Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.118753-66-5,tert-Butyl 4-aminopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

(1) 4-Amino-1-tert-butoxycarbonylpiperazine (3.00 g), 4-fluoronitrobenzene (2.54 g) and N,N-diisopropylethylamine (8.82 g) were dissolved in N-methyl-2-pyrrolidone (30 mL), and the mixture was stirred at 80C for 18 hr. The reaction mixture was added to water and the mixture was extracted with ethyl acetate. The extract was washed with brine and dried. The solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography to give 1-tert-.butoxycarbonyl-4-(4-nitrophenyl)aminopiperidine (2.55 g) as a white solid.

118753-66-5, 118753-66-5 tert-Butyl 4-aminopiperazine-1-carboxylate 22029174, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; WELFIDE CORPORATION; EP1308439; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6,57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of Boc-piperazine (P/N: Lancaster L13363, 500 mg, 2.68 mmol) in DCM(30 ml) was added succinic anhydride (269 mg, 2.68 mmol). The reaction was stirred for 2 hours at ambient temperature. TLC analysis showed formation of succinylated Boc-piperazine (Rf= 0.50; 9:1:0.01 DCM-MeOH-AcOH, TLC developed by heating with 3% (w/v) solution of ninhydrin in EtOH). To this solution was added TFA (30 mL) and the mixture was then stirred for 1 h at ambient temperature. The volatile components of the mixture were removed under reduced pressure and the resulting oil dissolved in THF (30 mL) with minimum amount of water and adjustment of the pH to 9 by the addition of DIPEA. A solution of Fmoc-OSu (907 mg, 2.69 mmol) in THF (10 mL) was added and stirred for 1 h at ambient temperature. TLC analysis showed formation of a product (Rf = 0.55; 9:1:0.01 DCM-MeOH-AcOH, UV 254 nm, TLC developed by heating with 3% (w/v) solution of ninhydrin in EtOH). The volatile components of the mixture were then removed under reduced pressure and the resulting oil was dissolved in minimum volume of saturated NaHCO3. The aqueous solution was then extracted with Et2O (100 mL x 2), acidified (pH ~1) with HCI (1 M) and re-extracted with EtOAc (150 mL x 2). The combined EtOAc layers were dried over Na2SO4 and concentrated to give the product as colorless oil.

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; APPLERA CORPORATION; WO2007/87534; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 8benzyl 2-(4-isopropylpiperazine-1-carbonyl)-7-azaspiro[3.5]nonane-7-carboxylate Oxalyl chloride (2.39 mL, 27.3 mmol) was slowly added to a solution of Intermediate 5 (2.77 g, 9.13 mmol) in DCM (70 mL) at 0¡ã C. under N2. One drop of DMF was added and the reaction mixture was stirred for 2 h. Oxalyl chloride (1.59 mL, 18.2 mmol) was added and the reaction mixture was stirred for 1 more hour. The solvent was concentrated under vacuum and the residue was recovered in DCM (30 mL). The resulting solution was added to a solution of 1-isopropylpiperazine (1.171 g, 9.13 mmol) and Et3N (6.36 mL, 45.66 mmol) in DCM (150 mL) at 0¡ã C. The reaction mixture was stirred for 1 h. The solvent was concentrated and the product was purified on silica gel by MPLC using 3percent-5percent MeOH in DCM as eluent to provide title compound (1.810 g, 47.9percent) as a gum. 1H NMR (400 MHz, CDCl3) delta ppm 1.03 (d, J=6.25 Hz, 6H) 1.52 (br. s., 2H) 1.61 (br. s., 2H) 1.94-2.07 (m, 2H) 2.08-2.18 (m, 2H) 2.39-2.52 (m, 4H) 2.70 (quintet, J=6.54 Hz, 1H) 3.18 (qd, J=8.66, 8.40 Hz, 1H) 3.29-3.40 (m, 4H) 3.40-3.49 (m, 2H) 3.57-3.65 (m, 2H) 5.11 (s, 2H) 7.28-7.42 (m, 5H); MS m/z 414.3 [M+H]+ (ESI).

4318-42-7, The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; US2010/130477; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

3022-15-9, Piperazine-2-carboxylic acid dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Piperazine-2-carboxyilc acid dihydrochloride (15.0 g, 73.9 mmol) was dissolved in H2O (240 mL) and 1,4-dioxane (360 mL), and the solution was brought to pH 10 with 6 N NaOH in H2O. Di-tert-butyldicarbonate (28.3 g, 162 mmol) was added while maintaining the pH at 10 with 6 N NaOH in H2O. After 2 h, the reaction mixture was extracted with Et2O (3 x 200 mL). The aqueous layer was brought to pH 3 with 6 N HCl and was extracted with EtOAc (4 x 300 mL). The combined EtOAc extracts were dried over Na2SO4, filtered, and concentrated under reduced pressure to give 14.45 g (59%) of the desired product as an off- white solid. The material was used without further purification. LC-MS: RT = 8.16 min; [M+Na]+ = 353.1., 3022-15-9

The synthetic route of 3022-15-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CRITICAL THERAPEUTICS, INC.; WO2007/146066; (2007); 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

A solution of methyl 4-(((3-chloro-N-phenylpropyl)sulfonamido)methyl)benzoate (0.500 g, 1.309 mmol), (2R,6S)-2,6-dimethylpiperazine (0.299 g, 2.6 19 mmol) and potassium carbonate (0.27 1 g, 1.964 mmol) in N,N-dimethylformide (3 mL) was stuffed at 80 ¡ãC for 18 hr and cooled down to the room temperature to terminate the reaction. Then, water was added to the reaction mixture, followed by extraction with ethyl acetate. The organic layer was washed with aqueous saturated sodium chloride solution, dried with anhydrous MgSO4, filtered, and concentrated in vacuo. The residue was chromatographed (Si02, 4 g cartridge; methanol / dichloromethane = 0 percent to 10 percent) to give methyl4-(((3-((3R,5S)-3 ,5-dimethylpiperazin- 1 -yl)-N-phenylpropyl) sulfonamido)methyl)benz oate as white solid (0.5 15 g, 85.6 percent)., 21655-48-1

21655-48-1 cis-2,6-Dimethylpiperazine 6950261, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; LEE, Jaekwang; HAN, Younghue; KIM, Yuntae; CHOI, Daekyu; MIN, Jaeki; BAE, Miseon; YANG, Hyunmo; KIM, Dohoon; (644 pag.)WO2017/18803; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

170911-92-9, tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0174] A mixture of intermediate 31 (0.20 g, 0.70 mmol) and 4-(4-amino-phenyl)- piperazine-1-carboxylic acid tert-bntyl ester (0.22 g, 0.79 mmol) in acetic acid (4 mL) was sealed in a microwave reaction tube and irradiated with microwave at 150 C for 15 min. After cooling to room temperature, the cap was removed and the mixture concentrated. The residue was purified by HPLC and the corrected fractions combined and poured into saturated NaHCO3 solution (40 mL). The combined aqueous layers were extracted with EtOAc (2 x 30 mL) and the combined organic layers washed with brine, dried over anhydrous Na2SO4 and filtered. The filtrate was concentrated and the resulting solid dissolved in minimum amount of EtOAc and hexanes added until solid precipitated. After filtration, the title compound was obtained as an off white solid (0.10 g, 33%).[0175] 1H NMR (500 MHz, DMSO-d6): delta 2.10 (s, 3H), 3.16 (s, 8H), 3.73 (s, 3H), 6.83 (d, J= 9.0 Hz, 2H), 7.29 (d, J= 8.8 Hz, IH), 7.44 (dd, J = 8.7, 2.1 Hz, IH), 7.49-7.52 (m, 3H), 7.88 (s, IH), 8.32 (s, IH), 8.81 (s, IH) MS (ES+): m/z 425 (M+H)+.

170911-92-9, As the paragraph descriping shows that 170911-92-9 is playing an increasingly important role.

Reference£º
Patent; TARGEGEN, INC.; WO2007/53452; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

57260-71-6, Adding aniline, piperazine-1-carboxylic acid tert-butyl ester, acridine salt visible light catalyst, 2,2,6,6-tetramethylpiperidine-nitrogen-oxide to anhydrous dichloroethane,The reaction environment was then replaced with oxygen three times and irradiated with a blue LED for a reaction time of 10 h.After the reaction is completed, the filtrate is spun dry and separated by column chromatography.The title product was obtained as a colorless white solid, yield 95%.

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Shenzhen Lan Xin Technology Co., Ltd.; Huang Yong; Han Keheng; Zhou Haipeng; Zhang Qiang; Han Hui; Ding Xiaomei; Wang Leifeng; (7 pag.)CN108440451; (2018); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 13 Preparation of 4-(4-Isopropyl-piperazin-1-yl)-2-methyl-7-nitro-2,3-dihydro-isoindol-1-one To a suspension of 4-fluoro-2-methyl-7-nitro-2,3-dihydro-isoindol-1-one (5.0 g, 24 mmol) and potassium carbonate (3.32 g, 24 mmol), triethylamine (6.7 mL, 28.8 mmol) in dimethylsulfoxide (50 mL), 1-isopropyl piperazine (4.1 mL, 28.8 mmol) is added and the mixture is stirred at 60¡ã C. for 4 hours. The mixture is poured into iced water, and the resulting brown solids are collected by filtration and dried in vacuo at 50¡ã C. to afford 4-(4-Isopropyl-piperazin-1-yl)-2-methyl-7-nitro-2,3-dihydro-isoindol-1-one as brown solids in 91percent yield. Rf=0.14 (AcOEt). 1H-NMR (400 MHz, CDCl3, delta, ppm): 1.09 (s, 3H), 1.11 (s, 3H), 2.70 (t, 4H), 2.80-2.74 (m, 1H), 3.19 (s, 3H), 3.21 (t, 4H), 4.37 (s, 2H), 7.01 (d, 1H), 7.78 (d, 1H).

4318-42-7, The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Kawahara, Eiji; Miyake, Takahiro; Roesel, Johannes; US2008/293708; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1030377-21-9, (S)-1-Boc-2-(Hydroxymethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,1030377-21-9

To (S)-2-hydroxymethyl-piperazine-1 -carboxylic acid fe/t-butyl ester (2.00 g, 9.25 mmol) in DMA (10 mL) is added ie f-butyl-chloro-dimethyl-silane (2.09 g, 13.9 mmol) and imidazole (1 .89 g, 27.7 mmol), and the reaction mixture is stirred for 24 h at rt. The reaction mixture is diluted with NH4CI-solution and extracted with EtOAc. The organic layer is washed with water and brine, dried over Na2S04, filtered and concentrated under reduced pressure. The residue is purified by silica gel column chromatography to give the title compound. (0573) Yield: 2.80 g (92%)

1030377-21-9 (S)-1-Boc-2-(Hydroxymethyl)piperazine 22884145, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HYDRA BIOSCIENCES, INC.; BOUYSSOU, Thierry; GOTTSCHLING, Dirk; HEINE, Niklas; SMITH KEENAN, Lana Louise; LOWE, Michael D.; RAZAVI, Hossein; SARKO, Christopher Ronald; SURPRENANT, Simon; TAKAHASHI, Hidenori; TURNER, Michael Robert; WU, Xinyuan; (182 pag.)WO2019/81637; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1001180-21-7, (R)-tert-Butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 9:; Triethylamine (4.33 ml, 31.1 mmol; degassed with nitrogen 30 minutes prior to use) and formic acid (1.36 ml, 36.1 mmol; degassed with nitrogen 30 minutes prior to use) were added to a solution of (R)-tert-butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H- cyclopenta[d]pyrimidin-4-yl)piperazine-l -carboxylate (9.75 g, 29.3 mmol) in DCM (210 mL; degassed with nitrogen 30 minutes prior to use). The mixture was stirred for 5 minutes, then a Ru catalyst (0.0933 g, 0.147 mmol) was added. The reaction was stirred under positive nitrogen pressure overnight (18 hours). The reaction mixture was concentrated to dryness and dried on high vacuum. The impure material was flashed on Biotage 65M loaded 1:1 DCM:ethyl acetate 500 mL flushed, then 1 :4 DCM:ethyl acetate until product (2nd spot), then gradient to neat ethyl acetate, then 25:1 DCM:MeOH eluted rest of product. The fractions were combined and concentrated on a rotary evaporator. The residue was concentrated again from DCM/hexanes to give a mixture of tert-butyl 4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine- 1-carboxylate (major) and tert-butyl 4-((5R,7S)-7-hydroxy-5-methyl-6,7-dihydro-5H- cyclopenta[d]pyrimidin-4-yl)piperazine-l -carboxylate (minor) (9.35 g, 95.3% yield) as a beige foam. LC/MS (APCI+) m/z 335 [M+H]+. IH NMR (CDC13) shows 88% de by integration of carbinol methine.

1001180-21-7, The synthetic route of 1001180-21-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ARRAY BIOPHARMA INC.; GENENTECH, INC.; MITCHELL, Ian, S.; BLAKE, James, F.; XU, Rui; KALLAN, Nicholas, C.; XIAO, Dengming; SPENCER, Keith, Lee; BENCSIK, Josef, R.; LIANG, Jun; SAFINA, Brian; ZHANG, Birong; CHABOT, Christine; DO, Steven; WO2008/6040; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics