Month: July 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

Example 18; iV”-(2-Ammophenyl)-4-(3-chloro-5-{[4-(2-methoxyethyl)piperazin-l-yl]niethyl}pyridin-2- yl)benzamide; A solution of tert-bvyl (2-{[4-(3-chloro-5-formylpyridin-2- yl)benzoyl]amino}phenyl)carbamate (Method 1; 181 mg, 0.40 mmol) in dichloromethane (4 ml) was added to l-(2-methoxyethyl)piperazine (102 mg, 0.70 mmol). The reaction mixture was stirred for 5 minutes before addition of titanium (IV) isopropoxide (240 mul, 0.8 mmol). The reaction was allowed to stir at ambient temperature for 2 hours then sodium borohydride (61 mg, 1.60 mmol), added followed by methanol (0.4 ml). The reaction mixture was stirred for 2 hours then a further portion of sodium borohydride (61 mg, 1.60 mmol) added the reaction mixture was left to stir overnight (20 hours). Saturated aqueous sodium hydrogencarbonate solution (5 ml) was added, followed by water (5 ml) and dichloromethane (5 ml). The mixture was stirred for 30 minutes and the organic phase separated by filtration through an 1ST phase separating cartridge, and the aqueous extracted again with dichloromethane. The combined organic extracts were evaporated to dryness and the residue purified by flash chromatography on silica eluting with ethyl acetate followed by a rising gradient of methanol in ethyl acetate (0-20% v/v) to afford the protected product. This was taken up in dichloromethane (3 ml) and treated with trifiuoroacetic acid (1 ml) then at ambient temperature for 22 hrs. The reaction mixture was diluted with dichloromethane and poured onto an SCX-2 cartridge (5g). The cartridge was washed with dichloromethane (25 ml) and methanol (50 ml) before eluting products with a 2M solution of ammonia in methanol (50 ml). The ammoniacal fraction was evaporated to dryness and the resultant residue triturated with diethyl ether/isohexane to afford the title compound (78 mg, 41%); MMR Spectrum: (CDCl3) delta 2.61 (m, 10H), 3.35 (s, 3H), 3.53 (t, 2H), 3.58 (s, 2H), 3.88 (s, 2H), 6.87 (m, 2H), 7.11 (m, IH), 7.38 (d, IH), 7.84 (d, 2H), 7.88 (s, 2H), 8.00 (d, 2H), 8.53 (s, IH); Mass Spectrum: M+H+ (35Cl) 480.

13484-40-7, The synthetic route of 13484-40-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2006/75160; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

31166-44-6, 1-Cbz-Piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of bromide 61 (180 mg, 0.5 mmol), Cu20 (8 mg, 0.1 eq.) and 1 -Z-piperazine (0.5 mL, 2.5 mmol) in water (1 .0 mL) was stirred in a seal tube at 100 °C for 18 h. The reaction was cooled and the residue was extracted with EtOAc (3 x 25 mL). The combined organic layers were dried on MgS04, filtered and concentrated in vacuo. The crude reaction mixture was purified by flash column chromatography on silica gel [DCM/MeOH (2percent MeOH)] to give 89 as colourless solid (220 mg, 89percent), which was used in the next step without further purification. (0603) 1H NMR (500 MHz, CDCU, deltaEta): 7.37-7.30 (m, 5H, Ar), 5.74 (d, J = 2.5 Hz, 1 H, C3-H), 5.64 (s, 1 H, C5-H), 5.16 (s, 2H, CH2-Ph), 4.39-4.06 (m, 3H, C7-H, C1 1 -H, C12-H), 3.77 (dd, J = 15.0, 6.0 Hz, 1 H, C7-H), 3.60 (m, 4H, C13-H), 3.27 (m, 4H, C14-H), 3.01 (m, 2H, C1 1 -H C12-H), 2.87 (s, 1 H, C10-H), 2.35 (s, 1 H, C8-H), 1 .97 (d, J = 12.5 Hz, 1 H, C9-H), 1 .89 (d, J = 12.5 Hz, 1 H, C9-H), 1 .40-1 .18 (s, 9H, Boc); 13C NMR (125 MHz, CDCI3, 5C): 164.3 (CO), 156.4 (CO), 155.1 (CO), 154.6 (C4), 148.3 (C6), 136.4 (Ar), 128.5 (2C, Ar), 128.1 (Ar), 127.9 (2C, Ar), 96.4 (C3), 95.0 (C5), 80.1 (q Boc), 67.7 (CH2-Ph), 50.6, 50.5 (C1 1 , C12), 47.9 (C7), 46.1 (2C, C13), 43.1 (2C, C14), 35.4 (C10), 28.1 (3C, Boc), 27.7 (C8), 26.5 (C9); HRMS (ESI+): calculated for C28H37N4O5: 509.2758, found [M+H]+: 509.2733.

31166-44-6, 31166-44-6 1-Cbz-Piperazine 643495, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; THE UNIVERSITY OF BRISTOL; GALLAGHER, Timothy Charles; REGO CAMPELLO, Hugo; (154 pag.)WO2018/33742; (2018); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

DECP (5.9 ml; 0.0395 mol) was added to a stirring solution of l-(l,l-dimethylethyl)-4- (4-carboxyphenyl)-l-piperazinecarboxylic acid ester (10 g; 0.0326 mol) and 4- methoxybenzylamine (4.7 ml; 0.036 mol) in Et3N (9.2 ml; 0.0655 mol) and CH2Cl2 (250 ml). The reaction mixture was stirred at room temperature for 18 hours. Saturated NaHCO3 solution (150 ml) was added and the mixture was stirred for 30 minutes. Then H2O (100 ml) was added and the mixture was stirred for 30 minutes. The layers were separated and CH2Cl2-layer was dried with MgSO4, evaporated, co-evaporated with toluene and dried at 50 0C in vacuum for 3 hours. Yield : 15.21 g of intermediate 53 (107 %)., 162046-66-4

162046-66-4 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid 2795508, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; JANSSEN PHARMACEUTICA N.V.; WO2008/148868; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

67455-41-8, 4-(Piperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A solution of amine (1 mmol) and alpha,beta-unsaturated nitriles or carbonyl compounds (1.2 mmol) was added to SWCNT-TEAP (1 mg) and the mixture was stirred at 25 C for 1 min. The completion of the reactions was monitored using TLC. The product formed in the one-phase system, was extracted with diethyl ether. The resulting organic phase extract was washed with a saturated aqueous NaHCO3 solution, and then dried over anhydrous Na2SO4. The solvent was removed and the residue was further purified by recrystallization or silica gel chromatography. The reaction products were analyzed with 1H and 13C NMR spectroscopy. 1H and 13C NMR of entry 1-5 are given below:

67455-41-8, As the paragraph descriping shows that 67455-41-8 is playing an increasingly important role.

Reference：
Article; Attri, Pankaj; Choi, Eun Ha; Kwon, Gi-Chung; Bhatia, Rohit; Gaur, Jitender; Arora, Bharti; Kim, In Tae; Bulletin of the Korean Chemical Society; vol. 35; 10; (2014); p. 3035 – 3040;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

7H-Indolo[2,1-a][2]benzazepine-10-carboxamide, 6-[1-cyclobutyl-4-(1-cyclopentylpiperazin-4-ylcarbonyl)-1H-pyrazol-5-yl]-13-cyclohexyl-3-methoxy-N-[(1-methylethyl)sulfonyl]- A 2 dram vial was charged with 1H-pyrazole-4-carboxylic acid, 1-cyclobutyl-5-[13-cyclohexyl-3-methoxy-10-[[[(1-methylethyl)sulfonyl]amino]carbonyl]-7H-indolo[2,1-a][2]benzazepin-6-yl]-(60 mg, 0.091 mmol), DMF (1 mL), 4-methylmorpholine (0.030 mL, 0.274 mmol), 1-cyclopentylpiperazine (15.50 mg, 0.100 mmol) and o-benzotriazol-1-yl-N,N,N’,N’-tetramethyluronium tetrafluoroborate (TBTU) (32.3 mg, 0.100 mmol). The rxn was stirred for 1 hour. LCMS indicates the rxn was complete, 766.36 at 4.11 minutes. It was diluted with ether, washed with saturated ammonium chloride then brine, dried (MgSO4) and evaporated giving a yellow solid. The solid was dissolved in DCM, the solution was added to a Thomson silica gel column and the column was eluted with DCM/methanol (0% to 5%). The appropriate fractions (TLC) were combined and evaporated giving a light yellow solid. The solid was triturated in ether/hexane giving the product (52 mg, 0.065 mmol, 71.5% yield) as a light yellow powder. HPLC: 99.6%. LCMS: 793.43 at 3.77 minutes., 21043-40-3

The synthetic route of 21043-40-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Bristol-Myers Squibb Company; US2009/280083; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 5-fluoro-2-methyl-3-nitrobenzaldehyde (D32, 10 g) and (S)-tert-butyl 2-methylpiperazine-1 -carboxylate (12.03 g) in DCM (120 mL) was added drops of acetic acid (3.28g). The mixture was stirred at RT for an hour. Sodium triacetoxyhydroborate (23.15 g) was added in ice-bath. The mixture was stirred at RT overnight and quenched with sat. NaHCO3 solution. The organic layer was dried with anhydrous Na2SO4, filtered and concentrated in vacuo to afford the title compound (22.17 g). MS (ESI): C18H26FN304 requires 367; found 368 [M+H].

169447-70-5, As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXOSMITHKLINE (CHINA) R & D COMPANY LIMITED; DENG, Jing; LEI, Hui; MA, Xin; REN, Feng; CAI, Wei; LIN, Xichen; WO2015/180613; (2015); A1;,
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, General procedure: To amixture of substituted benzoic acid obtained in the last step (0.12 mmol) in 5mL DMF, 2-(7-aza-1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluroniumhexafluorophosphate (HATU, 0.18 mmol), ethyldiisopropylamine (DIPEA, 0.24 mmol)and 4-((4-methylpiperazin-1-yl)methyl)-3- (trifluoromethyl)aniline (0.1 mmol)was added. The resulting mixture was stirred at room temperature overnight. Thenthe reaction was extracted with ethyl acetate, washed with brine, dried overanhydrous Na2SO4, filtered and concentrated to give thecrude product, which was further purified by column chromatography to affordthe final compounds.

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

Reference：
Article; Han, Mei; Li, Shan; Ai, Jing; Sheng, Rong; Hu, Yongzhou; Hu, Youhong; Geng, Meiyu; Bioorganic and Medicinal Chemistry Letters; vol. 26; 23; (2016); p. 5679 – 5684;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

55276-43-2, 1-Methanesulfonylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6-Bromo-1-chlorophthalazine (18 mg, 74 umol) and 1-(methylsulfonyl)piperazine (91 mg, 554 mumol) were dissolved in dichloromethane/methanol when the reaction mixture was concentrated by evaporation under a nitrogen line. The concentrate was heated to 120 C. for 6 h to give the title compound. MS (ES+): 373 (M+H)+., 55276-43-2

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

Reference：
Patent; Amgen Inc.; US2006/199817; (2006); 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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A 100 mL round-bottom flask was charged with 4-(morpholin-4-yl)-2- (trifluoromethyl)benzaldehyde (1.00 g, 3.86 mmol, 1.00 equiv), tert-butyl (2S)-2- methylpiperazine-l-carboxylate (0.850 g, 4.24 mmol, 1.10 equiv), 1 ,2-dichloroethane (20 mL). The mixture was stirred for 30 min at room temperature. Sodium triacetoxyborohydride (2.40 g, 1 1.3 mmol, 3.00 equiv) was added. The resulting solution was stirred overnight at room temperature, diluted with H20 (20 mL), extracted with dichloromethane (3 x 15 mL). The organic layers were combined and washed with brine (50 mL), dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was chromatographed on a silica gel column with ethyl acetate/petroleum ether (20/80) to provide 1.70 g (99% yield) of tert- butyl (2S)-2-methyl-4-[[4-(morpholin-4-yl)-2-(trifluoromethyl)phenyl]methyl]piperazine-l- carboxylate as yellow oil. LCMS (ESI, m/z): 444 [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; ABIDE THERAPEUTICS; THE SCRIPPS RESEARCH INSTITUTE; CISAR, Justin, S.; GRICE, Chery, A.; JONES, Todd, K.; NIPHAKIS, Micah, J.; CHANG, Jae, Won; LUM, Kenneth, M.; CRAVATT, Benjamin, F.; WO2013/103973; (2013); 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.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

To a solution of 1-tert-butyl 3-methyl piperazine-1,3-dicarboxylate (2.44 g, 10 mmol) in DCM (50 mL) was added phenylboronic acid (2.35 g, 20 mmol), Cu(OAc)2 (1.82 g, 10 mmol) and pyridine (1 .58 g, 20 mmol) in turns with stirring. The reaction mixture was stirred at ambient temperature for 24 hrs under an oxygen atmosphere. The reaction mixture was filtered and filtrate was concentrated. The residue was purified by column chromatography on silica gel(petroleum ether: EtOAc= 3:1) to afford compound Tnt 44-1 (2.74 g). MS-EST (mlz): 321 (M+1) Rf: 0.3 (PE : EtOAc= 3 : 1).

129799-08-2, The synthetic route of 129799-08-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK SHARP & DOHME CORP.; COBURN, Craig; MALETIC, Milana; LUO, Yunfu; QI, Zhiqi; YU, Tingting; SOLL, Richard; WO2015/70367; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics