Heterocyclic Building Blocks-piperazine

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.

Reference£º
Patent; KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO; WO2008/110586; (2008); A2;,
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55112-42-0, 4-Methyl-1-piperazinecarbonyl Chloride Hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

55112-42-0, Step 1: Preparation of racemic Zopiclone (I) Example- 1To a mixture of 6-(5-chloropyrid-2-yl)-5-hydroxy-7-oxo-5,6-dihydropyrrolo[3,4-b]pyrazine (100 g), DBU (173.9 g), pyridine (90.25 g) and dichloromethane (1000 ml), 1- chlorocarbonyl-4-methylpiperazine hydrochloride (151.56 g) was added and stirred for 5 hours at 20-25 C. On completion of the reaction, chilled water (1000 ml) was added to it to form a biphasic mixture and the organic phase was extracted. The aqueous phase was further extracted with dichloromethane (1000 ml). The organic phases were combined, washed with water (5 x 1000 ml) and evaporated under vacuum. The resultant solid residue was dissolved in acetonitrile (500 ml), charcoalized with activated carbon (5 gms), filtered on celite bed and washed with acetonitrile (2 x 50 ml). The filtrate and the acetonitrile washings were combined, cooled, stirred for 2 hours at 5 – 10C, filtered and dried to obtain zopiclone. (Yield: 81%; Purity: 99.65% by HPLC).

55112-42-0 4-Methyl-1-piperazinecarbonyl Chloride Hydrochloride 3016934, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; LUPIN LIMITED; WO2009/101634; (2009); A2;,
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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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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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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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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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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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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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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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