Month: February 2021

208167-83-3, tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of tert-butyl 4-(2-((4-(6-(4-benzamido-4-methylpiperidin-l- yl)pyridin-3-yl)-3-cyanopyrazolo[l,5-a]pyridin-6-yl)oxy)ethyl)piperazine-l-carboxylate. To a solution of N-(l-(5-(3-cyano-6-hydroxypyrazolo[l,5-a]pyridin-4-yl)pyridin-2-yl)-4- methylpiperidin-4-yl)benzamide (Intermediate P87, 157.2 mg, 0.3474 mmol) in DMA (3.5 mL) was added tert-Butyl 4-(2-chloroethyl)tetrahydro-l(2H)-pyrazinecarboxylate (172.8 mg, 0.6948 mmol) and cesium carbonate (565.9 mg, 1.737 mmol). The reaction mixture was stirred at 60C for 16 h. After cooling to ambient temperature, the reaction mixture was diluted with EtOAc and washed successively with water and saturated NaCl(aq). The combined organic extracts were dried over anhydrous Na2S04(S), filtered, and concentrated in vacuo to afford the title compound (assumed theoretical yield, 231 mg, 0.3474 mmol) in sufficient purity for step 2. MS (apci) m/z = 665.4 (M+H).

208167-83-3, As the paragraph descriping shows that 208167-83-3 is playing an increasingly important role.

Reference£º
Patent; ANDREWS, Steven W.; ARONOW, Sean; BLAKE, James F.; BRANDHUBER, Barbara J.; COLLIER, James; COOK, Adam; HAAS, Julia; JIANG, Yutong; KOLAKOWSKI, Gabrielle R.; MCFADDIN, Elizabeth A.; MCKENNEY, Megan L.; MCNULTY, Oren T.; METCALF, Andrew T.; MORENO, David A.; RAMANN, Ginelle A.; TANG, Tony P.; REN, Li; WALLS, Shane M.; (946 pag.)WO2018/71454; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

60% Sodium hydride (104 mg, 2.61 mmol) was added portionwise to te/t-butyl (S)-3- (hydroxymethyl)piperazine-l-carboxylate (414 mg, 1.91 mmol) in THF (5 ml) cooled to 0C over a period of 5 minutes, under nitrogen. The resulting mixture was stirred at 0C for 10 minutes then allowed to warm to room temperature and stirred for 30 minutes. 7-Bromo-5-fluoroquinazolin-4-ol (423 mg, 1.74 mmol) was added and the mixture heated at 65C and stirred for 4 hours. The reaction mixture was cooled to room temperature then 60% sodium hydride (104 mg, 2.61 mmol) added, then heated to 65C and stirred for a further 16 hours. The reaction mixture was diluted with EtOAc (100 ml), washed with water (10 ml) and the aqueous washing was extracted with EtOAc (50 ml). The organic phases were combined, dried with MgS04, filtered and evaporated to afford crude product. This was purified by flash silica chromatography, elution gradient 0 to 80% EtOAc in heptane, then 0- 20% MeOH in DCM. Pure fractions were evaporated to dryness to afford te/t-butyl (5)-3-(((7-bromo-4- hydroxyquinazolin-5-yl)oxy)methyl)piperazine-l-carboxylate (491 mg, 64%) as a white solid. IH NM (500 M Hz, DMSO, 27C) 1.38 (9H, s), 2.53 – 2.67 (2H, m), 2.78 (2H, s), 2.90 (2H, dd), 3.72 (IH, d), 3.86 – 3.98 (2H, m), 4.13 (IH, s), 7.19 (IH, d), 7.36 (IH, d), 8.00 (IH, s), 11.96 (IH, s). m/z: ES+ [M+H]+ 439

314741-40-7, As the paragraph descriping shows that 314741-40-7 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; BOYD, Scott; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; RAUBO, Piotr, Antoni; (144 pag.)WO2018/206539; (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.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

Example B .22Preparation of compound (173) A mixture of compound (37), 1-cyclopropyl-piperazine (0.0027 mol), tris(dibenzylidene- acetone)dipalladium (0.054 mmol), l,r-[l,r-binaphthalene]-2,2′-diylbis[l,l-diphenyl- phosphine (0.081 mmol) and 2-methyl-propanol, sodium salt (1 :1) (0.00162 mol) in THF (5 ml) was stirred at 8O0C for 40 minutes under microwave. The mixture was filtered and concentrated to give the crude product. The crude product was purified by high-performance liquid chromatography (C 18, eluent: CH3CN / water from 8 / 92 to 38 / 62 with 0.1% CF3COOH ). The pure fractions were collected and the organic solvent was evaporated. The aqueous mixture was basified with solid NaHCOs to pH = 8. The aqueous mixture was extracted with DCM (40 ml) twice. The combined organic layers was washed with de-ion water (20 ml). The separated organic fraction was dried over sodium sulfate, filtered off the solid and the solvent was evaporated. The product was obtained by lyophilization, yielding 0.04 g of compound (173)., 20327-23-5

20327-23-5 1-Cyclopropylpiperazine 4742004, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; JANSSEN PHARMACEUTICA NV; WO2009/132000; (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.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

A stirred mixture of 5-chloro-7-{[methoxy(methyl)amino]carbonyl}quinolin-8-yl trifluoromethanesulfonate (0.120 g, 0.301 mmol), l-(2-methoxyethyl)piperazine (0.0522 g, 0.362 mmol, from Aldrich), palladium acetate (1 mg, 0.006 mmol), 2,2′-bis(diphenylphosphino)-l,l’- binaphthyl (6 mg, 0.009 mmol), and cesium carbonate (0.14 g, 0.42 mmol) in tetrahydrofuran (3 mL) was heated at 65 C overnight. The mixture was cooled, diluted with dichloromethane, and filtered. The filtrate was washed with brine, dried over sodium sulfate, and evaporated to dryness. The resultant residue was purified on silica gel, eluting with 0 to 10% MeOH in dichloromethane, to give the desired product (63 mg, 53%). LCMS calculated forCi9H26ClN403(M+H)+: m/z = 393.2; found: 393.1.

13484-40-7, The synthetic route of 13484-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; INCYTE CORPORATION; LI, Yun-Long; COMBS, Andrew, P.; YUE, Eddy, W.; LI, Hui-Yin; WO2011/75630; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

187669-60-9, 1-(4-(Methylsulfonyl)phenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 81; 4-{2-[4-(4-Mcthancsulfonylphcnyl)pipcrazin-l-yl]-2-oxocthyl}pipcridinc-l- carboxylic acid tert-butyl ester; To a solution of 4-hydroxy-4-(3-hydroxypropyl)piperidine-l-carboxylic acid tert-butyl ester (1.00 g, 3.86 mmol) in DCM (60 mL) was added Dess-Martin periodinane (1.80 g, 4.24 mmol) and the mixture was stirred for Ih at rt, a further batch of Dess-Martin periodinane (0.20 g, 0.47 mmol). The reaction mixture was quenched with 2 M NaOH and extracted with Et2O, the aqueous phase was re-extracted with Et2O and the organic extracts were combined then washed with water, 2 M NaOH solution and brine, dried (MgSO4) and the solvent was removed under vacuum to give 2-hydroxy-l-oxa-8-azaspiro[4.5]decane-8-carboxylic acid tert-butyl ester. A solution of l-(4-methanesulfonylphenyl)piperazine (0.12 g, 0.50 mmol) and 2-hydroxy-l-oxa- 8-azaspiro[4.5]decane-8-carboxylic acid tert-butyl ester (0.14 g, 0.56 mmol) in anhydrous MeOH (2 mL) was heated at 750C for Ih, then NaBH4 (25 mg, 0.65 mmol) was added and the reaction was stirred for 2h. The solvent was removed under vacuum and the resulting residue was partitioned between water and DCM. The aqueous phase was re-extracted with DCM, the EPO organic extracts were combined and purified by flash chromatography eluting with 3:97 MeOH:DCM to afford the title compound: RT = 2.37 min; m/z (ES+) = 482.45 [M+H]+., 187669-60-9

187669-60-9 1-(4-(Methylsulfonyl)phenyl)piperazine 735904, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; PROSIDION LIMITED; WO2007/3964; (2007); 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.13349-91-2,1-(2,2,2-Trifluoroethyl)piperazine dihydrochloride,as a common compound, the synthetic route is as follows.

13349-91-2, The material so obtained was suspended in methylene chloride and a saturated methanolic ammonia solution (20 ml) was added. The resultant mixture was stirred at ambient temperature for 20 minutes. The mixture was filtered and the filtrate was evaporated at ambient temperature under vacuum. There was thus obtained 1- (2, 2, 2-TRIFLUOROETHYL) piperazine which was used without any additional purification

13349-91-2 1-(2,2,2-Trifluoroethyl)piperazine dihydrochloride 16312067, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2004/41829; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1359658-32-4, (R)-tert-Butyl 3-(methoxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation Example 406 To a mixture of tert-butyl (3R)-3-(methoxymethyl)piperazine-1-carboxylate (206 mg), methanol (3.09 mL), and a 36% aqueous formaldehyde solution (187 mg) was added 10% palladium-supported carbon (50% wet product) (76 mg), followed by stirring at room temperature for 4 hours under a hydrogen gas atmosphere (1 atm). The reactant was filtered through celite and then the solvent was evaporated under reduced pressure to obtain tert-butyl (3R)-3-(methoxymethyl)-4-methylpiperazine-1-carboxylate (231 mg) as an oily material., 1359658-32-4

As the paragraph descriping shows that 1359658-32-4 is playing an increasingly important role.

Reference£º
Patent; ASTELLAS PHARMA INC.; Matsuya, Takahiro; Kondoh, Yutaka; Shimada, Itsuro; Kikuchi, Shigetoshi; Iida, Maiko; Onda, Kenichi; Fukudome, Hiroki; Takemoto, Yukihiro; Shindou, Nobuaki; Sakagami, Hideki; Hamaguchi, Hisao; US2014/323463; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5521-39-1,5521-39-1, 2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[00215] Step 3 : A flask was charged with intermiediate 2 (50 mg, 0.16 mmol), 2-(4-(4- aminophenyl)piperazin-l-yl)ethanol (30.4 mg, 0.16 mmol), DIPEA (60uL), DMSO (2 mL). The reaction was stirred at room temperature for over. The crude product was purified with flash chromatography (0-10% MeOH-in DCM) to afford the desired product as light yellow solids (42 mg, 54% yield). 1H MR (400 MHz, DMSO-d6) delta 11.83 (br, 1H), 9.86 (br, 1H), 8.23 (s, 1H), 7.30 (d, J=8.4Hz, 2H), 7.00 (dd, J=5.6Hz, J = 10.4 Hz, 1H), 6.90 (d, J=8.8Hz, 2H), 6.34 (s, 1H), 3.51 (m, 2H), 2.84 (m, 2H), 2.41 (s, 3H), 2.11 (m, 2H), 1.03 ( s, 3H), 1.01 (s, 3H); ESI-MS: calcd for (C26H25F2N70) 489, found 490 (MH+).

The synthetic route of 5521-39-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NANTBIOSCIENCE, INC.; TAO, Chunlin; POLAT,, Tulay; WEINGARTEN, Paul; NALLAN, Laxman; ARP, Forrest; WANG, Qinwei; HO, David; (129 pag.)WO2016/138527; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 7: Ethyl 4-{3-methyl-(piperazin-1-yl)}-benzoate Dimethyl sulfoxide (5.0 ml) was added to 1.2 g of (+-)-2-methylpiperazine to prepare a suspension. Ethyl 4-fluorobenzoate (1.0 g) was added to the suspension, and the mixture was stirred at 120 C. for 6.5 hr and was then cooled to room temperature. The reaction solution was concentrated under the reduced pressure. The residue was purified by column chromatography on silica gel (development system: methylene chloride-methanol-concentrated aqueous ammonia=900:100:1) to prepare 1.1 g of the title compound. Physicochemical Properties of Intermediate 7, 109-07-9

As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference£º
Patent; Meiji Seika Kaisha, Ltd.; US6451800; (2002); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,162046-66-4

To a stirred solution of 5 -(2-aminothiazol-5 -yl)sulfanyl -2-methoxy-4-methyl- benzoic acid (530.46 mg, 1.79 mmol), 1-piperazin-1-ylprop-2-en-1-one; 2,2,2-trifluoroacetic acid (455 mg, 1.79 mmol) and DIPEA (3.93 mL, 8.95 mmol) in DMF (5 mL) was added HATU (680.56 mg, 1.79 mmol). After 2 h, 4-(4-tert-butoxycarbonylpiperazin-1-yl)benzoic acid (1.37 g, 4.47 mmol), HATU (1.70 g, 4.47 mmol) and DIPEA (3.93 mL, 8.95 mmol) inDMF (5 mL) was added. The resulting mixture was heated to 80 oC. After 4 h, the reaction mixture was extracted with EtOAc (2 x 100 mL), 2 M aq. citric acid (2 x 200 mL) and brine (100 mL). The combined organic extracts were dried over Na2504, filtered and concentrated. Silica gel chromatography (DCM, MeOH) afforded the title compound (471 mg). MS (ES) m/z 707.3 (M+H).

162046-66-4 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid 2795508, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CORVUS PHARMACEUTICALS, INC.; HUDSON, Ryan; BEAUSOLEIL, Anne-Marie; (616 pag.)WO2018/89261; (2018); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics