Month: August 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.112984-60-8,6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid,as a common compound, the synthetic route is as follows.

Synthesis of 6-Ffuoro-7-{4-[5-hydroxy-6-(2-methyl-5-nitro- imidazoi-I-yi)-hexyl]-piperazin-I-yi}-l -methyS-4-oxo-4H-2-thia-8b-aza- cyclobu a[a]naphthaSene-3-carboxylic acid (1 15): To a stin-ed solution of 6- Fluoro- 1 -methy-4-oxQ-7-piperazin- 1 -yl-4H-2-thia-8P-aza- cyclobuta[a]naphthalene-3-carboxylic acid, (HI) ( 1 .10 g, 3.16 mmol) in dimethylformamide (30ml) was added potassium carbonate (0.43g, 3.16 mmol) followed by addition of compound (II) (0.85g, 2.63 mmol) and the reaction 1 26 mixture was stirred at RT for 1 6h. The reaction mixture was diluted with ethyl acetate, washed twice with water and finally dried over sodium sulphate to obtain the crude mass. The crude was purified by flash column chromatography while euting with 3-5% methanol/dichloromethane mixture to obtain the pure compound (115) with 20% isolated yield. 1 H-NMR (400 MHz, DMSO) delta ppm: 1 .61 – 1 -68(6H, m, CH2), 2.1 (3H, d, J = 6 Hz, CH3), 2.44 (3H, s, CH3) , 2.54 (4H, m, 2 xCH2), 3.2 (4H, m, 2 xCH2), 3.9-4. 1 (2H. m, 2 x CH2N), 4.38( 1 H, d, J = 14, CHOH). 5.2 1 1 H, d, J = 4.4, OH), 6.38 ( 1 H, d, J = 5.6Hz, CHSN) 6.9 ( 1 H, d, J = 6.8, Ar-H). 7.78 ( 1 H, d, J = 1 4 Hz, Ar-H). 8.02 ( 1 H, s, Ar-H). ESI-MS (m/z): 575(M+H)

112984-60-8, As the paragraph descriping shows that 112984-60-8 is playing an increasingly important role.

Reference：
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; CHAWRAI, Suresh Rameshlal; GHOSH, Shamik; GHOSH, Sumana; JAIN, Nilu; SADHASIVAM, Suresh; BUCHTA, Richard; BHATTACHARYYA, Anamika; WO2015/114666; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-59-9, tert-Butyl 3-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3-METHYLPIPERAZINE-1-CARBOXYLIC acid test-butyl ester (160 mg; 0.80 MMOL ; 2 eq.) (prepared as reported in J. Med. Chem. 1993,36, 690-698), cesium carbonate (195 mg; 0.6 MMOL ; 1.5 eq. ), palladium acetate (9 mg; 0.04 MMOL ; 0.10 eq. ) and 2,2′- bis (diphenylphosphino)-1, 1′-binaphthyl (38 mg; 0.06 MMOL ; 0.15 eq. ) were added to a solution of 2-METHYLQUINOLIN-5-YL-TRIFLUOROMETHANESULFONATE (D1) (117 mg, 0.4 MMOL ; 1 eq) in dry toluene (2.5 mL) under nitrogen. The reaction mixture was stirred at reflux under nitrogen for 10 h. The reaction was cooled and filtered through a pad of celite which was then washed with DCM (50 mL). The filtrates was concentrated in vacuo and the crude product was purified by SPE cartridge (Si, 2g), eluting with 5percent ethylacetate in cyclohexane to afford 3-methyl-4-(2-methylquinolin-5-yl)piperazin-1- carboxylic acid tert-butyl ester as a yellow oil (84 mg; yield 62percent). MS; (ES) m/z: 341.45 [MH] +. C2OH27N302 requires 342. 4.APOS;H-NMR (300 MHz, CDCI3) 8 : 8.5 (d, 1H), 7.77 (d, 1 H), 7.61 (t, 1 H), 7.29 (d, 1 H), 7.12 (d, 1 H), 3.8-3. 6, m/m, 2H), 3. 4- 3. 3 (m, 1 H), 3. 2- 3. 1 (m, 1 H), 3.1-2. 9 (m, 2H), 2.74 (s, 3 H), 1.45 (s, 9H), 1.36 (d, 3H). This compound (84 mg) was dissolved in a mixture 3: 1 of trifluoroacetic acid: DCM (4 mL) and stirred at r. T. for 6h. The solvent was evaporated in vacuo and the residue purified on SCX cartridge (1G) to afford the title compound (D14) (44 mg; yield 76percent) MS; (ES) m/z: 241.45 [MH] +. C15H19N3 requires 242.4. 1H-NMR (300 MHz, CDCI3) 8 : 8.5 (d, 1H), 7.77 (d, 1 H), 7.61 (t, 1 H), 7.29 (d, 1 H), 7.12 (d, 1 H), 3.3 (m, 4H), 3.15 (m, 4 H), 2.74 (s, 3 H), 1.9 (m, 2H)., 120737-59-9

The synthetic route of 120737-59-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXO GROUP LIMITED; WO2004/46124; (2004); 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.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

A mixture of acetoxymethyl 4-nitrophenyl carbonate (1 mmol) and PDBTZ (1 mmol) in hexamethylphosphoramide (1.3 mL) is stirred at ambient temperature until complete by thin layer chromatography. The mixture is diluted with water (35 mL) and extracted with diethyl ether. The extract is washed (aqueous sodium hydroxide, water), dried (sodium sulfate), evaporated, and purified by flash chromatography to provide title compound., 5747-48-8

Big data shows that 5747-48-8 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; WO2008/79839; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13754-38-6, 1-Benzoylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 55Synthesis of TRV 1094 and TRV 1095toluene / 100C X = CI, BCW 109416h X = F, BCW 1095 TRV 1095[00288] To a degassed solution of 5-bromo-2-fluoro-N-phenylaniline (500 mg, 1.89 mmol), phenyl(piperazin-l -yl)methanonein, (538mg, 2,83 mmol) Cs2C03 ( 1.22g, 3.78 mmol), BINAP ( 55.9 mg, 0.09 mmol) in toluene was charged Pd2(dba)3 ( 86.4 mg, 0.09 mmol). The reaction was sealed under an atmosphere of argon and heated to 100 C for 7h. The mixture was cooled, filtered through celite, washed with ethyl acetate and then concentrated in vacuum. The residue was subjected to silica gel column chromatography (60 % hexane/ ethyl acetate) to furnish the title compound (4-(4- fluoro-3-(phenylamino)phenyl)piperazin-l -yl)(phenyl)methanone, TRV 1095 as an off white solid (387mg, 1.03 mmol) 55%. NMR (500 MHz, CDC13) delta (ppm) 2.90-4.00 (m, 8H), 5.77 (bs, 1H), 6.39 (m, 1H), 6.88 (m, 1 H), 6.97-7.01 (m, 2H), 7.12 (m, 2H), 7.30 (m, 2H), 7.40-7.50 (m, 5H).

13754-38-6, The synthetic route of 13754-38-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TREVENTIS CORPORATION; REED, Mark, A.; YADAV, Arun; BANFIELD, Scott, C.; BARDEN, Christopher, J.; WO2012/119035; (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.5317-33-9,3-(4-Methylpiperazin-1-yl)propan-1-ol,as a common compound, the synthetic route is as follows.

5317-33-9, General procedure: The syntheses of compounds 3-20 were carried out accordingto our previously reported method [17]. Briefly, at room temperature,the acid 2 (150 mg, 0.5 mmol) was acyl chlorinated withthionyl chloride (2.5 mL) and then esterized with various alcoholderivatives in chloroform. The reaction mixture was heated underreflux for 5 h to overnight, and cooled to room temperature. Thesolvent was evaporated under reduced pressure. The crude productwas purified by using silica gel column chromatography to give thetarget product.

The synthetic route of 5317-33-9 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Yang, Hui; Wang, Hao-Wen; Zhu, Teng-Wei; Yu, Le-Mao; Chen, Jian-Wen; Wang, Lu-Xia; Shi, Lei; Li, Ding; Gu, Lian-Quan; Huang, Zhi-Shu; An, Lin-Kun; European Journal of Medicinal Chemistry; vol. 127; (2017); p. 166 – 173;,
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.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.,694499-26-8

Methyl 3-azido-4-methylbenzoate (9.6 g, 0.5 mol) and 4-((4-methylpiperazine-1-substituted) methyl) -3- (Trifluoromethyl) aniline (13.7 g, 0.5 mol) was dissolved in re-distilled tetrahydrofuran (50.0 mL), and a solution of potassium tert-butoxide (16.8 g, 0.15 mol) in re-distilled tetrahydrofuran (50.0 mL) was slowly dropped. After 1 hour of reaction, the temperature was naturally raised to room temperature and the reaction was continued for 8 hours. After the reaction was completed, the solvent was spin-dried, extracted with EtOAc and water, and the organic phase was washed with saturated brine,Anhydrous Na2SO4 was dried, and the red solid obtained by silica gel column chromatography was the target product (13.5 g, yield: 61%).

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Chinese Academy Of Sciences Guangzhou Bio-pharmaceutical And Health Institute; Ding Ke; Li Yupeng; Shen Mengjie; Long Huoyou; Zhang Zhang; Leng Fang; Lu Xiaoyun; (51 pag.)CN103539784; (2016); B;,
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.5317-33-9,3-(4-Methylpiperazin-1-yl)propan-1-ol,as a common compound, the synthetic route is as follows.

Alternative preparation of 3-(4-methylpiperazin-1-yl)propyl{3-[3-(3,5-difluorophenyl)-6-oxo-6H-pyridazin-1-ylmethyl]phenyl}carbamate 600 mg (2.02 mmol) of bis(trichloromethyl) carbonate and 2.10 ml (15.1 mmol) of triethylamine is added successively to a solution, kept at 0 C., of 1.55 g (4.95 mmol) of 2-(3-aminobenzyl)-6-(3,5-difluorophenyl)-2H-pyridazin-3-one in 20 ml of dichloromethane. 850 mg (5.37 mmol) of 3-(N-methylpiperazine)propan-1-ol is then added, and the reaction mixture is stirred at room temperature for 18 hours. The reaction mixture is partitioned between 1 N NaOH and dichloromethane. The organic phase is dried over sodium sulfate and evaporated. The residue is chromatographed on a silica-gel column with dichloromethane/methanol: 3-(4-methylpiperazin-1-yl)propyl{3-[3-(3,5-difluorophenyl)-6-oxo-6H-pyridazin-1-ylmethyl]phenyl}carbamate as colourless crystals., 5317-33-9

The synthetic route of 5317-33-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK PATENT GESELLSCHAFT MIT BESCHRAeNKTER HAFTUNG; US2011/136819; (2011); 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.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: Methane sulfonyl chloride (58 muL, 0.7 mmol) and triethylamine (238 muL) was added to a solution of compound 2 (180 mg, 0.6 mmol) in dichloromethane (5 mL) and stirred at room temperature for 1 h. After completion of the reaction by TLC, ice water was added to quench the reaction. The mixture was extracted with dichloromethane (20 mL×3). The organic layer was washed with brine and dried over Na2SO4. The solid was filtered off, and the filtrate was concentrated under reduced pressure to give the methylsulfonylated product (210 mg, yield 93%). To a solution of the methylsulfonylated product (210mg, 0.6 mmol) in DMF (5 mL) was added K2CO3 (111 mg, 0.8 mmol), morpholine (93 muL, 1.0 mmol). The mixture was stirred at 90 C for 2 h. After completion of the reaction by TLC, The mixture was extracted with dichloromethane (20 mL×3). The organic layer was washed with brine and dried over Na2SO4. The solid was filtered off, and the filtrate was concentrated under reduced pressure. The residues were separated by silica gel column chromatography (V petroleum ether: V ethyl acetate = 8:1) to give CH-H-1 (108 mg, yield 53%). Under the same conditions, compounds CH-H-2 to CH-H-16 were obtained., 20327-23-5

The synthetic route of 20327-23-5 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Duan, Zhe; Liu, Jingqiu; Niu, Liping; Wang, Jun; Feng, Mingqian; Chen, Hua; Luo; Bioorganic and Medicinal Chemistry; vol. 27; 15; (2019); p. 3229 – 3236;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Bromo acetyl bromide (4.86 ml, 21.47 mmol, 1 eq) was added dropwise to a stirred ice cold mixture of the piperazine-1-carboxylic acid tert butyl ester (4.0 g, 21.47 mmol, 1 eq) and diisopropyl ethyl amine (12.05 g, 92.5 mmol, 4.3 eq) in dichloromethane (108 ml). The resulting mixture was washed with water (2*50 mL) and saturated sodium chloride solution (100 mL), and dried over MgSO4. After filtration, the solvent was evaporated and the residue was purified with chromatography with (ethyl acetate/n-hexane 1/1) to give the product (2.72 g, 41%) as a orange oil., 57260-71-6

The synthetic route of 57260-71-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Morphochem Aktiengesellschaft Fuer Kombinatorische Chemie; Hubschwerlen, Christian; Specklin, Jean-Luc; Baeschlin, Daniel; Schmitt, Christine; Mueller, Stefan; Cappi, Michael W.; US9133213; (2015); 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.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

a 4-(2-Amino-ethyl)-piperazine-1-carboxylic Acid Tert-butyl Ester A solution of N-tert-butoxycarbonyl-piperazin (5 g, 26.8 mmol), triethylamine (7.44 ml, 53.6 mmol), and chloroethylamine (3.11 g, 26.8 mmol) in dimethylformamide (50 ml) was stirred at room temperature for 72 hours. The reaction mixture was filtered, partitioned between H2O and ethyl acetate. The aqueous phase was lyophilized, the residue stirred with methanol and the precipitate collected by suction. The precipitate was purified by flash chromatography on silica gel (dichloromethane/methanol/aqueous ammonia=9/1/0.1) to give 1.6 g (26percent) of the desired product. MS m/z: 230 ((M+H)+, 91percent)., 57260-71-6

The synthetic route of 57260-71-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Aventis Pharma Deutschland GmbH; US6395737; (2002); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics