Heterocyclic Building Blocks-piperazine

630125-91-6,630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 4-chloro-3-nitrobenzoic acid (1.0 g, 4.97 mmol) in dichioromethane(10 mL) were added oxalyl chloride (500 jiL, 5.30 mmol) followed by catalytic amount ofDMF and the mixture was stirred at RT for 2 h. The mixture was concentrated under reducedpressure and the residue was dissolved in dichloromethane. The solution was cooled to 0 C;4-((4-ethylpiperazin- 1 -yl)methyl)-3 -(trifluoromethyl)aniline (Intermediate Cl) (1.0 g, 3.30mmol) was added to the reaction mixture followed by DIPEA (1.5 mL, 8.30 mmol). The resultant mixture was stirred overnight at RT. The mixture was diluted with water and extracted twice with ethyl acetate. The combined organic extracts were washed with saturated sodium bicarbonate solution, water and brine. The solution was dried over anhydrous sodiumsulfate, filtered and concentrated. The residue thus obtained was purified by columnchromatography to yield 1.43 g of the desired product. ?H NMR (400 MHz, DMSO-d6) oe0.98 (t, J 7.2 Hz, 3H), 2.28-2.39 (m, 1OH), 3.57 (s, 2H), 7.74 (d, J 8.4 Hz, 1H), 7.98-8.04(m, 2H), 8.16 (s, 1H), 8.27 (dd, J, = 2.4 Hz, J2 = 8.4 Hz, 1H), 8.65 (s, 1H), 10.77 (s, 1H).

The synthetic route of 630125-91-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLENMARK PHARMACEUTICALS S.A.; PATEL, Vinod; REDDY, Venkateshwar; GHARAT, Laxmikant Atmaram; CHAUDHARI, Sachin Sundarlal; DAS, Sanjib; VELGALETI, Ranganadh; SHAH, Daisy Manish; BAJPAI, Malini; (262 pag.)WO2018/215668; (2018); 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.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 97 3-(2-chlorophenyl)-7-methylsulfanyl-2H-pyrimido[5,4-e][1,3]oxazin-4-one (130 mg, 0.423 mmol, 1.0 eq) in 5 mL of 24 toluene was added 25 m-CPBA (224 mg, 0.84 mmol, 2.0 eq) and stirred at rt for 30 min. 66 Tert-butyl 4-(4-aminophenyl)piperazine-1-carboxylate (117 mg, 0.423 mmol, 1.0 eq) and 27 DIPEA (163 mg, 1.27 mmol, 3.0 eq) were added and allowed to stir at rt for 12 h. Reaction was monitored by LCMS. After completion of reaction, solvent was removed under reduced pressure. Residue was diluted with saturated NaHCO3 solution and extracted with CH2Cl2 (100 mL¡Á2). Combined organic layer was washed with brine solution (50 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure to give crude product which was purified by flash chromatography to afford 100 tert-butyl 4-[4-[[3-(2-chlorophenyl)-4-oxo-2H-pyrimido[5,4-e][1,3]oxazin-7-yl]amino]phenyl]piperazine-1-carboxylate (120 mg, 52.8%). LCMS: 296 [M+1]+, 170911-92-9

The synthetic route of 170911-92-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; giraFpharma LLC; Chakravarty, Sarvajit; PHAM, Son Minh; Kankanala, Jayakanth; AGARWAL, Anil Kumar; PUJALA, Brahmam; SONI, Sanjeev; ARYA, Satish K.; PALVE, Deepak; KUMAR, Varun; (360 pag.)US2019/106436; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 29 Preparation of 6-(2-carbamoyl-4-methylpiperazin-l-yl)-2-(4-(4- (trifluoromethyl) phenoxy)phenyl)pyrimidine-4-carboxamide (Cpd No. 81) Scheme 61 1 -tert-butyl 3-methyl 4-(2-chloro-6-(methoxycarbonyl)pyrimidin-4-yl)piperazine- 1 ,3-dicarboxylate: A mixture of 1-tert-butyl 3-methyl piperazine-l ,3-dicarboxylate (5.133 g, 21.01 mmol), methyl 2,6-dichloropyrimidine-4-carboxylate (4.354 g, 21.03 mmol), and iPr2NEt (4.0 mL, 23.0 mmol) in acetonitrile (50 mL) was heated at 50C for 4 h. After cooling, the reaction mixture was evaporated in vacuo and the residue chromatographed over silica gel with 20-70% EtOAc in hexanes. The product fractions were evaporated in vacuo to give 1-tert-butyl 3-methyl 4-(2-chloro-6- (methoxycarbonyl)pyrimidin-4-yl)piperazine-l,3-dicarboxylate as a very pale yellow powder (6.626 g, 15.97 mmol, 76% yield). LC/MS: m/z= 415.2 [M+H]+., 129799-08-2

The synthetic route of 129799-08-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PURDUE PHARMA L.P.; NI, Chiyou; PARK, Minnie; SHAO, Bin; TAFESSE, Laykea; YAO, Jiangchao; YOUNGMAN, Mark; WO2013/30665; (2013); 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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution of 2-CHLORO-5-METHANESULFONYL-BENZOIC acid (102mg, 0.43 mmol) in dimethylformamide (20 ml) were successively added TBTU (153mg, 0.48 mmol), N- ETHYLDIISOPROPYLAMINE (0.28 ML, 2.17 mmol) and 1- (4-TRIFLUROMETHYLPHENYL) piperazine (ABCR F07741NB, [30459-17-7], 100 mg, 0.43 mmol). The reaction was then stirred at room temperature for two hours, then concentrated in vacuo and purified by column chromatography (SI02, 50g, heptane/ethylacetate = 0 to 100%), to give the title compound as a colorless gum (170 mg, 0.38 mmol). MS (m/e): 464.3 (M+NH4+, 100%), 30459-17-7

30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; WO2005/23260; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

208167-83-3, tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(a) Preparation of N-[1-butyl-4-[3-{2-(4-tert-butoxycarbonyl-1-piperazinyl)ethoxy}phenyl]-1,2-dihydro-2-oxo-1,8-naphthyridin-3-yl]-N’-(2,6-diisopropylphenyl)urea STR99 The title compound was obtained in the same manner as in Example 41 from N-[4-(3-hydroxyphenyl)-1,2-dihydro-2-oxo-1,8-naphthyridin-3-yl]-N’-(2,6-diisopropylphenyl)urea and 1-tert-butoxycarbonyl-4-(2-chloroethyl)piperazine. 1 H-NMR delta (CD3 OD) 8.63 (1H, dd, J=4.6 Hz, 1.7 Hz), 7.75 (1H, dd, J=7.9 Hz, 1.7 Hz), 7.47 (1H, dd, J=8.2 Hz, 7.9 Hz), 7.04-7.30 (5H, m), 6.93-7.04 (2H, m), 4.60-4.73 (2H, m), 4.05-4.10 (2H, m), 3.38-3.53 (4H, m), 2.92-3.10 (2H, m), 2.55-2.68 (2H, m), 2.36-2.54 (4H, m), 1.95-2.10 (2H, m), 1.70-1.90 (2H, m), 1.45-1.62 (2H, m), 1.49 (9H, s), 1.15 (12H, d, J=6.6 Hz), 1.05 (3H, t, J=7.3 Hz)

208167-83-3, The synthetic route of 208167-83-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Sumitomo Pharmaceuticals Company, Ltd.; US5843957; (1998); A;,
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.115761-79-0,1-(2,4-Difluorophenyl)piperazine,as a common compound, the synthetic route is as follows.

The dimethyl acetal intermediate (40 mg, 0.13 mmol) from subpart (a) above was suspended in 2 mL of CH2Cl2 and 0.2 mL of 2: 1 solution of TFA/H2O was added. The resulting reaction mixture was stirred at room temperature for 4 hours. It was then neutralized with 0.25 mL of triethylamine. 1-(2,4-Difluoro-phenyl)-piperazine (40 mg, 1.5 eq. , prepared by reacting piperazine with 1-bromo-2,4-difluorobenzene according to the procedure described in WO 01/92264 A1), was added, followed by 140 mg of Na(OAc)3BH. The resulting reaction mixture was stirred at room temperature for 2 hours. It was then concentrated and then purified by preparative HPLC to afford N5-{2-[4-(2,4-difluoro-phenyl)-piperazin-1-yl]-ethyl}-2-furan-2-yl-[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7-diamine. 1H NMR (DMSO-d6) delta 7.90 (br s, 2 H), 7.80 (d, J = 1.0 Hz, 1 H), 7.05 (d, J = 3.6 Hz, 1 H), 7.10-7.50 (m, 3 H), 6.68 (dd, J = 3.6 Hz, 1.0 Hz, 1 H) 3.20-2.75 (m, 12 H) ppm. MS: m/z: 442 [M + H] +., 115761-79-0

115761-79-0 1-(2,4-Difluorophenyl)piperazine 2734637, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BIOGEN IDEC MA INC.; WO2004/92170; (2004); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21655-48-1, cis-2,6-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of the compound obtained in step a (120 mg, 0.42 mmol) in DCE (2 mL), DIPEA (166 mg, 1 .28 mmol), c/’s-2,6-dimethylpiperazine (122 mg, 1 .06 mmol) and NaBH(OAc)3 (181 mg, 0.85 mmol) were added and the mixture was stirred at rt for 16 h. NaHCC>3 sat solution was added, extracted with DCM and the organic layer was concentrated under vacuum. Purification by flash chromatography, silica gel, gradient Hex to 100% acetone afforded the title product (126 mg, 78% yield). HPLC (Method B): Ret, 4.10 min; ESI+- MS m/z, 379.1 (M+H).

21655-48-1, The synthetic route of 21655-48-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ESTEVE PHARMACEUTICALS, S.A.; ALMANSA-ROSALES, Carmen; CUEVAS-CORDOBES, Felix; (77 pag.)WO2019/77106; (2019); 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.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

57260-71-6, A mixture of compound tert-butyl piperazine-1 carboxylate (3.725 g, 20 mmol) and potassium carbonate (5.53 g, 40 mmol) in anhydrous dichloromethane (30 mL) was cooled to 0 C., cyclopropanecarbonyl chloride (2.30 g, 22 mmol) was then added dropwise. After the addition, the mixture was stirred at room temperature overnight. The mixture was diluted with dichloromethane (100 mL), washed with 10% citric acid (50 mL), followed by saturated sodium bicarbonate (50 mL), brine (100 mL), dried over anhydrous sodium sulfate, and concentrated to give tert-butyl 4-(cyclopropanecarbonyl)piperazine-1-carboxylate (3.7 g, yield 73%) as a white solid. 1H-NMR (400 MHz, CDCl3) delta (ppm): 0.76-0.81 (m, 2H), 0.98-1.03 (m, 2H), 1.49 (s, 9H), 1.69-1.75 (m, 1H), 3.46-3.48 (m, 4H), 3.63-3.65 (m, 4H); LC-MS (ESI) m/z: 255(M+1)+.

As the paragraph descriping shows that 57260-71-6 is playing an increasingly important role.

Reference£º
Patent; LEAD THERAPEUTICS, INC.; US2010/35883; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

252990-05-9, Methyl (R)-1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Lithium aluminium hydride (1M in THF, 26 ml) was added to a solution of L-TERT- butyl 2-methyl (2R)-piperazine-1, 2-dicarboxylate (2. 55 g) in THF (70 ml) AT-40C, then the reaction was warmed to room temperature. The solution was stirred for 1 hour, then cooled to 0C and quenched by sequential addition of water (1 ml), sodium hydroxide (2N, 1 ml) and then water (2 ml). The resulting slurry was filtered and concentrated in vacuo to give TERT- butyl (2R)-2-(hydroxymethyl) piperazine-1-carboxylate (2.37 g, > 100%); NMR spectrum (DMSO-d6,373K) 1.40 (s, 9H), 2.58 (m, 1H), 2. 82 (M, 3H), 2. 92 (bs, 1H), 2.98 (d, 1H), 3.43 (m, 1H), 3.65 (M, 2H), 3.80 (M, 1H) ; Mass spectrum MH+ 217.

252990-05-9, The synthetic route of 252990-05-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/26152; (2005); 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