Month: June 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.304897-49-2,tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

In a round bottomed flask under nitrogen atmosphere commercially available benzoic acid (1.1 mmol) or sulphonyl chloride was suspended in 75 ml of anhydrous DCM. Then HOBt (1.4 mmol) and EDO HCI (1.1 mmol) were added and the resulting mixture stirred at room temperature for 2 hours. Then a solution of intermediates (X) (compounds of examples 4-6 of Table 2) (1.1 mmol) in 75 ml of dry DCM was addedand the mixture stirred at 40 00 upon completion. The reaction mixture was left to cool to room temperature, washed with a saturated aqueous solution of NH4CI, then aqueous HCI 0.5M, aqueous NaOH 1 M and finally with a saturated aqueous solution of NaHCO3. The organic layer was separated, dried over sodium sulphate, filtered and evaporated under vacuum. The resulting crude product was purified by flashchromatography on silica gel, eluting with a gradient from cyclohexane/AcOEt 1/1 to100% AcOEt. The collected fractions were evaporated to give the compounds of examples 7-10,14., 304897-49-2

As the paragraph descriping shows that 304897-49-2 is playing an increasingly important role.

Reference：
Patent; ROTTAPHARM BIOTECH S.R.L.; ARTUSI, Roberto; CASELLI, Gianfranco; ROVATI, Lucio; (78 pag.)WO2016/146220; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

59878-57-8, (d) Library Synthesis (5a-h)To a solution of 3-(4-oxo-3,4,5,6,7,8-hexahydro-phthalazin-1-ylmethyl)-benzoic acid (4) (20 mg, 0.07 mmol), in DCM (1 ml) was added HBTU (53 mg, 0.140 mmol), triethylamine (20 muL, 0.140 mol) and amine (0.140 mmol). The reaction mixture was stirred for 18 hours at room temperature and concentrated in vacuo. The crude samples were submitted for preparative HPLC purification.

As the paragraph descriping shows that 59878-57-8 is playing an increasingly important role.

Reference：
Patent; Javaid, Muhammad Hashim; Menear, Keith Allan; Martin, Niall Morrison Barr; Smith, Graeme Cameron Murray; Rudge, David Alan; Roberts, Craig Anthony; US2009/23727; (2009); 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

To a solution of Int-12 (100 mg, 0.312 mmol) and 2-methoxy-4-(4-methylpiperazin-l-yl)aniline (75 mg, 0.343 mmol) in 2-methoxyethanol (2 mL) was added 4 M HC1 in dioxane (0.086 mL, 0.343 mmol). The solution was stirred and heated at 110 C for 14 h. Then, additional 2-methoxy-4-(4-methylpiperazin-l-yl)aniline (18 mg, 0.081 mmol) and 1 drop of 4 M HC1 (aq) were added and the mixture was further irradiated under microwave conditions for 15 minutes at 160 C. The solution was concentrated under reduced pressure and partitioned between saturated NaHCC and DCM (20 mL each). The aqueous layer was re-extracted with DCM (20 mL). The organic layers were combined, dried (Na2S04), filtered, and concentrated under reduced pressure. The resulting crude mixture was purified by flash chromatography (Si02) eluting with DCM in MeOH (0% to 10%) to provide the title compound as a brown foam (75 mg, 48%). HPLC: 98% [tR = 8.7 min, 45% MeOH, 55% water (with 0.1% TFA), 20 min. lH NMR (400 MHz, DMSO-ifc): delta 7.87 (d, / = 8.8 Hz, 1H), 7.84 (s, 1H), 7.33-7.22 (m, 4H; 1H disappeared on D20 shake), 7.19-7.11 (m, 1H), 6.60 (d, J = 2.5 Hz, 1H), 6.42 (dd, / = 8.8, 2.5 Hz, 1H), 3.81 (s, 3H), 3.58 (q, / = 6.6 Hz, 2H), 3.10-3.05 (m, 4H), 3.03 (t, J = 6.6 Hz, 2H), 2.46-2.42 (m, 4H), 2.21 (s, 3H). HPLC-MS (ESI+): m/z 507.2 [45%, (M35C137C1+H)+], 505.2 [50%, (M35C135C1+H)+], 254.2 [60%, (M35C137C1+2H)2+], 253.2 [100%, (M35C135C1+2H)2+]. LC-MS (ESI+): 505.2 [100%, (M35C135C1+H)]. HRMS (ESI+): m/z calcd for C24H27C12FN60S (M+H)+ 505.1680, found 505.1683.

122833-04-9, The synthetic route of 122833-04-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; H. LEE MOFFITT CANCER CENTER & RESEARCH INSTITUTE; MAHAJAN, Nupam P.; MAHAJAN, Kiran N.; LAWRENCE, Nicholas J.; LAWRENCE, Hirshani R.; (85 pag.)WO2017/23899; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

694499-26-8, General procedure: To a solution of 8a-e (20 mmol) and triethylamine (40 mmol) indichloromethane (20 ml), a solution of 4a-f (1.5 eq) in dichloromethane(10 ml) was added dropwise at room temperature over20 min and stirred overnight. The mixture was washed with saturatedaqueous sodium bicarbonate and brine. After removing thesolvent under reduced pressure, the crude product was purifiedby flash chromatography on silica gel, eluting with dichloromethaneand methanol (10-30%), yielding the title compounds.

As the paragraph descriping shows that 694499-26-8 is playing an increasingly important role.

Reference：
Article; Yao, Dahong; Wang, Jing; Wang, Guan; Jiang, Yingnan; Shang, Lei; Zhao, Yuqian; Huang, Jian; Yang, Shilin; Wang, Jinhui; Yu, Yamei; Bioorganic Chemistry; vol. 68; (2016); p. 112 – 123;,
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.,4318-42-7

Oxalyl chloride (47.7 kg, 375.8 mol) was added to a solution of oxazole-5-carboxylic acid (32.88 kg, 290.8 mol) in isopropyl acetate (144 kg) maintaining the temperature at 52-58 °C. The temperature was increased to 58.5 °C, stirred for 5 h and then cooled to 20 °C. The reaction mixture was added to a solution of l-(isopropyl)piperazine (41 kg, 319.8 mol) and potassium carbonate (118.4kg) in isopropyl acetate (348 kg) and water (103 kg) maintaining the temperature below 25 °C. The reaction was stirred for 15 mins, the temperature was increased to 33 °C and the organic phase washed with water (191 kg), concentrated under reduced pressure to 95 L and cooled to 20 °C. n- Heptane (157 kg) was added and the crystallisation stirred for 2 h, and the product filtered off, washed with n-heptane (157 kg) and dried under vacuum 40 °C to give the title compound (57.14 kg, 88.0percent). (0441) *H NMR (400 MHz, CDC -d) delta ppm 7.94 (s, 1 H), 7.56 (s, 1 H), 3.91-3.73 (m, 4 H), 2.75 (spt., J=6.5 Hz, 1 H), 2.63-2.52 (m, 4 H) and 1.06 (d, J=6.6 Hz, 6 H).

4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; CAMPOS, Sebastien Andre; PATEL, Vipulkumar Kantibhai; DALTON, Samuel Edward; (74 pag.)WO2018/29126; (2018); 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.,21655-48-1

Preparation 5 tert-Butyl (cis)-3,5-dimethyl-1-piperazinecarboxylate STR50 (cis)-3,5-Dimethylpiperazine (5.01 g) was dissolved in dioxan (9 ml) and water (4 ml), di-tert butyldicarbonate (9.59 g) was added and the reaction mixture was stirred at room temperature for 18 hours. The solvent was then removed under reduced pressure and the remaining aqueous solution was basified to pH 9.0 with 2N aqueous sodium hydroxide solution. The product was then extracted twice with ethyl acetate, the combined organic layers were dried over magnesium sulphate and the solvent removed under reduced pressure. The crude product was purified by column chromatography on silica gel eluding with a solvent system of 93:7:1, by volume, dichloromethane:methanol:0.88 aqueous ammonia solution to afford tert-butyl (cis)-3,5-dimethyl-1-piperazinecarboxylate (6.40 g) as a yellow liquid. 1 H-NMR (CDCl3)delta:3.90 (2H, bs), 2.80 (2H, m), 2.30 (2H, m), 1.45 (9H, s), 1.40 (1 H, bs), 1.05 (6H, d). MS:215 (MH+).

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

Reference：
Patent; Pfizer Inc; US6166011; (2000); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5308-25-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5308-25-8,1-Ethylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of compound 88 (2 g, 9.8 mmol, 1 eq) in DMSO (10 mL) was added K2CO3 (2.7 g, 19.7 mmol, 2 eq), 1-ethylpiperazine (compound 89, 1.7 g, 14.7 mmol, 1.5 eq) and TBAI (36 mg, 0.098 mmol, 0.01 eq). The reaction mixture was stirred at 120 C for 2 h. After cooling down to rt, the mixture was diluted with water (30 mL), thus formed solid was filtered, rinsed with water (5 mL x 3), and dried to afford the desired product (1.5 g, 65%) as a yellow solid which was used to the next step directly. NMR (300 MHz, CDC ): delta 8.19- 8.14 (m, 2 H), 7.23-7.19 (m, 1 H), 3.53-3.45 (m, 4 H), 2.79-2.65 (m, 4 H), 2.57-2.50 (m, 2 H), 1.19 (t, J= 7.2 Hz, 3 H).

5308-25-8 1-Ethylpiperazine 79196, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BEIJING XUANYI PHARMASCIENCES CO., LTD.; SONG, Yuntao; CHEN, Xiaoqi; (188 pag.)WO2019/35008; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,694499-26-8

3,5-Diiodo-4-methylbenzoic acid (194.0 mg, 0.5 mmol)To the mixture is added SOCl2 (0.73 mL, 10 mmol), and a catalytic amount of DMF is added dropwise,Stir at room temperature for 20 hours. The solution is dried under vacuumIntermediate (3,5-Diiodo-4-methyl-benzoyl chloride)(178.9 mg, 0.44 mmol, 88%, white solid) were obtained.4-[(4-methyl-1-piperidinyl) methyl] -3- (trifluoromethyl) -benzenamine (94.6 mg, 0.35 mmol), N, N-diisopropylethylamine(73 muL, 0.42 mmol), DMAP (1.2 mg, 0.01 mmol) in THF (2.4 mL)Dissolved in water, to which the intermediate (170.7 mg, 0.42 mmol) is added,Stir at room temperature for 2 hours. Add water and extract with ethyl acetate,It concentrated under reduced pressure with an evaporator.The resulting residue is purified by silica gel column chromatography (chloroform: methanol = 10: 1) to give compound 1(180.0 mg, 0.28 mmol, 80%, pale yellow solid) were obtained.

694499-26-8 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 46838908, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Kyoto University; Arkray Corporation; Saji, Hideo; Kimura, Hiroyuki; Matsuda, Hirokazu; Nakanishi, Shuichi; (27 pag.)JP2019/64986; (2019); A;,
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

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

129779-30-2, (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of /er/-butyl (3/^,5.V)-3,5-dimethylpiperazine- 1 -carboxylate (compound Id, CAS: 129779-30-2, PharmaBlock, Catalog: PB125871, 100 mg, 467 pmol) and K2C03 (129 mg, 933 pmol) in MeCN (5 mL) was added l-bromo-4-(bromo methyl) benzene (compound le, CAS: 589-15-1, Accela ChemBio, Catalog: SY001367, 117 mg, 467 pmol). The resultant mixture was heated to 80 C for 14 hrs, then cooled to room temperature. The reaction mixture was filtered and the filter cake was washed with EA (10 mL). The combined filtrate was concentrated in vacuo and purified by flash chromatography (silica gel, 12 g, 10% to 50% EtOAc in PE). The purified intermediate was dissolved in DCM (2 mL) and TFA (0.5 mL) was added. The reaction mixture was stirred at room temperature for 3 hrs, then concentrated to afford a crude compound If, MS: calc?d 283 and 285 [(M+H)+], measured 283 and 285 [(M+H)+], 129779-30-2

The synthetic route of 129779-30-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; DEY, Fabian; QIU, Zongxing; ZHU, Wei; ZOU, Ge; (55 pag.)WO2020/20800; (2020); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics