Month: August 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.196811-66-2,tert-Butyl 4-carbamothioylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of tert-butyl 4-carbamothioylpiperazine-1-carboxylate (0.5 g, 2.08 mmol) in dioxane (10 mL), triethyl amine (0.22 mL, 2.6 mmol) and 2-bromo-1-phenylethan-1-one (0.52 g, 2.6 mmol) were added at rt. The resulting mixture was stirred at 90 C for 20 h. The completion of the reaction was monitored by TLC. It was diluted with water and extracted with EtOAc. The organic layer was separated, dried over anhydrous Na2SO4, concentrated under vacuum. The resulting crude product was taken as such for the next step. Yield: 86% (0.5 g, colorless liquid)., 196811-66-2

The synthetic route of 196811-66-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASCENEURON SA; QUATTROPANI, Anna; KULKARNI, Santosh S.; GIRI, Awadut Gajendra; (243 pag.)WO2016/30443; (2016); 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

Example 98 1-(4-methoxyphenyl)-3-(methylsulfonyl)-6-[4-(2-oxo-1-piperazinyl)phenyl]-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one To 6-(4-iodophenyl)-1-(4-methoxyphenyl)-3-(methylsulfonyl)-1,4,5,6-tetrahydro-7H-pyrazolo(3,4-c)pyridin-7-one (0.55 g, 1.0 mmol), 4-benzyloxycarbonylpiperazin-2-one (0.35 g,1.4 mmol),and K2CO3 (0.23 g,1.6 mmol) was added DMSO (5 mL). The mixture was degassed with N2. CuI (39 mg, 0.21 mmol) was added and the reaction was heated to 130 C. for 18 h. The reaction was diluted with EtOAc and water, extracted with EtOAc, and dried (MgSO4). Purification of the intermediate by chromatography on silica gel using 5%MeOH/CH2Cl2 was followed by deprotection in refluxing TFA. Purification by HPLC and freeze-drying afforded 175 mg (27%) of a white solid; High Resolution Mass Spec (M+H)+for C24H26N6O5S 496.1650.

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

Reference：
Patent; Pinto, Donald J.P.; Quan, Mimi L.; Orwat, Michael J.; Li, Yun-Long; Han, Wei; Qiao, Jennifer X.; Lam, Patrick Y.S.; Koch, Stephanie L.; US2003/191115; (2003); 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

6-Fluoro-2-methyl-3-(oxiran-2-yl)benzonitrile (12.0 g, 67.7 mmol) and (5)-4-N-BOC-2-hydroxymethylpiperazine (22.0 g. 102 mmol) were suspended in ethanol (100 mL) then heated in a microwave apparatus for 30 minutes at 150 C. The reaction mixture was cooled and evaporated dryness. The residue was purified by MPLC chromatography through a 330g Redi-sep column eluting with 5%MeOH/95% EtOAc solvent system to yield the title compound. LC-MS : M+l= 394., 314741-40-7

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PIO, Barbara; PASTERNAK, Alexander; SHAHRIPOUR, Aurash; TANG, Haifeng; WALSH, Shawn; WO2013/90271; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

75336-86-6, (R)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

75336-86-6, 15g of compound 6,150 ml of dichloromethane was added to the reaction flask.Cool down to 0 C,Dissolve in 100 mL of dichloromethane16.5g of Boc-anhydride was added to the reaction flask and stirred for 1 hour.Point plate monitoring, after the reaction, filtering,The filtrate was spun dry, added with 100 mL of water, stirred, filtered, and the filtrate was added with saturated 10 g of potassium carbonate and stirred with methyl tert-butyl ether ether.Extract, dry over sodium sulfate, spin dry,Adding petroleum ether, stirring and crystallizing under cooling to obtain 25 g of compound 7;

75336-86-6 (R)-2-Methylpiperazine 7330434, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Tonghua Normal College; Geng Xiaoyu; Xue Mingxing; Zang Hao; Liu Xuekun; Sun Renshuang; Xue Changsong; Zhang Haifeng; (13 pag.)CN109438423; (2019); 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.485841-52-9,(S)-1,2-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of (R)-3-cyclohexyl-2, 3-dihydropyrrolo [1,2, 3-de] -1, 4-benzoxazine-6- carboxylic acid (120 mg, 0.421 mmol) and (S)-1, 2-dimethylpiperazine (62 mg, 0.547 mmol) in N,N-dimethylformamide (3.0 mi) was added 1- (3-dimethylaminopropyl)-3- ethylcarbodiimide (97 mg, 0.505 mmol) and 1-hydroxy benzotriazole (68 mg, 0.505 mmol). The mixture was stirred at room temperature for 18 h, then partitioned between dichloromethane and water. The aqueous layer was extracted with dichloromethane, and combined organic layers were washed with brine, dried over Na2SO4 and concentrated. The residue was purified by flash chromatography eluting with 0-20% (v/v) methanol in ethyl acetate to afford the title compound as the free base. Hydrochloride salt formation was achieved by the addition of hydrogen chloride (2 M solution in diethyl ether; 0.5 mi) to a solution of the free base in diethyl ether (2 ml) and ethanol (1 ml). The solvent was removed in vacuo and the precipitate was dried to afford title compound (1: 1 hydrochloride salt) as a solid (84 mg, 0.20 mmol). ‘H NMR (400MHz, CD30D) 81. 00-1. 35 (5H, m), 1.39 (3H, d, J 4. 8), 1.58 (1H, d, J 12.0), 1.60-1. 70 (1H, m), 1.70-1. 82 (3H, m), 1.82-1. 90 (1H, m), 2.96 (3H, s), 3.20- 3.70 (5H, m), 4.20-4. 30 (2H, m), 4.40-4. 70 (2H, m), 4.71 (1H, d, J 10.0), 6.67 (1H, d, J 8.2), 7.08 (1H, t, J8. 2), 7.21 (1H, d, J 8.2), 7.74 (1H, s); EsIMS : m/z = 382.1 [M+H] +, 268.1

485841-52-9, The synthetic route of 485841-52-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; AKZO NOBEL N.V.; WO2005/58327; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

934-98-5, 2-(4-Methylpiperazin-1-yl)ethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

ethyl (7R,20S)-18-chloro-1-(4-fluorophenyl)-10-[(4-methoxyphenyl)methoxy]-19-methyl-15-[2-(4-methylpiperazin-1-yl)ethyl]-7,8,15,16-tetrahydro-14H-17,20-etheno-13,9-(metheno)-6-oxa-2-thia-3,5,15-triazacyclooctadeca[1,2,3-cd]indene-7-carboxylate To a mixture of Example 65K (8.8 g) in a mixture of anhydrous dichloromethane (100 mL) and acetic acid (20 mL) was added 2-(4-methylpiperazin-1-yl)ethanamine (3.16 g). The mixture was stirred at room temperature for 1 hour before sodium triacetoxyborohydride (7.02 g) was added. The reaction mixture was stirred at room temperature overnight. The volatiles were removed by rotary evaporation, and the residue was dissolved in tetrahydrofuran (45 mL) and water (7.5 mL). The mixture was cooled to 0° C., and trifluoracetic acid (45 mL) was added. After the addition, the cooling bath was removed, and the mixture was stirred at room temperature for 4 hours. The mixture was diluted with ethyl acetate. The mixture was washed with a pre-cooled diluted sodium hydroxide mixture (contained about 60 mL of 50percent sodium hydroxide, pH 10) and brine. The organic phase was concentrated. The residual intermediate was dissolved in anhydrous dichloromethane (100 mL). Anhydrous magnesium sulfate (25 g) was added. The mixture was stirred at room temperature overnight before sodium triacetoxyborohydride (7.02 g) was added. The reaction mixture was stirred at room temperature for 4 hours. The mixture was filtered, and the filtrate was directly purified by silica gel chromatography (0-20percent methanol containing 3percent ammonium hydroxide in dichloromethane) to provide the title compound. MS (ESI) m/z 850 (M+H)+., 934-98-5

As the paragraph descriping shows that 934-98-5 is playing an increasingly important role.

Reference：
Patent; AbbVie Inc.; AbbVie Deutschland GmbH & Co. KG; Brady, Patrick B.; Braje, Wilfried; Dai, Yujia; Doherty, George A.; Gong, Jane; Jantos, Katja; Ji, Cheng; Judd, Andrew S.; Kunzer, Aaron R.; Lai, Chunqiu; Mastracchio, Anthony; Risi, Roberto M.; Song, Xiaohong; Souers, Andrew J.; Sullivan, Gerard M.; Tao, Zhi-Fu; Teske, Jesse A.; Wang, Xilu; Wendt, Michael D.; Yu, Yiyun; Zhu, Guidong; Penning, Thomas D.; (218 pag.)US2019/55264; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The compound (R) -4- tert-butoxycarbonyl-2-methyl-piperazine (0.5g, 2.5mmol) and triethylamine (1.1mL,7.5mmol) was dissolved in dry Tetrahydrofuran (10mL), and at room temperature, to this solution was addeddropwise trimethylsilyl isocyanate (1.0mL, 7.5mmol), stirred at room temperature Stirred 1.5h, and ice water (10mL), tetrahydrofuran spin, the aqueous phase with ethyl acetate (30mL × 3). The organic phase was dried overanhydrous Na 2 SO 4 Dried to remove the solvent, the concentrated solution separated by columnchromatography (eluent: DCM / MeOH (v / v) = 40/1), to give a white solid 500mg: (R) -4–carbamoyl-3-methyl-piperazine-1-carboxylate, yield: 82%., 163765-44-4

As the paragraph descriping shows that 163765-44-4 is playing an increasingly important role.

Reference：
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

115761-79-0, 1-(2,4-Difluorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 2- (5-amino-2- (furan-2-yl) -7H-pyrazolo [4, 3-e] [1, 2, 4] triazolo [1, 5-c] pyrimidin-7-yl) -2-phenylpropanoic acid (50 mg, 0.13 mmol) , 1- (2, 4-difluorophenyl) piperazine (25 mg, 0.13 mmol) , HATU (59 mg, 0.16 mmol) and DIEA (33 mg, 0.26 mmol) in DMF (5 mL) was stirred at rt for 2 hrs. The solution was added with water (10 mL) , extracted with ethyl acetate (10 mL) and washed with brine (10 mL) . The organic layer was dried, concentrated and purified by column chromatography (PE: EA = 2: 1) and preparative TLC (DCM: MeOH = 20: 1) to get the desired product (20 mg, 28%) .1H NMR (400 MHz, DMSO-d6) delta 8.31 (s, 1H) , 8.08 (br. s, 2H) , 7.95 (d, J = 4.0Hz, 1H) , 7.30-7.11 (m, 7H) , 6.92-6.86 (m, 2H) , 6.74 (d, J = 4.0Hz, 1H) , 3.71 (br. s, 2H) , 3.45-3.40 (m, 2H) , 3.16-2.90 (m, 4H) , 2.35 (s, 3H) ppm. MS: M/e 570 (M+1)+

115761-79-0, The synthetic route of 115761-79-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; BEIGENE, LTD.; ZHANG, Guoliang; SUN, Hanzi; ZHOU, Changyou; (253 pag.)WO2020/20097; (2020); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8,5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(a) 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine. 11-Piperazinyldibenzo[b,f][1,4]thiazepine (0.1 mole), sodium carbonate (0.18 mole), sodium iodide (0.016 mole) and 2-chloroethoxyethanol (0.108 mole) were combined together in toluene (250 ml) and N-methylpyrrolidone (55 ml). The reaction was heated at reflux over 24 hours. The reaction was cooled and washed with water (1 x 175 ml., 2 x 60 ml.). The organic phase was dried by azeotropic distillation. A solution of fumaric acid (0.06 mole) in ethanol (110 ml) was added to the toluene solution at 60-70C. On cooling the hemifumarate salt crystallized out and was isolated by filtration in 75% yield, m.pt 172-173C.

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; IMPERIAL CHEMICAL INDUSTRIES PLC; EP282236; (1988); 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.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of the product from the previous step (1.0 g, 4.7 mmol) in CH2Cl2 (20 mL) at 0 C were added TEA (2.0 ml, 14 mmol) and methanesulfonyl chloride (0.641 g, 5.60 mmol) and the resulting mixture was stirred RT for 3 h. The mixture was concentrated under reduced pressure. The residue was purified via silica gel chromatography (5 – 100 % EtOAc in hexanes) to afford a colorless liquid. The residue was taken up in CH2CI2 (20 mL), 4 N HCl in dioxane (3.5 mL, 14 mmol) was added and the mixture was stirred at RT for 14 h. A white ppt was collected by vacuum filtration to afford the title compound (716 mg, 80 % yield).

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

Reference：
Patent; BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM; CHEMPARTNER CORPORATION; DI FRANCESCO, Maria, Emilia; JONES, Philip; CARROLL, Christopher, Lawrence; CROSS, Jason, Bryant; JOHNSON, Michael, Garrett; LIVELY, Sarah; (187 pag.)WO2018/218197; (2018); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics