6 Sep 2021 News Some tips on Butyl piperazine-1-carboxylate

50606-32-1 Butyl piperazine-1-carboxylate 21963126, apiperazines compound, is more and more widely used in various fields.

50606-32-1,50606-32-1, Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

50.3. 4-[(R)-2-tert-Butoxycarbonylamino-3-(diethoxy-phosphoryl)-propionyl]-piperazine-l- carboxylic acid butyl ester: To a solution of intermediate 50.2 (7.37 g) in DCM (95 mL), THF (24 mL) and DIPEA (16.3 mL) were added HOBT (3.83 g) and EDC-HCl (4.78 g), and the reaction mixture was stirred at RT for 10 min. Subsequently, piperazine- 1 -carboxylic acid butyl ester (5.31 g) was added and the mixture stirred at RT for 2.5 h. The reaction mixture was diluted with DCM, the org. phase washed with sat. aq. NaHCO3 and the aq. phase re-extracted with DCM. The combined org. phases were washed with brine, dried over Na2SO^ and concentrated to dryness. Purification by CC (EtOAc/MeOH 1:0 to 9: 1) gave 7.66 g of the desired product. LC-MS: tR = 0.94 min; [M+H]+: 494.00

50606-32-1 Butyl piperazine-1-carboxylate 21963126, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; ACTELION PHARMACEUTICALS LTD; CAROFF, Eva; HILPERT, Kurt; HUBLER, Francis; MEYER, Emmanuel; RENNEBERG, Dorte; WO2010/116328; (2010); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

6 Sep 2021 News Brief introduction of 2-Methylpiperazine

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

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

Example 1 In a 100 ml four-neck flask, 5.00 g (= 0.0499 mole) of racemic 2-methylpiperazine was placed, and 44 g of 1-butanol (water content 0.05 wt%) was added for dissolution. The solution was cooled to 0C, and 8.47 g of benzyl chlorocarbonate (= 0.0489 mole, purity by HPLC determination analysis 98.5 wt%, 0.98 molar time) was added dropwise in a liquid temperature range from 0 to 8C. Then, stirring was carried out at 0 to 5C for 2 hours, and the reaction solution was partially sampled and determined by the internal standard method (internal standard: anisole). As a result, the reaction yield of 1-benzyloxycarbonyl-3-methylpiperazine was 83.9% (based on the amount of 2-methylpiperazine). The reaction solution was further stirred at room temperature for 12 hours and analyzed. As a result, the reaction yield was 85.1%. Example 3 A reaction was performed as described for Example 1, except that the amount of benzyl chlorocarbonate used was changed from 8.47 g to 10.1 g (= 0.0597 mole, 1.17 molar times). As a result, the reaction yield of 1-benzyloxycarbonyl-3-methylpiperazine was 93.8% (based on the amount of 2-methylpiperazine) after lapse of 2 hours at 0 to 5C. Stirring was carried out at room temperature for further 12 hours, being followed by analysis. As a result, the reaction yield was 95.1%., 109-07-9

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

Reference:
Patent; Toray Fine Chemicals Co., Ltd.; EP1548010; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

6 Sep 2021 News Downstream synthetic route of cis-2,6-Dimethylpiperazine

21655-48-1, The synthetic route of 21655-48-1 has been constantly updated, and we look forward to future research findings.

21655-48-1, cis-2,6-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Methyl 4-fluorobenzoate (4.6 g, 29.7 mmol) was dissolved in DMSO (20 mL), followed by the addition of K2CO3 (12.3 g, 89.1 mmol) and 1-ethylpiperazine (7.6 mL, 59.4 mmol). The mixture was heated to 110 °C and stirred for 10 h before being cooled to room temperature and diluted with water (50 mL) and EtOAc (200 mL). The organic phase was washed with brine (50 mL), dried over Na2SO4, filtered, and concentrated. The residue was purified by silica gel column chromatography using CH2Cl2?MeOH (10:1) to get 4a (6.4 g, 89.2percent) as a yellow solid.

21655-48-1, The synthetic route of 21655-48-1 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Cui, Jing; Peng, Xia; Gao, Dingding; Dai, Yang; Ai, Jing; Li, Yingxia; Bioorganic and Medicinal Chemistry Letters; vol. 27; 16; (2017); p. 3782 – 3786;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

6 Sep 2021 News Some tips on 1-Cyclopropylpiperazine

20327-23-5, As the paragraph descriping shows that 20327-23-5 is playing an increasingly important role.

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.

The title compound (pale beige solid, 26.5 mg, 40%) was prepared by a procedure similar to Example 400 using (S)-2-methyl-4-(5-(4,4,5,5-tetramethyl- l,3,2-dioxaborolan-2-yl)pyridin-2-yl)mo holine (50 mg, 80% purity, 0.16 mmol) and N-(5-bromo-4-fluoro-2-((3S,5R)-3,4,5-trimethylpiperazin-l-yl)phenyl)-6-oxo-4- (trifluoromethyl)-l,6-dihydropyridine-3-carboxamide (50.5 mg, 0.1 mmol). 1H NMR (500MHz, METHANOL-d4) delta = 8.32 (s, 1H), 7.97 (s, 1H), 7.92 (br d, J=8.4 Hz, 1H), 7.79 (br d, J=8.8 Hz, 1H), 7.07 (d, J=12.1 Hz, 1H), 6.95 – 6.90 (m, 2H), 4.16 (br d, J=12.7 Hz, 1H), 4.10 – 3.99 (m, 2H), 3.75 – 3.66 (m, 2H), 3.07 (br d, J=10.5 Hz, 2H), 2.96 (dt, J=3.4, 12.3 Hz, 1H), 2.70 – 2.56 (m, 5H), 2.41 (s, 3H), 1.26 (d, J=6.2 Hz, 3H), 1.19 (d, J=5.7 Hz, 6H); LCMS [M + H]+ 603.6.

20327-23-5, As the paragraph descriping shows that 20327-23-5 is playing an increasingly important role.

Reference:
Patent; ONTARIO INSTITUTE FOR CANCER RESEARCH (OICR); AL-AWAR, Rima; ZEPEDA-VELAZQUEZ, Carlos Armando; PODA, Gennady; ISAAC, Methvin; UEHLING, David; WILSON, Brian; JOSEPH, Babu; LIU, Yong; SUBRAMANIAN, Pandiaraju; MAMAI, Ahmed; PRAKESCH, Michael; STILLE, Julia Kathleen; (1053 pag.)WO2017/147700; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

6 Sep 2021 News New learning discoveries about 1-Ethylpiperazine

5308-25-8, As the paragraph descriping shows that 5308-25-8 is playing an increasingly important role.

5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a solution of substituted piperazines (0.9819mmol) in dry DMF (4mL), triethylamine (0.27mL, 1.9638mmol) and potassium iodide (16.29mg, 0.0981mmol) were added at RT under N2 atmosphere. Compound 2 (0.4g, 0.9819mmol) was added to the above reaction mixture and resultant mixture was heated at 125C. After the reaction was complete, as indicated by TLC, DMF was evaporated in vacuo. The obtained residue was diluted with 20mL of water. The compound was extracted with CH2Cl2 (3×5mL). The organic layers were collected, washed with saturated brine solution, dried over anhydrous MgSO4 and concentrated in vacuo. The resultant crude was purified by column chromatography [CH2Cl2/MeOH (1-10%)] to get the title compounds.

5308-25-8, As the paragraph descriping shows that 5308-25-8 is playing an increasingly important role.

Reference:
Article; Suresh, Narva; Nagesh, Hunsur Nagendra; Renuka, Janupally; Rajput, Vikrant; Sharma, Rashmi; Khan, Inshad Ali; Kondapalli Venkata Gowri, Chandra Sekhar; European Journal of Medicinal Chemistry; vol. 71; (2014); p. 324 – 332;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Simple exploration of 1-(Cyclopropylmethyl)piperazine

57184-25-5, 57184-25-5 1-(Cyclopropylmethyl)piperazine 965875, apiperazines compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.57184-25-5,1-(Cyclopropylmethyl)piperazine,as a common compound, the synthetic route is as follows.

4-Cyclopropylmethyl-piperazine-1-carboxylic Acid 4-[2-(4-chloro-phenyl)-ethylcarbamoyl]-phenyl Ester The title compound was prepared from 4-[2-(4-chloro-phenyl)-ethylcarbamoyl]-phenyl chloroformate and 1-cyclopropylmethyl-piperazine, yield 18%. White crystals, m.p. 225-226 C.; IR (KBr): nu 1710 (ester C=O), 1661 (amide C=O) cm-1.

57184-25-5, 57184-25-5 1-(Cyclopropylmethyl)piperazine 965875, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; Ebdrup, Soren; de Jong, Johannes Cornelis; Jacobsen, Poul; Hansen, Holger Claus; Vedso, Per; US2003/166644; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Simple exploration of 1-(2-Hydroxyethyl)-4-methylpiperazine

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

5464-12-0,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

Sodium hydride (60percent, 0.87 g, 21.80 mmol) was added to diglyme (10 mL). A solution of 2-(4-methyl-piperazin-1-yl)-ethanol (3.14 g, 21.80 mmol) in diglyme (10 mL) was added slowly. The reaction mixture was heated at 40 00 for 1 hour, 4-chloro-pyridin- 2-ylamine (1.40 g, 10.9 mmol) was added and the reaction mixture was heated at 8000 for 1 hour, then at 15700 for 16 hours. The reaction mixture was cooled, diluted with water (20 mL), and THF (20 mL) was added, then NaCI. The organic phase was separated, and the aqueous phase was extracted with THF. The combined organic phase was dried, and the solvent was evaporated. Diethyl ether was added to the residue. The resulting solid was filtered, washed with ether, and dried to afford a white solid (1.86 g, 72percent), (M+H)=237.

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ASTEX THERAPEUTICS LIMITED; SAXTY, Gordon; MURRAY, Christopher William; BERDINI, Valerio; PAGE, Lee William; ROOMANS, Susan; TAMANINI, Emiliano; BUCK, Ildiko Maria; DAY, James Edward Harvey; CARR, Maria Grazia; LEE, Lydia Yuen Wah; WO2015/4481; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Some tips on 1-Methylpiperazin-2-one hydrochloride

109384-27-2, 109384-27-2 1-Methylpiperazin-2-one hydrochloride 17060766, apiperazines compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

[0348] Methyl-2-piperazinone hydrochloride (1:1) (300 mg, 1.99 mmol) was combined with dichloromethane (20 mL) to give a light yellow suspension. N,N-Diisopropylethylamine (309 mg, 417 mul, 2.39 mmol) was added at 0 C. Subsequently 3-(4-cyanophenyl)-2-oxaziridinecarboxylic acid 1,1-dimethylethyl ester (441 mg, 1.79 mmol) in dichloromethane (10 mL) was added during 35 min at 0 C. and the reaction mixture was stirred for 1 h at 0 C. Afterwards the reaction mixture was concentrated in vacuo and the residue was purified by flash chromatography (silica gel, 20 g, 0% to 100% ethyl acetate in n-heptane) to deliver an oil contaminated with 4-cyano-benzaldehyde. This material was purified by a second chromatography (aminophase 5 g, ethyl acetate/n-heptane 1/1) to give the title compound (67 mg, 15%) as white solid; GC-MS (EI) 229.0 (M)+

109384-27-2, 109384-27-2 1-Methylpiperazin-2-one hydrochloride 17060766, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; Grether, Uwe; Hebeisen, Paul; Mohr, Peter; Ricklin, Fabienne; Roever, Stephan; US2013/65876; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

3 Sep 2021 News New learning discoveries about 2-Methylpiperazine

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

109-07-9, {4- [5-BROMOTHIOPHEN-2-YL]-PYRIMIDIN-2-YL}- (2, 2,6, 6-TETRAMETHYL-PIPERIDIN-4-YL)-AMINE, (Step C of Example 5,395 mg, 1 MMOL), Pd (OAC) 2 (20 mg), R- (+)-BINAP (20 mg), 2- methylpiperazine (500 mg, 5 mmol) and NaOtBu (400 mg, 4 mmol) were dissolved in 1,4- dioxan (6 ml) and refluxed for 3 hours. The reaction mixture was poured on water and extracted 3 times with EtOAc. The combined organic phases were dried over sodium sulfate, filtered through a bed of silicagel (TBME/MeOH/ammonia : 90/10/1) and purified via preparative HPLC to give the title compound as yellow crystals. Yield: 10 mg (2%). MS (ESI): 415 [M+H] + LH-NMR (CDCI3) : No. (ppm) 8.12 (d, 1H), 7.43 (d, 1 H), 6.73 (d, 1H), 6.10 (d, 1H), 4. 88 (br d, 1 H), 4.45 (m, 1H), 3.48 (br d, 2H), 2.90-3. 17 (M, 5H), 2.59 (br t, 1H), 2.13 (br d, 2H), 1.41-1. 79 (m, 14H), 1.18 (d, 3H).

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

Reference:
Patent; NOVARTIS AG; NOVARTIS PHARMA GMHBH; WO2004/89913; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

3 Sep 2021 News Some tips on 1-Methanesulfonylpiperazine

55276-43-2 1-Methanesulfonylpiperazine 709161, apiperazines compound, is more and more widely used in various fields.

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

(S)-Epichlorohydrin (48.0 mL, 0.612 mol) was added to a stirred solution of piperazine N-methylsulfonamide (87.3 g, 0.532 mol) in ethanol (1.33 L) at room temperature. The reaction mixture was stirred for 18 h and the white solid precipitate which formed was collected by filtration and washed with ethanol to provide the title intermediate (107.7 g) as a white solid which was used without further purification. (m/z): [M+H]+ calcd for C8H17ClN2O3S, 257.07; found, 257.2. 1H-NMR (DMSO): delta(ppm) 5.09 (d, 1H), 3.84 (m, 1H), 3.65 (dd, 1H), 3.55 (dd, 1H), 3.09 (m, 4H), 2.37 (dd, 1H), 2.86 (s, 3H), 2.50-2.58 (m, 4H), 2.45 (dd, 1H).

55276-43-2 1-Methanesulfonylpiperazine 709161, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; Theravance, Inc.; US2006/276482; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics