Month: June 2021

138775-02-7, (R)-4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

PREPARATIVE EXAMPLE 5; The title compound from Prepartive Example 4 (9.6 gm, 26.3 mmol) was dissolved in absoluteEtOH (100 mL) in a hydrogenation vessel. The vessel was flushed with N2 and 10% Pd/C (3.0g, 50% by weight with water) was added. The mixture was hydrogenated at 55 psi of H2 for 18 hours during which time a precipitate formed. When the reaction was complete (TLC, 30% MeOH/NH3/CH2Cl2), the reaction mixture was filtered through a pad of celite, and the pad washed with EtOH followed by distilled H2O. The filtrate was evaporated to ?1/3 the volume and distilled H2O (200 mL) was added. The resulting solution was extracted with EtOAc (contains pure N,N-Di-Boc-2-carboxy-piperazine which was saved). The water layer was evaporated to dryness with azeotropic removal of residual H2O with methanol (2X) to give pure product (3.98g)., 138775-02-7

The synthetic route of 138775-02-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SCHERING CORPORATION; EP1140904; (2005); B1;,
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

A mixture of 5.6 g (35 mmol) 2-chloro-4-nitropyridine, 5.75 g (37 mmol) 1-cyclo- pentyl piperazine and 4,59 g (35 mmol) N,N-diisopropylethylamine in 35 ml DMF and 12 ml water was heated to 95 0C for 3 h . After evaporation to dryness the residue was taken up in 150 ml NaHCO3 aq. and 150 ml ethyl acetate. The aqueous phase was extracted two times with 150 ml ethyl acetate each and the combined organic phases were washed twice with 10O1 ml NaHCO3 aq each and 100 ml NaCl aq. sat. and dried with MgSO4 and evaporated to dryness. The residue was purified with columnchromatography to^yield 2.85 g (29 %) l-cyclopentyl-4~(4-nitro-pyridin-2-yl)- piperazine (m/e): 277.3 (MH+; 100%) and 4.47 g (47 %) l-(2-chloro-pyridin-4-yl)-4- cyclopentyl-piperazine (m/e): 266.3 (MH+; 100%)., 21043-40-3

As the paragraph descriping shows that 21043-40-3 is playing an increasingly important role.

Reference：
Patent; F.HOFFMANN-LA ROCHE AG; WO2006/63718; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 2,3-dichloropyrazine (2.80 g, 18.8 mmol), racemic 2- methylpiperazine (1.88 g, 18.8 mmol) and K2CO3 (3.90 g, 28.2 mmol) in acetonitrile (25 mL) was heated at 65 C for 15 h with stirring. The reaction mixture was filtered and concentrated. The crude product was purified by flash chromatography on silica gel using CHCl3/MeOH (15: 1) as eluent to give 3.2 g (79%) of the title compound. MS m/z 213 (M+H) +., 109-07-9

As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference：
Patent; BIOVITRUM AB; WO2004/9586; (2004); A1;,
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

To a solution of imidazole (15.7 g, 231 mmol) in DCM (100 mL) was added SOCh (8.25 g, 69.4 mmol, 5.03 mL) at 0 C. The reaction mixture was stirred at 15 C for 1 hour. To the mixture was added tert-butyl (3R)-3-(hydroxymethyl)piperazine-l-carboxylate (5 g, 23.1 mmol) in DCM (100 mL) at -70 C. The reaction mixture was stirred at 15 C for 12 hour. Upon completion, the reaction mixture was quenched by saturated NH4CI (100 mL) and separated, the aqueous layer was extracted with DCM (40 mL).The combined organic layers were washed with brine (20 mL), dried over Na2S04, filtered and concentrated under vacuum to give tert-butyl (3aR)-l-oxo-3a,4,6,7-tetrahydro-3H-oxathiazolo[3,4-a]pyrazine-5-carboxylate (5.8 g, 22.1 mmol, 95.6% yield) as a brown solid., 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; 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

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.

Step-2: To a solution of (E)-methyl 1-acetyl-3-(ethoxy(phenyl)methylene)-2-oxo-2,3-dihydro-1H-pyrrolo[2,3-b]pyridine-6-carboxylate (2.6 g, 7.10 mmol) in DMF (5 mL) was added N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide (1.94 g, 7.43 mmol) at RT and the reaction mixture was heated to 110 C. and stirred for 1 h. The reaction mixture was allowed to cool to RT, treated with piperidine (3 mL) and stirred for 30 min. The reaction mixture was evaporated and the resultant residue was purified by silica gel column chromatography using 5% CH3OH in dichloromethane as eluent to afford (Z)-methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxo-2,3-dihydro-1H-pyrrolo[2,3-b]pyridine-6-carboxylate as yellow solid. MS (ES+): m/z 541.1 (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.; LIM, Dong Sung; OEHLEN, Lambertus J.W.M.; JUNG, Dawoon; US2015/306078; (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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: A solution of intermediate4a or 4b (1mmol), corresponding aliphatic amine (2mmol), K2CO3 (2mmol) in DMF was stirred at room temperature overnight. DMF was removed in vacuo and then H2O was added. The layer was extracted with CH2Cl2 (15mL×3). Organic layers were dried on Na2SO4 and the solvent was removed under pressure. Compounds were purified by column chromatography using dichloromethane/methanol as an eluent to give 5a-11a and 12b-21b.

21655-48-1, 21655-48-1 cis-2,6-Dimethylpiperazine 6950261, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Wang, Yu; Chen, Shaowei; Hu, Gang; Wang, Jiao; Gou, Wenfeng; Zuo, Daiying; Gu, Yucheng; Gong, Ping; Zhai, Xin; European Journal of Medicinal Chemistry; vol. 143; (2018); p. 123 – 136;,
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.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

In a 5 ml_ glass microwave vial equipped with a magnetic stirring bar and nitrogen flow at room temperature was placed the methyl 4-bromo-1-(4-bromo-5- (isopropylthio)thiazol-2-yl)-3-methyl-1 H-pyrazole-5-carboxylate prepared as described above with respect to Compound 1 (150 mg, 0.330 mmol), the 1-cyclopropylpiperazine (42 mg, 0.33 mmol), Cs2C03(537 mg, 1.65 mmol), XantPhos (19 mg, 0.033 mmol) and dioxane (3 ml_). Nitrogen was bubbled in the solvent for 10 minutes followed by the addition of the catalyst RuPhos Pd G1 (27 mg, 0.033 mmol). The vial was capped and placed in an oil bath at 105 C for 16 h. The product was purified by flash chromatography (dry packing) on silica gel using a gradient 0 to 10% EtOAc in hexanes to give the title compound (28 mg, 0.055 mmol, 17%) as a yellow oil. MS (m/z): 500.0 [M+1]+., 20327-23-5

20327-23-5 1-Cyclopropylpiperazine 4742004, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BANTAM PHARMACEUTICAL, LLC; SIDDIQUI, Arshad, M.; CIBLAT, Stephane; DERY, Martin; CONSTANTINEUA-FORGET, Lea; GRAND-MAITRE, Chantal; BRUNEAU-LATOUR, Nicolas; SHIPPS, Gerald, W.; COOPER, Alan, B.; OZA, Vibha; KOSTURA, Matthew, W.; LUTHER, Michael; LEVINE, Jedd; (174 pag.)WO2018/102453; (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.5271-27-2,1-Methyl-3-phenylpiperazine,as a common compound, the synthetic route is as follows.

-Methyl-3-phenylpiperazine (17.6 g; 0.1 mol) was dissolved in 100 dichloromethane.Triethylamine (5 ml; ca 0.03 mol) was added. A solution of methyl chlorooxalate (10 ml; 0.10 mol) in dichloromethane was slowly added under cooling. After the total addition, 5271-27-2

As the paragraph descriping shows that 5271-27-2 is playing an increasingly important role.

Reference：
Patent; N.V. ORGANON; WO2007/144409; (2007); 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.

(2S,6R) and (2R,6S)-1-(-2,6-Dimethylpiperazin-1-yl)ethanone. To a solution of cis-3,5-dimethylpiperazine-1-carboxylic acid t-butylester (1.0 g, 4.666 mmol) in CH2Cl2 (10 mL), TEA (0.715 mL, 5.133 mmol) and acetyl chloride (0.364 mL, 5.133 mmol) were added. The reaction mixture was stirred at rt. for 2 hr. Then it was quenched with water and acidified with 1N HCl solution. Extracted with CH2Cl2 (2×50 mL) and the organic layers were combined, dried (MgSO4) and concentrated to give a yellowish solid. It was then dissolved in CH2Cl2 (10 mL) and TFA (2 mL) was added. The reaction mixture was stirred at rt. for 3 hr. TFA and solvent were evaporated to give a yellowish thick oil as final product as TFA salt. (1.1 g, 93% yield). MS m/z 157(MH+), Retention time: 0.208 min. 1H NMR (500 MHz, CHLOROFORM-D) delta ppm 1.38 (d, J=7.02 Hz, 6H) 2.09 (s, 3H) 3.06 (dd, J=12.97, 5.04 Hz, 2H) 3.25 (d, J=13.43 Hz, 2H) 4.27-4.73 (m, 2H)., 129779-30-2

129779-30-2 (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 10822535, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Bristol-Myers Squibb Company; US2007/270406; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

192130-34-0, tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A resealable tube was charged with 4-chloro-2-(3-fluoro-4-(2-(piperidin-1-yl)ethoxy)phenyl)-3-phenylfuro[2,3-b]pyridine 6e (0.096 g, 0.213 mmol), 4-N-(tert-butoxycarbonyl)-1-aminoethylpiperazine (0.098 g, 0.426 mmol), potassium carbonate (0.589 g, 4.26 mmol), and toluene (3 mL). The Pd/BINAP solution was added along with 1.5 mL of toluene, and the system was flushed with argon. The tube was sealed and the mixture stirred at 130° C. for 20 h. The reaction mixture was partitioned between ethyl acetate and saturated aqueous sodium bicarbonate solution. The aqueous phase was separated and extracted with ethyl acetate. The combined organic phases were washed with saturated aqueous sodium chloride solution, dried over anhydrous sodium sulfate, filtered and concentrated to afford an orange brown oil. This oil was purified via preparative thin layer chromatography (eluting with 95:5:0.5, dichloromethane/methanol/ammonium hydroxide) to afford tert-butyl 4-(2-(2-(3-fluoro-4-(2-(piperidin-1-yl)ethoxy)phenyl)-3-phenylfuro[2,3-b]pyridin-4-ylamino)ethyl)piperazine-1-carboxylate (not shown) as a yellow oil. MS (MH+) 644.4; Calculated 643 for C37H46FN5O4., 192130-34-0

The synthetic route of 192130-34-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Nunes, Joseph J.; Martin, Matthew W.; White, Ryan; McGowan, David; Bemis, Jean E.; Kayser, Frank; Fu, Jiasheng; Liu, Jinqian; Jiao, Xian Yun; US2006/46977; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics