Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.655225-01-7,tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

General procedure: 2,5-Dihydroxybenzaldehyde (1.0 eq.) and cesium carbonate (1.0 eq.) were suspended in DMF and the suspension, warmed to 60 ¡ãC for 15 min. After cooling down to rt, the corresponding bromide (1.1 eq.) was added in DMF (0.5 M concentration of 2,5-dihydroxybenzaldehyde) and the reaction was stirred at rt for 2h for benzylic haloalkanes or at 60 ¡ãC overnight for aliphatic haloalkanes. The solvents were evaporated and the crude dissolved in water and ethyl acetate. The aqueous phase was extracted with ethyl acetate (3x) and the combined organic layers were dried over magnesium sulfate, filtered and the solvent evaporated. The crude product was purified by flash chromatography., 655225-01-7

655225-01-7 tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate 15946441, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Hernandez-Olmos, Victor; Knape, Tilo; Heering, Jan; von Knethen, Andreas; Kilu, Whitney; Kaiser, Astrid; Wurglics, Mario; Helmstaedter, Moritz; Merk, Daniel; Schubert-Zsilavecz, Manfred; Parnham, Michael J.; Steinhilber, Dieter; Proschak, Ewgenij; Bioorganic and Medicinal Chemistry; vol. 27; 21; (2019);,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.300543-56-0,(R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine,as a common compound, the synthetic route is as follows.

Example 2a) [2- [4- [ (4-chlorophenyl)phenylmethyl] -1-piperazinil] ethoxy] – acetonitrile dihydrochlorideCharge 2400 mL of acetonitrile to the reaction vessel, add 400 g of (-) -1- [ (4-chlorophenyl) phenylmethyl ] -4-piperazine, 300 g Na2CO3, 20 g KI and 300 g of 2- (2-chloroethoxy) acetonitrile in turn under stirring.Stir and gradually raise the temperature to 110-115 0C. Keep the temperature for 20 hours, after the reaction is completed, cool the mixture to 80-90 0C and add 25 g of activated carbon and stir for 20 minutes. Filter off carbon and wash cake with appropriate amount of acetonitrile. Into combined filtrate in? troduce dry HCl gas until pH value reaches 0.5-1. Continue to stir the slurry for 20 minutes and filter. Wash the cake with appropriate amount of ethanol and dry at 50-550C for 10 hours to obtain 520 g of the title product.The yield 95%, HPLC (area) 95 %. The obtained [2- [4- [(4- chlorophenyl) phenylmethyl] -1-piperazinyl] ethoxy] -acetonitrile dihydrochloride has in the X-ray powder diffractogram the peaks at about: 8.5; 18.5; 19.1; 22.7; 24.9; 25.7; 25.9 in 28.7 +/- 0.2 2Theta.b) Maceration of a crude [2- [4- [ (4-chlorophenyl)phenylmethyl] – 1-piperazinyl] ethoxy] -acetonitrile dihydrochloride10 g of [2- [4- [ (4-chlorophenyl) phenylmethyl] -1-piperazinyl] ethoxy] -acetonitrile dihydrochloride were suspended in 30 mL of methanol. The suspension was heated to the boiling tempera? ture and stirred at this temperature for at least 20 minutes. Thereafter the suspension was cooled to 0 0C and stirred at this temperature for one hour. The precipitate was filtered, washed with cold methanol and dried. HPLC (area) 98 %., 300543-56-0

As the paragraph descriping shows that 300543-56-0 is playing an increasingly important role.

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Patent; KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO; WO2008/110586; (2008); A2;,
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115619-01-7, 4-(4-Ethylpiperazin-1-yl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 5 (0.16g, 0.77mmol), H2O (0.4ml) and AcOH (1.6ml) was mixed with the 84 (0.22g, 1.00mmol) and then refluxed for overnight. The reaction was quenched by saturated NaHCO3 (aq.) and the mixture was extracted by ethyl acetate (30ml x 3). The residue was purified by flash column over silica gel (dichloromethane: methanol = 9: 1, Rf = 0.35) to afford 88 (0.22g, 73.54%) as a pale yellow solid. 1H-NMR (500MHz, CDCl3): 5 1.16 (t, J= 7.5 Hz, 3H), 2.52 (q, J= 7.5 Hz, 2H), 2.66 (t, J= 5.0 Hz, 4H), 2.88 (d, J= 5.0 Hz, 3H), 3.25 (t, J= 5.0 Hz, 4H), 4.84 (s, 1H), 5.51 (s, 1H), 6.51 (s, 1H), 6.95 (d, J= 8.5 Hz, 2H), 7.23 (d, J= 8.5 Hz, 2H), 7.42-7.43 (m, 3H), 8.31-8.33 (m, 2H).

115619-01-7, As the paragraph descriping shows that 115619-01-7 is playing an increasingly important role.

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Patent; TAIPEI MEDICAL UNIVERSITY; YEN, Yun; LIOU, Jing-Ping; CHEN, Chun-Han; (70 pag.)WO2017/15400; (2017); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.,122833-04-9

10208] Step 1. To a mixture of 2-methoxy-4-(4-methylpip- erazin-1-yl)aniline (Combi-l3locks mc, Cat: SS-3744; 342 mg, 1.55 mmol) and tert-butyl (3-(2-(methylsulfinyl)-7-ox- opyrido[2,3-d]pyrimidin-8(7H)-yl)phenyl)carbamate (52) (521 mg, 1.30 mmol)intert-butanol(lOmL, 105 mmol) was added DIEA (0.57 mE, 3.25 mmol). The reactionmixture was heated at 800 C. in an oil bath for 21 h. The resulting brown suspension was concentrated under reduced pressure and the crude solid was suspended in Et20 (ca. 20 mE) and filtered affording the crude material of tert-butyl (3-(2-((2-methoxy- 4-(4-methylpiperazin-1 -yl)phenyl)amino)-7-oxopyrido[2,3- d]pyrimidin-8(7H)-yl)phenyl)carbamate (la) as a green solid. mlz (ESI, +ve ion) 558.0 (M+H). ?H NMR (400 MHz, DMSO-d5) oe ppm 9.57 (1H, s), 8.73 (1H, s), 8.14 (1H, s), 7.89 (1H, d, J9.4 Hz), 7.57 (1H, d, J8.4 Hz), 7.42 (3H, t, J8.0Hz), 7.28 (1H, d, J8.8 Hz), 6.87 (1H, d, J8.6 Hz), 6.53 (1H, d, J2.3 Hz), 6.43 (1H, d, J9.4 Hz), 6.05 (1H, br. s.), 3.73- 3.82 (3H, m), 3.06 (4H, br. s.), 2.36-2.47 (4H, 2.15-2.26 (3H, s), 1.45 (9H, s).

122833-04-9 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline 20136253, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; TASKER, Andrew; WURZ, Ryan; PETTUS, Liping H.; HERBERICH, Bradley J.; US2014/249131; (2014); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate (500 mg, 2.05 mmol), (4-fluorophenyl)boronic acid (575 mg, 4.11 mmol), copper(II) acetate (372 mg, 2.05 mmol) and pyridine (0.33 ml, 4.09 mmol) were suspended in anhydrous DCM (10 ml) with 4A molecular sieves (500 mg). The mixture was stirred for 16 hours at ambient temperature, then for 5 hours at 35 C. Air was bubbled through the mixture for 10 min, then it was stirred for 18 hours at ambient temperature. Air was bubbled through the mixture for 10 min, then it was stirred at 35 C. for 6 hours and at ambient temperature for 72 hours. Additional (4-fluorophenyl)boronic acid (286 mg, 2.05 mmol) was added and the reaction was stirred for 4 hours at 35 C. The reaction was cooled to ambient temperature and filtered through celite. The filtrate was partitioned with sat. aq. NaHCO3 (20 ml). The organic layer was separated and the aqueous extracted with DCM (2¡Á20 ml). The organics were combined and concentrated in vacuo to give a green oil. The oil was purified via flash column chromatography using a gradient of 0-50% EtOAc in heptane. The product containing fractions were combined and concentrated in vacuo to afford the title compound as a yellow oil (213 mg, 26%). 1H NMR (250 MHz, Chloroform-d) delta 7.01-6.90 (m, 2H), 6.87-6.78 (m, 2H), 4.47 (d, J=13.4 Hz, 1H), 4.32-4.22 (m, 1H), 4.09 (s, 1H), 3.63 (s, 3H), 3.59-3.46 (m, 1H), 3.37 (dd, J=13.3, 4.2 Hz, 1H), 3.28-3.00 (m, 2H), 1.46 (s, 9H). LCMS Method 3-Tr=1.90 min, (ES+) (M+H+) 339.2.

129799-08-2, As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

Reference£º
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (519 pag.)US2018/127370; (2018); A1;,
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262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Method 1A suspension of methyl-3-[methoxy(phenyl)methylene]-2-oxoindoline-6- carboxylate (10,0 g; 0,032 mol) and N-(4-aminophenyl)-N-methyl-2-(4- methylpiperazin-1-yl)acetamide (8,6 g; 0,032 mol) in a mixture of methanol (72 ml) and N,N-dimethylformamide (18 ml) is heated to reflux. After 7 h of refluxing the suspension is cooled down to 0 C and stirring is maintained for additional 2 h. The solid is filtered, washed with methanol (40 ml) and dried to afford 15,4 g (88,1 %) of the “anilino” compound as yellow crystals. 1H-NMR (500 MHz, DMSO-de) delta: 11 ,00 (s, 1 H, 23-H); 12,23 (s, 19-H); 7,61 (t; J = 7,1 Hz, 1 H, 33-H); 7,57 (t, J = 7,5 Hz, 2 H, 32-H + 34-H); 7,50 (d, J = 7,7 Hz, 2 H, 31 -H + 35-H); 7,43 (d, J = 1 ,6 Hz, 1 H, 29-H); 7,20 (dd, J = 8,3; 1 ,6 Hz, 1 H, 27-H); 7,13 (d, J = 8,3 Hz, 2 H, 14-H + 18-H); 6,89 (d, 8,3 Hz, 2 H, 15-H + 17-H); 5,84 (d, J = 8,3 Hz, 1 H, 26-H); 3,77 (s, 3 H, 40-H3); 3,06 (m, 3 H, 12-H3); 2,70 (m, 2 H, 8-H2); 2,19 (m, 8 H, 2-H2, 3-H2, 5-H2, 6-H2); 2,11 (s, 3 H, 7-H3). 13C-NMR (126 MHz, DMSO-d6) delta: 54,5 (C-2 + C-6); 52,2 (C-3 + C-5); 45,6 (C-7); 59,1 (C- 8); 168,5 (C-9); 36,6 (C-12); 140,1 (C-13); 127,6 (C-14 + C-18); 123,8 (C-17 + C-15); 137,0 (C-16); 158,3 (C-20); 97,5 (C-21 ); 170,1 (C-22); 136,2 (C-24); 128,9 (C-25); 117,2 (C-26); 121 ,4 (C-27); 124,0(C-28); 109,4 (C-29); 131 ,9 (C- 30); 128,4 (C-31 + C-35); 129,4 (C-32 + C-34); 130,4 (C-33); 166,3 (C-37); 51 ,7 (C-40). MS (m/z): 540 (M + H)+. Anal, calcd. for C3iH33N5O4: C, 69.00; H, 6.16; N, 12.98. Found: C, 68.05; H, 6.21 ; N, 12.81., 262368-30-9

As the paragraph descriping shows that 262368-30-9 is playing an increasingly important role.

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Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; WO2009/71524; (2009); A2;,
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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

To a solution of 6b (1 eq.) in isopropanol the amine 11 (2.5eq.) and DIPEA (4eq.) wereadded. The reaction mixture was refluxed for 2h. After that time, isopropanolwas evaporated under reduced pressure. The resulting residue was dissolved withEtOAc, washed with water and finally with an aqueous solution of ammoniumchloride. The organic phase was evaporated under reduced pressure. The residuewas purified by flash chromatography on silica gel (CH2Cl2:MeOH98:2) to give the desired compound 10bin 76% yield. 1H NMR (400 MHz, CDCl3): delta(ppm) 2.28 (s,3H); 2.51 (t, J=8, 4H); 3.14 (t, J=8, 4H); 4.63-4.71 (m, 3H); 4.82-4.88 (m,1H); 5.44 (t, J=8, 1H); 6.84 (d, J=8, 2H); 7.18-7.30 (m, 6H); 7.74 (s, 1H);8.28 (s, 1H). 13C NMR (200 MHz, CDCl3): delta(ppm) 46.66;48.79; 54.94; 58.60; 116.21; 128.80; 128.92; 132.84; 134.86; 150-34; 155.47.MS: m/z 497 [M+H]+. Anal. Calcd. for C25H27Cl2N7:C, 60.48; H, 5.48; N, 19.75; found: C, 60.28; H, 5.17; N, 19.25.

216144-45-5, 216144-45-5 4-(4-Methylpiperazin-1-yl)benzylamine 2776493, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Radi, Marco; Bernardo, Vincenzo; Vignaroli, Giulia; Brai, Annalaura; Biava, Mariangela; Schenone, Silvia; Botta, Maurizio; Tetrahedron Letters; vol. 54; 38; (2013); p. 5204 – 5206;,
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1284243-44-2, tert-Butyl 4-(4-fluorophenyl)-3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Hydrogen chloride (4 N in 1 ,4-dioxane) (4 mL, 32 mmol) was added and the mixture was stirred at room temperature for several hours. The solvent was evaporated to give the title compound (0.135 g, quantitative) as a white solid. 1H NMR (400 MHz, DMSO-Qf6) delta ppm 9.79 (br. s., 1 H) 7.34 – 7.41 (m, 2 H) 7.25 – 7.34 (m, 2 H) 3.82 – 3.92 (m, 4 H) 3.53 (d, 2 H).

1284243-44-2, 1284243-44-2 tert-Butyl 4-(4-fluorophenyl)-3-oxopiperazine-1-carboxylate 67085032, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXOSMITHKLINE LLC; BANKA, Anna; CATALANO, John, G.; CHONG, Pek, Yoke; FANG, Jing; GARRIDO, Dulce, Maria; PEAT, Andrew, James; PRICE, Daniel, J.; SHOTWELL, John, Brad; TAI, Vincent; ZHANG, Huichang; WO2011/41713; (2011); A2;,
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120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 7-bromo-4,6-dichloro-8-fluoroquinazoline (2.4 g, 8.25 mmol) in dichloromethane (25 mL) at RT, tert-butyl 2-methylpiperazine-1-carboxylate (3.3 g, 16.5 mmol) and Et3N (5.3 g, 41.25 mmol) was added. The resulting mixture was stirred at RT for 40 min. The mixture was extracted with dichloromethane. The organic layer was washed with 1N HCl, water, saturated NaHCO3 solution and brine. The organic dried over Na2SO4 and concentrated. The residue was washed with mixture of petroleum ether/ ethyl acetate = 5:1 to afford the desired product as a white solid (2.8 g, 74 % yield)., 120737-78-2

As the paragraph descriping shows that 120737-78-2 is playing an increasingly important role.

Reference£º
Patent; ARAXES PHARMA LLC; LI, Liansheng; FENG, Jun; LONG, Yun Oliver; LIU, Yuan; WU, Tao; REN, Pingda; LIU, Yi; (335 pag.)WO2016/164675; (2016); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.76003-29-7,1-Boc-3-Oxopiperazine,as a common compound, the synthetic route is as follows.

76003-29-7, To a solution of tert-butyl 3- oxopiperazine-l-carboxylate (2.0g, 9.99 mmol) in DCM (20 ml) was added triethyloxonium tetrafluoroborate (2.0 lg, 10.99 mmol) and stirred at rt. The mixture was partitioned between EtOAc and aq NaHC03 (sat’d) and aqueous layer was extracted with EtOAc (3x). Combined organic layer was washed with brine, dried over MgS04, filtered, concentrated to give the title product as viscous oil. LC/MS:[M-56+ i] = 173.3

The synthetic route of 76003-29-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; CHOBANIAN, Harry; PIO, Barbara; GUO, Yan; DING, Fa-Xiang; DONG, Shuzhi; WALSH, Shawn, P.; JIANG, Jinlong; KIM, Dooseop; WO2015/95097; (2015); A2;,
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