Month: September 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.278788-66-2,(R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

DIPEA (10.41 mL, 59.63 mmol) was added to 4,7-dichloro-6-iodo-3-nitroquinoline (10 g, 27.1 mmol) and tert-butyl (3R)-3-(hydroxymethyl)piperazine-1-carboxylate (10.55 g, 48.79 mmol) in IPA (200 mL). The resulting mixture was stirred at 80 C. for 4 h. The solvent was removed in vacuo. The crude product was purified by flash silica chromatography (0 to 80% EtOAc in petroleum ether) to afford tert-butyl (3R)-4-(7-chloro-6-iodo-3-nitroquinolin-4-yl)-3-(hydroxymethyl)piperazine-1-carboxylate (6.2 g, 42%) as a yellow solid; m/z: ES+ [M+H]+=549.

278788-66-2, As the paragraph descriping shows that 278788-66-2 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; Kettle, Jason Grant; Bagal, Sharanjeet; Robb, Graeme Richard; Smith, James Michael; Goldberg, Frederick Woolf; Cassar, Doyle Joseph; Feron, James Lyman; US2019/177338; (2019); 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.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a mixture of 6j (0.812 g, 1.86 mmol, 1.0 equiv) in n-BuOH (30 mL) was added tert-butyl-4-(2-aminoethyl)piperazine-1-carboxylate (2.80 g, 13.0 mmol, 7.0 equiv). After heating at 100¡ã C. for 24 hrs, the solvent was removed in vacuo. The resulting residue was purified by silica gel chromatography (5percent MeOH:CH2C12) to afford carbamate 8c. MS (MH+) 630.1; Calculated 629.3 for C38H39N5O4.

192130-34-0, 192130-34-0 tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate 1514400, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Nunes, Joseph J.; Martin, Matthew W.; White, Ryan; McGowan, David; Bemis, Jean E.; Kayser, Frank; Fu, Jiasheng; Liu, Jinqian; Jiao, Xian Yun; US2006/46977; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

6531-38-0, 2,2′-(Piperazine-1,4-diyl)diethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6531-38-0, Example 35 (compound No.14*); l,4-bis{2-[4-fluorobenzyl)amino]ethyl}piperazine; To a solution of l,4-bis(2-aminoethyl)piperazine (0.43 g, 2.5 mmol) and 4- fluorobenzaldehyde (0.59 mL, 5.5 mmol) in absolute ethanol (20 mL), 3 A molecular sieves are added. After stirring the mixture at room temperature for 5h, NaBH4 (0.47 g,12.5 mmol) was added portionwise and the mixture was stirred for 12h at room temperature. The reaction was quentched by dropwise addition of water (20 mL) and ethanol was removed under reduced pressure. The aqueous residue was extracted with CH2Cl2 (3 x 30 mL). Combined organic layers were extracted with HCl IM. The combined aqueous layers were neutralized with NaOH IM and extracted with CH2Cl2. Combined organic layers were dried over MgSO4. Crude compound is purified by thick-layer chromatography (CH2Cl2/MeOH : 80/20).

The synthetic route of 6531-38-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM); UNIVERSITE DU DROIT ET DE LA SANTE – LILLE II; WO2006/51489; (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.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 (synthesized according to Example 5, Step 1, 1.31 g, 5.36 mmol) in isopropanol (15 mL), tert-butyl 3-bromo-2,4-dioxopiperidine-1-carboxylate obtained in the first step (1.3 g, 4.46 mmol) was added at rt. The reaction mixture was stirred overnight at 90 C. It was cooled down to rt and evaporated under reduced pressure. Water (10 mL) was added and the desired product was extracted with diethyl ether (2 x 30 mL), dried over Na2SO4 and concentrated, affording the title product. Yield: 74% (1.42 g, yellow solid). LCMS: (Method A) 239.0 (M- Boc+H), Rt. 0.70 min, 48.39% (Max)., 196811-66-2

As the paragraph descriping shows that 196811-66-2 is playing an increasingly important role.

Reference£º
Patent; ASCENEURON S. A.; QUATTROPANI, Anna; KULKARNI, Santosh, S.; GIRI, Awadut Gajendra; (247 pag.)WO2017/144639; (2017); 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.142-64-3,Piperazine Dihydrochloride,as a common compound, the synthetic route is as follows.

5.1.5 Preparation of 1-(2-fluorobenzoyl)piperazine (5) A solution of 2-fluorobenzoic acid (7.00 g, 0.05 mol) and CDI (8.90 g, 0.055 mol) was stirred in dry THF (30 mL) at room temperature for 30 min. In a separate round bottom flask add piperazine (10.76 g, 125 mmol) and piperazine dihydrochloride (20.0 g, 125 mmol) in 60 mL of water. Stir the reaction mixture for 5 min and add 14.0 g of NaCl. Add this brine solution to the round bottom flask containing acyl imidazole. Stir the reaction mixture for 5 hour. The mixture was filtered and the filtrate distilled by rotary evaporation to remove THF. The aqueous layer was washed with ethyl acetate (3 * 10 mL) to remove diacylated product. The PH of the aqueous layer was adjusted to about 9 using saturated solution of NaOH and washed with ethyl acetate (4 * 30 mL). The aqueous layer was discarded. The organic layer was washed with water (4 * 25 mL), dried over anhydrous Na2SO4 and concentrated by rotary evaporation and purified by flash chromatography to afford 1-(2-fluorobenzoyl)piperazine as colourless solid (4.90 g, 48%). The other intermediates 1-(2-chlorobenzoyl)piperazine (6) and 1-[3-(trifluoromethyl)benzoyl]piperazine (7) were prepared by using the general procedure described above.

142-64-3, As the paragraph descriping shows that 142-64-3 is playing an increasingly important role.

Reference£º
Article; Dong, Jinyun; Lu, Wen; Pan, Xiaoyan; Su, Ping; Shi, Yaling; Wang, Jinfeng; Zhang, Jie; Bioorganic and Medicinal Chemistry; vol. 22; 24; (2014); p. 6876 – 6884;,
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.954388-33-1,(R)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

954388-33-1, (a) [2S]-1-Benzyloxycarbonyl-4-t-butoxycarbonyl-2-methoxycarbonylmethylpiperazine A solution of [2R]-1-benzyloxycarbonyl-4-t-butoxycarbonylpiperazine-2-carboxylic acid (prepared as in Example 1(b) and 2(a)) (4.7 g) in ethyl acetate (70 ml) containing N-methylmorpholine (1.76 ml) at 0 C. was treated with isobutyl chloroformate (2.37 ml) for 3 hours and the solution was filtered and added to an excess of diazomethane and left at room temperature for 18 hours. It was evaporated to dryness to afford the diazoketone, which was_ dissolved in dry methanol (120 ml) and treated with silver benzoate (1.99 g) in triethylamine (19.9 ml), with cooling in ice. The solution was stirred in the dark at room temperature for 18 hours, evaporated to dryness, dissolved in ethyl acetate, washed with sodium bicarbonate solution and dried over sodium sulfate. It was chromatographed on silica gel, eluding with ethyl acetate-hexane to afford an oil (3.15 g) (94% ee by chiral HPLC).

As the paragraph descriping shows that 954388-33-1 is playing an increasingly important role.

Reference£º
Patent; SmithKline Beecham Corporation and SmithKline Beecham p.l.c.; US2003/203917; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

54699-92-2, 4-Methyl-1-piperazineacetic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

54699-92-2, Example 13; General Method for the Preparation of Active Esters of N-Substituted Piperazine Acetic Acid from Trifluoroacetate Esters; A solution of the trifluoroacetate in THF (0.58 M, 1.2 equiv) was added to a solid sample of N-methyl piperazine acetic acid and mixed in a vortex or shaker until a homogeneous solution was obtained. The reaction of the carboxylic acid with the trifluoroacetate ester was generally complete within 30 min for all cases except N-hydroypyrrolidinone (NHP, 18 h). The progress of conversion to the active ester was monitored by ES-MS. The amount of product and any starting material (N-MPA) could be determined by direct infusion of a sample of the reaction (in ethanol) into the ES-MS. In some cases the active ester product was precipitated as dihydrochloride salt by the addition of a solution by addition of HCl solution in dioxane (4 M, 50% volume of the reaction) followed by washing with THF, ethyl acetate and hexanes. In other cases the product was isolated from the reaction as the mono TFA salt. Addition of TFA could be performed if the bis-TFA salt was desired. Dhbt ester, Calculated MH+ = 304.14 Found = 304.20 NHP ester, Calculated MH+ = 242.15 Found = 242.20 4-NP ester, Calculated MH+ = 280.13 Found = 280.20 1H NMR (400 MHz, CDCl3) d 8.20 (d, 2H, J=9.2 Hz, aromatic protons), 7.25 (d, 2H, J=9.2 Hz, aromatic protons), 3.69-3.40 (broad, 2H, ring protons), 3.57 (s, 2H, -CH2-CO-), 3.15-2.90 (broad, 6H, ring protons), 2.78 (s, 3H, -CH3). Pfp ester, Calculated MH+ = 325.10 Found = 325.10 Pcp ester, Calculated MH+ = 404.95 Found = 405.90 3-NP ester, Calculated MH+ = 280.13 Found = 280.20 NHS ester, Calculated MH+ = 256.13 Found = 256.10

The synthetic route of 54699-92-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Applera Corporation.; US2005/148771; (2005); A1;; ; Patent; Applera Corporation.; US2005/148774; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

169448-87-7, (R)-tert-Butyl 2-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of the product of Example 75 step i) (300mg), (f?>2-(hydroxymethyl)piperazine- 1-carboxylic acid, terf-butyl ester (465mg) and sodium triacetoxyborohydride (608mg) in dichloromethane (2OmL) was stirred under nitrogen for 16 hours. The reaction was partitioned between dichloromethane and water, the organics were then collected and concentrated to dryness. The residue was purified by HPLC to give the title compound (230mg) as a solid. MS: APCI(+ve) 519 (M+H)+1H NMR DMSO-Cl6 8.54 (d, J = 4.2 Hz, 1 H), 8.35 (d, J = 8.3 Hz, 1 H), 7.97 (d, J = 1.5 Hz, 1 H), 7.69 – 7.64 (m, 2H), 7.54 (dd, J = 8.2, 1.4 Hz, 1 H), 7.49 (s, 1 H), 4.46 (t, J = 5.4 Hz, 1 H), 3.93 – 3.79 (m, 2H), 3.55 – 3.44 (m, 2H), 3.28 – 3.20 (m, 2H), 2.89 – 2.77 (m, 3H), 2.75 – 2.67 (m, 1H), 2.63 – 2.52 (m, 2H), 2.25 (d, J = 2.3 Hz, 3H), 2.07 – 1.87 (m, 2H), 1.67 – 1.58 (m, 1 H), 1.31 – 1.19 (m, 1H), 0.74 – 0.66 (m, 2H), 0.60 – 0.54 (m, 2H), 0.52 – 0.45 (m, 2H), 0.44 – 0.38 (m, 2H), 169448-87-7

As the paragraph descriping shows that 169448-87-7 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2008/122765; (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.13889-98-0,1-Acetylpiperazine,as a common compound, the synthetic route is as follows.

Intermediate 9 (3.0 g, 0.89 mmol) in NMP (15 mL) was treated with 1-acetyl- piperazine (2.8 g, 22 mmol) and DIPEA (5.7 g, 44 mmol) and heated in a sealed tube at 140C for 72 h. The reaction mixture was cooled to r.t. and diluted with ethyl acetate/ water. The organic phase was washed (water, brine), dried (phase separation cartridge) and evaporated in vacuo. The resulting residue was purified by silica flashchromatography, eluting with 50-60% EtOAc in isohexane, to give the title compound (3.4 g 89%) as a cream solid. deltaEta (CDC13) 7.95 (IH, s), 7.53 (IH, dd, J 8.9, 6.0 Hz), 7.16 (IH, t, J 8.9 Hz), 5.08-5.02 (IH, m), 3.95-3.90 (IH, m), 3.78-3.73 (2H, m), 3.64 (IH, m), 3.61-3.40 (2H, m), 3.19-3.15 (2H, m), 2.59 (3H, d, J2.4 Hz), 2.17 (3H, s), 1.58 (3H, d, J 6.5 Hz), 1.48-1.42 (9H, m).

13889-98-0, 13889-98-0 1-Acetylpiperazine 83795, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; UCB PHARMA S.A.; ALLEN, Daniel, Rees; BUeRLI, Roland; HAUGHAN, Alan, Findlay; MATTEUCCI, Mizio; OWENS, Andrew, Pate; RAPHY, Gilles; SHARPE, Andrew; WO2011/58108; (2011); 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.1235865-77-6,2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

Compound L, the free base of venetoclax (4-(4-{[2-(4-chlorophenyl)-4,4- dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4- ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide), may be prepared as follows. Compound K (3.39 g), Compound A (1.87 g), 1-ethyl-3-[3- (dimethylamino)propyl]-carbodiimide hydrochloride (2.39 g), and 4-dimethylaminopyridine (1.09 g) were stirred in CH2Cl2 (40 mL) for 24 hours. The reaction was cooled and chromatographed on silica gel with 25-100% ethyl acetate/hexanes, then 10% methanol/ethyl acetate with 1% acetic acid, to give the product (1.62 g, 32%) as a solid.1H NMR (300 MHz, dimethylsulfoxide-d6) 11.65 (br s, 1H), 8.55 (br s, 1H), 8.04 (d, 1H), 7.89 (dd, 1H), 7.51 (m, 3H), 7.33 (d, 2H), 7.08 (m, 1H), 7.04 (d, 2H), 6.68 (dd, 1H), 6.39 (d, 1H), 6.19 (d, 1H), 3.84 (m, 1H), 3.30 (m, 4H), 3.07 (m, 4H), 2.73 (m, 2H), 2.18 (m, 6H), 1.95 (m, 2H), 1.61 (dd, 2H), 1.38 (m, 2H), 1.24 (m, 4H), 0.92 (s, 6H)., 1235865-77-6

1235865-77-6 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid 66713100, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ACERTA PHARMA B.V.; HAMDY, Ahmed; ROTHBAUM, Wayne; IZUMI, Raquel; LANNUTTI, Brian; COVEY, Todd; ULRICH, Roger; JOHNSON, Dave; BARF, Tjeerd; KAPTEIN, Allard; (732 pag.)WO2016/24230; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics