Tag: M.W:300-400

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.181955-79-3,1,4-Di-Boc-piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

Intermediate 141 : (+/-)-1 ,4-bis(1 ,1-dimethylethyl) 2-methyl 1 ,2,4-piperazinetricarboxylate; In a 500 ml. round-bottomed flask, 22.6 g of intermediate 140 (68.4 mmole) were dissolved in 160 ml. of DCM and 40 ml. of methanol to give a colorless solution. 58 ml. of Trimethylsilyl diazomethane (1 16 mmole) were added dropwise keeping the internal temperature below +2 0C. The solution was allowed to reach RT and was stirred at RT for 2 h. The mixture was carefully evaporated under reduced pressure (Tbath = 35C) and the solid residue was triturated with 100 ml. of pentane, filtered and dried in vacuo to obtain 21 g of desired product as a white solid. The mother liquor was concentrated in vacuo to give 2.5 g of the title compound. UPLC-MS [Acquity UPLC BEH C18, 50×21 mm, 1.7 mum, Mobile phases: A: H2O +0.1% HCOOH/B: MeCN+0.06% HCOOH. Gradient: t=0 min: 97%A, 3% B, t= O.i min 94%A, 6%B t=0.6min 30%A, 70%B t=1.10min 1%A, 99%B t=1.45 min 97%A, 3%B t=1.50min 97%A ,3%B flow rate: 1 ml/min, UV range wavelength 210-350nm]: R1 = 0.80 min, m/z (ES): 344 [M+H]+, 367 [M+Na]+., 181955-79-3

As the paragraph descriping shows that 181955-79-3 is playing an increasingly important role.

Reference：
Patent; GLAXO GROUP LIMITED; WO2008/148853; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

112257-12-2, tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 4-(2-bromo- acetyl)-piperazine-l-carboxylic acid tert-butyl ester (0.39 g, 1.3 mmol) and 2-nitro-6,7- dihydro-5H-imidazo[2,l-b][l,3]oxazin-6.Sr-ol (0.2 g, 1.08 mmol) in DMF (9 ml) was cooled to -60 0C and treated with sodium hydride (50 mg, 1.3 mmol) and warmed to room temperature over 2 h. The mixture was diluted with ethyl acetate, washed with water dried over sodium sulfate and concentrated. The residue is purified by silica gel chromatography (5% methanol in dichloromethane) to give 4-[2-(2-nit?>-6,7-dihydro-5H- imidazo[2,l-b][l,3]oxazin-6S-yloxy)-acetyl]-piperazine-l-carboxylic acid tert-butyl ester as a yellow oil (314 mg, 77%). ESI MS m/z 434 (M + Na+); 1H NMR (400 MHz, CDCl3) delta 7.48 (s, IH), 4.48-4.40 (m, IH), 4.40-4.22 (m, 4H), 3.38-3.44 (s, 2H), 3.42-3.30 (m, 8H), 1.42 (s, 9H)., 112257-12-2

The synthetic route of 112257-12-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CUMBRE PHARMACEUTICALS INC.; WO2008/8480; (2008); 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.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,as a common compound, the synthetic route is as follows.

6-Fluoro- 1 -methyl-4-oxo-7-(piperazin- 1 -yl)- 1 H,4H- [1,3 ]thiazeto[3 ,2-a] quinoline-3-carboxylic acid (3 g, 8.60 mmol) was suspended in DMF (50m1) under argon atmosphere and heated at 90 C. After obtaining a clear solution,triethylamine (2.4 ml , 17.10 mmol), compound A (2.12 g, 6.50 mmol) and tetrabutylammonium bromide (107 mg, 0.33 mmol) were added. Then the reaction mixture washeated for another 20 h at 90 C. After completion of the reaction, it was allowed to cool to room temperature and ethyl acetate was added into the reaction mixture. The obtained precipitate was filtered and filtrate was evaporated to dryness. The crude mass was re-dissolved in DCM and methanol and excess amount diethyl ether was added into this solution to obtain a brown mass which was purified by flash column chromatography over silica gel and pure compound 2 was elutedwith3% methanol-DCMmixture as a beige solid (250 mg) with 8% isolated yield. 1H NMR (CDC13):3 14.23 (brs, 1H, COOH), 7.92 (s, 1H, ArH), 7.89 (d, 1H, JAB = 12.0 Hz, ArH), 6.38 (d, 1H, JAB = 8Hz, ArH), 6.09 (q, 1H, JAB = 4 Hz,SCHN), 4.5 1-4.41 (m, 2H, NCH2), 3.26-3.20 (m, 4H, CH2N), 2.74(t, 2H, JAB = 4 Hz, NCH2), 2.69-2.67 (m, 4H, CH2N), 2.20 (d, 3H, JAB = 4 Hz, CH3). ESI-MS (mlz):503.20 (M+H)., 112984-60-8

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 124225, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; GHOSH, Shamik; GHOSH, Sumana; SINHA, Mau; SADHASIVAM, Suresh; BHATTACHARYYA, Anamika; MAVUDURU, Siva Ganesh; TANDON, Nupur; KUMAR, Deepak; (149 pag.)WO2017/17631; (2017); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1001180-21-7, (R)-tert-Butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 11: Triethylamine (4.33 mL, 31.1 mmol; degassed with nitrogen 30 minutes prior to use) and formic acid (1.36 mL, 36.1 mmol; degassed with nitrogen 30 minutes prior to use) were added to a solution of (R)-tert-butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H- cyclopenta[d]pyrimidin-4-yl)piperazine-l-carboxylate (9.75 g, 29.3 mmol) in DCM (210 mL; degassed with nitrogen 30 minutes prior to use). The mixture was stirred for 5 minutes, and then a Ru catalyst (0.0933 g, 0.147 mmol) was added. The reaction was stirred under positive nitrogen pressure overnight (18 hours). The reaction mixture was concentrated to dryness and dried on high vacuum. The impure material was flashed on Biotage 65M loaded 1:1 DCM:ethyl acetate 500 mL flushed, then 1 :4 DCM:ethyl acetate until product (2nd spot), then gradient to neat ethyl acetate, then 25:1 DCM:MeOH eluted rest of product. The fractions were combined and concentrated on a rotary evaporator. The residue was concentrated again from DCM/hexanes to give a mixture of tert-butyl 4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H- cyclopenta[d]pyrimidin-4-yl)piperazine-l-carboxylate (major) and tert-butyl 4-((5R,7S)-7- hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-l-carboxylate (minor) (9.35 g, 95.3% yield) as a foam. LC/MS (APCI+) m/z 335 [M+H]+. 1H NMR (CDCl3) showed 88% diastereoselectivity by integration of carbinol methine., 1001180-21-7

As the paragraph descriping shows that 1001180-21-7 is playing an increasingly important role.

Reference：
Patent; ARRAY BIOPHARMA INC.; GENENTECH, INC.; WO2009/89453; (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.182618-86-6,1-Boc-4-(4-Nitrophenyl)piperazine,as a common compound, the synthetic route is as follows.,182618-86-6

The solvent was removed and the residue was taken up with methanol, Pd-C (10%) was added and stirred under hydrogen overnight at room temperature and then filtered through Celite and concentrated in vacuo. The crude product was purified by flash chromatography to afford 0.457 g product (60%).

As the paragraph descriping shows that 182618-86-6 is playing an increasingly important role.

Reference：
Article; Mou, Jianfeng; Park, Ann; Cai, Yu; Yuan, Junying; Yuan, Chengye; Bioorganic and Medicinal Chemistry Letters; vol. 25; 15; (2015); p. 3057 – 3061;,
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.149057-19-2,4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

54b. 4-Benzyl 1-terf-butyl 2-(methylcarbamoyl)piperazine-1,4- dicarboxylate4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (1.70 g, 4.70 mmol), DMF (20 ml_), diisopropylethylamine (2.50 mL, 14.1 mmol) and methylamine hydrochloride (0.350 g, 5.20 mmol) were mixed together at room temperature under argon for 10 minutes. 2-(7-aza-1 H- benzotriazole-1-yl)-1 ,1 ,3,3-tetramethyluronium hexafluorophosphate (HATU, 2.00 g, 5.20 mmol) was then added to the reaction mixture in one portion. The mixture was stirred at room temperature under argon for 18 hours. The reaction mixture was then poured into water (100 mL) and extracted with ethyl acetate (4 x 25 mL). The combined organic phases were washed with saturated ammonium chloride (3 x 15 mL), water (3 x 15 mL) and brine (70 mL). The combined organic phases were then dried over sodium sulfate, filtered and concentrated in vacuo. The product, obtained as a white foam (0.91 g, 2.4 mmol, 51%) was purified by column chromatography (gradient elution 20:80 ethyl acetate: hexanes to 100% ethyl acetate), Rf = 0.10 (50:50 ethyl acetate: hexanes); 1H-NMR (400 MHz, CDCI3) delta 7.39-7.33 (m, 5H), 5.17 (br s, 2H), 4.68-4.58 (m, 2H), 3.98-3.88 (m, 2H), 3.23-3.08 (m, 4H), 2.07 (s, 3H), 1.50 (S, 9H); Mass spectrum (ESI +ve) m/z 378.0 (MH+)

149057-19-2, 149057-19-2 4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid 2756778, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BIKAM PHARMACEUTICALS, INC.; GARVEY, David, S.; LAROSA, Gregory, J.; GREENWOOD, Jeremy, Robert; BREWER, Mark, L.; QUACH, Tan; COTE, Jamie, B.; BERMAN, Judd; WO2010/147653; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics