Tag: M.W:200-300

122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of IV-l-c (28 mg, 0.1 mmol), 2-methoxy-4-(4-methylpiperazin-l- yl)benzenamine (22 mg, 0.1 mmol), X-Phos (4.3 mg), Pd2(dba)3 (5.5 mg) and K2CO3 (41.5 mg, 0.3 mmol) in 1.2 mL of /-BuOH was heated at 100 0C in a seal tube for 4 h. Then the reaction was filtered through celite and eluted with dichloromethane. The dichloromethane was removed in vacuo and the resulting crude product was purified by reverse-phase prep-HPLC using a water (0.05% TFA)/acetonitrile (0.05% TFA) gradient to afford the title compound IV-I as TFA salt (20 mg). 1H NMR (600 MHz, CD3OD) 5 8.1 (s, IH), 7.78 (dd, J= 1.2, 7.8 Hz, IH), 7.71 (d, J= 7.2 Hz, IH), 7.57- 7.54 (m, IH), 7.28-7.23 (m, 2H), 6.76 (d, J= 2.4 Hz, IH), 6.67 (dd, J= 1.2, 8.4 Hz, IH), 3.92-3.86 (m, 5H), 3.66-3.60 (m, 2H), 3.46 (s, 3H), 3.45 (s, 3H), 3.28-3.24 (m, 2H), 3.14-3.06 (m, 2H), 2.97 (s, 3H). MS (ESI) m/z 460 (M+H)+., 122833-04-9

As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference：
Patent; DANA FARBER CANCER INSTITUTE; GRAY, Nathanael, S.; DENG, Xianming; KWIATKOWSKI, Nicholas, Paul; WO2010/80712; (2010); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1403898-64-5, (2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation 18: (2R,5R)-4-{2-[6-(4-FI uoro-benzyl)-3,3-di methyl-2,3-di hydro-pyrrolo[3,2- b]pyridi n-I -yI]-2-oxo-ethyl}-5-hydroxymethyl-2-methyl-pi perazi ne-I -carboxylic acid tert-butyl esterFinely ground potassium iodide (7.5 g, 45.26 mmol) was added to a mixture of (2R,5R)-5-hydroxymethyl-2-methyl-piperazine-1-carboxylic acid teit-butyl ester (5.7 g, 24.89 mmol), 2-chloro- 1 -[6-(4-fluorobenzyl)-3, 3-dimethyl-2, 3-dihydro-pyrrolo[3,2-b]pyridin- 1 -yl]-ethanone hydrochloride (8.35 g, 22.63 mmol) potassium carbonate (12.5 g, 90.51 mmol) and acetonitrile (100 mL) under nitrogen. The mixture was stirred at 20 00 overnight. The mixture was partitioned between water (300 mL) and EtOAc (300 mL) and the organic phasewas dried and evaporated in vacuo to give the title compound (12.14 g). MS: [M+H] = 527.

1403898-64-5, As the paragraph descriping shows that 1403898-64-5 is playing an increasingly important role.

Reference：
Patent; ASTEX THERAPEUTICS LIMITED; CHESSARI, Gianni; JOHNSON, Christopher Norbert; PAGE, Lee William; BUCK, Ildiko Maria; DAY, James Edward Harvey; HOWARD, Steven; SAXTY, Gordon; MURRAY, Christopher William; WO2014/60770; (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.692058-21-2,1-Boc-4-(2,2,2-trifluoroethyl)piperazine,as a common compound, the synthetic route is as follows.

[19121 Step 2: Synthesis of 1-(2.2.2-trifluoroethyl)piperazine[19131 Tert-butyl 4-(2,2,2-trifluoroethyl)piperzine- 1 -carboxylate (2.000 g, 7.455 mmol) was dissolved in methylene chloride (10 mL) / trifluoroacetic acid (5 mL) at room temperature, and the solution was stirred at the same temperature for 17 hours. The reaction mixture was concentrated under reduced pressure to remove the solvent, and the concentrate was crystallized from ethyl acetate (20 mL) at room temperature and filtered, and the resulting solid was washed with ethyl acetate and dried to afford the desired compound (0.457 g, 23.1 %) as a white solid.

692058-21-2, As the paragraph descriping shows that 692058-21-2 is playing an increasingly important role.

Reference：
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; SONG, Hyeseung; LEE, Changgon; KWAK, Dalyong; LEE, Jaeyoung; BAE, Suyeal; KIM, Yuntae; BAE, Daekwon; HA, Nina; BAE, Miseon; KIM, Jihyun; WO2015/137750; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To solution of compound 3 (1 equiv) in 20 ml of ACN,NaI (1.2 equiv) was added and the mixture was refluxed for 30 min and cooled to room temperature. Subsequently,K2CO3 (1.2 equiv) and appropriate phenylpiperazine derivative(1.2 equiv) were added. Then the mixture was refluxedfor 4h. At the end of this period, the mixture was evaporatedto dryness then the product was solidified with ice-cold waterand crystallized from appropriate solvent.

30459-17-7, As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference：
Article; Kilic, Burcu; Erdogan, Merve; Gulcan, Hayrettin O.; Aksakal, Fatma; Oruklu, Nihan; Bagriacik, Emin U.; Dogruer, Deniz S.; Medicinal Chemistry; vol. 15; 1; (2019); p. 59 – 76;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

3022-15-9, Piperazine-2-carboxylic acid dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Piperazine-2-carboxyilc acid dihydrochloride (15.0 g, 73.9 mmol) was dissolved in H2O (240 mL) and 1,4-dioxane (360 mL), and the solution was brought to pH 10 with 6 N NaOH in H2O. Di-tert-butyldicarbonate (28.3 g, 162 mmol) was added while maintaining the pH at 10 with 6 N NaOH in H2O. After 2 h, the reaction mixture was extracted with Et2O (3 x 200 mL). The aqueous layer was brought to pH 3 with 6 N HCl and was extracted with EtOAc (4 x 300 mL). The combined EtOAc extracts were dried over Na2SO4, filtered, and concentrated under reduced pressure to give 14.45 g (59%) of the desired product as an off- white solid. The material was used without further purification. LC-MS: RT = 8.16 min; [M+Na]+ = 353.1.

3022-15-9, 3022-15-9 Piperazine-2-carboxylic acid dihydrochloride 2723757, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; CRITICAL THERAPEUTICS, INC.; WO2007/146066; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 121Exam le 121a ieri-Butyl 4-(6-Nitropyridin-3-yl)-3-oxopiperazine-l-carboxylate 121aA 250-mL single-neck round-bottomed flask equipped with a magnetic stirrer and reflux condenser was charged with 2-nitro-5-bromopyridine (1.00 g, 5.00 mmol), 2-oxo-4- (ieri-butoxycarbonyl)piperazine (1.01 g, 5.00 mmol), cesium carbonate (3.58 g, 11.0 mmol) and 1,4-dioxane (40 mL). After bubbling nitrogen through the result-ing solution for 30 min, Xantphos (246 mg, 0.425 mmol) and tris(dibenzylidene-acetone)dipalladium(0) (230 mg, CGIPHARM60WO0.250 mmol) were added, and the reaction mixture was heated at reflux for 6 h. Water (30 mL) and ethyl acetate (150 mL) were added after the reaction mixture was cooled to room temperature. The resulting mixture was filtered through a bed of Celite 521. The organic layer of the filtrate was separated and the aqueous layer was extracted with ethyl acetate (2 x 50 mL). The combined organic layers were washed with brine (30 mL), dried over sodium sulfate and purified by column chromatography to afford a 96% yield (1.55 g) of 121a as an amber oil: ]H NMR (300 MHz, CDC13) delta 8.67 (d, 1H, J = 2.4 Hz), 8.32 (d, 1H, J = 8.7 Hz), 8.15 (dd, 1H, / = 8.7, 2.4 Hz), 4.33 (s, 1H), 3.89 (m, 4H), 1.48 (s, 9H); MS (ESI+) mJz 323.1 (M+H)., 76003-29-7

The synthetic route of 76003-29-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GILEAD CONNECTICUT, INC.; GENENTECH, INC.; CURRIE, Kevin S.; WANG, Xiaojing; YOUNG, Wendy B.; WO2012/31004; (2012); 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.

NEt3 (12.9 mL, 92.47 mmol) was added to tert-butyl (3R)-3-(hydroxymethyl)piperazine-1-carboxylate (10 g, 46.24 mmol), tert-butylchlorodimethylsilane (10.45 g, 69.35 mmol) and 4-dimethylaminopyridine (0.282 g, 2.31 mmol) in DCM (200 mL) at rt. The resulting suspension was stirred at rt for 16 h. The solvent was removed in vacuo. The crude product obtained was purified by flash silica chromatography (0 to 9% MeOH in DCM) to afford tert-butyl (3R)-3-({[tert-butyl(dimethyl)silyl]oxy}methyl)piperazine-1-carboxylate (15 g, 98%) as a pale yellow gum; 1H NMR (300 MHz, DMSO, 30 C.) 0.05 (6H, s), 0.89 (9H, s), 1.40 (9H, s), 2.27 (1H, s), 2.41 (1H, s), 2.48-2.54 (2H, m), 2.71 (1H, s), 2.78-2.90 (1H, m), 3.33-3.57 (2H, m), 3.74 (1H, d), 3.86-3.96 (1H, m).

278788-66-2, 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; ASTRAZENECA AB; Kettle, Jason Grant; Bagal, Sharanjeet; Robb, Graeme Richard; Smith, James Michael; Goldberg, Frederick Woolf; Cassar, Doyle Joseph; Feron, James Lyman; US2019/177338; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

216144-45-5, 4-(4-Methylpiperazin-1-yl)benzylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Stage 3: 1′-[4-(4-methylpiperazin-1-yl)benzyl]-2’H-spiro[cyclopentane-1,3′-imidazo[2,1-b]quinazoline]-2′,5′(1’H)-dione hydrochloride[4-(4-methylpiperazin-1-yl)benzyl]amine (950 mg) is added to methyl 1-(2-chloro-4-oxoquinazolin-3(4H)-yl)cyclopentane carboxylate (520 mg) in anhydrous THF (2 mL) placed in a ?Biotage? reaction tube. The reaction tube is sealed with a cap, stirred at ambient temperature for 1 hour then placed in a ?Biotage? micro-wave and heated under magnetic stirring at 100 C. for 1 hour. The mixture is 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 the free base. The corresponding hydrochloride salt is formed by adding a 1N HCl solution in ethyl ether to the solution of the free base in ethyl acetate. The precipitate obtained is filtered and dried in order to produce the expected hydrochloride compound (235 mg, 27% yield from Stage 2).MS/LC: calculated MM=443.5; m/z=444.3 (MH+)NMR (1H, 400 MHz, CDCl3): delta2.07 (s, 2H), 2.19 (s, 6H), 2.90 (s, 3H), 3.61 (m, 6H), 4.06 (m, 2H), 5.55 (s, 2H), 7.27 (m, 2H), 7.46 (m, 1H), 7.77 (m, 3H), 8.24 (AB, 1H), 8.68 (AB, 1H), 13.35 (s, 1H).

216144-45-5, 216144-45-5 4-(4-Methylpiperazin-1-yl)benzylamine 2776493, apiperazines compound, is more and more widely used in various fields.

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

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.

Step 2: (S)-tert-butyl-2-methyl-4-(1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indol-7-yl)piperazine-1-carboxylate To a rt solution of 7-bromo-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indole (3.8 g, 11.64 mmol) in anhydrous toluene (100 mL) was added (S)-tert-butyl-2-methylpiperazine-1-carboxylate (2.79 g, 13.98 mmol), Pd2(dba)3 (1.07 g, 1.17 mmol), t-BuONa (2.24 g, 23.29 mmol), and BINAP (1.45 g, 2.33 mmol) under nitrogen. The reaction mixture was stirred at 80 C. for 3 hrs, then cooled to rt, diluted with H2O (200 mL), and extracted with EtOAc (100 mL*2). The combined organic layers were washed with brine (100 mL), dried over Na2SO4, filtered, and concentrated in vacuo. The crude product was purified by chromatography (silica, EtOAc/PE=1/10) to afford (S)-tert-butyl-2-methyl-4-(1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indol-7-yl)piperazine-1-carboxylate (2.6 g, 5.83 mmol, 50.1%) as a yellow oil. ESI-MS (EI+, m/z): 446.3 [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; (136 pag.)US2019/389843; (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.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

In 2 mL of dimethyl acetamide were combined tert-butyl 4- chloro-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-carboxylate (1.0 g, 3.7 mmol), triethylamine (1.0 mL, 7.4 mmol), and benzyl 1-piperazinecarboxylate (0.86 mL, 4.4 mmol). The reaction vessel was sealed and the reaction mixture was heated to 90 C with stirring. After 5 hours, the reaction was diluted with brine and extracted with methyl t-butyl ether. The combined organic layers were washed sequentially with saturated ammonium chloride and brine, dried over MgSC”4, and concentrated under reduced pressure to a thick oil. The oil was chromatographed (RediSep, 24 g) eluting withl : l ethyl acetate/Hexanes to give tert-butyl 4-(4- ((benzyloxy)carbonyl)piperazin-l-yl)-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-carboxylate (1.3 g, 2.9 mmol, 77 % yield). ES+APCI MS m/z 454.2 [M+H]+., 31166-44-6

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

Reference：
Patent; MIRATI THERAPEUTICS, INC.; ARRAY BIOPHARMA, INC.; FISCHER, John, P.; FELL, Jay, Bradford; BLAKE, James, F.; HINKLIN, Ronald, Jay; MEJIA, Macedonio, J.; HICKEN, Erik, James; CHICARELLI, Mark, Joseph; GAUDINO, John, J.; VIGERS, Guy, P.A.; BURGESS, Laurence, E.; MARX, Matthew, Arnold; CHRISTENSEN, James, Gail; LEE, Matthew, Randolf; SAVECHENKOV, Pavel; ZECCA, Henry, J.; (529 pag.)WO2017/201161; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics