Tag: M.W:200-300

848482-93-9,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.848482-93-9,(S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

(S)-4-Boc-2-piperazinecarboxylic acid (530 mg, 2.17 mmol) was dissolved in MeOH (25 mL) and formaldehyde (1.76 mL, 37 wt % in water, 21.7 mmol) was added. The reaction mixture was stirred for 30 min, NaBH(OAc)3 (0.92 g, 4.34 mmol) was added and the reaction mixture was stirred for 2 h. The solvents were removed in vacuo and the residue was purified by reverse phase column chromatography. The residue and benzyl homopiperazine (0.41 g, 2.17 mmol) were dissolved in DMF (20 mL) and cooled to 0 C. DIPEA (0.59 g, 4.56 mmol) and HBTU (0.82 g, 2.17 mmol) were added and the reaction mixture was stirred for 3 h. The solvents were removed in vacuo and the residue was partitioned between DCM (100 mL) and water (50 mL). The organic fraction was washed with 1M aq Na2CO3 (25 mL), brine (25 mL), dried (MgSO4) and concentrated in vacuo. The residue was purified by reverse phase column chromatography to give the title compound (0.64 g, 71%) as a light yellow gum. LCMS (ES+): 417.4 [MH]+.

The synthetic route of 848482-93-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Proximagen Limited; Savory, Edward Daniel; Stewart, Allson; Cartey, Allison; Brown, Giles; Simpson, Iain; Oliver, Kathryn; Patient, Lee; Higginbottom, Michael; Cole, Andrew Graham; US2013/289020; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step B. 4-[4-(2-Ethyl-butyrylamino)-2-fluoro-phenvH-piperazine-1-carboxylic acid tert-butyl ester. 4-(4-Amino-2-fluoro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester(4.54 g, 15.4 mmol) and DIPEA (2.95 ml_, 16.9 mmol) were dissolved in DCM (90.0 ml.) and cooled to 00C. 2-Ethyl-butyryl chloride (2.28 ml_, 16.2 mmol) was added slowly. The resulting mixture was then stirred at 00C for 1 h and at room temperature for 4 h. The resulting mixture was then washed with water, 1 N NaOH solution and water. The organic phase was dried (Na2SO4), filtered and concentrated to yield a residue. Chromatography of the residue (SiO2, 0-8 % acetone/DCM) yielded the title compound.MS (ESI) mass calculated for C21H32FN3O3, 393.50, m/z measured, 394.6 [M+H]+ 1H NMR (CDCI3): 7.50 (dd, J = 13.9, 2.4, 1 H), 7.22 (s, 1 H), 7.15-7.07 (m,1 H), 6.88 (t, J = 9.0, 1 H), 3.63-3.52 (m, 4H), 3.00-2.92 (m, 4H), 2.06-1.93 (m, 1 H), 1.75-1.65 (m, 2H), 1.59-1.52 (m, 2H), 1.48 (s, 9H), 1.00-0.88 (m, 6H)., 154590-35-9

As the paragraph descriping shows that 154590-35-9 is playing an increasingly important role.

Reference：
Patent; JANSSEN PHARMACEUTICA N.V.; WO2009/79597; (2009); 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.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

To a solution of propylene oxide (4.0 mL, 57 mmol) in DCM (160 mL) was added 2.0M of trimethylaluminum in toluene (27 mL, 54 mmol) at -78 °C under N2. After being stirred at that temperature for 10 min, a solution of benzyl piperazine-l-carboxylate (from Aldrich, 9 mL, 40 mmol) in DCM (60 mL) was added. The resulting reaction mixture was stirred at -78 °C for 30 min. The reaction was then allowed to warm up to 0 °C, stirring for another 30 min. To the reaction mixture was added sodium fluoride (8.2 g, 200 mmol) in one portion, followed by water (5.2 mL, 290 mmol) slowly and periodically at 0 °C. The resulting suspension was rapidly stirred for 1 h at 0 °C and filtered through a short column of Celite and the column was subsequently washed with DCM (120 mL). The combined filtrates were dried over Na2S04, concentrated and purified on silica gel (eluting with 0-10percent MeOH in DCM) to provide the desired product (9.6 g, 76percent). LCMS calculated forCi5H23 203(M+H)+: m/z = 279.2; Found: 279.3. 3/4 NMR (500 MHz, DMSO-d6): delta 7.39-7.31 (5H, m), 8.07 (2H, s), 4.29 (1H, J= 4.0 Hz), 3.75 (1H, m), 3.38 (4H, br s), 2.38 (4H, m), 2.24 (1H, dd, J= 12.5 and 7.0 Hz), 2.17 (1H, dd, J= 12.5 and 7.0 Hz), 1.04 (3H, d, J= 6.0 Hz) ppm.

31166-44-6, As the paragraph descriping shows that 31166-44-6 is playing an increasingly important role.

Reference：
Patent; INCYTE CORPORATION; RODGERS, James, D.; LI, Yun-Long; SHEPARD, Stacey; WANG, Haisheng; WO2011/28685; (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.196811-66-2,tert-Butyl 4-carbamothioylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 1-tert-butoxycarbonyl-4-thiocarbamoylpiperazine (Reference Example 150) (88mg, 0.35 mmol) in acetonitrile (20 ml) was added 1,2-bis(4-methoxyphenyl)-2-bromo-1-ethanone (Reference Example 14) (117 mg, mmol), and the mixture was stirred at room temperature for 2 hours. The reaction solution was concentrated under a reduced pressure, and the residue was purified by chromatography (silica gel, n-hexane/ethyl acetate) to give a title compound (81 mg, 0.17 mmol, 48%) as a white solid. 1H-NMR (400 MHz, CDCl3) delta: 1.49 (9H, s), 3.47-3.61 (8H, m), 3.79 (3H, s), 3.81 (3H, s), 6.78 (2H, d, J = 8.8 Hz), 6.82 (2H, d, J = 8.8 Hz), 7.21 (2H, d, J = 8.8 Hz), 7.44 (2H, d, J = 8.8 Hz).

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

Reference：
Patent; TORAY INDUSTRIES, INC.; EP2009006; (2008); A1;,
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

To a solution of 1 ,1-dimethylethyl 4-amino-1 -piperazinecarboxylate (270 mg, 1.34 mmol) in DCM-DMF (4:1 , 15 ml_) were added 3-oxo-3,4-dihydro-2H-pyrido[3,2- i?][1 ,4]thiazine-6-carboxylic acid (283 mg, 1.34 mmol), EDC (250 mg, 1.61 mmol) and HOBT (217 mg, 1.61 mmol). After 12h, the solution was concentrated and the residue purified via column chromatography (silica, 1% MeOH in DCM (1% NH4OH)) yielding the title compound as a yellow foam (412 mg, 78 %): LCMS (ES) m/e 394 (M+H)+., 118753-66-5

The synthetic route of 118753-66-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXO GROUP LIMITED; WO2006/20561; (2006); 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.169447-86-3,(S)-tert-Butyl 2-benzylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The synthesis of compounds of this embodiment is shown in FIG. 1. As shown, pyridine, quinolines or isoquinolines were coupled with various piperazines through nucleophilic aromatic substitution or Hartwig Buchwald aryl amination., 169447-86-3

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

Reference：
Patent; UNIVERSITY OF SOUTH FLORIDA; YALE UNIVERSITY; WO2008/79945; (2008); 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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A solution of 2-bromo-5-fluoropyridine (3.52 g, 20 mmol), (S)-tert-butyl 2- methylpiperazine-1-carboxylate (2 g, 11.36 mmol), t-BuONa (1.922 g, 20 mmol), BINAP (623 mg, 1 mmol), and Pd2(dba)3 (458 mg, 0.5 mmol) in dry toluene (20 mL) was stirred under N2 at 80 C for 16 h. The reaction mixture was concentrated and the mixture was purified by chromatography (silica, EtOAc/PE =1/10) to afford (S)-tert-butyl 4-(5-fluoropyridin-2-yl)-2- methylpiperazine-1-carboxylate (2.9 g, 9.82 mmol, 86%) as a yellow oil. ESI-MS (EI, m/z):296.2 [M+H]., 169447-70-5

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NAVITOR PHARMACEUTICALS, INC.; O’NEILL, David John; SAIAH, Eddine; KANG, Seong Woo Anthony; BREARLEY, Andrew; BENTLEY, Jonathan; (565 pag.)WO2018/89433; (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.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

Compound 1 A mixture of Intermediate 1 (100 mg, 0.33 mmol), 2-methoxy-4-(4-methylpiperazin-l- yl)aniline (73 mg, 0.33 mmol),, and DIPEA (0.08 ml, 0.49 mmol) in DMSO (5 ml) was stirred at room temperature for 30 min. After checking the TLC, the mixture was added to water (100ml). After cooled with ice-bath, the solids were collected by filtration, washed by water. The crude product was purified by column chromatography (silica gel, 0-15% MeOH in DCM) to give the desired product as yellow solids (64 mg, 40% yield). 1H NMR (400 MHz, DMSO-de) delta 11.34 (br, 1H), 9.45 (br s, 1H), 8.15 (s, 1H), 7.13 (m, 2H), 6.93 (m, 1H), 6.65 (m, 1H), 6.50 (m, 1H), 6.23 (s, 1H), 3.77 (s, 3H), 3.18 (m, 4H), 2.46 (m, 4H), 2.39 (s, 3H), 2.23 (s, 3H); ESI-MS: calcd for C26H26FN702 487, found 488 (MH+). HPLC: retention time: 18.63 min. purity: 96%., 122833-04-9

The synthetic route of 122833-04-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NANTBIOSCIENCE, INC.; TAO, Chunlin; POLAT,, Tulay; WEINGARTEN, Paul; NALLAN, Laxman; ARP, Forrest; WANG, Qinwei; HO, David; (129 pag.)WO2016/138527; (2016); 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

To a solution of Intermediate 2 (1.0 g, 4.1 mmol) in anhydrous dichloromethane (40 mL) was added triethylamine (0.82 mL, 5.9 mmol) and 3-methoxy-4-tert-butylbenzoyl chloride* (1.11 g, 4.9 mmol). The resultant mixture was stirred at ambient temperature for 18 hours and washed with water. The organic phase was separated and evaporated to a gum, then purified by chromatography over silica gel using cyclohexane-ethyl acetate (4: 1, 3: 1 and then 2: 1 v/v) as eluent. The fractions containing the desired product were combined and evaporated to give the title compound as an amorphous solid. MS calcd for (C23H34N206 + H) + : 435. Found: (M+H) + = 435. * Prepared from 3-methoxy-4-tert-butylbenzoic acid (J. Org. Chem. (1961) 26,1732) using thionyl chloride., 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; GLAXO GROUP LIMITED; WO2005/79799; (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.262368-30-9,N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide,as a common compound, the synthetic route is as follows.

To a stirred solution of methyl 2-oxo-2,3-dihydro-lH-pyrrolo[3,2- b]pyridine-6-carboxylate (0.18 g, 0.9366 mmol) in acetic anhydride (4 ml) was added triethyl orthobenzoate (0.630 g, 2.8098 mmol) at RT and the mixture was refluxed for 3 h at 110 C. The reaction mixture was evaporated and the resulting residue was used as such into next step without purification. [000163] Step-2: To a stirred solution of product from step-1 (0.18 g) in DMF (4 ml) was added N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-l-yl)acetamide (0.180 g, 0.6861 mmol) at RT and the reaction mixture was heated at 110 C for 1 h. The reaction mixture was cooled to RT and stirred with triethyl amine (1 ml) for half an hour. The reaction mixture was evaporated and the crude product was purified by column chromatography using 0 to 10% methanol in dichloromethane as eluent to afford (Z)-methyl l-acetyl-3-((4-(N-methyl-2-(4- methylpiperazin- 1 -yl) acetamido)phenylamino)(phenyl)methylene)-2-oxo pyrrolo[3,2-b]pyridine-6-carboxylate as yellow solid. MS (ES+): m/z 583.4 (MH+).

262368-30-9, As the paragraph descriping shows that 262368-30-9 is playing an increasingly important role.

Reference：
Patent; ANGION BIOMEDICA CORP.; PANICKER, Bijoy; MISHRA, Rama, K.; JUNG, Dawoon; OEHLEN, Lambertus, J.W.M.; LIM, Dong, Sung; WO2013/112959; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics