Month: June 2021

4318-42-7,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.

Synthesis of (IS, 2R) and (1R, 2S)-2-(4-chlorophenyl)-l’-(2-(4-isopropylpiperazin-l- yl)ethyl)spiro[cyclopropane-l,3′-indolin]-2′-one; A mixture of (1R, 2S) and (I S, 2R)-2-(2-(4-chlorophenyl)-2′-oxospiro[cyclopropane-l,3′- indoline]-l’-yl)acetaldehyde (0.1 mmol), (l-Isopropyl)piperazine (0.15 mmol) and acetic acid (catalytic amount) in DCM (2 ml) was stirred for 20 minutes at room temperature. The mixture was cooled to 0 °C and NaBH(OAc)3 (2 mmol) was added carefully. The mixture was warmed to room temperature and stirred for 14 hours at room temperature. The mixture was concentrated under reduced pressure and dissolved in DMF. Purification by preparative HPLC gave the title product as colorless oil (35 mg). LC/MS m/e calcd. for C25H3oClN30: 423, observed (M+H)+: 424.1 1HNMR(400 MHz, MeOD-d4) 5ppm 1.37 (d, J=6.57 Hz, 6 H) 2.18 (dd, J=8.46, 5.94 Hz, 2 H) 2.46 – 2.64 (m, 1H) 2.85 (d, J=3.54 Hz, 2 H) 3.22 (s, 2 H) 3.50 (d, J=6.57 Hz, 2 H) 3.90 – 4.27 (m, 2 H) 6.09 (d, J=7.58 Hz, 1H) 6.76 (s, 1 H) 7.10 (d, J=7.83 Hz, 1 H) 7.16 – 7.25 (m, 3 H) 7.33 (d, J=8.59 Hz, 2 H).

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; CHEN, Li; HUANG, Mengwei; FENG, Lichun; HE, Yun; YUN, Hongying; WO2011/69298; (2011); A1;,
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

P-toluene sulfonic acid (269 mg, 1.56 mmol) was added to 6-(2-chloro-5-fluoropyrimidin-4-yl)-8-fluoro-2-methyl-3-(prop-1-en-2-yl)imidazo[1,2-a]pyri dine (compound 17, 250 mg, 0.78 mmol) and 2-methoxy-4-(4-methylpiperazin-1-yl)aniline (compound 6, 172 mg, 0.78 mmol) in isopropyl alcohol (10 mL), and reacted under a microwave at 180 C. for 1.5 hours. The reaction mixture was concentrated under reduced pressure, the residue was adjusted to basic with saturated sodium bicarbonate, extracted with dichloromethane (30 mL×3), the organic phase was combined, washed with brine (30 mL) and dried over anhydrous sodium sulfate, the solvent was removed, and the filtrate was separated on column chromatography (eluant:dichloromethane/methanol (v/v)=13:1), to afford 50 mg of a pale yellow solid as a crude, which was purified with preparative TLC (DCM/MeOH v/v=12/1) to afford 32 mg of a pale yellow solid, yield was 8.8%. LC-MS(APCI): m/z=466.5 (M+1); 1H NMR (400 MHz, CDCl3) (delta/ppm) 8.77 (s, 1H), 8.32 (d, J=3.6 Hz, 1H), 8.18 (d, J=8.7 Hz, 1H), 7.75 (d, J=12.1 Hz, 1H), 7.52 (s, 1H), 7.50-7.45 (m, 1H), 6.63-6.58 (m, 1H), 6.58-6.55 (m, 1H), 3.90 (s, 3H), 3.24-3.17 (m, 4H), 2.66-2.59 (m, 4H), 2.50 (s, 3H), 2.37 (s, 3H)., 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; Shenzhen TargetRx, Inc.; Wang, Yihan; Ren, Xingye; Jin, Jian; Li, Huanyin; Ai, Yixin; (162 pag.)US2019/152954; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

16154-72-6, 3-Chloro-4-(4-methylpiperazin-1-yl)benzenamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of compound 10a (155mg, 0.4mmol) and 3-chloro-4-fluoroaniline (70mg, 0.48mmol) in isopropanol (6mL) was stirred for 24h. After cooled to room temperature, the mixture was filtered and washed with chill isopropanol (3mL) and the residue was treated with aqueous NaHCO3 (10mL) and extracted with EtOAc/MeOH (20:1, 20mL). The organic layer was washed with brine, dried over Na2SO4, and concentrated under reduced pressure. Purified by silica-gel column chromatography (DCM/MeOH, 100/1), Rf=0.23. Drying gave 163mg (yield, 82.3%) of the title compound as white solid;

16154-72-6, As the paragraph descriping shows that 16154-72-6 is playing an increasingly important role.

Reference：
Article; Yin, Siyuan; Tang, Chunming; Wang, Bin; Zhang, Ying; Zhou, Liliang; Xue, Lingjing; Zhang, Can; European Journal of Medicinal Chemistry; vol. 120; (2016); p. 26 – 36;,
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.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.,934-98-5

General procedure: To a solution of 6-amino-4-anilinoquinazoline or 4-(1-phenylethyl)quinazoline-4,6-diamine (0.23 mmol) in acetonitrile(5 mL), CDI (0.11 g, 0.69 mmol) was added. The reaction mixture was stirred at room temperature for 8 h when lots of solidproduced. To this suspension, the solution of 2-(4-methylpiperazin-1-yl)ethylamine in 5 mL of acetonitrile was added. Then, the mixture was stirred at room temperature for 2 h, refluxed for another 2 h, cooled to room temperature and concentrated under reduced pressure. The residue was added water (20 mL) and the mixture was extracted with dichloromethane (20 mL 3). The organic layer was combined, washed with brine (20 mL), dried(Na2SO4), concentrated under reduced pressure and purified bychromatography on silica gel (dichloromethane/methanol = 15:1,v/v) to give compounds 4a or 4b as yellow powder. 4.1.60. 1-(2-(4-Methylpiperazin-1-yl)ethyl)-3-(4-((3-(trifluoromethyl)phenyl)amino)quinazolin-6-yl)urea (4a)Yield 45.5percent. Mp: 169.8?170.5 C. 1H NMR (DMSO-d6): d 9.96 (s,1H, N-H), 9.03 (s, 1H, N-H), 8.54 (s, 1H, N-H), 8.46 (d, 1H, Ar-H,J = 2.0 Hz), 8.29 (s, 1H, Ar-H), 8.21 (d, 1H, Ar-H, J = 8.0 Hz), 7.83(dd, 1H, Ar-H, J1 = 2.0 Hz, J2 = 8.8 Hz), 7.74 (d, 1H, Ar-H,J = 8.8 Hz), 7.62 (t, 1H, Ar-H, J = 8.0 Hz), 7.44 (d, 1H, Ar-H,J = 7.6 Hz), 6.35 (t, 1H, Ar-H, J = 5.2 Hz), 3.20?3.29 (m, 4H,2 CH2), 2.41?2.49 (m, 8H, 4 N-CH2), 2.27 (s, 3H, N-CH3). 13CNMR (DMSO-d6): d 157.4, 155.6, 152.5, 145.9, 141.0, 139.2, 130.0,129.5, 128.8, 126.7, 124.7 (d, JC?F = 261 Hz), 126.0, 119.8, 118.4,116.2, 109.3, 57.6, 54.7 (2 CH2), 52.4 (2 CH2), 45.5, 36.9. ESIHRMSm/z: calcd for C23H27F3N7O [M+H]+: 474.2229; found:474.2224.

The synthetic route of 934-98-5 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Zuo, Sai-Jie; Zhang, Sai; Mao, Shuai; Xie, Xiao-Xiao; Xiao, Xue; Xin, Min-Hnag; Xuan, Wei; He, Yuan-Yuan; Cao, Yong-Xiao; Zhang, San-Qi; Bioorganic and Medicinal Chemistry; vol. 24; 2; (2016); p. 179 – 190;,
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.639068-43-2,tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

639068-43-2, General procedure: To a stirred solution of compound 13a-b, 17a-b (1.0 mmol) inCH3CN (20 mL) were added N-Boc-piperazine (180.9 mg,0.9 mmol), K2CO3 (205.9 mg, 1.5 mmol), KI (166.0 mg, 1.0 mmol)and 18-crown-6 (26.4 mg, 0.1 mmol) at room temperature. Themixture was stirred overnight at 80 C and filtered. The filtrate wasdiluted by DCM and washed by brine. The organic layer was concentrated for next step. To a stirred solution of the abovecompounds in DCM (20 mL) was added TFA (3 mL) at room temperature.The mixture was stirred for 3e4 h and concentrated toafford the crude products 15a-o and 19a-f in a yield of 35%e42%. Toa stirred solution of above crudes in anhydrous MeOH (10 mL) wasadded BTZ core compound 11 (403.2 mg, 1.0 mmol) and Et3N(0.2 mL, 1.5 mmolj) at room temperature. The mixture was stirredfor 1e3 h at 40 C and concentrated. The residue was purified bysilica gel column (DCM: MeOH 20: 1) to give 1a-f and 2a-e (25%e41% for two steps).

639068-43-2 tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 22219990, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Wang, Apeng; Lv, Kai; Tao, Zeyu; Gu, Jian; Fu, Lei; Liu, Mingliang; Wan, Baojie; Franzblau, Scott G.; Ma, Chao; Ma, Xican; Han, Bing; Wang, Aoyu; Xu, Shijie; Lu, Yu; European Journal of Medicinal Chemistry; vol. 181; (2019);,
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.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution of l-(2-hydroxyethyl)piperazine (51.7 g, 398 mmol) in DCM (500 mL) was added NEt3 (70.0 mL, 526 mmol) and dicarbonate (80.0 g, 367 mmol). The reaction mixture was stirred overnight at r.t. and then washed with IM aq Na2CO3 solution (2 x 300 mL). The organic phase was dried (MgSO4) and concentrated in vacuo to give tert-bvXy 4-(2-hydroxyethyl)piperazine-l-carboxylate (66.0 g, 72%) as a colourless oil.

103-76-4, As the paragraph descriping shows that 103-76-4 is playing an increasingly important role.

Reference：
Patent; BIOVITRUM AB (publ); WO2009/147221; (2009); 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.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

2-Methoxy-4-(4-methylpyridazin-1-yl)phenylamine (2.21 g, 1.0 eq) was added to compound l-1 (3.7 g, 1. Oeq) n-butanol (70 ml) In the solution, the reaction was carried out at 90 C for 2-3 hours. After the reaction was completed by TLC, the mixture was cooled to room temperature, filtered, washed and dried to give a red solid (4.6 g)., 122833-04-9

As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference：
Patent; Chengdu University; Zhao Lifeng; Gou Xiaojun; (47 pag.)CN109384788; (2019); A;,
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

934-98-5, The dichloropyrimidine (3.29 gm, 0.01 moles) was dissolved in n-butanol (30 mL) and N-methyl-N’-(2-aminoethyl)piperazine (3.0 gm, 2.1 X 10″2 moles) was added. This mixture was heated to 1 15°C. forming a dark orange solution. After 2 hours, TLC (silica, 25percent methanol in methylene chloride) showed some remaining starting material along with a single product. Diisopropylethylamine (02.58 gm, 0.02 moles) was added along with additional N-methyl-N’- (2-aminoethyl)piperazine (1.0 gm, 7.0 X 10″3 moles) and this solution was heated at 1 15°C. for an additional 2 hours. After cooling the reaction was diluted with hexane (100 mL) and this solution was extracted with water (50 mL). The hexane solution was dried over magnesium sulfate, filtered and the solvents were removed under reduced pressure. The remaining orange solid was boiled in hexane (50 mL) and then cooled on ice. The solid was isolated by filtration, washed with hexane and dried. Yield was 3.0 gm, (55percent).

The synthetic route of 934-98-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; JANUS BIOTHERAPEUTICS, INC.; LIPFORD, Grayson, B.; ZEPP, Charles, M.; WO2012/167053; (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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

In a 25 mL round bottom flask was added 100 mg (0.22 mmol) of Intermediate 4, 59.8 mg (0.26 mmol) of 1-(4-trifluoromethylphenyl)piperazine, 182 mg (1.32 mmol) of potassium carbonate, 15 mL of acetonitrile,The reaction was carried out at 86[deg.] C. for 16 h. TLC showed that the starting material was completely reacted. Stop the reaction, filter, and concentrate. The crude product was purified by column chromatography on silica gel, eluent: V (ethyl acetate): V (petroleum ether) = 1:3 to give 35.2 mg of a white solid. Yield: 33%.

30459-17-7, The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Yuan Mu; Chen Hong; Ye Bibo; Yang Zonglin; (17 pag.)CN107573302; (2018); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59702-31-7, 1-Ethylpiperazine-2,3-dione is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

500 ml of ethylene glycol dimethyl ether and 28.4 g of 4-ethyl-2,3-bisperoxazine were sequentially added to a 1 L three-necked flask, and the mixture was evenly stirred. 4.6 g of sodium metal was added and the mixture was heated to reflux for 10 hours.Cooled to 5 C,Stirring in batches by adding a good configuration of the triphosgene solution,The reaction temperature was controlled not to exceed 10 C,Adding filtrate to remove the activated carbon, filter to remove activated carbon, the filtrate vacuum drying, drying, in a white solid, that is, N, N, N-dimethylformamide, N, N-dimethylformamide, Carbonyl-bis- (4-ethyl-2,3-bisperoxypyrazine) was obtained The preparation method was the same as that of Example 1 except that the reaction temperature of sodium bisoxypiperazine and triphosgene was -15 C, and the obtained N, N’-carbonyl-bis- (4-ethyl- Piperazine)The yield of 4-ethyl-2,3-bisperoxypiperazine was 95%. The purity was 98.5% by HPLC., 59702-31-7

59702-31-7 1-Ethylpiperazine-2,3-dione 108812, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Shandong Ai Fu Special Technology Co., Ltd.; Gao, Aihong; Feng, Weichun; Zhang, Jianwen; Ji, Xiaohong; Liu, Lixiu; Liu, Maoling; Wang, Liqin; (6 pag.)CN105524001; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics