Month: September 2021

169447-86-3, (S)-tert-Butyl 2-benzylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparative Example beta; Preparation of 2-[(S)-4-Boc-3-benzylpiperazinyl]-6-chloropyrazine 115; To a solution of 2,6-dichloropyrazine 114 (0.1 g, 0.67 mmol.) and (S)-1-Boc-2- benzylpiperazine 107 (0.37 g, 1.34 mmol) in dioxane (2 mL) and trifluoromethylbenzene (2 mL) was added diisopropylethylamine (0.26 g, 2.0 mmol). The reaction mixture was heated in a microwave reactor at 1800C for 20 minutes. Ethyl acetate (100 mL) was added. The organic layer was washed with saturated ammonium chloride solution, water and brine. The organic layer was dried over sodium sulfate. The organic solvent was evaporated under reduced pressure. The crude product was purified by flash column chromatography to yield the desired 2- [(S)-4-Boc-3-benzylpiperazinyl]-6-chloropyrazine 115 (0.234 g, 0.6 mmol).

169447-86-3, As the paragraph descriping shows that 169447-86-3 is playing an increasingly important role.

Reference：
Patent; SCHERING CORPORATION; WO2007/126964; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

59878-57-8, General procedure: Compounds 1a-l and compounds 15-19 were synthesized in the same reaction: In a dichloromethane solution (2-3 mL) of chloroacetylchloride(1.1 eq), a dichloromethane solution (8-10 mL) of the appropriate piperazine (1 eq) and triethylamine (2.5 eq) was added dropwise and the reaction mixture was stirred overnight at room temperature under a nitrogen atmosphere. The reaction mixture was evaporated and the residue was extracted with ethylacetate-brine. The organic layer was dried over Na2SO4 and chromatographed on silica preparative TLC to give the desired products.When the reaction was run for 2 h, compounds 1a-l were the mainproducts (>90%).

The synthetic route of 59878-57-8 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Papadopoulou, Maria V.; Bloomer, William D.; Rosenzweig, Howard S.; O’Shea, Ivan P.; Wilkinson, Shane R.; Kaiser, Marcel; European Journal of Medicinal Chemistry; vol. 103; (2015); p. 325 – 334;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 7-benzyl-2,4-dichloro-6,8-dihydro-5H-pyrido [3,4-d] pyrimidine (5.00 g, 17.0 mmol) and 1-tert-butyl 2-methylpiperazine-1,2-dicarboxylate (4.24 g, 17.3 mmol) in DMSO (80 mL) was added DIEA (5.49 g, 42.5 mmol, 7.42 mL). After stirring at 55° C. for 12 hours, the mixture was diluted with ethyl acetate (100 mL), washed with brine (3 150 mL), dried over Na 2SO 4, filtered and concentrated under vacuum. The residue was purified by column chromatography (SiO 2, PE/EA=3/1) to give 1-tert-butyl 2-methyl 4-(7-benzyl-2-chloro-6,8-dihydro-5H-pyrido[3,4-d] pyrimidin-4-yl)piperazine-1,2-dicarboxylate (8.00 g, 15.9 mmol, 93.8% yield) as a yellow oil. ES+APCI MS m/z 502.1[M+H] +.

129799-15-1, As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference：
Patent; Mirati Therapeutics, Inc.; Array BioPharma Inc.; Blake, James F.; Burgess, Laurence E.; Chicarelli, Mark Joseph; Christensen, James Gail; Cook, Adam; Fell, Jay Bradford; Fischer, John P.; Marx, Matthew Arnold; Mejia, Macedonio J.; Savechenkov, Pavel; Vigers, Guy P.A.; Smith, Christopher Ronald; Rodriguez, Martha E.; US2019/144444; (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.13754-38-6,1-Benzoylpiperazine,as a common compound, the synthetic route is as follows.

13754-38-6, Example 18 N-{[1-(2-(4-benzoylpiperazine-1-yl)propane-1-yl)-pyrrolidine-(3R)-yl-carbamoyl]-methyl}-3-trifluoromethylbenzamide 400 mg (1 . 07 mmol) N-{[1-(2-hydroxypropyl)-pyrrolidine-(3R)-yl-carbamoyl]-methyl}-3-trifluoromethylbenzamide and 0.18 ml (1.29=01, 1.2 eq.) triethylamine described at manufacturing example 6 were dissolved to 20 ml dichloromethane and cooled to 3 C. under argon gas. 135 mg (1.18 mmol, 1.1 eq.) methansulfonyl chloride was slowly added to reaction solution and was stirred at same temperature for 30 min. 20 ml purified water was added and then organic layer was separated and concentrated with decompression. After 10 ml acetonitrile were added to obtained residues and dissolved them, 444 mg (3.21 mmol) potassium carbonate and 202 mg (1.06 mmol) 1-benzoylpiperazine were added. After stirring for 2 hours at room temperature, 15 ml saturated sodium chloride aqueous solution was added to reaction solution and was extracted twice with 15 ml ethylacetate. After organic layer was collected and dried with anhydrous magnesium sulfate, it was concentrated with decompression. 30 mg (51%) target compound as light-yellow solid was yielded by purifying obtained residues with chromatography using silicagel (mobile phase:dichloromethane/methanol=5:1 and 1:1). 1H NMR (400 MHz, DMSO-d6) 1.05 (3H, s), 1.55-1.65 (1H, m), 2.00-2.10 (1H, m), 2.15-2.25 (1H, m), 2.28-2.55 (9H, m), 2.70-2.85 (2H, m), 3.17 (1H, d), 3.54-3.65 (2H, m), 3.87 (2H, d), 4.10-4.20 (1H, m), 7.35-7.40 (2H, m), 7.40-7.47 (3H, m), 7.74 (1H, t), 7.92 (1H, d), 8.14 (1H, s), 8.18 (1H, d), 8.23 (1H, s), 9.01 (1H, t) MS (M)+ 545.6

The synthetic route of 13754-38-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; YANG JI CHEMICAL CO., LTD.; US2012/190689; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

4-Methyl-l-piperazinecarbonyl chloride hydrochloride (19.9 mg, 0.1 mmol) was added to a solution of 16 (20 mg, 0.05 mmol) and anhydrous pyridine (25 muml, 0.3 mmol) in 3% allyl alcohol in dry methylene chloride (4 ml) and the mixture was stirred for 16 h. Purification of the crude product on silica gel yielded 17 (23.6 mg, 91%). 1NMRDMSOd6) delta 12.03 (s, IH), 8.41 (s, IH), 8.21 (s, IH), 8.01 (d, IH, J=8.4 Hz), 7.88 (d, IH, J=8.4 Hz), 7.82 (dd, IH, J=8.4 Hz), 7.58 (t, IH, J=8.1 Hz), 7.51 (d, IH, J=8.4 Hz)5 7.46 (t, IH, J=7.6 Hz), 7.37 (s, IH), 4.86 (t, IH, J=10.8 Hz), 4.57 (dd, IH, J=10.8 Hz), 4.38 (in, IH), 4.06 (dd, IH, J=I 0.8 Hz), 3.86 (dd, IH, J=I 1 Hz), 3.41 (br, 4H), 3.29 (br, 4H), 2.82 (s, 3H), 2.57 (s, 3H).

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

Reference：
Patent; MEDAREX, INC.; WO2007/51081; (2007); 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.244132-27-2,(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

To a solution of 2-[4-(4-amino-phenylethynyl)-l-methyl-lH-pyrazol-3-yl]-4- chloro-phenol 4C (3.24 g, 10 mmol) in methylene chloride (250 mL) was added acid 3 (5.43 g, 12 mmol) and diisopropylcarbodiimide (2.3 mL, 15 mmol) at rt. The reaction was stirred at ambient temperature overnight. The solvent was removed under vacuum and the residue was purified on column to give 6.5 g of product in 86percent yield.

244132-27-2, 244132-27-2 (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid 7128304, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; XTL BIOPHARMACEUTICALS LTD; WO2008/48589; (2008); A2;,
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

To a 250 mL round bottom flask was added 5 g (18.1 mmol) of crude I-f,Nitro-lH-pyrazole-3-carboxylic acid (3.1 g, 19.9 mmol)EDC · HCl 4.1 g (21.7 mmol),HOBt 2.9 g (21.7 mmol) and anhydrous DMF 50 mL,Stir at room temperature for 24 hTLC detects the disappearance of the starting material (methanol: chloroform = 1:10).The reaction solution was poured into 200 mL of ice water,Precipitation of a large number of light yellow solid, standing,Consider the yellow solid,The crude product was recrystallized from a mixed solvent of ethyl acetate and methanol to give 4.7 g of (I-g)Yield 62.4%., 170911-92-9

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

Reference：
Patent; China Pharmaceutical University; Lu Shuai; Wang Yue; Zhi Yanle; Yao Chao; Lu Tao; Li Baoquan; Chen Puzhou; Bao Jiyin; (27 pag.)CN107245073; (2017); 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.38216-72-7,1-tert-Butylpiperazine,as a common compound, the synthetic route is as follows.

A. Synthesis of l-(4-(4-fert-butylpiperazin-l-yl)(phenyl)methyl)piperidin-l-yl)ethanone; [0092] 1-tert-butylpiperazine (4.48 g, 20.8 mmol), l-(4-(chloro(phenyl)methyl)piperidin-l-yl)ethanone (5.77 g, 22.9 mmol), K2CO3 (7.2 g, 52.1 mmol), and KI (22.9 mmol) were combined in dry DMF (150 mL). The reaction was refluxed overnight. Upon completion of the reaction, the DMF was removed under reduced pressure. The resulting crude was taken up in water (75 mL) and washed with EtOAc (3 x 100 mL). The organic portions were combined, dried (Na2SO4) and concentrated. The product was purified by silica gel chromatography (2.5:2.5:95 Et3N/MeOH/EtOAc, Rf 0.4) and isolated as a red oil (2.66 g, 36%).

38216-72-7, 38216-72-7 1-tert-Butylpiperazine 3530572, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; NEUROMED PHARMACEUTICALS LTD.; WO2008/31227; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5464-12-0, Compound 132 was synthesized according to the following production scheme.

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SBI BIOTECH CO., LTD.; CRYSTALGENOMICS, INC.; US2011/190299; (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.132710-90-8,1-Boc-4-(3-hydroxypropyl)piperazine,as a common compound, the synthetic route is as follows.

Triphenylphosphine (2.059 g, 7.85 mmol), tert-buty 4-(3-hydroxypropyl)piperazine-l- carboxylate (1.692 g, 6.93 mmol) and diisopropyl (E)-diazene-l,2-dicarboxylate (1.587 g, 7.85 mmol) were mixed in THF (20 mL) at 0 C, and then 4-chloro-3-hydroxy-5-nitrobenzamide (1 g, 4.62 mmol) was added. The reaction solution was maintained at RT for 16 hrs then the brown reaction solution was partitioned between sat. NaHC03 (aq) and EtOAc. The organic layer was washed with brine, dried over MgSCM, concentrated and purified on silica gel (20 %- 80 % (3:1 EtOAc/EtOH) / Hexane, with 2% NH4OH; 330 g RediSep column). Desired fractions were combined and concentrated to give the title compound as a white solid (970 mg, 47 % yield). *H NMR (400 MHz, DMSO-t) delta ppm 8.30 (s, 1 H), 8.05 (d, 3=1.77 Hz, 1 H), 7.88 (d, J=1.77 Hz, 1 H), 7.80 (s, 1 H), 4.28 (t, J=6.21 Hz, 2 H), 3.31 (br. s., 4 H), 2.48 (t, J=7.10 Hz, 2 H), 2.33 (t, J=4.94 Hz, 4 H), 1.96 (t, J=6.59 Hz, 2 H), 1.40 (s, 9 H). LCMS (LCMS Method K): Rt = 0.69 min, [M+H]+ = 443.4.

132710-90-8, As the paragraph descriping shows that 132710-90-8 is playing an increasingly important role.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; CHARNLEY, Adam Kenneth; DARCY, Michael G.; DODSON, Jason W.; DONG, Xiaoyang; HUGHES, Terry V.; KANG, Jianxing; LEISTER, Lara Kathryn; LIAN, Yiqian; LI, Yue; MEHLMANN, John F.; NEVINS, Neysa; RAMANJULU, Joshi M.; ROMANO, Joseph J.; WANG, Gren Z.; YE, Guosen; ZHANG, Daohua; (451 pag.)WO2017/175147; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics