Tag: M.W:200-300

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.

General procedure: To a solution of acid chloride 3a-b (1.0 equiv.), triethylamine (3.0 equiv.) in dry THF, was added arylpiperazines (1.2 equiv.) in dry THF dropwise. The mixture was stirred for 1 h at room temperature. The reaction mixture was diluted with EtOAc, washed with water and brine, dried over anhydrous MgSO4, and concentrated in vacuo. The crude product was purified by flash column chromatography on silica gel (EtOAC:hexanes = 1:1-1:5) to yield the desired products (4a-j). Compound 4d: 1H NMR (300 MHz, CDCl3) delta 7.52 (d, J = 8.6 Hz, 2H), 6.95 (d, J = 8.6 Hz, 2H), 3.92 (m, 4H), 3.37 (s, 4H), 3.03 (m, 2H), 2.56 (m, 1H), 2.35 (m, 1H), 2.13 (m, 1H), 1.34 (m, 2H), 0.96 (s, 9H).

30459-17-7, The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Song, Jiho; Lee, Kiho; Kim, Doran; Kim, Jongmin; Lee, Seul; Shin, Jun Seob; Kim, Dong-Seok; Min, Kyung Hoon; Bulletin of the Korean Chemical Society; vol. 35; 2; (2014); p. 666 – 668;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

694499-26-8, A solution of 2 ml trimethylaluminium (2 M in toluene, 4 mMol) is added to a stirred solution of 355 mg (1.3 mMol) 4-(4-methyl-piperazin-1-ylmethyl)-3- trifluoromethyl-phenylamine in 20 ml toluene at 10 0C under an argon atmosphere. After 1 h at r t, a solution of 436 mg (1.3 mMol) 6-(6-acetylamino- pyrimidin-4-ylmethyl)-naphthalene-1-carboxylic acid methyl ester (Step 9.2) in 5 ml THF is added and the reaction mixture is heated at 90 0C for 45 min. After cooling to 5 0C, a solution of sat. aqueous ammonium chloride (50 ml) is added dropwise. The mixture is poured into EtOAc and filtered over hyflo. The separated aq. phase is extracted with EtOAc. The combined organic phases are washed with water and brine, dried (Na2SO4) and concentrated. The crude product is purified by chromatography (SiO2, CH2CI2 / EtOH/ NH3 90:9:1) and is recrystallised from hot EtOAc and hexane to afford the title compound as a colourless solid: m.p.: 202-2040C.

As the paragraph descriping shows that 694499-26-8 is playing an increasingly important role.

Reference：
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2007/104538; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

304897-49-2, tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-(4-Carboxy-phenyl)-thiazole-2-carboxylic acid, (100 mg, 0.4 mmol) was combined with HATU (304 mg, 0.8 mmol). This mixture was dissolved in 3 mL of DMF and DIEA (1.0 mmol, 0.17 mL) was added to the solution. Reaction mixture was stirred at room temperature for 30 minutes. To this was added 4-(4-amino-benzyl)-piperazine-l- carboxylic acid tert-butyl ester (233.1 mg, 0.8 mmol). Reaction mixture was heated at 6O0C overnight. The crude was purified using reverse phase HPLC to give the desired product.

304897-49-2, 304897-49-2 tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate 12045001, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; GENELABS TECHNOLOGIES, INC.; WO2008/154601; (2008); 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.278788-66-2,(R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

278788-66-2, To Intermediate I 3 (3.99 g, 21.7 mmol) was added tert-butyl (3i?)-3-(hydroxy- methyl)piperazine-l -carboxylate (5.21 g, 24 mmol), and the mixture was suspended in 1,4-dioxane (100 mL). To this was added DIPEA (4.6 mL, 26 mmol) and the mixture was heated at 80C for 1 h. Further DIPEA (9 mL) was added and the mixture was heated at 100C for 48 h. The reaction mixture was cooled to r.t. and concentrated in vacuo, to yield an orange solid which was triturated with water/ether/dichloromethane and filtered. The solid was discarded, and the filtrate was concentrated in vacuo. The resulting orange oil was purified by flash column chromatography on silica [Biotage SNAP 200g, Isolera, gradient elution (80% EtOAc/isohexanes to 100% EtOAc; followed by 100% DCM to 20% MeOH/DCM)], to yield the title compound (4.51 g, 57.1%) as a yellow oil. LCMS (ES+) 364.8 [M+H]+, RT 1.20 minutes (method 3).

278788-66-2 (R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820286, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; UCB PHARMA S.A.; KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&D; FORD, Daniel James; FRANKLIN, Richard Jeremy; GHAWALKAR, Anant Ramrao; HORSLEY, Helen Tracey; HUANG, Qiuya; REUBERSON, James Thomas; VANDERHOYDONCK, Bart; WO2014/96423; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

55121-99-8, (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

55121-99-8, A solution of 4-(4-methylpiperazine-1-carbonyl)aniline (1.03g, 4.56 mmol) in THF (50 mL) was cooled to 0C and LiAlH41 M in THF (14 mL, 14 mmol) was added dropwise. The mixture was let to warm to room temperature, and then refluxed for 3 h. After cooling to 0C Na2SO4.10H2O was added and the solution was filtered off. The solution was concentrated and purified by silica flash chromatography with 0 to 5% MeOH in DCM to give 4-[(4- methylpiperazin-1-yl)methyl]aniline (500 mg, 53% yield). MS found for C12H19N3 as (M+H)+ 206.3.

The synthetic route of 55121-99-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; PHARMACYCLICS LLC.; ATALLAH, Gordana, Babic; CHEN, Wei; JIA, Zhaozhong, J.; POZZAN, Alfonso; RAVEGLIA, Lucal, Francesco; ZANALETTI, Riccardo; (815 pag.)WO2016/196776; (2016); 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.196811-66-2,tert-Butyl 4-carbamothioylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of tert-butyl 4-carbamothioylpiperazine-1-carboxylate (0.5 g, 2.08 mmol) in dioxane (10 mL), triethyl amine (0.22 mL, 2.6 mmol) and 2-bromo-1-phenylethan-1-one (0.52 g, 2.6 mmol) were added at rt. The resulting mixture was stirred at 90 C for 20 h. The completion of the reaction was monitored by TLC. It was diluted with water and extracted with EtOAc. The organic layer was separated, dried over anhydrous Na2SO4, concentrated under vacuum. The resulting crude product was taken as such for the next step. Yield: 86% (0.5 g, colorless liquid)., 196811-66-2

The synthetic route of 196811-66-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASCENEURON SA; QUATTROPANI, Anna; KULKARNI, Santosh S.; GIRI, Awadut Gajendra; (243 pag.)WO2016/30443; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

196811-66-2, tert-Butyl 4-carbamothioylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

196811-66-2, l-[5-methyl-4-(trifluoromethyl)-l,3-thiazol-2-yl]piperazine hydrochloride To a mixture of tert-butyl 4-(aminocarbonothioyl)piperazine-l-carboxylate (200 mg, 0.82 mmol) and 3-bromo-l,l,l-trifluorobutan-2-one (204 mg, 0.99 mmol) in xylene (20 mL) was added triethylamine (454 mul, 3.26 mmol). The reaction mixture was refluxed (140 0C) for 16 hours and concentrated in vacuo. Purification by column chromatography eluting with isohexane to 25% ethyl acetate / isohexane gave a cream solid (210 mg). This was stirred in methanol reagent 10 (15 mL) at room temperature for 16 hours. Reaction mixture was concentrated to dryness to give a pale yellow solid (230 mg) which was used crude directly in the next step (230 mg, > 100 % yield) MS (-ve ESI) : 252 (M-H)+

The synthetic route of 196811-66-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2009/1127; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

196811-66-2, tert-Butyl 4-carbamothioylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2-chloro-l-(4,5-dihydro-5-phenyl-3-isoxazolyl)ethanone (i.e. the product of Example 7, Step C) (0.450 g, 2.018 mmol) and 1,1-dimethylethyl 4-(amino- thioxomethyl)-l-piperazinecarboxylate (i.e. the product of Example 7, Step A) (0.5 g, 2.04 mmol) in ethanol (10 mL) was added triethylamine (0.204 g, 2.013 mmol), and the reaction mixture was stirred at room temperature for 12 h. The reaction mixture was concentrated 01464783 under reduced pressure, and the residue was partitioned between, ethyl acetate (30 mL) and water (30 mL). The organic layer was separated and washed with brine (25 mL), dried (Na2SO4), and. concentrated under reduced pressure. The crude residue was purified by column chromatography using 20 % ethyl acetate in petroleum ether as eluant to give 700 mg of the title compound as a white solid.1H NMR (CDCl3) delta 1.48 (s, 9H), 3.30 (m. IH), 3.54 (m, 8H)5 3.74 (m, IH)5 5.71 (m, IH)3 6.91 (s, IH), 7.40-7.29 (m, 5H).

196811-66-2, As the paragraph descriping shows that 196811-66-2 is playing an increasingly important role.

Reference：
Patent; E. I. DU PONT DE NEMOURS AND COMPANY; WO2008/13622; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

118753-66-5, tert-Butyl 4-aminopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[00229] Step-3: Synthesis tert-butyl 4-((6-bromo-7-fluoro-3-nitroquinolin-4- yl)amino) piperazine- 1 -carboxylate, 4: [00230] DIPEA (26.72mL, 0.15712mo1) was added to a stirred solution of 6- Bromo-4-chloro-7-fluoro-3-nitroquinoline, 9 (24g, 0.07856mo1) and tert-butyl 4-aminopiperazine-1-carboxylate (18.97g, 0.09427mo1) in DMF, 200mL at 0 00. The reaction mixture was allowed to room temperature and stirred for 2h. Reaction was monitored by TLC (30%EtOAc in hexane), after completion of reaction, diluted with water (l5OmL), the precipitated yellow solid was filtered-off, washed with water and dried under vacuum. The crude material was purified by column chromatography by using5i02 (15% EtOAc in Hexane) to afford of tert-butyl4-((6-bromo-7-fluoro-3-nitroquinolin-4- yl) amino) piperazine-1-carboxylate, 4 (30g, 81%). 1H NMR (300MHz, CDCI3): O 10.42 (5, 1H), 10.22-10.19 (d, 1H), 9.36 (5, 1H), 7.67-7.64 (d, 1H), 4.35-4.25 (t, 2H), 3.46-3.08 (t, 4H), 2.84-2.65 (t, 2H), 1.50 (5, 9H); LCMS: mlz= 469.9 (M+1) and 471.9 (M+2).

118753-66-5, As the paragraph descriping shows that 118753-66-5 is playing an increasingly important role.

Reference：
Patent; NOVARTIS AG; BOCK, Mark Gary; MOEBITZ, Henrik; PANIGRAHI, Sunil Kumar; PODDUTOORI, Ramulu; SAMAJDAR, Susanta; WO2015/22663; (2015); 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.303-26-4,1-((4-Chlorophenyl)(phenyl)methyl)piperazine,as a common compound, the synthetic route is as follows.

A vessel is charged with 250 ml of tetrahydrofurane, 25 ml of methanol and 5.0 ml (60 mmol) concentrated hydrochloric acid (37% by weight). The mixture is cooled to the temperature of 15 0C and under intense stirring, 5.5 g ( 84 mmol) pulverized zinc are added. Subsequently at a temperature between 5 tolO 0C, 12.5 g (25.1 mmol) (R)-(+)-4- (4-chloropheny l)-phenylmethyl-piperazine- 1 -carboxylic acid 2,2,2-trichloroethylester hydrochloride (compound of the Example 6) are added in several portions. The suspension is stirred for one hour at room temperature. At the end of the reaction, the unreacted zinc is filtered off, the filtrate is mixed with 150 ml of water and 150 ml of ethylacetate, the organic layer is separated, washed with aqueous 5 % by weight sodium hydrogen carbonate solution, dried and the solvent is evaporated. The residue is dissolved in 100 ml of ethylacetate and is added dropwise with stirring to 80 ml of 10 g/100 ml hydrochloric acid solution prepared in ethylacetate. The suspension containing the crystalline salt, which starts precipitating almost instantly after the addition, is cooled, the product is filtered off, washed with diethylether and dried.Yield: 7.7 g (85.4 %) white crystals Melting temperature, 198-202 0C.Elemental Analysis {calculated on the basis of the Formula C17H19C1N2.2HC1 (359.7)}:Calculated:C: 56 .76 H: 5 .88 Cl: 29.57 N: 7.79Measured: C: 56. ,45 H: 5 .74 Cl: 29.25 N: 7.61Optical purity (chiral high performance liquid chromatography): 98.7, 303-26-4

As the paragraph descriping shows that 303-26-4 is playing an increasingly important role.

Reference：
Patent; EGIS GYOGYSZERGYAR NYRT.; WO2007/66163; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics