCM : MeOH = 10 :1) to afford the title compound.

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; WO2013/28474; (2013); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.170911-92-9,tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of 6-iodo-8-methyl-2-(methylthio)pyrido[2,3- d]pyrimidin-5(8H)-one (100 mg, 0.30 mmol) in toluene (2mL) at 0 C under nitrogen was added mCPBA (<77% pure)(78 mg, 0.35 mmol) in DCM (2 mL) . After 30 mi DIPEA(0.157 mL, 0.90 mmol) was added, followed by the additionof tert-butyl 4-(4-aminophenyl)piperazine-1-carboxylate(92 mg, 0.33 mmol) in toluene (1.0 mL) . The reactionmixture was stirred at 60 C until deemed complete byLCMS analysis. The reaction mixture was cooled to RT and diluted with DCM (15 mL) and brine (10 mL) and extracted. The organic portion was dried (Phase Separator) and concentrated in vacuo. The residue obtained was purified by flash chromatography (0-100%, EtOAc in cyclohexane) toafford the title compound (44.0 mg, 26%) as a yellow solid. LCMS (Method A) : = 1.33 mi m/z = 563 [M+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; ALMAC DISCOVERY LIMITED; ROUNTREE, James Samuel Shane; O’DOWD, Colin Roderick; BURKAMP, Frank; BELL, Mark Peter; WO2015/19037; (2015); A1;,
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Piperazines – an overview | ScienceDirect Topics

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 27(3R)-tert-butyl 3-methyl-4-(7-(methylsulfonyl)-7-azaspiro[3.5]nonane-2-carbonyl)piperazine-1-carboxylate Oxalyl chloride (0.127 mL, 1.46 mmol) was slowly added to a solution of Intermediate 26 (120 mg, 0.49 mmol) in DCM (12 mL) at 0 C. One drop of DMF was added and the reaction mixture was stirred for 4 h. The solvent was concentrated. The residue was quickly recovered in DCM (5 mL) and added to a solution of (R)-tert-butyl 3-methylpiperazine-1-carboxylate (97 mg, 0.49 mmol) and Et3N (0.338 mL, 2.43 mmol) in DCM (12 mL) at 0 C. The reaction mixture was allowed to warm to ambient temperature and stirred for 1 h. The solvent was concentrated and the product was purified on silica gel (24 g) by MPLC using 5% MeOH and 10% acetone in DCM as the eluent to provide title compound (111 mg, 53.3%) as a solid. 1H NMR (400 MHz, CHLOROFORM-d) delta ppm 1.14 (d, J=7.03 Hz, 2H) 1.22 (d, J=6.64 Hz, 2H) 1.47 (s, 9H) 1.63-1.72 (m, 2H) 1.72-1.84 (m, 2H) 1.92-2.30 (m, 4H) 2.76 (s, 3H) 2.78-3.03 (m, 2H) 3.11 (t, J=5.66 Hz, 2H) 3.14-3.29 (m, 4H) 3.30-3.42 (m, 1H) 3.84 (br. s., 1H) 4.30-4.82 (m, 1H); MS m/z 430.3 [M+H]+ (ES+)., 163765-44-4

As the paragraph descriping shows that 163765-44-4 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; US2010/130477; (2010); A1;,
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122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Exam pe 20olizine-7-carboxamideThis compound was prepared from its corresponding ester, using the same sequence of reactions as described for Exampe I using ntermediate F as starting material. The esterwas subsequently reacted with 2,6-diethylanihne according to procedures described in Examp?e 1. Purification was performed using preparative HPLC to afford the tifle compound (13.5 mg, 23.2%). Data: LCMS (C) Rt:12.686 mm; m/z 566.4 (M+H)., 122833-04-9

As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference£º
Patent; NETHERLANDS TRANSLATIONAL RESEARCH CENTER B.V.; DE MAN, Adrianus Petrus Antonius; BUIJSMAN, Rogier Christian; STERRENBURG, Jan Gerard; UITDEHAAG, Joost Cornelis Marinus; DE WIT, Joeri Johannes Petrus; ZAMAN, Guido Jenny Rudolf; WO2015/155042; (2015); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.883554-88-9,4-Carbamoyl-piperazine-1-carboxylic acid tert-butyl ester,as a common compound, the synthetic route is as follows.

883554-88-9, Intermediate 28: Piperazine-1-carboxylic acid amide hydrochloride; [] 4-Piperazine-1-carboxylic acid tert-butyl ester (1.0g, 5.4mmol), acetic acid (3ml) and water (5ml) were mixed together. Potassium cyanate (2.25g, 27.7mmol) was added portionwise as a solution in water (5ml) and stirred for 4 hours, during which time a solid precipitated. The solid was filtered, re-dissolved in DCM (20ml), dried over MgSO4, filtered, the filter cake washed with DCM (5vol) and concentrated in vacuo to give a white solid (0.38g). The white solid (0.38g) was dissolved in methanol (3.8ml) and 1,4-dioxane (0.7ml), 4M HCl in 1,4-dioxane (2.5ml, 10mmol) was added to the reaction and stirred overnight. The reaction was concentrated in vacuo to give the title compound (0.28g, 31% over 2 steps) as a white solid.1H NMR (400MHz, DMSO-d6) delta9.18 (br s, 2H), 3.91 (br s, 2H), 3.45 (br s, 4H), 2.93 (br s, 4H).

As the paragraph descriping shows that 883554-88-9 is playing an increasingly important role.

Reference£º
Patent; Warner-Lambert Company LLC; EP1593679; (2005); A1;,
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Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.76003-30-0,1-Boc-2-methyl-3-oxopiperazine,as a common compound, the synthetic route is as follows.,76003-30-0

Step 2: Synthesis of iert-butyl 3-ethoxy-2-methyl-5,6-dihydropyrazine-l(2H)-carboxylate lbTo a solution of 1.2b (24 g, 87 mol) in anhydrous DCM (250 mL) at 0 C under N2 atmosphere was added a pre-made solution of triethyloxonium tetrafluoroborate (19.92 g, 105 mmol) in anhydrous DCM (50 mL). The reaction mixture was allowed to warm to RT and stirred for 30 min whereupon saturated solution of NaHC03 (400 mL) was added. The extracted aqueous layer was then washed with DCM (200 ml) and the combined organic extracts were subsequently washed with brine (300 mL), dried over MgS04, filtered and further dried in vacuo to obtain the title intermediate lbas colorless oil. (20.7 g, 98 ).LCMS: P = 98 , retention time = 1.8 min, (M+H+H20)+: 261; 1H-NMR (CDC13): delta 4.30 (br, 1H), 4.11-4.01 (m, 2H), 3.84 (br, 1H), 3.48-3.40 (m, 2H), 2.90 (br, 1H), 1.32 (d, J = 6.9, 3H), 1.26 (t, J = 7.1, 3H).

76003-30-0 1-Boc-2-methyl-3-oxopiperazine 12638300, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; EUROSCREEN S.A.; HOVEYDA, Hamid; DUTHEUIL, Guillaume; FRASER, Graeme; ROY, Marie-Odile; EL BOUSMAQUI, Mohamed; BATT, Frederic; WO2013/50424; (2013); A1;,
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1188265-73-7, tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step B: tert – butyl 3-(2-hydroxyethvn-4-(2-(4-methyl-l-oxo-l,3-dihvdroisobenzofuran-5-yl-2-oxoethyPpiperazine- 1 -carboxylate : tert-Butyl 3-(2-hydroxyethyl) piperazine-1 -carboxylate (6.91 g, 30.0 mmol) and 5-(2-bromoacetyl)-4-methylisobenzofuran-l(3H)-one (6.73 g, 25 mmol) were dissolved in tetrahydrofuran (100 mL) then added Hunig’s base (8.73 mL, 50.0 mmol) and stirred at RT overnight. The reaction was poured into brine and extracted with EtOAc (2x). The combined organic layer was dried over Na2S04, filtered and evaporated to dryness. The crude product was chromatographed through an ISCO Redi-Sep 330g column and eluted with 5% MeOH /DCM solvent system to the title compound. LC-MS (IE, m/z): 419 [M + 1]+ ., 1188265-73-7

As the paragraph descriping shows that 1188265-73-7 is playing an increasingly important role.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; WO2013/28474; (2013); A1;,
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Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129779-30-2,(3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a 20 mL microwave reactor vial was added (3R,5S)-tert-butyl 3,5-dimethylpiperazine- 1 -carboxylate (250 mg, 1.1 67mmol), 1,3 -dibromo-5 -fluorobenzene(592 mg, 2.333 mmol), C52CO3 (950 mg, 2.92 mmol) and toluene (4 mL). The vessel was purged and degassed with N2, then 2,2?-bis(diphenylphosphino)- 1,1 ?-binaphthalene(109 mg, 0.175 mmol) and palladium(II) acetate (52.4 mg, 0.23 3 mmol) were added. The reaction vessel was purged and degassed again. The reaction vessel was capped and the mixture was stirred at 110 C overnight. The reaction mixture was filtered and washed with MeOH and then solvent was removed. The crude was diluted with EtOAc (20 mL),and washed with H20 (20 mL). The orange organic layer was washed with brine, dried over with MgSO4, then concentrated to give crude tert-butyl 4-(3-bromo-5-fluorophenyl) piperazine-1-carboxylate, which was then dissolved in 20% TFA in DCM. The mixture was stirred for 2 hours, concentrated, and then purified by SCX resin (CUBCX1-HL (Benzenesulfonyl, H.L. Resin, 5 g) to provide 1 -((cis)-4-(3 -bromo-5 -fluorophenyl)-3 ,5-dimethylpiperazine, which used directly for next step. LCMS (M+H) = 287.1, 289.1 (1:1 ratio).

129779-30-2, As the paragraph descriping shows that 129779-30-2 is playing an increasingly important role.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; BHIDE, Rajeev S.; BATT, Douglas G.; CHERNEY, Robert J.; CORNELIUS, Lyndon A.M.; LIU, Qingjie; MARCOUX, David; NEELS, James; POSS, Michael A.; QIN, Lan-ying; RUAN, Zheming; SHI, Qing; SRIVASTAVA, Anurag S.; TINO, Joseph A.; WATTERSON, Scott Hunter; (532 pag.)WO2016/64957; (2016); A1;,
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Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of l-(4-(bromomethyl)benzyl)pyridin-2(lH)-one (600 mg, 2.15 mmol, 1.0 eq) in CH3CN (5 mL) were added K2CO3 (0.89 g, 6.45 mmol, 3.0 eq) and 1-tert-butyl 2-methyl piperazine-l,2-dicarboxylate (1.05 g, 4.32 mmol, 2.0 eq). The mixture was heated at 80 C overnight, and then concentrated to dryness under reduced pressure. The residue was mixed with water (10 mL) and extracted with EA (10 mL X 3). The combined organic layers were washed with brine (10 mL), dried over anhydrous Na2S04 and concentrated. The residue was purified via flash chromatography to afford 1-tert-butyl 2-methyl 4-(4-((2-oxopyridin-l(2H)- yl)methyl)benzyl)p

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; LIFESCI PHARMACEUTICALS, INC.; MCDONALD, Andrew; WO2015/103317; (2015); A1;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.960283-58-3,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate hydrochloride,as a common compound, the synthetic route is as follows.

Description 103; 1 ,1 -Dimethylethyl (2S)-4-[(2-chloro-4-nitrophenyl)methyl]-2-methyl-1 – piperazinecarboxylate (D103); A mixture of crude 1-(bromomethyl)-2-chloro-4-nitrobenzene (D102) (0.391 g), 1 ,1- dimethylethyl (2S)-2-methyl-1-piperazinecarboxylate hydrochloride (0.407 g, 1.72 mmol) and Hunig’s base (0.625 ml_, 3.59mmol) in dry DMF (3 mL) was stirred at room temperature for 10 minutes. The reaction mixture was concentrated to give an orange oil which was dissolved in DCM and washed with water (x2) and brine, then dried and concentrated to give an orange oil. Purification by column chromatography eluting with 0-30% EtOAc/pentane gave the title compound as a yellow oil (0.199 g). deltaH (CDCI3, 400MHz) 8.24 (1 H1 d), 8.12 (1 H, dd), 7.77 (1 H, d), 4.24 (1 H, br.s), 3.85 (1 H, d), 3.63 (2H, s), 3.14 (1 H, td), 2.76 (1 H, m), 2.59 (1H, m), 2.33 (1H, dd), 2.18 (1 H, m), 1.47 (9H1 s), 1.28 (3H1 d). MS (ES): MH+ 370/372,

960283-58-3, 960283-58-3 (S)-tert-Butyl 2-methylpiperazine-1-carboxylate hydrochloride 45072182, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXO GROUP LIMITED; WO2008/729; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics