Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To compound 4 (183mg , 0.8 mmol) in DCM (3 ml), was added DIPEA ( 0.278 ml, 2 eq) and then propionyl chloride (130mg, 1 mmol) . The reaction was stirred at room temperature for lhr. The mixture was concentrated and partitioned between ethyl acetate and water, ethyl acetate layer was separated and dried, concentrated, then HC1 in dioxane ( 4N, 2 ml) was added. The mixture was stirred at room temperature for lhr, concentrated to afford crude 5a. It was then diluted with dry DMF ( 5 ml), was added, followed by addition of DIPEA (0.278ml, 1.6 mmol) and then (Biotin-LC-LC-NHS ( 454mg, O.Smmol). The mixture was stirred at room temperature for 12 hrs. The mixture was diluted with water, extracted with ethyl acetate. The organics were concentrated and then purified by HPLC to yield the desired product 6a ( 390 mg). NMR: pass, 192130-34-0

The synthetic route of 192130-34-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NESTEC S.A.; SELVARAJ, Fabiyola; PRINCEN, Fred; SINGH, Sharat; WO2014/188377; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 5-methyl-3-isoxazole-4-carbonyl chloride (1.19g, 5.37mmol) in dioxane (15ml, anhydrous) was added dropwise to a cooled mixture (0C) containing l-(4-trifluoro- methylphenyl)-piperazine (1.24g, 5.38mmol commercially available) and pyridine (0.81ml, O.Olmol) in dioxane (25ml, anhydrous). The reaction solution was allowed to attain ambient temperature. Water was added to the solution affording a precipitation that was isolated by filtration. Re-crystallization from a mixture of MeOH/Acetonitrile (2: 1) afforded white crystalline compound (1.74g, 75%). 1H-NMR (400 MHz, DMSO-d6) delta 7.61-7.60 (m, 2H), 7.49-51 (m, 5H), 7.01-6.99 (m, 2H), 3.75 (br, 2H), 3.32 (br, 4H), 2.94 (br, 2H), 2.48 (s, 3H). 13C-NMR (400 MHz, DMSO-d6) delta 169.6(s), 162.4(s), 160.5(s), 153.6(s), 131.0(d), 129.8(d, 2H), 129.1(s), 128.2(d, 2C), 127.0 (q, 4JCF = 3.7 Hz, CCF3, 2C), 125.8 (q, lJ CF = 270.1 Hz, CCF3), 119.6 (q, 2JCF = 32.0 Hz, CCF3),115.4(d, 2C), 112.0(s), 48.0 (t, 4CH2), 12.1(q).

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

Reference：
Patent; VIRONOVA AB; HOMMAN, Mohammed; KINGI, Ngarita; BERGMAN, Jan; ENGQVIST, Robert; WO2013/171334; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

170911-92-9, tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 184 3-(2,6-dichlorophenyl)-2-methyl-7-methylsulfanyl-2H-pyrimido[5,4-e][1,3]oxazin-4-one (100 mg, 0.290 mmol, 1.0 eq) in 24 toluene (10 mL) was added 25 m-CPBA (100 mg, 0.58 mmol, 2.0 eq) and allowed to stir at rt for 30 min. 66 Tert-butyl 4-(4-aminophenyl) piperazine-1-carboxylate (107 mg, 0.35 mmol, 1.10 eq) and 27 DIPEA (149 mg, 1.16 mmol, and 4.0 eq) were added and allowed to stir at rt for 1 h. Progress of reaction was monitored by LCMS. After completion of reaction, solvent was removed under reduced pressure. Crude residue was suspended in 20 mL of 7 water, extracted with ethyl acetate (50 mL×2). Combined organic layer was washed with water (20 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. Crude residue was purified by flash chromatography using 19 ethyl acetate: 20 hexane to obtain 185 tert-butyl 4-[4-[[3-(2,6-dichlorophenyl)-2-methyl-4-oxo-2H-pyrimido[5,4-e][1,3]oxazin-7-yl]amino]phenyl]piperazine-1-carboxylate (100 mg, 59.1%). (0326) LCMS: 585 [M+1]+

170911-92-9, The synthetic route of 170911-92-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; giraFpharma LLC; Chakravarty, Sarvajit; PHAM, Son Minh; Kankanala, Jayakanth; AGARWAL, Anil Kumar; PUJALA, Brahmam; SONI, Sanjeev; ARYA, Satish K.; PALVE, Deepak; KUMAR, Varun; (360 pag.)US2019/106436; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

53788-49-1, tert-Butyl 4-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

53788-49-1, Example 45 (4-Hexyl-piperazin-1-yl)-(1H-indol-2-yl)-methanone Indole-2-carboxylic acid (5.2 g) in THF (200 mL) was treated with carbonyldiimidazole (4.8 g) and stirred at ambient temperature for 10 min whereupon 4-methyl-piperazine-1-carboxylic acid tert-butyl ester (5.0 g) was added. The mixture was stirred at ambient temperature for 72 h and the solvent removed under reduced pressure. The residue was dissolved in ethyl acetate and washed with saturated sodium bicarbonate solution. The organic portion was separated, dried over sodium sulfate and filtered, and solvent was evaporated to afford a solid. Recrystallization from hot ethanol afforded 4-(1H-Indole-2-carbonyl)-piperazine-1-carboxylic acid tert-butyl ester (4.2 g).

53788-49-1 tert-Butyl 4-methylpiperazine-1-carboxylate 11401394, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Carruthers, Nicholas I.; Chai, Wenying; Dvorak, Curt A.; Edwards, James P.; Grice, Cheryl A.; Jablonowski, Jill A.; Karlsson, Lars; Khatuya, Haripada; Kreisberg, Jennifer D.; Kwok, Annette K.; Lovenberg, Timothy W.; Ly, Kiev S.; Pio, Barbara; Shah, Chandravadan R.; Sun, Siquan; Thurmond, Robin L.; Wei, Jianmei; Xiao, Wei; US2003/207893; (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.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

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.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

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

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.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of Intermediate H (190 mg, 0.67 mmol) in DMF (3 mL) were added tert-butyl 3,3-dimethylpiperazine-1-carboxylate (171.3 mg, 0.80 mmol), HATU (329.2 mg, 0.87 mmol) and DIPEA (232 tL, 1.3 mmol) and the mixture was stirred at rt ON. The reaction mixture was then diluted with EtOAc, washed with water and brine consecutively, dried over anhydrous sodium sulfate, filtered and concentrated to dryness. The residue was purified by flash chromatography eluting with EtOAc/hexanes 0-50% in 20 CV to obtain tertbutyl 4- [8-ethyl-6-(4-fluorophenyl)imidazo[ 1 ,2-b]pyridazine-2-carbonyl] -3,3 -dimethylpiperazine-1-carboxylate (235 mg) as a white solid. ?H NMR (400 MHz, CDC13) oe 8.32 (s, 1H), 8.04-7.86 (m, 2H), 7.26 (s, 1H), 7.22-7.11 (m, 2H), 4.39-3.92 (m, 2H), 3.73 -3.40 (m, 4H), 3.09 (m, 2H), 1.65 – 1.59 (m, 6H), 1.50 – 1.40 (m, 12H). LC-MS: 482.5 (M+H).

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

Reference：
Patent; VERTEX PHARMACEUTICALS INCORPORATED; FARMER, Luc J.; FOURNIER, Pierre-Andre; LESSARD, Stephanie; LIU, Bingcan; ST-ONGE, Miguel; STURINO, Claudio; SZYCHOWSKI, Janek; YANNOPOULOS, Constantin; WO2015/48245; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics