Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.325145-35-5,(S)-tert-Butyl 2-ethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 5-chloro-1- (chloromethyl) -2-methyl-3-nitrobenzene (D23 1.232 g) in DMF (20 mL) were added (S) -tert-butyl 2-ethylpiperazine-1-carboxylate (1 g) and K2CO3(1.935 g) at 60. After stirring overnight the mixture was poured into ice/water and then extracted with DCM (3×100 mL) . The combined organic layers were dried over Na2SO4 filtered and concentrated to give a yellow oil which was purified by column chromatography (eluting with EAPE5) to give the title compund (1.3 g) as a yellow solid. MS (ESI) C19H28ClN3O4requires 397 found 398 [M+H]+., 325145-35-5

The synthetic route of 325145-35-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXOSMITHKLINE (CHINA) R&D COMPANY LIMITED; LEI, Hui; MA, Xin; REN, Feng; LIN, Xichen; MARQUIS, Robert W., Jr.; WO2015/180614; (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.170911-92-9,tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

c (6 g, 21.63 mmol), triethylamine (3.28 g, 32.45 mmol) were added to 100 mL of CH 2 Cl 2 under ice-cooling, and then 3-chloro-benzoyl chloride (4.54 g, 25.96 mmol) was gradually added dropwise. After being transferred to room temperature, stirring for 2 hours;After the reaction was completed, it was quenched by adding 50 mL of water, and then 50 mL of CH2Cl2 solvent was added.After washing with water (50 mL × 3), the organic phase was dried over anhydrous magnesium sulfate,Evaporation to dry d (7.60 g); yield: 84.47%,, 170911-92-9

As the paragraph descriping shows that 170911-92-9 is playing an increasingly important role.

Reference：
Patent; Zhejiang University; Zhengzhou University; Sun Yi; Liu Hongmin; Xu Tiantian; Li Yanan; Yu Bin; Ma Qisheng; Hou Tingjun; Pan Peichen; Xiong Xiufang; (37 pag.)CN110156729; (2019); A;,
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

A vial was charged with (S)-tert-butyl 3 -(hydroxymethyl)piperazine-l -carboxylate (367.3 mg, 1.647 mmol) and 2-(tert-butoxymethyl)oxirane (243.3 mg, 1.850 mmol) in ethanol (3 mL). The mixture was heated at 120 C for 30 min using microwave. The mixture was cooled to room temperature, concentrated to remove all of solvents. The residue was purified with flash column chromatography on silica gel using 1-10% methanol in dichloromethane to afford the final product as colorless oil (497.5 mg) in 87% yield. NMR (500 MHz, Chloroforn /) delta 3.86 – 3.80 (m, 2H), 3.71 – 3.68 (m, lH), 3.53 – 3.41 (m, 2H), 3.40 – 3.35 (m, 2H), 3.24 (dd, J = 9.1, 6.6 Hz, 1H), 3.10 (br, 1H), 2.91 (m, 1H), 2.83 – 2.75 (m, 1H), 2.48 (dd, J = 13.1, 7.6 Hz, 2H), 2.39 – 2.30 (m, 1H), 1.44 (s, 9H), 1.18, 1.17 (2s, 9 H). MS for C17H34N2O5: 347.2 (MH+)., 314741-40-7

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NEKTAR THERAPEUTICS (INDIA) PVT. LTD.; NEKTAR THERAPEUTICS; SHARMA, PANKAJ; KHATRI, VIJAY KUMAR; GU, XUYUAN; SONG, YUAN; SHEN, MICHAEL LIXIN; SAUTHIER, JENNIFER RIGGS; ANAND, NEEL K.; KOZLOWSKI, ANTONI; ODINECS, ALEKSANDRS; RILEY, TIMOTHY A.; REN, ZHONGXU; MU. YONGQI; SHEN, XIAOMING; YUAN. XUEJUN; AURRECOECHEA, NATALIA; O’MAHONY, DONOGH JOHN ROGER; WO2015/92819; (2015); 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.16154-72-6,3-Chloro-4-(4-methylpiperazin-1-yl)benzenamine,as a common compound, the synthetic route is as follows.

To a solution of 3.0 g (13.3 mmol) OF 4- (3-CHLORO-4-METHYLPIPERAZIN-1-YL) aniline and 2.22 mL (16.0 mmol) of triethylamine in 36 mL of dichloromethane, 6.0 g (15.3 mmol) of 1, 3-bis (TERT-BUTOXYCARBONYL)-2-TRIFLUOROMETHANESULFONYLGUANIDINE were added. The reaction mixture was stirred at room temperature for 72 hours. The solution was diluted with FURTHER dichloromethane, washed with water and the solvent dried over NA2S04 and evaporated in vacuo. The residue was purified by chromatography on a silica gel column (eluant dichloromethane/methanol 92/8) giving 5.4 g (86.2% yield) of a protected intermediate, that was treated with 60 mL OF 4 N HC1 in dioxane. The mixture was stirred at room temperature overnight. The solvent was removed under reduced pressure, the residue redissolved in water, the resulting solution neutralized and the product extracted with ethyl acetate. The solvent was removed under reduced pressure to give 2.4 g (78.7% yield) of the title compound. H NMR (400 MHz, DMSO-d6) 8 ppm 2.23 (s, 3 H) 2.48 (m, 4 H) 2.90 (m, 4 H) 5.38 (bs, 4 H) 6.72 (dd, J2. 44,8. 42 Hz, 1 H) 6.82 (d, J2. 44, 1 H) 7.01 (d, J8. 42 Hz, 1 H).

16154-72-6, As the paragraph descriping shows that 16154-72-6 is playing an increasingly important role.

Reference：
Patent; PHARMACIA ITALIA S.P.A.; WO2004/104007; (2004); 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.

5747-48-8, A solution of PDBTZ (1 mmol) and alpha-acetoxyethyl 4-nitrophenyl carbonate (1 mmol) in hexamethylphosphoramide (1.3 rnL) is stirred at ambient temperature until complete by thin layer chromatography. The mixture is diluted with water (35 mL) and extracted with diethyl ether. The extract is washed (aqueous sodium hydroxide, water), dried (sodium sulfate), evaporated, and purified by flash chromatography to provide the title compound.

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; WO2008/79839; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,154590-35-9

Combine the product of Preparation 17, Step 3 (2.2 g, 6.7 mmol) and 2-chloroethyl isocyanate (0.64 ml, 7.4 mmol) in DMF (30 ml). Heat at 60 C. 18 h, allow to cool and partition with CH2Cl2 and water. Dry (MgSO4) and concentrate to obtain the crude urea as a yellow solid.

As the paragraph descriping shows that 154590-35-9 is playing an increasingly important role.

Reference：
Patent; Schering Corporation; US2005/239795; (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.278788-66-2,(R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Diisopropylethylamine (156 mL, 894 mmol) was added to a stirred, room temperature mixture of 3-(2-Bromo-acetyl)-6-fluoro-2-methyl- benzonitrile (176 g, 688 mmol) and (i?)-4-N-Boc-2-hydroxymethyl-piperazine (149 g, 688 mmol) in THF (3500 mL) and the mixture was stirred at room temperature for 18 h. The reaction was diluted with 3 L EtOAc, washed 2x with 1500 mL 10%> w/w NaHC03 aqueous solution, dried over MgS04, filtered and concentrated. The residue was purified by column chromatography on silica gel (40-80% EtOAc/Hexanes, linear gradient), to provide the title compound ., 278788-66-2

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

Reference：
Patent; MERCK SHARP & DOHME CORP.; PIO, Barbara; PASTERNAK, Alexander; SHAHRIPOUR, Aurash; TANG, Haifeng; WALSH, Shawn; WO2013/90271; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

502649-29-8, 1-Boc-3-Benzylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

502649-29-8, A solution of l-benzyl-2-methyl-lH-pyrrole-3-carboxylic acid (150 mg) , tert-butyl 3-benzylpiperazine-l-carboxylate(193 mg) , WSC-HCl (174 mg) , HOBt (139 mg) and DMF (10 ml) was stirred at room temperature for 12 hr. Then, the mixture was poured into a saturated aqueous sodium bicarbonate solution and extracted with ethyl acetate. The extract was washed successively with water and brine and dried over anhydrous sodium sulfate, and then the solvent was evaporated in vacuo. The residue was subjected to silica gel column chromatography, and the fraction eluted with ethyl acetate-hexane (1:9 to 1:3) was concentrated in vacuo to give an amorphous solid (140 mg) . 110 mg of the resulting amorphous was dissolved in dichloromethane (2 ml), and TFA (2 ml) was added thereto. After stirring at room temperature for 2 hr,. the mixture was poured into a saturated aqueous sodium bicarbonate solution (50 ml) and extracted with ethyl acetate. The extract was washed with brine and dried over anhydrous sodium sulfate, and then the solvent was evaporated in vacuo. The residue was subjected to silica gel column chromatography, and eluted with ethyl acetate-methanol (1:1). The target fraction was concentrated, and then the residue was dissolved in ethyl acetate. The mixture was acidified with a 4 N hydrogen chloride-ethyl acetate solution, and then concentrated in vacuo to give the desired product (45 mg) as an amorphous solid. MS (ESI+, m/e) 374 (M+l)

The synthetic route of 502649-29-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; WO2007/94513; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

132710-90-8, 1-Boc-4-(3-hydroxypropyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of tert-butyl 4-(3-hydroxypropyl)piperazine-l-carboxylate (7.0 g, 28.64 mmol) in THF (50 mL), was added triethylamine (8 mL, 57.29 mmol) at room temeperature. After 5 min, benzoyl chloride (3.66 mL, 31.51 mmol) was added dropwise at 0 C under inert atmoshphere. After addition, the resultant reaction mixture was stirred at room temperature for 1 h. After completion of reaction (monitored by TLC), the reaction was quenched with water (100 mL) and extracted with ethyl acetate (3 X 250 mL). The combined organic layer was dried over anhydrous sodium sulphate and concentrated – – under reduced pressure to afford 43 (7.8 g) as a off-white solid. *H NMR (400 MHz, CDC13): delta 8.06 – 8.00 (m, 2H), 7.59 – 7.52 (m, 1H), 7.48 – 7.40 (m, 2H), 4.38 (tj = 6.6 Hz, 2H), 3.50 – 3.39 (m, 4H), 2.53 (t, / = 7.3 Hz, 2H), 2.43 (br t, / = 4.9 Hz, 4H), 1.98 (quin, / = 6.8 Hz, 2H), 1.46 (s, 9H); LCMS (M+H) = m/z 349.7 [M+H+]; purity~83%., 132710-90-8

132710-90-8 1-Boc-4-(3-hydroxypropyl)piperazine 16217800, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; TOPADUR PHARMA AG; NAEF, Reto; TENOR, Hermann; (135 pag.)WO2017/85056; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

548762-66-9, (2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Half of the solid from the previous step was treated with N,N-diisopropylethylamine (0.5 mL, 3 mmol), DMSO (0.5 mL, 7 mmol) and (2S,5R)-2,5-dimethyl-piperazine-1-carboxylic acid tert-butyl ester (273 mg, 1.27 mmol) and the reaction mixture was heated at 120 C overnight, concentrated by rotary evaporation, dissolved in a small amount of DCM and purified by silica gel chromatography (0-50% ethyl acetate:hexanes) to produce the title intermediate (288 mg, 29 % yield) as a yellow solid. (m/z): [M+H]+ calcd for C24H27F4N4O4 591.09, 593.09 found 593.2.

548762-66-9, As the paragraph descriping shows that 548762-66-9 is playing an increasingly important role.

Reference：
Patent; Theravance Biopharma R&D IP, LLC; MCKINNELL, Robert Murray; LONG, Daniel D.; VAN ORDEN, Lori Jean; JIANG, Lan; LOO, Mandy; SAITO, Daisuke Roland; ZIPFEL, Sheila; STANGELAND, Eric L.; LEPACK, Kassandra; OGAWA, Gavin; HUANG, Xiaojun; ZHANG, Weijiang; EP2635571; (2015); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics