Month: July 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

To a solution of CBz-piperazine (0.84 ml_, 4.36 mmol) in CH2CI2 (22 ml_) was added EDC (0.918 g, 4.79 mmol), HOBt (0.645 g, 4.77 mmol), Boc-D-Pip- OH (1.03 g, 4.50 mmol), and triethylamine (0.74 mL, 5.31 mmol) and the reaction stirred at room temperature for 5 days. The reaction was diluted with CH2CI2 and washed with sat. NaHCO3, 1 N HCI, sat. NaHCO3, and brine. The organic layer was dried over Na2SO4, filtered, and concentrated to produce 1.87 g (-99percent) of crude title compound: LCMS (m/z): 432.2 (M + H)., 31166-44-6

The synthetic route of 31166-44-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SMITHKLINE BEECHAM CORPORATION; WO2007/70865; (2007); A2;,
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.182618-86-6,1-Boc-4-(4-Nitrophenyl)piperazine,as a common compound, the synthetic route is as follows.

Pd on C 10% (0.3 % p/p) was added to a solution of terf-butyl 4-(4-nitrophenyl)piperazine-l-carboxylate (1 eq) in a mixture (1 : 1 ratio) MeOH : EtOAc (0.03 M). The atmosphere in the reaction vessel was charged with H2 (1 arm.) and the reaction stirred vigorously for 2 h. At this time, the reaction mixture was filtered through a pad of celite and concentrated in vacuo to afford the title compound (quant); MS (ES+) m/z 278 (M+H)+

182618-86-6, 182618-86-6 1-Boc-4-(4-Nitrophenyl)piperazine 3380696, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Istituto Di Ricerche Di Biologia Molecolare P. Angeletti SpA; WO2006/38039; (2006); 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.106261-48-7,4-((4-Methylpiperazin-1-yl)methyl)benzoic acid,as a common compound, the synthetic route is as follows.

A mixture of compound 5 (20 mg, 0.05 mmol), 4- (N-methyl-piperazyl)- methyl-benzoic acid (14 mg, 0.06 mmol), 0- (7-azabenzotriazol-1-yl)-N, N, N’, N’- tetramethyl-uronium hexafluorophosphate (23 mg, 0.06 mmol) and diisopropylethylamine (8 mg, 0.06 mmol) in methylene chloride (2 mL) is stirred at room temperature over night. LCMS purification afforded N-(3-{2-[6-(3-dimethylamino-phenylamino)-pyrimidin-4-yl]- phenylamino}-phenyl)-4-(4-methyl-piperazin-1-ylmethyl)-benzamide (9.2 mg, 30 % yield): ‘H NMR 400 Hz (CDCl3) b 2.51 (s, 3H), 2. 61 (br, 4H), 2.78 (br, 4H), 2.97 (s, 6H), 3.58 (s, 2H), 6.57 (m, 1H), 6.68 (m, 2H), 6.84 (m, 1H), 6.97 (m, 1H), 7.10 (m, 2H), 7.18 (m, 1H), 7.26 (m, 2H), 7.40 (d, J = 8.12 Hz, 2H), 7.46 (d, J = 8.12 Hz, 2H), 7.54 (s, br, 1H), 7.79 (d, J = 8. 14 Hz, 2H), 7.86 (s, 1H), 8.69 (s, 1H); MS m/z (M+H) 613.30., 106261-48-7

Big data shows that 106261-48-7 is playing an increasingly important role.

Reference：
Patent; IRM LLC; WO2005/33086; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Synthesis of e-Ffuoro–methyl-T-l^ l-Cl-methyl-S-nitro-iniidazol- l-y)-ethyl]-piperazm-l -yl}-4-oxo-4H-2-th5a-8b-aza-cyclobiita[a]naphihafene- 3-carboxyfic acid (119): To a stirred solution of 6-Fluoro- l -methyl-4-oxo-7- piperazin- 1 -yl-4H-2-ihia-8 -aza-cyclobuta[a]naphihaiene-3-earboxyiic acid, (II) (5. 1 6g. 14,76 mmol ) in dimethylforrnarnide ( 1 00ml) was added potassium carbonate (2.03g, 14.76 mmol) followed by addition of compound (I) (2g, 7.2 mmol) and the reaction mixture was heated at 90 C for 16h. The reaction mixture was di luted 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 eluting with 4-5% methanol/dichlorornethane mixture to obtain the pure compound ( 1 19) with 20% isolated yield. FontWeight=”Bold” FontSize=”10″ H-NMR (400 MHz, CDCI3) 5ppm: 2.12 (3H, d, J = 6.4 Hz, CH3), 2.52 (3H, s, CH3), 2.64 (4H, m, 2 xCH2), 2.72(2H, t, J = 6 Hz, CH2), 3.1 1 -3. 18 (4H, m, 2 x CH2), 4.43-4.49 (2H, m, CH2N). 5.8-5.9 ( 1 H, q, J,= 6.4Hz, J2 = 1 2.8Hz, CHSN), 6.3 (3 H, d, J = 6.8Hz, Ar- H), 7.92 (1 H, s, Ar-H), 7.95 ( 1 H, s, Ar-H). ESf-MS (m/z): 503 (M+H)

112984-60-8, The synthetic route of 112984-60-8 has been constantly updated, and we look forward to future research findings.

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.128102-16-9,(R)-4-Benzyl 1-Boc-2-methylpiperazine-4-carboxylate,as a common compound, the synthetic route is as follows.

A solution of 4-benzyl 1-tert-butyl 2-methylpiperazine-1,4-dicarboxylate (4.8 g, 14.4 mmol) in methanol (25 mL) was added 480 mg of 10% Pd/C and stirred at room temperature under hydrogen overnight. Filtered and concentrated to give the title product (2.8 g, yield 97%) as colorless oil. 1H-NMR (400 MHz, CDCl3) delta (ppm): 1.21 (d, J=6.8 Hz, 3H), 1.46 (s, 9H), 2.64-2.70 (m, 1H), 2.74-2.78 (m, 1H), 2.88-3.01 (m, 3H), 3.78 (d, J=12.4 Hz, 1H), 4.16 (m, 1H); LC-MS (ESI) m/z: 201 (M+1)+, 128102-16-9

The synthetic route of 128102-16-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; LEAD THERAPEUTICS, INC.; US2010/35883; (2010); 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.13889-98-0,1-Acetylpiperazine,as a common compound, the synthetic route is as follows.

In a three neck flask, under inert atmosphere (N2), is added 7.19g (27.2mmol) ofD in 150ml of DCM. The mixture is cooled to 0C. Then 5.75g (30mmol) of EDCI, 4.05g (30mmol) of HOBt and 3.85g (30mmol) of acetylpiperazine are added in this order. The temperature of 0C is maintained for 1 hour and the mixture is allowed to warm to 20C over 18 hours. Then 50ml of water are added and a solution of HCl 1M is added to obtain an acidic aqueous phase. The solution is extracted with DCM. The crude product is purified by column chromatography (Eluant: 90/10 DCM/MeOH) to give 9.04g (yield=89%) of the title compound, Example 115, as a white solid. NMR 1H (DMSO d6) : delta 2.04 (s, 3H), 3.62-3.40 (m, 8H), 4.10-3.85 (m, 2H), 4.12 (d, 1H), 4.30 (d, 1H), 6.62 (t, 1HAr), 6.95 (d, 1HAr), 7.26 (d, 1HAr), 7.48 (t, 1HAr), 7.70 (m, 2HAr), 7.77 (s, 1HAr)., 13889-98-0

As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference：
Patent; CEPHALON, INC.; CEPHALON FRANCE; EP1586559; (2005); 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.

Example 10 2-(2-(4-dibenzo[b,f][1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol OR 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine A 1 liter round bottom flask equipped with stirring rod, thermo pocket, water condenser was charged with solution of 11-piperazinyldibenzo[b,f][1,4]thiazepine in toluene 350 cc [63.0 g (0.22 moles)] and the mixture was stirred for 15 min 25-30 C., and, to which, was added sodium carbonate [41.0 gm (0.39 moles)], tetra butyl ammonium bromide [16.0 gm (0.05 moles)] and 2-(2-chloroethoxy)ethanol [32.0 gm (0.257 moles)] at room temperature. The reaction mixture was heated to reflux at 110-112 C. The reaction mixture was maintained at reflux for 10-12 hrs. The reaction mixture was analyzed by HPLC (to check absence of compound of formula IV) and was cooled to 25 C. to 30 C. To which, was added 150 cc DM water. Then the reaction mixture was stirred for 30 min at 25-30 C. The layers were separated and the aqueous layer extracted with 50 cc toluene. The extracts and the organic layer were combined, and the pH was adjusted to 2-3 using 1N HCl solution in DM (demineralized) water, the reaction mixture was then stirred for 30 min at 25-30 C. The layers were separated and the aqueous layer washed with 100 cc toluene twice. To the aqueous layer was added 250 cc toluene, and the pH was adjusted to 8-10 using sodium carbonate, the reaction mixture was stirred for 30 min at 25-30 C. The layers were separated and the aqueous layer extracted with 125 cc toluene. The extracts and the organic layer were combined, and washed with DM (demineralized) water 300 cc twice. The organic layer was distilled-off under vacuum below 70 C. to afford 2-(2-(4-dibenzo[b,f]-[1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol Purity of 2-(2-(4-dibenzo[b,f]-[1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol was 99.0 (area % by HPLC).

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

Reference：
Patent; Kansal, Vinod Kumar; Ahmad, Suhail; Lal, Kanhaiya; Patil, Bhatu Tumba; US2008/241949; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 43A tert-butyl (2S)-4-[(6-{[5-(difluoromethyl)pyridin-2-yl]oxy}quinolin-2-yl)carbonyl]-2-methylpiperazine-1-carboxylate The product from Example 14A (200 mg, 0.632 mmol) was subjected to the conditions described in Example 14B, substituting (S)-tert-butyl 2-methylpiperazine-1-carboxylate for tert-butyl piperazine-1-carboxylate to give 155 mg (49%) of the titled compound., 120737-78-2

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; AbbVie Inc.; Bogdan, Andrew; Cowart, Marlon D.; DeGoey, David A.; Jinkerson, Tammie K.; Koenig, John R.; Kort, Michael E.; Liu, Bo; Matulenko, Mark A.; Nelson, Derek W.; Patel, Meena V.; Peltier, Hillary; Scanio, Marc J.; Wakefield, Brian D.; US2015/218102; (2015); 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.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.

C the steps of the compound (50 mg, 0.16 mmol), 4 – ((4-methyl-piperazinyl) methyl) aniline (0.176 mmol), 1 – (3-dimethylamino-propyl) – 3-ethyl carbodiimide hydrochloride (0.24 mmol), 1-hydroxybenzotriazole and triazazole (0.24 mmol) and triethylamine (50 microliters) dissolved in dry N, N-dimethyl formamide in (3 ml), stir at room temperature overnight. Water 20 ml, ethyl acetate (10 ml, 5 times) extraction, extraction fluid after full and salt water washing, drying by anhydrous sodium sulfate, column chromatography (dichloromethane/methanol =1/10) separated to obtain title compound 20 mg per litre. MS:m/z, 499.2(M+H)., 70261-82-4

As the paragraph descriping shows that 70261-82-4 is playing an increasingly important role.

Reference：
Patent; CHIA TAI TIANQING PHARMACEUTICALGROUP CO LTD; Beijing Centaurus Biopharma Technology?Co.,?Ltd.; XIAO, DENGMING; LIANG, ZHI; HU, YUANDONG; HU, QUAN; ZHANG, QINGHUI; HAN, YONGXIN; WANG, HUAN; PENG, YONG; KONG, FANSHENG; LUO, HONG; (60 pag.)CN103130792; (2016); B;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5308-25-8,5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A solution of compound 2 (0.55 mmol), 1-substituted piperazine (0.83 mmol) and pyridine (0.8 mmol) in 10 mL THF (tetrahydrofuran) was stirred at room temperature overnight. When the reaction was completed, the solvent was evaporated under reduced pressure. The residues were dissolved in ethyl acetate and washed with water and saturated sodium chloride solution. After drying over anhydrous Na2SO4, the solvent was removed under reduced pressure to get crude product. The pure products were obtained by recrystallizing from ethanol.

The synthetic route of 5308-25-8 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Wu, Zhilin; Ding, Na; Tang, Yuting; Ye, Jiao; Peng, Junmei; Hu, Aixi; Research on Chemical Intermediates; vol. 43; 8; (2017); p. 4833 – 4850;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics