Month: November 2020

5317-33-9, 3-(4-Methylpiperazin-1-yl)propan-1-ol is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 7. General Procedure 1: Di-tert-butyl azodicarboxylate (0.478 g, 2.08 mmol) was added portion wise to a mixture of product step 6 (1.66 mmol), 3-(4-methyl-piperazin-1-yl)-propan-1-ol (synthesis described below, 0.276 g, 1.74 mmol), and triphenylphosphine (0.544 g, 2.08 mmol) in dichloromethane (20 mL) at r.t. If necessary, further alcohol was added. After stirring for 2 h, the solution was concentrated to 10 mL, mounted on silica and chromatographed (gradient, dichloromethane to dichloromethane_methanol=3:2) to obtain the desired ethers (73%). Example 2 Synthesis of 4-chloro-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]-quinazoline The compound was synthesized according to general procedure 1 from 4-chloro-7-hydroxy-6-methoxyquinazoline. LC/ESI-MS: mn/z=351 [M+H]., 5317-33-9

As the paragraph descriping shows that 5317-33-9 is playing an increasingly important role.

Reference£º
Patent; Ehlert, Jan; Herz, Thomas; Krauss, Rolf; Kubbutat, Micheal; Lang, Martin; Pegoraro, Stefano; Schachtele, Christoph; Totzke, Frank; Zirrgiebel, Ute; US2007/149523; (2007); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.112984-60-8,6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid,as a common compound, the synthetic route is as follows.

Example 2; Preparation of (R)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid (Compound 3); Racemic ulifloxacin (105 g) was dissolved in DMSO (1500 mL). L-tartrate (27 g) solution in DMSO (405 mL) was added to the racemic ulifoxacin solution with agitation. Cloudiness and precipitation appeared. After 20 hours of agitation at an ambient temperature, the mixture was filtered and dried under vacuum to yield 82 g of solid. The solid was recrystallized in DMSO to yield 34 g of (R)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid-L-tartrate salt. The salt was dispersed in water and the dispersion was neutralized with 2% NaOH aqueous solution to a pH value of 7 to 8. The precipitate was filtered and dried to yield 22 g of (R)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid. It had specific rotation [alpha]D20=+139.2 (c=0.15, 0.1 mol/L NaOH), optical purity e.e>95%., 112984-60-8

112984-60-8 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid 124225, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Chen, Mao; Zhu, Shaoxuan; Zheng, Lizhen; Liu, Xuebin; Wang, Yuping; Xu, Shuwen; US2011/28444; (2011); 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.112257-12-2,tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of 2-((lH-indol-4-yl)oxy)-6-(trifluoromethyl)isonicotinonitrile 1 (150 mg, 0.5 mmol) (from Example 49, Step 1) in DMF (12 mL) at 0 C, were added fert-butyl 4-(2-bromoacetyl)piperazine-l-carboxylate 2 (228 mg, 0.74 mmol), Cs2C03 (324 mg, 0.99 mmol) and n-Bu4NBr (8 mg, 0.02 mmol). The reaction mixture was warmed to RT and stirred for 12 h. The mixture was quenched with water (30 mL) and extracted with EtOAc (2 x 30 mL). The combined organic extracts were washed with brine (20 mL), dried (Na2S04), filtered and concentrated under reduced pressure to obtain the crude. The crude was triturated with Et20 (2 x 10 mL) to afford compound 3 (150 mg, 57%) as white solid. 1H NMR (500 MHz, OMSO-d6): delta 8.32 (s, 1H), 8.09 (s, 1H), 7.47 (d, J= 8.1 Hz, 1H), 7.40 (d, J= 3.2 Hz, 1H), 7.29 (t, J= 8.0 Hz, 1H), 7.03 (d, J= 7.8 Hz, 1H), 6.31 (d, J= 3.2 Hz, 1H), 5.37 (s, 2H), 3.72-3.70 (m, 2H), 3.59-3.56 (m, 4H), 3.48-3.46 (m, 2H), 1.56 (s, 9H); LC-MS (ESI): m/z 474.0 (M+ – Tiu).

112257-12-2, As the paragraph descriping shows that 112257-12-2 is playing an increasingly important role.

Reference£º
Patent; PHARMAKEA, INC.; ROWBOTTOM, Martin W.; HUTCHINSON, John Howard; CALDERON, Imelda; (202 pag.)WO2016/144703; (2016); A1;,
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Piperazines – an overview | ScienceDirect Topics

74879-18-8, (S)-(+)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

74879-18-8, Tn a sealed tube, 2- (2, 8-dimethylimidazo [1 ,2-b]pyridazin-6-yl)-7-fluoro-pyrido [1,2- a]pyrimidin-4-one (Intermediate 2; 33 mg, 0.107 mmol), and (S)-2-methylpiperazine (43 mg, 0.427 mmol, 4.0 eq.) were stuffed in DMSO (2 mL) at 120C overnight. The solvent was removed 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 Na2SO4 andconcentrated in vacuo. The crude was purified by column chromatography (Si02, CH2C12/MeOH=95/5 to 90/10) to afford the title product (18 mg, 43%) as a light yellow solid. MS m/z 390.3 [M+H?i.

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

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;,
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Piperazines – an overview | ScienceDirect Topics

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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Piperazines – an overview | ScienceDirect Topics

5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5308-25-8, 1-(bromomethyl)-4-nitro-2-(trifluoromethyl)benzene (34 g, 120 mmol) obtained in above was dissolved in dichloromethane (300 mL), followed by stirring. The reaction solution was added with 1-ethylpiperazine (15.97 mL, 126 mmol) and DIPEA (27.2 mL, 156 mmol), followed by further stirring for about 3 hours at room temperature. The reaction mixture was diluted with dichloromethane, and washed with a saturated aqueous solution of sodium bicarbonate and brine. The organic layer was dried over anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to obtain the title compound (21.7 g, 57%). 1H-NMR Spectrum (300 MHz, DMSO-d6): delta 8.52 (d, 1H), 8.40 (s, 1H), 8.09 (d, 1H), 3.71 (s, 2H), 2.35 (m, 10H), 1.00 (t, 3H) MS (ESI+, m/z): 318 [M+H]+

The synthetic route of 5308-25-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; HANMI PHARM. CO., LTD; Bae, In Hwan; Son, Jung Beom; Han, Sang Mi; Kwak, Eun Joo; Kim, Ho Seok; Song, Ji Young; Byun, Eun Young; Jun, Seung Ah; Ahn, Young Gil; Suh, Kwee Hyun; US2014/371219; (2014); A1;,
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Piperazines – an overview | ScienceDirect Topics

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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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

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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Piperazines – an overview | ScienceDirect Topics

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.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; WO2009/71524; (2009); 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.181955-79-3,1,4-Di-Boc-piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

181955-79-3, Step 2-Formation of methyl 1,4-di-tert-butoxycarbonyl piperazine-2-(R)-carboxylate. 1,4-Di-tert-butoxycarbonylpiperazine-2-(R)-carboxylic acid (70 g, 212 mmol) was dissolved in acetonitrile (1.3 L). Cs2CO3 (110 g, 340 mmol) was added and the mixture stirred for 30 minutes at room temperature before the addition of methyl iodide (28 ml, 450 mmol). The reaction mixture was stirred at room temperature overnight, solids were filtered and the filtrate concentrated in vacuo. The resulting oil was dissolved in EtOAc and any insoluble material filtered. The filtrate was concentrated in vacuo to give methyl 1,4-di-tert-butoxycarbonylpiperazine-2-(R)-carboxylate (69 g, 95%). LC/MS Calcd for [M+H]+ 345.2. found 145.1 (-Boc X 2). Step 3-Formation of methyl piperazine-2-(R)-carboxylate dihydrochloride.

181955-79-3 1,4-Di-Boc-piperazine-2-carboxylic acid 11255979, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; SYMPHONY EVOLUTION, INC.; US2011/82114; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics