Month: September 2021

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To the product of Step 3 (1.00 g, 3.3 mmol) and DIPEA (0.88 ml, 5.1 mmol) in CH2Cl2 (15 ml) add trifluoroacetic anhydride (0.57 ml, 4.1 mmol). Stir 2 h and add a second portion each of DIPEA and anhydride. Stir 1 h and wash with satd. NaHCO3, then water. Dry (MgSO4) and concentrate to obtain the amide as a yellow solid., 154590-35-9

154590-35-9 tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate 16203630, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Schering Corporation; US2005/239795; (2005); 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.

R)- l -Boc-3-(Hydroxymethyl)piperazine (10 g, 46.2 mmol) was dissolved in a mixture of DCM (180 ml) and sat. NaHC03 (180 ml). CBZ-C1 (6.60 ml, 46.2 mmol) was dissolved in DCM (15 ml) and added dropwise with vigorous stirring. The mixture was stirred for 2.5 hours. The layers were separated and the aqueous phase was extracted with DCM. The combined organic phases were washed with brine, dried over Na2S04 and the solvent was removed in vacuo to give an oil which was used in the next step without purification.

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; MERCK SHARP & DOHME CORP.; MSD R&D (CHINA) CO., LTD; WILLIAMS, Peter D.; MCCAULEY, John A.; BENNETT, David Jonathan; BUNGARD, Christopher J.; CHANG, Lehua; CHU, Xin-Jie; DWYER, Michael P.; HOLLOWAY, M. Katharine; KEERTIKAR, Kartik M.; LOUGHRAN, H. Marie; MANIKOWSKI, Jesse J.; MORRIELLO, Gregori J.; SHEN, Dong-Ming; SHERER, Edward C.; SCHULZ, Jurgen; WADDELL, Sherman Tim; WISCOUNT, Catherine M.; ZORN, Nicolas; TUMMANAPALLI, Satyanarayana; SIVALENKA, Vijayasaradhi; HU, Bin; JI, Tao; ZHONG, Bin; WO2015/13835; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

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

314741-39-4, (S)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of Example 1(c) in dry tetrahydrofuran (40ml) at 0C was treated with lithium aluminium hydride (0.50g) and the mixture was stirred at 0C for 1.5 hours.. The cooled solution was treated dropwise with a solution of 2M sodium hydroxide until a white precipitate had formed.. Dichloromethane and anhydrous sodium sulfate were added and the solution was filtered and evaporated to give a pale yellow oil (3.0g). MS (+ve ion electrospray) m/z 217 (MH+).

314741-39-4, 314741-39-4 (S)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 1501855, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SmithKline Beecham plc; EP1187828; (2004); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

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.

To a solution of Intermediate E (59 mg, 0.20 mmol) in DMF (3 mL) were added tert-butyl 3,3-dimethylpiperazine-1-carboxylate (50.7 mg, 0.24 mmol), HATU (97.4 mg, 0.26 mmol) and DIPEA (51 mg, 69 .iL, 0.39 mmol) and the resulting mixture was stirred at rt ON. The reaction mixture was then diluted with EtOAc, washed with water and brine consecutively, dried over anhydrous sodium sulfate, filtered and concentrated to dryness. The residue was purified by flash chromatography eluting with EtOAc/Hexanes 0-50% in 20 CV to obtain tert-butyl 4- [6-(4-fluorophenyl)-8-isopropyl-imidazo[ 1 ,2-b]pyridazine-2-carbonyl] – 3,3-dimethyl-piperazine-1-carboxylate (58 mg) as a white solid. ?H NMR (400 MHz, CDC13) oe 8.33 (s, 1H), 8.11 -7.87 (m, 2H), 7.24-7.10 (m, 3H), 4.28 (s, 2H), 3.77 -3.43 (m, 5H), 1.61 (s, 6H), 1.51 – 1.40 (m, 15H). LC-MS: 497.5 (M+H)., 259808-67-8

The synthetic route of 259808-67-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; VERTEX PHARMACEUTICALS INCORPORATED; FARMER, Luc J.; FOURNIER, Pierre-Andre; LESSARD, Stephanie; LIU, Bingcan; ST-ONGE, Miguel; STURINO, Claudio; SZYCHOWSKI, Janek; YANNOPOULOS, Constantin; WO2015/48245; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

301673-16-5, tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Sodium hydroxide (IN aqueous solution, 20 mL, 20 mmol) was added to a solution of Intermediate B (2.59 g, 10.7 mmol) in EtOH (20 mL), and the reaction mixture was heated to 70 0C for 1 h. Upon cooling to rt, the EtOH was removed under reduced pressure. The aqueous solution was diluted with THF (40 mL) and benzyl chloroformate (1.60 mL, 10.7 mmol) was added. After 1 h, the reaction mixture was diluted with water (50 mL) and was extracted with EtOAc (3 x 50 mL). The combined organics were dried over Na2SO4, filtered, and concentrated under reduced pressure. The material was purified by column chomatography (20 to 40percent EtOAc in Hexane gradient) to give 3.16 g (85percent) of the desired product as a thick oil. LC-MS: RT = 8.41 min., [M+H]+ = 373.1.

301673-16-5, As the paragraph descriping shows that 301673-16-5 is playing an increasingly important role.

Reference：
Patent; CRITICAL THERAPEUTICS, INC.; WO2007/146066; (2007); A2;,
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.120737-59-9,tert-Butyl 3-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

1-(tert-Butoxycarbonyl)-3-methylpiperazine (Oakwood Co., 1.36 g), 5-bromo-2-chlorobenzotrifluoride (Tokyo Chemical Industry CO., LTD., 2.0 g), 2-(di-tert-phosphino)biphenyl (STREM, 41 mg), tris(dibenzylideneacetone)dipalladium (Aldrich Co., 62 mg) and sodium tert-butoxide (980 mg) were added to toluene (10 ml), and the mixture was stirred with heating at 60°C for 3 hr. After completion of the reaction, the insoluble material was filtered off, and the filtrate was evaporated under reduced pressure. The obtained residue was purified by silica gel column chromatography (elution solvent: hexane-ethyl acetate (7:1-3:1)). A 4N hydrochloric acid-ethyl acetate solution was added to the obtained solid and the mixture was stirred for 5 hr. Diethyl ether was added thereto, and the precipitated solid was collected by filtration to give 1-[4-chloro-3-(trifluoromethyl)phenyl]-2-methylpiperazine hydrochloride (692 mg, yield 32percent). 1H-NMR(400MHz,DMSO-d6)delta(ppm): 1.11-1.23 (3H,m), 3.01-3.30(5H,m), 4.27-4.31(1H,m), 7.21-7.55(3H,m), 9.10(1H,s), 9.61(1H,s)., 120737-59-9

Big data shows that 120737-59-9 is playing an increasingly important role.

Reference：
Patent; Mitsubishi Pharma Corporation; EP1714961; (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.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

To a stirred solution of 4-((4-ethylpiperazin- 1 -yl)methyl)-3-(trifluoromethyl)aniline (Intermediate Cl) (150 mg, 0.52 mmol) in THF (20 mL) was added triphosgene (54 mg, 0.18 mmol) and the resulting mixture was stirred at 70 C. After 1 h of heating the mixture wasconcentrated under reduced pressure and the residue was dissolved in THF (20 mL). That solution was added dropwise to a stirred mixture of tert-butyl 4-(5-amino-2-chlorophenoxy)- 6H-pyrimido [5,4-b] [1 ,4]oxazine-8(7H-carboxylate (step 1 intermediate) (150 mg, 0.40 mmol) and triethylamine (172 jiL, 1.19 mmol) in THF (20 mL) at RT. The resultant mixture was stirred for 2 h at 70 C. The mixture was cooled to RT and quenched with water. Theaqueous mixture was extracted twice with ethyl acetate. The combined organic layers were washed with water followed by brine. The solution was dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure. The residue thus obtained was purified by silica gel column chromatography to yield 100 mg of the desired product. ?H NMR (400 MHz, DMSO-d6) oe 1.09 (t, J= 7.2 Hz, 3H), 1.50 (s, 9H), 2.42-2.5 1 (m, 1OH), 3.54 (br s, 2H),3.94 (t, J= 8.4 Hz, 2H), 4.40 (t, J= 7.6 Hz, 2H), 7.29 (dd, J, = 2.4 Hz, J2 = 8.0 Hz, 1H), 7.48(d, J 8.8 Hz, 1H), 7.55-7.94 (m, 3H), 7.95 (s, 1H), 8.05 (s, 1H), 9.15 (s, 1H), 9.20 (s, 1H)., 630125-91-6

The synthetic route of 630125-91-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLENMARK PHARMACEUTICALS S.A.; PATEL, Vinod; REDDY, Venkateshwar; GHARAT, Laxmikant Atmaram; CHAUDHARI, Sachin Sundarlal; DAS, Sanjib; VELGALETI, Ranganadh; SHAH, Daisy Manish; BAJPAI, Malini; (262 pag.)WO2018/215668; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics