Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.216144-45-5,4-(4-Methylpiperazin-1-yl)benzylamine,as a common compound, the synthetic route is as follows.

Stage 3: methyl 4-[2-[4-(4-methylpiperazin-1-yl)benzyl]amino-4-oxoquinazolin-3(4H)-yl]butanoateTriethylamine (0.4 mL) and [4-(4-methylpiperazin-1-yl)benzyl]amine (300 mg) are successively added to a solution of methyl 4-(2-chloro-4-oxoquinazolin-3(4H)-yl)butanoate (140 mg) in tetrahydrofuran (3 mL). The mixture is stirred at ambient temperature for 24 hours then water and ethyl acetate are added. After decantation and extractions, the combined organic phases are washed with salt water, dried over Na2SO4 then concentrated under reduced pressure at 40 C. Purification by flash chromatography on silica gel (eluent: dichloromethane/methanol 95:5) produces the expected compound in the form of beige crystals (131 mg, 58% yield from Stage 1).MS/LC: calculated MM=449.2; m/z=450.2 (MH+)NMR (1H, 400 MHz, DMSO-d6): delta 1.85 (t, 2H), 2.21 (s, 3H), 2.40 (m, 6H), 3.08 (m, 4H), 3.54 (s, 3H), 4.05 (t, 2H), 4.54 (d, 2H), 6.86 (AB, 2H), 7.08 (t, 2H), 7.18 (AB, 1H), 7.25 (AB, 2H), 7.48 (t, 1H), 7.52 (t, 1H), 7.89 (AB, 1H).

216144-45-5, The synthetic route of 216144-45-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SOCIETE DE CONSEILS DE RECHERCHES ET D’APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.); US2010/144714; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

132710-90-8, 1-Boc-4-(3-hydroxypropyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of tert-butyl 4-(3 -hydroxypropyl)piperazine- 1 -carboxylate (1.52 g, 6.2 mmol), Ph3P (2.46 g, 9.4 mmol), 12 (2.40 g, 9.4 mmol) and imidazole (1.28 g, 18.6 mmol) in DCM (100mL) was stirred at room temperature for 5 h and then diluted with DCM (200 mL). The organic layer was washed with brine, dried over anhydrous sodium sulfate, filtered and evaporated. The residue was purified by chromatography (PE : EtOAc = 5 : 1) to provide tert-butyl 4-(3- iodopropyl)piperazine- 1 -carboxylate (1 .10 g, 50%) as a colorless oil.

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

Reference：
Patent; PRINCIPIA BIOPHARMA, INC.; VERNER, Erik; BRAMELD, Kenneth Albert; WO2015/120049; (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.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

630125-91-6, Example 69 Preparation of ethyl6-(3-(3-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)ureido)phenyl)-1H-indazole-3-carboxylate To a stirred solution of 4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)benzeneamine (30.6 mg) in 1,4-dioxane (1 Ml), was added 4-nitrophenylchloroformate (21.6 mg) at room temperature. After 60 C. at 1 h, them mixture was cooled to rt and ethyl 6-(3-aminophenyl)-1H-indazole-3-carboxylate (30 mg) was added. The mixture was stirred at 90 C. for 12 h. Ethyl acetate and water were added and the aqueous layer was extracted with ethyl acetate three times. The combined organic layer was dried over magnesium sulfate and concentrated under reduced pressure. The residue was triturated in ethyl acetate/hexane to give 6-(3-(3-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)ureido)phenyl)-1H-indazole-3-carboxylate (16.2 mg). 1H NMR (400 MHz, DMSO-d6) delta13.98 (s, 1H), 9.09 (s, 1H), 8.93 (s, 1H), 8.15 (8.4 Hz, 1H), 7.99 (s, 1H), 7.93 (s, 1H), 7.81 (s, 1H), 7.62 (m, 3H), 7.43 (br d, J=4.4 Hz, 2H), 7.28 (m, 1H), 4.41 (q, J=7.2 Hz, 2H), 3.54 (s, 2H), 2.49 (m, 10H), 1.39 (t, J=7.2 Hz, 3H).

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

Reference：
Patent; Sim, Tae Bo; Son, Jung Beom; Kim, Hwan; Park, Dong Sik; Choi, Hwan Geun; Ham, Young Jin; Hah, Jung Mi; Yoo, Kyung Ho; Oh, Chang Hyun; Lee, So Ha; Ha, Jae Du; Cho, Sung Yun; Kwon, Byoung Mog; Han, Dong Cho; US2012/130069; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

278788-60-6, (R)-1-Boc-Piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Trimethylsilyl diazomethane (2M in hexane, 14 ml) was added dropwise to a solution of (2R)-L-(TERT-BUTOXYVARBONYL) piperazine-2-carboxylic acid (5 g) in methanol (100 ml) and DCM (115 ml), and the solution stirred at room temperature for 16 hours. The solvent was concentrated in vacuo and the residue purified by chromatography, eluting with ethyl acetate then 5% methanol / 7N ammonia in ethyl acetate, to give 1-tert-butyl 2-methyl (2R)- PIPERAZINE-1, 2-dicarboxylate as an oil (2.55 g, 48%); NMR spectrum (DMSO-d6) 1.40 (s, 9H), 2.10 (bs, 1H), 2.52 (m, 1H), 2.72 (dd, 1H), 2.82 (d, 1H), 2.97 (m, 1H), 3.29 (d, 1H), 3.61 (d, 1H), 3.67 (s, 3H), 4.43 (m, 1H) ; Mass spectrum MH+ 245.

278788-60-6, As the paragraph descriping shows that 278788-60-6 is playing an increasingly important role.

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

REFERENCE EXAMPLE 19 A mixture of methyl 4-(tert-butoxycarbonyl)piperazine-2-carboxylate (3.5 g) obtained in Reference Example 16, 3,4,5-trimethoxybenzyl chloride (4.6 g), potassium carbonate (6.0 g) and acetonitrile (80 ml) is refluxed by heating for 10 hours while stirring. The reaction mixture is concentrated under reduced pressure. The concentrate is added to water and extracted with ethyl acetate. The organic layer is washed with water and dried, then the solvent is distilled off under reduced pressure. The residue is purified by means of a silica gel column chromatography (hexane:ethyl acetate =3:2) to afford methyl 4-tert-butoxycarbonyl-1-(3,4,5-trimethoxy-benzyl)piperazine-2-carboxylate as a colorless oily product (5.2 g).

129799-08-2, 129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Takeda Chemical Industries, Ltd.; US4997836; (1991); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

259808-67-8, 1-Boc-3,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 3,3-diemethyl-piperazine-1-carboxylic acid tert-butyl ester (720 mg) and triethylamine (0.59 mL) in dichloromethane (10 mL) at 0 C. was added dropwise methanesulfonyl chloride (0.30 mL). The reaction mixture was stirred at room temperature for 16 h and then quenched with water (10 mL) and extracted into dichloromethane (2*20 mL). The combined organic layers were washed with saturated aqueous brine solution (2*20 mL), dried (MgSO4) and concentrated to give 4-methanesulfonyl-3,3-dimethyl-piperazine-1-carboxylic acid tert-butyl ester as a white solid (914 mg, 93%).

259808-67-8, As the paragraph descriping shows that 259808-67-8 is playing an increasingly important role.

Reference：
Patent; Piramed Limited; Genentech, Inc.; US2008/76758; (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.129779-30-2,(3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Preparation 6 tert-Butyl (cis)-4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]-3,5-dimethyl-1-piperazinecarboxylate STR51 Potassium carbonate (1.79 g) was added to a solution of tert-butyl (cis)-3,5-dimethyl-1-piperazinecarboxylate (2.57 g) [see Preparation 5] in acetronitrile (10 ml). The reaction mixture was stirred at room temperature for 5 minutes, after which time N(2-bromoethyl) phthalimide (3.36 g) was added and the mixture was stirred for a further 4 hours. Sodium iodide (0.1 g) was added and the reaction mixture was heated to reflux for 18 hours. The mixture was then cooled and the solvent removed under reduced pressure. The residue was partitioned between ethyl acetate and water, the organic layer was separated, dried over magnesium sulphate and the solvent removed under reduced pressure. The crude product was purified by column chromatography on silica gel eluding with a solvent gradient of 4:1:0, changing to 0:95:5, by volume, hexane:ethyl acetate:0.88 aqueous ammonia solution. to afford tert-butyl (cis)-4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]-3,5-dimethyl-1-piperazinecarboxylate (0.94 g) as an oil. 1 H-NMR (CDCl3)delta: 7.85 (2H, m), 7.75 (2H, m), 3.90 (2H, m), 3.75 (2H, t), 2.95 (2H, t), 2.70-2.50 (4H, m), 1.45 (9H, s), 1.20 (6H, d). MS: 388 (MH+).

129779-30-2, As the paragraph descriping shows that 129779-30-2 is playing an increasingly important role.

Reference：
Patent; Pfizer Inc; US6166011; (2000); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

278788-66-2, (R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

PREPARATIVE EXAMPLE 9; STEP B; (Bhattacharyya, S. Tetrahedron Lett. 1994,35, 2401.) [] A mixture of the title compound from Step A (1.09 g, 5.04 mmol, 1.0 eq.), paraformaldehyde (300 mg, ? 10.08 mmol, 2.0 eq.), and titanium isopropoxide (1.5 ml, 5.04 mmol, 1.0 eq.) in absolute ethanol (5 ml) was stirred at 70 C for 30 minutes and at room temperature for another 30 minutes. Sodium borohydride (195 mg, 5.04 mmol, 1.0 eq.) was added to the colorless solution. The solution was stirred at room temperature for 12h and at 60 C for another 3h. The solution was cooled to 0 C and treated with a 2.0M aqueous ammonia solution (25 ml, 50.00 mmol, excess) to give a snow-white suspension. The suspension was filtered through a Celite 521 plug and the filtrate was extracted with diethyl ether (4 x 25 ml). The ethereal extracts were combined and washed with brine (10 ml), dried over Na2SO4, filtered, and concentrated under house vacuum at 30 C. The residue was flash chromatographed (CH2Cl2 : 10% NH4OH/MeOH = 9:1 v/v) over silica gel to give the title compound (1.10 g, 95%) as a light-yellow, viscous oil. MS (EI): m/z 231 ([M+H]+, 59%), 175(B+). HR-MS(FAB):Calculated for C11H22N2O3 ([M+H]+): 231.1709. Found: 231.1716.

278788-66-2, As the paragraph descriping shows that 278788-66-2 is playing an increasingly important role.

Reference：
Patent; SCHERING CORPORATION; EP1140904; (2005); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1188265-73-7, tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1188265-73-7, Intermediate 11 2-[1-(5-Aminothiazolo[5,4-d]pyrimidin-7-yl)piperazin-2-yl]ethanol trifluoracetate salt [0231] To a solution of Intermediate 4 (0.38 g, 2.06 mmol) in DMF (20 mL) were added tert-butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate (1 g, 4.12 mmol) and DIPEA (0.4 g, 3.0 mmol). The reaction mixture was heated at 100 C. for 5 h, allowed to cool, then stirred at room temperature for 2 days. The reaction mixture was concentrated in vacuo, then partitioned between water and DCM. The organic phase was separated and concentrated in vacuo. The resulting crude material was purified by column chromatography (silica gel: 100-200 mesh, MeOH:DCM gradient 0% to 20%) to give a pale yellow foam. The foam was dissolved in DCM (1 mL) and TFA (2 mL) and stirred for 1 h. The reaction mixture was concentrated in vacuo, then triturated with diethyl ether, to give the title compound (0.6 g) as a sticky yellow solid. LCMS (ES+) 281 (M+H)+, RT 0.361 minutes (method 3).

1188265-73-7 tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate 53407692, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Brookings, Daniel Christopher; Ford, Daniel James; Franklin, Richard Jeremy; Ghawalkar, Anant Ramrao; Kulisa, Claire Louise; Neuss, Judi Charlotte; Reuberson, James Thomas; US2014/315885; (2014); 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.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The compound (S) -5- (1 – ((tert-butoxycarbonyl) amino) ethyl) -2- (3- (cyclopropylmethoxy) -4-(difluoromethoxy) phenyl ) -oxazole-4-carboxylic Acid (250mg, 0.53mmol), 1-Boc-2- methylpiperazine(130mg, 0.64mmol), 1- ethyl-3- (3-dimethylaminopropyl) carbodiimide hydrochloride Salt (155mg, 0.80mmol)and N- hydroxy-7-aza-benzotriazole (182mg, 1.33mmol) was dissolved in dichloromethane (15mL), and 0 Cunder conditions to this solution was added dropwise N, N- diisopropylethylamine (0.37mL, 2.14mmol), stirredat room temperature 5h, was added water (10mL × 2)Washing the organic phase was dried over anhydrous Na2 SO 4, the solvent was removed concentrate was subjected to column chromatography (eluent: Petroleumether/ EtOAc (V / v) = 2/1), to give 215mg of colorless viscous material, yield: 60%.

120737-78-2, 120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics