Month: July 2021

4318-42-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

Step 1 (1H-Indol-6-yl)-(4-isopropyl-piperazin-1-yl)-methanone A mixture of 1 g (6 mmol) indole-6-carboxylic acid (commercially available), 0.96 g (0.7 mmol) 1-(2-propyl)-piperazine (commercially available), 2.39 g (7 mmol) TBTU and 4 g (31 mmol) DIPEA in 30 ml THF was stirred for 1 h at room temperature. After evaporation of all volatiles Na2CO3 (10percent aq.) and ethyl acetate was added. The mixture was extracted with ethyl acetate and the combined organic fractions were washed with NaCl (sat. aq.), dried with Na2SO4 and evaporated to dryness. The residue was purified by flash column chromatography on silica eluding with a mixture formed from DCM, MeOH and NH3 aq. to yield after evaporation of the combined product fractions 1.64 g (97percent) of the title compound as light yellow solid. MS (m/e): 272.5 (MH+).

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference：
Patent; Nettekoven, Matthias; Roche, Olivier; US2008/32976; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

78818-15-2, Benzyl 3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

78818-15-2, Step 1 4-Benzyloxycarbonyl-[1-(2-oxo-2-(adamant-1-yl))ethyl]piperazin-2-one To a round bottomed flask were added 4-benzyloxycarbonylpiperazin-2-one (234.26 mg, 1.0 mmol) along with N,N-dimethylforamide (5.0 ml), and sodium hydride (73.0 mg (60%), 1.0 mmol). After the evolution of hydrogen had ceased the reaction was allowed to stir for an additional 30 minutes. To this was added 1 adamantyl bromomethyl ketone (257.18 mg, 1.0 mmol). The reaction stirred at Rt. for 18hrs. The reaction was poured into water (25 ml) and extracted with ethylacetate (2*25 ml). The ethylacetate layer was washed with brine and dried (MgSO4). Solvent removal yielded 4-benzyloxycarbonyl-[1-(2-oxo-2-(adamant-1-yl)ethyl]piperazin-2-one. 400 Mhz H1 NMR (CDCl3): 1.68-1.91(m,12H), 2.06 (br s,3H), 3.32(t,2H), 3.77(t,2H), 4.20(s,2H), 4.34(s,2H), 5.16(s,2H), 7.36(m,5H). The material was used with out further purification.

As the paragraph descriping shows that 78818-15-2 is playing an increasingly important role.

Reference：
Patent; Eng, Wai-Si; Lobell, Robert B.; Lumma, William C.; Smith, Anthony M.; US2002/72081; (2002); 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.106261-48-7,4-((4-Methylpiperazin-1-yl)methyl)benzoic acid,as a common compound, the synthetic route is as follows.

Intermediate 42: W-(5-bromo-2-cyano-4-pyrimidinyl)-4-[(4-methyl-1 -piperazinyl) methyl]-W-(2-methylpropyl)benzohydrazide trifluoroacetate. Preparation of 4-[(4-methyl-1-piperazinyl)methyl]benzoyl chloride.Intermediate 38 (500 mg, 2.13 mmol) was dissolved in thionyl chloride (5 ml). The reaction mixture was refluxed for 6 hours. The solvent was evaporated in vacuo and the crude product was used without any further purification.To a stirred solution of Intermediate 41 (200 mg, 0.74 mmol) in pyridine (10 ml_), a mixture of the previously prepared acid chloride (539 mg, 2.13 mmol) and DIPEA (0.26 ml_, 1.48 mmol) in dry THF (10 ml.) was added and the resulting reaction mixture was stirred at room temperature for 2 hours. The solvent was evaporated in vacuo and the crude reaction mixture was purified by flash chromatography (silica gel, dichloromethane:methanol). The solid was repurified by HPLC (H2O, 0.1%TFA:ACN) to give the title compound. 1H NMR (300 MHz, DMSO) delta ppm: 11.36 (s, 1 H), 8.64 (s, 1 H), 7.92 (d, 2H), 7.48 (d, 2H), 3.98 (m, 1 H), 3.73 (s 2H), 3.38 (m, 4H), 3.02 (m 4H), 2.78 (s, 3H) 2.42 (m, 1 H), 2.05 (m, 1 H), 0.94 (d, 6H). [ES+ MS] m/z 486 (M)+.

106261-48-7, As the paragraph descriping shows that 106261-48-7 is playing an increasingly important role.

Reference：
Patent; GLAXO GROUP LIMITED; WO2008/107368; (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.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.

59878-57-8, EXAMPLE 2 4-Amino-2-[4-(cyclopropylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline N-(Cyclopropylcarbonyl)piperazine (3.08 g., 0.02 mole) and 2-chloro-4-amino-6,7-dimethoxyquinazoline (4.74 g., 0.02 mole) are reacted according to the procedure of Example 1(a). The crude product crystallized from ethanol affords analytically pure 4-amino-2-[4-(cyclopropylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline, m.p. 283.5-285.5 C. (corr.). Analysis. Calcd. for C18 H23 N5 O3 (percent): C, 60.49; H, 6.49; N, 19.59. Found (percent): C, 60.56; H, 6.46; N, 19.41.

As the paragraph descriping shows that 59878-57-8 is playing an increasingly important role.

Reference：
Patent; Mead Johnson & Company; US4060615; (1977); A;,
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.7365-45-9,2-(4-(2-Hydroxyethyl)piperazin-1-yl)ethanesulfonic acid,as a common compound, the synthetic route is as follows.

7365-45-9, General procedure: Larger Scale Production of Nucleotide Analogs. (0230) The process described for small-scale batches is scalable to larger batches by using proportionate amounts of compounds. As an alternate to the small-scale batches described above, larger scale batches were prepared. Here, reaction mixtures having a total volume of 0.25 ml (>10× the volume of the small-scale batch) and containing 40 mM of a reagent from Table 1, 10 mM magnesium acetate, 80 muM dATP, 50 mug/ml BSA, and 5.84 muM p41 subunit (containing 0.64 M glycerol following dilution in the glycerol diluent described above) were incubated for 30 min at 70 C. Incubation with the p41 subunit and TLC analysis on PEI plates showed greater than 60% conversion of starting material (i.e., the reagent and dNTP) into nucleotide analog products (dNMP derivatives). Experiments were also performed using heavy isotopes incorporated in dNTP, but the presence of a heavy isotope did not alter the utilization of dNTP in the reaction. (0231) Samples from reaction mixtures were analyzed using a capillary reverse phase liquid chromatography system coupled to an Orbitrap Discovery mass spectrometer in negative mode. Negative mode nanospray mode was set to -1.5 kV, and chromatographic flow rate was <20 nl/min. Fragmentation was achieved using high collision dissociation at 45% energy. Isotope-labeled samples were run both individually and combined. By analyzing the mass difference between heavy and light fragmentation pattern, the identity of each fragmentation peak was established. As the paragraph descriping shows that 7365-45-9 is playing an increasingly important role. Reference：
Patent; THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY OF COMMERCE; MEMORIAL SLOAN KETTERING CANCER CENTER; UNIVERSITY OF MARYLAND; Marino, John P.; Kelman, Zvi; Hurwitz, Jerard; Giulian, Gary G.; (45 pag.)US9534243; (2017); B2;,
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.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Intermediate 9: 2,2-Dimethyl-piperazine-l-carboxylic acid benzyl ester trifluoro acetate 9.1 : 2,2-Dimethyl-piperazine- 1 ,4-dicarboxylic acid 1 -benzyl ester 4-tert-butyl ester To a solution of 18.5 g (82.0 mmol) 3,3-dimethyl-piperazine-l-carboxylic acid tert-butyl ester in 150 mL DCM at RT was added 30.0 mL (174 mmol) DIPEA. The mixture was cooled with ice and a solution of 14.0 mL (93.2 mmol) benzyl chloroformate in 60 mL DCM was added drop wise. The reaction mixture was stirred at RT over night and quenched with saturated aqueous sodium bicarbonate solution. The product was extracted with DCM. The organic layers were combined, dried over sodium sulfate and concentrated in vacuo. Yield: 23.0 g (81%) ESI-MS: m/z = 249 (M-BOC+H)+ Rt(HPLC): 1.60 min (method 1)

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

Reference：
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HEIMANN, Annekatrin; DAHMANN, Georg; GRUNDL, Marc; MUELLER, Stephan Georg; WELLENZOHN, Bernd; WO2013/87805; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of ferf-butyldimethylsilyl chloride (1.53 g, 10.17 mmol) in DCM (10 ml) was added dropwise to (S)-4-N-Boc-2-hydroxymethyl-piperazine (2 g, 9.25 mmol) and triethylamine (2.58 ml, 18.49 mmol) in DCM (50 ml) at 20C over a period of 5 minutes under air. The resulting solution was stirred at 20C for 16 hours then evaporated to dryness. The residue was purified by flash silica chromatography, elution gradient 0 to 5% EtOH in EtOAc. Pure fractions were evaporated to dryness to afford ferf-butyl (S)-3-(((ferf-butyldimethylsilyl)oxy)methyl)piperazine-l-carboxylate (2.84 g, 93%) as a colourless oil. 1H NMR (500 MHz, CDCI3) 0.00 (s, 6H), 0.84 (s, 9H), 1.40 (s, 9H), 2.48 (s, 1H), 2.6 – 2.87 (m, 3H), 2.92 (d, 1H), 3.41 (dd, 1H), 3.52 (s, 1H), 3.85 (s, 2H)., 314741-40-7

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; LAMONT, Scott, Gibson; KEMMITT, Paul, David; GOLDBERG, Frederick, Woolf; (158 pag.)WO2019/215203; (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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

A mixture of (R) -tert-butyl 3-methylpiperazine-1-carboxylate (500 mg, 2.50 mmol) , propionic acid (0.22 mL, 3.00 mmol) , EDCI (718 mg, 3.74 mmol) and HOAT (850 mg, 6.24 mmol) in DCM (15 mL) was stirred at 0 , and DIPEA (1.7 mL, 9.99 mmol) was added dropwise. After the addition, the mixture was stirred at rt for 16 h and washed with water (10 mL × 2) . The organic layer was dried over anhydrous Na2SO4 and concentrated. The residue was purified by silica gel chromatography eluted with Petroleum ether/EtOAc (v/v) 2/1 to give (R) -tert-butyl 3-methyl-4-propionylpiperazine-1-carboxylate as colorless oil (630 mg, 95) .1H NMR (400 MHz, CDCl3) : delta ppm 4.76, 4.36 (m, m, 0.5H, 0.5H) , 4.00-3.94 (m, 1H) , 3.85-3.76 (m, 1H) , 3.53, 3.29 (m, m, 0.5H, 0.5H) , 2.98-2.96 (m, 1H) , 2.83-2.74 (m, 2H) , 2.34-2.26 (m, 2H) , 1.45 (s, 9H) , 1.13 (t, J 7.0 Hz, 6H) .

163765-44-4, 163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (2016); 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.197638-83-8,1-Boc-4-(4-Formylphenyl)piperazine,as a common compound, the synthetic route is as follows.

Example 24 te/t-Butyl 4-(4-(6-bromo-7-(4-(4-chlorobenzyl)piperazin-1-yl)-3H-imidazo[4,5- C6H4CI), 7.41 (m, 4H, C6H4CI), 7.07 (d, J = 8.9 Hz1 2H) and 8.04 (d, J = 8.9 Hz, 2H)(2,6-C6H4 and 3,5-C6H4), 8.17 (s, 1H, imidazo[4,5-/b]pyridine 5-H), 13.23 (br s, 1H, imidazo[4,5-b]pyridine N-H);LC (Method B) – MS (ESI, m/z): Rt = 4.55 min – 666, 668, 670 [(M+H)+, BrCI isotopic pattern]., 197638-83-8

The synthetic route of 197638-83-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CHROMA THERAPEUTICS LTD.; WO2009/1021; (2008); 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 asolution of 3-(chloroacetyl)-2-methylbenzonitrile (1.7 g, 8.8 mmol) in THF (17.6 mL) was added (R)-4-N-boc-2-hydroxymethyl-piperazine (2.279 g, 10.54 mmol) and DIPEA (3.07 mL, 17.56 mmol) at rt. The reaction mixture wasstirred at rt over the weekend. After concentration, the residue was partitioned between EtOAc and aqueous NaHCO3(saturated). The aqueous layer was extracted with EtOAc (2x). The combined organic phase was washed with brine,dried over anhydrous MgSO4, and filtered. Concentration was followed by purification by prep TLC (silica gel; 10%MeOH/DCM) to give the title compound: LC/MS (M+1)+ = 374.14

278788-66-2, The synthetic route of 278788-66-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Merck Sharp & Dohme Corp.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; (128 pag.)EP2744499; (2016); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics