Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.118753-66-5,tert-Butyl 4-aminopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

118753-66-5, General procedure: To a well-stirred solution of intermediate 5a (2.0 g,5.29 mmol) in ethanol (10 mL) was added 1-amino-4-methylpiperazine 9a (0.61 g, 5.29 mmol) and a drop of acetic acid,and the mixturewas stirred at 78 C for 2 h. The mixturewas cooledto room temperature and the resulting solid was collected byfiltration and purified by column chromatography to give the targetcompounds 6a-1 as a yellow solid in 75% yield. M.p: 228-230 C;

118753-66-5 tert-Butyl 4-aminopiperazine-1-carboxylate 22029174, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Wu, Yachuang; Ding, Xiudong; Yang, Yifeng; Li, Yingxiu; Qi, Yinliang; Hu, Feng; Qin, Mingze; Liu, Yajing; Sun, Lu; Zhao, Yanfang; European Journal of Medicinal Chemistry; vol. 185; (2020);,
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5747-48-8,5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 2: l-(4-Dibenzo[b,f] [l,4]thiazepin-ll-yl-piperazin-l-yl)-propan-l-oneA suspension of propionic acid (1 mmol) and 1-hydroxybenzotriazole (1 mmol) in dichloromethane (4 rnL) is treated with l-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (1.1 mmol) and triethylamine (1.2 mmol). A solution of PDBTZ (1 mmol) in dichloromethane (4 mL) is added and the mixture is stirred at ambient temperature for 20 hours. The reaction mixture is washed (water, brine), dried (sodium sulfate), and evaporated. The crude material is purified by flash chromatography to provide the title compound.

As the paragraph descriping shows that 5747-48-8 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; WO2008/79838; (2008); A1;,
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197638-83-8, 1-Boc-4-(4-Formylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,197638-83-8

Compound 23 was synthesized as show n Scheme 4.

The synthetic route of 197638-83-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; COMBS, Colin; MULLER, Gerhard; DAMEN, Eddy; NAGAMOTO-COMBS, Kumi; (73 pag.)WO2017/100703; (2017); A1;,
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1403898-64-5, (2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A stirred solution of 113 7-bromo-4,6-dichloro-8-fluoro-3-nitroquinoline (2 g, 5.88 mmol) and 180 tert-butyl (2R,5R)-5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate (1.355 g, 5.88 mmol) in 142 MeCN (30 mL) was treated with 56 DIPEA (1.025 mL, 5.88 mmol) and the reaction mixture stirred at 80 C. for 75 min. The reaction mixture was concentrated in vacuo and purified by flash silica chromatography (0 to 40% 57 EtOAc in 58 heptane) to give 444 tert-butyl (2R,5R)-4-(7-bromo-6-chloro-8-fluoro-3-nitroquinolin-4-yl)-5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate (2.6 g, 83%) as a yellow solid; m/z: ES+ [M+H]+ 533/535.

1403898-64-5, The synthetic route of 1403898-64-5 has been constantly updated, and we look forward to future research findings.

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;,
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163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 3-[6-(6-methoxy-pyridin-3-yl)-quinazolin-4-yl]-benzoic acid (100mg, 0.254 mmol) in 2 mL of D F, was added HBTU (144 mg, 0.381 mmol) and DI PEA (0.177 mL, 1 .016 mmol). The reaction mixture was stirred at rt for 30 min, (R)-3-methyl-piperazine- 1 -carboxylic acid tert-butyl ester (76 mg, 0.381 mmol) was added and the resulting reaction mixture stirred for a further 2h at rt. The reaction was quenched with H20, and extracted with CH2CI2. The organic layer was washed with brine, dried over MgS04, filtered and evaporated under vacuum. The residue was dissolved in 3ml of CH2CI2 and TFA ( 1 ml) was added. The reaction mixture was stirred at ambient temperature for 2h. After this period of time, the mixture was concentrated and purified by preparative reverse phase Gilson H PLC and subsequent neutralization of the combined fractions over PL-HC03 MP gave the title compound (29 mg, 26% yield) as a white powder. 1H-N R (400 MHz, DMSO-d8, 298 K): delta ppm 1 .23 (d, 3 H) 2.55-3.2 (m, 7 H) 3.91 (s, 3H) 6.95 (d, 1 H) 7.62 (d, 1 H) 7.72 (t, 1 H) 7.81 (s, 1 H) 7.98 (d, 1 H) 8.1 1 (d, 1 H) 8.22 (d, 2 H) 8.38 (d, 1 H) 8.59 (s, 1 H) 9.38 (s, 1 H). MS: 440.1 [M-H ] Rt(2”= 0.89 min., 163765-44-4

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; COOKE, Nigel Graham; FERNANDES GOMES DOS SANTOS, Paulo Antonio; FURET, Pascal; HEBACH, Christina; HOeGENAUER, Klemens; HOLLINGWORTH, Gregory; KALIS, Christoph; LEWIS, Ian; SMITH, Alexander Baxter; SOLDERMANN, Nicolas; STAUFFER, Frederic; STRANG, Ross; STOWASSER, Frank; TUFILLI, Nicola; VON MATT, Anette; WOLF, Romain; ZECRI, Frederic; WO2013/88404; (2013); A1;,
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5294-61-1,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5294-61-1,N-(2,6-Dimethylphenyl)-2-(piperazin-1-yl)acetamide,as a common compound, the synthetic route is as follows.

Part C. Synthesis of N-(2,6-dimethylphenyl)-2-[4-(2-hydroxy-4phenylbutanoyl) piperazinyl]acetamide (7) To a solution of 5 in 10ml DMF (0.263g, 1.07mmol) was added compound 6 (0.25g, 1.39mmol), HBTU (0.526g, 1.4mmol), triethylamine (0.108g, 1.07mmol) and DMAP (0.030g, 0.25mmol). The solution was allowed to stir at room temperature for 48h. The solution was concentrated in vacuo. The residue was taken into EtOAc (100ml) and washed with saturated sodium bicarbonate (3*50ml). The organic layer was dried over sodium sulfate and concentrated in vacuo. The residue was purified using prep. TLC (10:1 DCM/MeOH) to afford compound 7: Mass spectrum (M+1)=410.44.

The synthetic route of 5294-61-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Blackburn, Brent K.; Zablocki, Jeff; Elzein, Elfatih; Nudelman, Grigory; US2001/44541; (2001); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.192330-11-3,(R)-1-Boc-Piperazine-3-carboxylic acid,as a common compound, the synthetic route is as follows.

Prep(167a): (21(at)-4-(tert-butoxycarbonyl)-1-(cyclopentylmethyl)piperazine-2-carboxylic acid In a round bottom flask, (2R)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (1.50 g, 6.52 mmol) in THF (20 mL) was dissolved, then cyclopentanecarbaldehyde (0.70 mL, 7.62 mmol) with acetic acid (1.20 mL) was added and then stirred for 0.5 hours. Next, NaBH(OAc)3 (2.07 g, 9.77 mmol) was added over 5 minutes and then stirred for 12 hours. The mixture was filtered though a cellose filter. The mother liquid was concentrated and placed on the high vacuum to afford (2R)-4-(tert-butoxycarbonyl)-1- (cyclopentylmethyl)piperazine-2-carboxylic acid as a white solid (1.98 g, 97.4%). 1 H NMR (400 MHz, DMSO-d6) No. ppm: 3.48-3.40 (m, 1 H), 3.36-3.25 (m, 2H), 3.12-3.00 (m, 2H), 2.28-2.24 (m, 1 H), 2.17 (bs, 1H), 2.08-2.08-2.01 (m, 1H), 1.69-1.59 (m, 2H), 1.55-1.44 (m, 4H), 1.38 (s, 9H), 1.35-1.20 (m, 2H), 1.14- 1.06 (m, 1 H). LCMS (ESI) : m/z. 313.2., 192330-11-3

192330-11-3 (R)-1-Boc-Piperazine-3-carboxylic acid 6558430, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; PFIZER INC.; WO2005/108359; (2005); A1;,
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259808-67-8, 1-Boc-3,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 1 ,1-dimethylethyl 3,3-dimethyl-1-piperazinecarboxylate (100mg, 0.467mol) in tetrahydrofuran (1 OmL) was added triethylamine (0.098ml_, 0.700 mmol) followed by dropwise addition of benzoyl chloride (0.06OmL, 0.513mmol). The reaction mixture was allowed to stir for 30 minutes. The reaction mixture was diluted with DCM (1OmL) and the solution was washed with saturated sodium bicarbonate solution (1OmL, twice), then (0.1 M, aq) HCI (1OmL). The organic layer was dried (MgSO4), filtered and concentrated in vacuo to yield 1 ,1-dimethylethyl 3,3-dimethyl-4- (phenylcarbonyl)-i-piperazinecarboxylate as a colourless oil (162mg, 100%), MS ES+ve m/z 319 (M+H)To 1 , 1 -dimethylethyl 3,3-dimethyl-4-(phenylcarbonyl)-1 -piperazinecarboxylate (162mg, 0.509 mmol) was added 1 M hydrochloric acid in 1 ,4 dioxane (1 OmL), followed by the addition of 3 drops of water. The reaction mixture was allowed to stir for 62hours. The reaction mixture was reduced in vacuo to yield colourless oil. The colourless oil was dissolved in methanol (1 OmL) and passed down a SCX-2 column washing with two column volumes methanol and eluting the product with three column volumes of 2N ammonia solution in methanol The fraction containing eluted product was reduced in vacuo to yield 2,2-dimethyl-1-(phenylcarbonyl)piperazine as a white solid (81 mg, 63%), MS ES+ve m/z 219 (M+H). To a solution of 2,2-dimethyl-1-(phenylcarbonyl)piperazine (81 mg, 0.318 mmol) in DCM (5m L) was added DIPEA (0.172mL, 0.986 mmol), followed by gradual addition of 4-cyanobenzenesulfonyl chloride (70.5mg, 0.350 mmol). The reaction mixture was allowed to stir for 1 hour.The reaction mixture was diluted with DCM (1 OmL) and the solution was washed with saturated sodium bicarbonate solution (1 OmL, twice), then with distilled water (1OmL). The organic layer was dried (MgSO4), filtered and reduced in vacuo to yield a transparent oil (160mg).The oil was then dissolved in 1 :1 MeCN/DMSO (0.9ml) and purified using MDAP (over 3 batches). The fractions containing product were combined and reduced in vacuo to yield the title compound as a white solid (48mg, 32%)1H-NMR (CDCI3) 51.58 (6H, s), 3.00 (2H, s), 3.15 (2H, t, J=5.6Hz), 3.47 (2H, t, J=5.6Hz), 7.31-7.48 (5H, m), 7.84-7.93 (4H, m).MS ES+ve m/z 384 (M+H).

259808-67-8, 259808-67-8 1-Boc-3,3-Dimethylpiperazine 22710387, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXO GROUP LIMITED; BESWICK, Paul, John; CAMPBELL, Alister; CRIDLAND, Andrew; GLEAVE, Robert, James; PAGE, Lee, William; WO2010/102663; (2010); A1;,
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3022-15-9, Piperazine-2-carboxylic acid dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of piperazine-2-carboxylic acid dihydrochloride (25.0 g, 123 mmol), dioxane (180 ml) and 5N aqueous sodium hydroxide solution (90 ml) was added dropwise di-tert-butyl dicarbonate (62.7 g, 288 mmol) under ice-cooling. The mixture was stirred at room temperature for 4 hr, and the solvent was evaporated under reduced pressure. The residue was washed with ether, and acidified to pH=2-3 with concentrated hydrochloric acid under ice-cooling, and the mixture was extracted with ethyl acetate. The extract was dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure to give the object product (31.5 g, 77.6%) as a solid. 1H-NMR (CDCl3) delta; 1.44 (18H, s), 2.87 (1H, br s), 3.08-3.23 (2H, m), 3.76-4.10 (2H, m), 4.51-4.75 (2H, m), 5.07 (1H, br s)., 3022-15-9

As the paragraph descriping shows that 3022-15-9 is playing an increasingly important role.

Reference£º
Patent; Matsumoto, Takahiro; Kamo, Izumi; Nomura, Izumi; US2009/318412; (2009); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

Example 8: 6-[[2-(Cyclopropylcarbonyl)amino-pyridin-4-yl]oxy]-naphthalene-1-carboxylic acid [4-[(4-methyl-1-piperazinyl)methyl]-3-trifluoromethyl-phenyl]amide; Under an argon atmosphere, a stirred solution of 4-[(4-methyl-1-piperazinyl)methyl]-3- (trifluoromethyl)benzenamine (0.131 g, 0.48 mmol) in dry toluene (5 ml_) is treated with a solution Of AIMe3 (0.6 mL of 2 M in toluene; 1.1 mmol) at 18C. After 30 min, a solution of 3- [[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]oxy]-1-naphthalenecarboxylic acid, methyl ester (0.174 g, 0.48 mmol) in toluene (5 ml_) is added and the mixture is heated for 2 h at 85- 95C. The cooled mixture is then added to a saturated aqueous solution of NH4CI, stirred for 30 min and extracted with ethyl acetate. The combined extracts are washed (brine), dried (Na2SO4) and solvent is evaporated off under reduced pressure to give a residue, which is purified by column chromatography (SiO2; dichloromethane/methanol/aqueous ammoniaNH3(d 0.88) 95:4.5:0.5) to afford the title compound as a colourless solid, m.p.: 218- 2200C., 694499-26-8

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£º
Patent; NOVARTIS AG; WO2008/125691; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics