Tag: M.W:300-400

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.154590-34-8,tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Preparation 10 :; 4- (4-Amino-2-fluoro-phenyl)-piperazine-l-carboxylic acid tert-butyl ester:; To a solution of 4-(2-fluoro-4-nitro-phenyl)-piperazine-1-carboxylic acid tert- butyl ester (9.00 grams, 27.7 mmol), obtained in preparation 7, in methanol and THF (4: 1,140 mL) was added ammonium formate (6.98 grams, 111 mmol) followed by the addition of 10% Pd-C (1.47 grams, 13.8 mmol) and stirred at 25-35 C for 5 hours. The reaction mixture was filtered through a pad of celite and washed thoroughly with methanol. Removal of volatiles left a pasty mass, which was diluted with water and extracted with ethyl acetate (150 mL x 3). The combined organic layer was washed with water followed by brine and dried over sodium sulfate. Evaporation of solvent produced the title amine (7.75 grams, 95%). ‘H NMR (CDC13) : 8 6.78 (t, J= 9.1 Hz, 1H), 6.47-6. 38 (m, 2H), 3.57 (t, J= 4.8 Hz, 4H), 2.90 (t, J= 4.8 Hz, 4H), 1. 48 (s, 9H), IR (KBr, cm-1) : 3451,3347, 1681. CI-MS (m/z) : 296 (M++1), 282,240, 196.153, 106,96.

154590-34-8, The synthetic route of 154590-34-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DR. REDDY’S LABORATORIES LTD.; WO2005/82892; (2005); 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

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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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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

150407-69-5, (S)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,150407-69-5

Step 2: 1 -Benzyl 4-fert-butyl 2-methyl (2,SV1.2.4-piperazinetricarboxylate (AA2); A solution of TMS-diazomethane (2.0 M in Et2O, 4.0 eq.) was added to a stirred 0.16 M solution of AAl in a toluene-MeOH mixture (2:1). The reaction mixture was stirred overnight at RT. Solvents were removed under reduced pressure. The residue was purified by column chromatography on silica gel, eluting with 20 to 100% EtO Ac/petroleum ether to give the title compound in 92 % yield. 97% ee by SFC. [CC]D20 -10.6 (c 1.00, CHCl3). 1H NMR (300 MHz, CDCl3, 300K) delta 7.37 (5H, m), 5.18 (2H, m), 4.79-4.57 (2H, m), 4.10-3.90 (2H, m), 3.75 (1.5H, s), 3.70 (1.5H, s), 3.34-3.30 (IH, m), 3.10 (IH, dd, J = 13.6, 4.4 Hz), 2.86 (IH, m), 1.45 (9H, s). MS (ES+) Ci9H26N2O6 requires 378, found: 401 (M+Na)+.

150407-69-5 (S)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid 1512536, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A.; BRANCA, Danila; FERRIGNO, Federica; HERNANDO, Jose, Ignacio, Martin; JONES, Philip; KINZEL, Olaf; MALANCONA, Savina; MURAGLIA, Ester; PALUMBI, Maria, Cecilia; PESCATORE, Giovanna; SCARPELLI, Rita; WO2010/23480; (2010); 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.479353-63-4,1-Boc-4-(4-Carboxybenzyl)piperazine,as a common compound, the synthetic route is as follows.

A mixture of compound 5 (1.0 g, 2.81 mmol), compound 7a (0.98 g, 4.19 mmol), HATU (1.28 g, 3.37mmol) in DMF (20 mL) was cooled to 0C and DIPEA (1.95 mL, 11.24 mmol) was added. The reaction mixture was allowed to warm to room temperature and stirred for 15 min. Saturated aqueous sodium bicarbonate (20 mL) was added and the resulting mixture was extracted with ethyl acetate (50 mL><2). The combined extracts were dried over anhydrous sodium sulfate and concentrated. The residue was purified by flash column chromatography on silica gel (petroleum ether/ethyl acetate = 3 : 1 to 1 : 1) to afford compound 8a (1.29 g, 80% yield) as a yellow solid. 479353-63-4, 479353-63-4 1-Boc-4-(4-Carboxybenzyl)piperazine 2795516, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; INHIBIKASE THERAPEUTICS, INC.; WERNER, Milton, H.; KELLY, Terence, A.; (74 pag.)WO2016/172528; (2016); 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.154590-34-8,tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 4-(2-fluoro-4-nitro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (29.1 g, 89.4 mmol) in MeOH (150 mL) and DCM (10 mL) mixture was added Raney Ni (5.5 g) and the Parr shaker was charged with hydrogen to 50 psi for 1 h. The initial yellow solution became clear and the content was filtered, washed with MeOH and the combined filtrate evaporated to dryness. The residue was dissolved in dry dioxane (20 mL) and a 4M HC1 solution in dioxane (30 mL) was added. The solution was warmed to 45 C in a water bath and stirred vigorously overnight producing a white precipitate. After filtering and washing with cold dioxane and diethyl ether and drying in vacuo, 23.1 g (96%) of the title compound was isolated as a white solid. N1HMR (400 MHz, DMSO-4 delta (ppm): 10.5 (br. s., 1 H), 9.63 (br. s., 2H), 8.0 (br. s., 2H), 7.29 (d, J = 12.6 Hz, 1 H), 7.20 – 7.19 (m, 2H), 3.24 (d, J = 4.8 Hz, 4H), 3.19 (br. s., 4H). 19F NMR (376 MHz, DMSO-d6) delta (ppm): – 120.36 (dd, J = 13.6, 7.2 Hz, IF)., 154590-34-8

154590-34-8 tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate 16203508, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ANACOR PHARMACEUTICALS, INC.; HERNANDEZ, Vincent, S.; DING, Charles; PLATTNER, Jacob; ALLEY, Michael, Richard Kevin; ZHANG, Yong-Kang; ZHANG, Yanchen; WO2011/37731; (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.171504-98-6,Methyl 1,4-Bis(Boc)-2-piperazinecarboxylate,as a common compound, the synthetic route is as follows.

LiHMDS (9.9 mL of 1 M, 9.9 mmol) was added to a solution of 1,4-di-tert-butyl 2-methyl piperazine-1,2,4-tricarboxylate (2.0 g, 5.8 mmol) in THF (30 mL) at -78 C under N2. After 45 minutes, iodomethane (615 muL, 9.9 mmol) in THF (5 mL) was added slowly. The mixture was allowed to warm slowly to ambient temperature and stirred overnight. The reaction mixture was partitioned between DCM and saturated aqueous NH4Cl solution. The organic phase was dried, filtered and concentrated in vacuo. The residue was purified by column chromatography (silica, DCM/MeOH elution) to give 1,4-di-tert-butyl 2-methyl 2-methylpiperazine-1,2,4- tricarboxylate as a colourless oil (1.5 g, 72%); MS m/z: 359 (M+H)+

171504-98-6, The synthetic route of 171504-98-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK PATENT GMBH; VERTEX PHARMACEUTICALS INCORPORATED; BAYLY, Andrew; BLEICH, Matthew; CHARRIER, Jean-Damien; DODD, James; DURRANT, Steven; ENO, Meredith Suzanne; ETXEBARRIA I JARDI, Gorka; EVERITT, Simon; FRAYSSE, Damien; KELLY, Shazia; KNEGTEL, Ronald; MOCHALKIN, Igor; MORTIMORE, Michael; NORTH, Kiri; PORICHIS, Filippos; PULLIN, Robert; RUTHERFORD, Alistair; STORCK, Pierre-Henri; TWIN, Heather Clare; XIAO, Yufang; (1159 pag.)WO2019/148132; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

113028-17-4, Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 8: Preparation of Ulifloxacin;Tertiary butanol (5.55It), 6-fluoro-l-methyl-4-oxo-7-(l-piperazinyl)-4H-[l,3]thiazeto [3,2- a]quinoline-3-carboxylic acid ethyl ester (1.1 lkg), potassium hydroxide (0.37kg) and water (2.75 It) were added at room temperature. The reaction mixture was heated to 600C and maintained for 1.5 hours. Reaction completion was checked by TLC. This was followed by the addition of water (22.2 It) and acetic acid (0.39 It). The reaction mixture was filtered, washed with water followed by slurry wash with acetone (2.22 It) twice and dried to obtain 0.95 kg of ulifloxacin having purity 97.56% by HPLC., 113028-17-4

The synthetic route of 113028-17-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; IND-SWIFT LABORATORIES LIMITED; WO2009/93268; (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.509073-62-5,tert-Butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,509073-62-5

To a degassed solution of tert-butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate (2c, 4.1 g, 12.3 mmol, 1 equiv.) in anhydrous MeOH (40 mL) was added Pd/C (10% wt., dry; 600 mg). The reaction was sealed, fitted with a H2 balloon and then stirred for 3 h at room temperature. The reaction mixture was filtered through Celite and then concentrated to obtain the product 2d as a white foam (3.7 g, 12 mmol, 98% yield).

509073-62-5 tert-Butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate 2764459, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; DANA-FARBER CANCER INSTITUTE, INC.; GRAY, Nathanael S.; DOBROVOLSKY, Dennis; HUANG, Hai-Tsang; (182 pag.)WO2018/98288; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics