Month: August 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

To a solution of 1-tert-butyl 3-methyl piperazine-1,3-dicarboxylate (2.44 g, 10 mmol) in DCM (50 mL) was added phenylboronic acid (2.35 g, 20 mmol), Cu(OAc)2 (1.82 g, 10 mmol) and pyridine (1 .58 g, 20 mmol) in turns with stirring. The reaction mixture was stirred at ambient temperature for 24 hrs under an oxygen atmosphere. The reaction mixture was filtered and filtrate was concentrated. The residue was purified by column chromatography on silica gel(petroleum ether: EtOAc= 3:1) to afford compound Tnt 44-1 (2.74 g). MS-EST (mlz): 321 (M+1) Rf: 0.3 (PE : EtOAc= 3 : 1).

129799-08-2, The synthetic route of 129799-08-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK SHARP & DOHME CORP.; COBURN, Craig; MALETIC, Milana; LUO, Yunfu; QI, Zhiqi; YU, Tingting; SOLL, Richard; WO2015/70367; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

196811-66-2, tert-Butyl 4-carbamothioylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

a) 4-(5-Hydroxymethyl-thiazol-2-yl)-piperazine-l-carboxylic acid tert-butyl ester; To a solution of 179 mmol 30% aqueous hydrogen peroxide in 60 ml water was added 1 N aqueous sodium hydroxide solution until the pH was 9. The reaction mixture was then cooled to 100C and 163 mmol acrolein was added dropwise. Further amounts of 1 N aqueous sodium hydroxide solution were added during the addition in order to maintain the pH of the reaction mixture between pH 8 and 9. The mixture was stirred for 30 min at 0 0C and then 40.8 mmol thiocarbamoyl-piperazine-1-carboxylic acid tert- butyl ester (prepared from tert-butyl 1-piperazinecarboxylate, 1,1′- thiocarbonyldiimidazole and ammonia according to the procedure of J. Med. Chem. 1998, 41, 5037-5054) was added. To the resulting suspension was added 25 ml ethanol and the mixture was heated at 80 0C for 30 min. The resulting solution was diluted with ethyl acetate/tetrahydrofuran (1:1) and the mixture was washed twice with brine. The organic phase was dried over sodium sulphate and concentrated in vacuo to afford the title compound as a yellow oil (yield 99%). MS (m/e): 300.3 (M+H+, 100%)., 196811-66-2

196811-66-2 tert-Butyl 4-carbamothioylpiperazine-1-carboxylate 12093220, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; WO2006/72436; (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

Comparative example 6 A reaction was carried out as described for Example 6, except that the solvent was changed from 44 g of ethanol to a mixed solvent consisting of 22 g of water and 22 g of ethanol (water content 50.0 wt%). As a result, the reaction yield of 1-benzyloxycarbonyl-3-methylpiperazine was 37.7% (based on the amount of 2-methylpiperazine)., 109-07-9

The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

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

74879-18-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: To a stirred mixture of homopiperazine (0.60 g, 6.00 mmol), 4-fluorobenzaldehyde (0.60 g, 5.00 mmol) in DCM (15 mL) wasadded AcOH (0.08 mL, 0.50 mmol) and the mixture was stirred atroom temperature for 0.5 h. Then sodium triacetoxyborohydride(1.60 g, 7.50 mmol) was added in portions. The reaction was stirredat the same temperature for 6 h. Finally, the mixture was dilutedwith saturated aqueous NaHCO3 (15.00 mL) followed by water(15.00 mL) and extracted with EtOAc (3 15.00 mL). The organiclayer was dried (MgSO4), filtered, and concentrated in vacuo. Theresidue was purified by column chromatography on silica gel (EtOAc/PE 5:1) to afford yellow oil (0.90 g, yield 77%).

74879-18-8 (S)-(+)-2-Methylpiperazine 2734219, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Hu, Suwen; Wang, Zhilong; Hou, Tingjun; Ma, Xiaodong; Li, Jing; Liu, Tao; Xie, Xin; Hu, Yongzhou; Bioorganic and Medicinal Chemistry; vol. 23; 5; (2015); p. 1157 – 1168;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of starting material (27 mg, 0.1 mmol), 2-methoxy-4-(4-methylpiperazin-1-yl)benzenamine (22 mg, 0.1 mmol), X-Phos (4.3 mg), Pd2(dba)3 (5.5 mg) and K2CO3 (41.5 mg, 0.3 mmol) in t-BuOH (1.5 mL) was heated at 100 C. in a seal tube for 4 h. The reaction was then filtered through celite, eluted with dichloromethane, and concentrated in vacuo. The residue was then purified by reverse-phase prep-HPLC to afford the title compound as the TFA salt (21.5 mg, 47%).

122833-04-9, 122833-04-9 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline 20136253, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; DANA-FARBER CANCER INSTITUTE, INC.; Gray, Nathanael S.; Waller, David; Choi, Hwan Guen; Wang, Jinhua; Deng, Xianming; (104 pag.)US2016/24115; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

350684-49-0, tert-Butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 166 N-[4-(4-tert-Butoxycarbonylpiperazin-1-ylcarbonyl)phenyl]-(2-chloro-5-nitrophenyl)carboxamide The title compound (0.70 g, yield 95%) was obtained according to the procedure described in Example 2 using 4-(4-tert-butoxycarbonylpiperazin-1-ylcarbonyl)aniline (0.46 g, 1.50 mmol), DMA (5 ml) and 2-chloro-5-nitrobenzoyl chloride (0.40 g, 1.80 mmol). 1H-NMR (400 MHz, DMSO-d6, TMS): delta(ppm) 1.41 (9H, s), 3.32-3.55 (8H, m), 7.45 (2H, d, J=8.5 Hz), 7.77 (2H, d, J=8.5 Hz), 7.91 (1H, d, J=8.8 Hz), 8.36 (1H, dd, J=2.7, 8.8 Hz), 8.50 (1H, d, J=2.7 Hz), 10.90 (1H, s); MS(FAB) m/z: 489 (M+H)+., 350684-49-0

As the paragraph descriping shows that 350684-49-0 is playing an increasingly important role.

Reference：
Patent; SANKYO COMPANY, LIMITED; US2003/134859; (2003); 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.

Preparation 6 (5-Bromo-l,2-benzothiazol-7- l)-[cz5,-3,5-dimethylpiperazin-l-yl]methanone To a mixture of 5-bromo-l,2-benzothiazole-7-carboxylic acid (10 g, 0.039 mol) and DMF (100 mL) is added cw-2,6-dimethylpiperazine (6.64 g, 0.058 mol) at 28 °C. The resulting mixture is cooled to 0 °C and HATU (22.1 g, 0.058 mol) is added in portions (internal temperature is 0 to 2 °C). The mixture is warmed to 25 °C and stirred at this temperature for 16 h. The mixture is concentrated under vacuum, poured into water (30 mL) and extracted with ethyl acetate (3 chi 50 mL). The combined organic portions are washed with saturated sodium bicarbonate solution (30 mL) and brine (30 mL). The organic portion is concentrated and the resulting residue is dissolved in a mixture of dichloromethane (30 mL) and water (30 mL). 6 N HC1 is added dropwise until a majority of the solid appears. The solid is collected by filtration. The aqueous phase of the filtrate is separated and combined with the solid cake, basified with sodium bicarbonate solution to pH 8, and then extracted with dichloromethane (3 chi 50 mL). The organic phase is concentrated to give the title compound (10.1 g, 74percent). LC-ES/MS m/z (79Br/81Br) 354/356 [M+H]+., 21655-48-1

As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

Reference：
Patent; ELI LILLY AND COMPANY; GENIN, Michael James; HOLLOWAY, William Glen; REKHTER, Mark David; (41 pag.)WO2016/81311; (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.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: In an oven-dried RB flask, 4-chloro-2-phenyl-1H-pyrrolo[3,2-c]pyridine 6b (250 mg, 1.09 mmol) and formaldehyde solution, 37 wt.percent in H2O (0.2 mL, 2.73 mmol) were mixed in glacial acetic acid(5 mL). N-methyl piperazine (273.8 mg, 2.73 mmol, CAS 109-01-3)was added drop wise at 0°C. The resulting mixture was stirred atroom temperature for 12 h. After completion of the reaction, the excess solvent was evaporated to dryness under reduced pressure.The residue was neutralized with 10percent NaHCO3 solution, the solidf ormed was collected by filtration, washed with water and dried.The crude product was purified by silica gel column chromatographyto provide title compound as an off-white solid (326.3 mg,88percent)., 4318-42-7

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Jose, Gilish; Suresha Kumara, Tholappanavara H.; Sowmya, Haliwana B.V.; Sriram, Dharmarajan; Guru Row, Tayur N.; Hosamani, Amar A.; More, Sunil S.; Janardhan, Bhavya; Harish; Telkar, Sandeep; Ravikumar, Yalegara Siddappa; European Journal of Medicinal Chemistry; vol. 131; (2017); p. 275 – 288;,
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.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

Reference Example 46] 1-Methylpiperazin-2-one [Show Image] An aqueous 1 N sodium hydroxide solution was added to a suspension of 1-methylpiperazin-2-one hydrochloride (19.6 g) of Reference Example 21-(3) in dichloromethane, and the resultant mixture was partitioned. Further, sodium chloride was added to the aqueous layer to saturate the layer, and then the aqueous layer was extracted with dichloromethane. The organic layers were combined and dried over anhydrous sodium sulfate. After separation by filtration, the solvent was evaporated under reduced pressure, and the title compound (5.90 g) was obtained as an oily product. ESI-MSm/z: 115(M+H)+.

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; DAIICHI PHARMACEUTICAL CO., LTD.; EP1785418; (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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Under an argon atmosphere, 3,4-difluoronitrobenzene(1.0 g, 6.29 mmol) in acetonitrile (15 mL)To the solution was added cis-3,5-dimethylpiperazine (861 mg, 7.55 mmol), N, N-diisopropylethylamine (2.19 mL,12.6 mmol), and the mixture was stirred at 80 ° C. for 2 hours.Water was added to the reaction solution, and the mixture was extracted with chloroform.The chloroform layer was washed with saturated brine and saturated brine,After drying over anhydrous magnesium sulfate, filtration,The solvent was distilled off. The resulting residue was purified by silica gel column chromatography (NH column, chloroform / methanol) to give the title compound (1.42 g, 89percent)., 21655-48-1

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

Reference：
Patent; Yakult Honsha Corporation; Abe, Atsuhiro; Mae, Satoyuki; Yamazaki, Ryuta; Sawaguchi, Yuichi; Sugimoto, Takuya; Sasai, Toshio; Nishiyama, Hiroyuki; Nagaoka, Masato; Matsuzaki, Ken; Kurita, Akinobu; Matsui, Makoto; Shingeyama, Takahide; (208 pag.)JP6378918; (2018); B2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics