Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

The preparation method of 4-hydroxyethylpiperazine ethanesulfonic acid includes the following steps: 1) Mix 260g (2mol) 2-hydroxyethylpiperazine, 165g (0.94mol) sodium 2-chloroethylsulfonate with 120mL water, stir well, the reaction solution becomes clear, the pH is about 10,Heat up to 85 , stop heating until the system self-heats to 103-105 ,The reaction is heated to reflux for 30min, the reaction is over, and the pH is about 8;2) Cool the reaction liquid to 60 C, add triethylamine to the reaction liquid to adjust the pH to 7-8, 1.5 L of absolute ethanol and 8 g of activated carbon, boil for 30 min, and filter while hot;3) Adjust the pH of the filtrate to 5 using glacial acetic acid, stir the filtrate and cool to 5 C to crystallize overnight,Filter and dry to obtain 310g of crude product, which is 95% by drying after titration inspection; 4) Dissolve the sample obtained in step 3) in 750 mL of ethanol and heat to reflux, Add 145mL of water, stir to dissolve, filter while hot, and the filtrate is cooled to 5 overnight, Filtration gave 181g of 4-hydroxyethylpiperazineethanesulfonic acid crystals, After drying, 175g of 4-hydroxyethylpiperazineethanesulfonic acid was obtained, and the content was 99.8% after titration; 5) Concentrate the mother liquor under reduced pressure to a volume of 30-40%, add activated carbon to boil for decolorization, filter while hot, the filtrate is cooled to 0-5 C, filtered, dried and recovered to obtain 15g of 4-hydroxyethylpiperazineethanesulfonic acid After titration, the content was 99.6%, and the total yield was 84.7%., 103-76-4

As the paragraph descriping shows that 103-76-4 is playing an increasingly important role.

Reference£º
Patent; Suzhou Yake Technology Co., Ltd.; Yuan Yongkun; (10 pag.)CN110683995; (2020); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129779-30-2,(3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A stirred solution of (3S,5R)-tert-butyl 3,5- dimethylpiperazine-1 -carboxylate (20 g, 93.0 mmol, 1 eq) in LiHMDS (200 mL) was cooled to 0C and 2,6-difluoropyridine (26.8 mL, 280.3 mmol, 3 eq), and xanthophos (3.24 g, 5 mmol, 0.06 eq) were added followed by Pd2(dba)3 (2.5 g, 2.7 mmol, 0.03 eq). Then, the resultant reaction mixture was stirred overnight at 80C. The reaction was monitored with TLC, and TLC indicated formation of a non-polar spot. The reaction mixture was quenched with ice water (100 mL), filtered through celite and washed with ethyl acetate. The layers were separated, and the aqueous layer extracted with ethyl acetate (2×150 mL) and washed with brine solution (1×100 mL). The combined organic layer was dried over Na2S04, and concentrated under reduced pressure to give crude product. The crude product was purified by column chromatography (silica gel, 100-200 mesh) using 0-5% ethyl acetate in petroleum ether as an eluent to afford (3R,5S)-tert-butyl 4-(6-fluoropyridin-2-yl)-3,5-dimethylpiperazine-1 -carboxylate (20 g, 37.73% yield) as a brown liquid. LCMS: m/z 310.54 (M+H).

129779-30-2, The synthetic route of 129779-30-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ONTARIO INSTITUTE FOR CANCER RESEARCH (OICR); AL-AWAR, Rima; ISAAC, Methvin; CHAU, Anh My; MAMAI, Ahmed; WATSON, Iain; PODA, Gennady; SUBRAMANIAN, Pandiaraju; WILSON, Brian; UEHLING, David; (191 pag.)WO2019/119145; (2019); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

A mixture of Example 18B (0.179 g, 1.0 mmol), l-methylpiperazin-2-one, hydrochloric acid (0.301 g, 2 mmol), and triethylamine (0.405 g. 4.0 mmol) in ethanol (10 mL) was heated under reflux for 16 hours. The solvent was removed, and the residue was purified by flash column chromatography on silica gel eluting with 1-5 % methanol in ethyl acetate to afford 0.21 g (82%) of the title compound.

109384-27-2, 109384-27-2 1-Methylpiperazin-2-one hydrochloride 17060766, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ABBOTT LABORATORIES; ABBOTT LABORATORIES TRADING (SHANGHAI)COMPANY, LTD.; HUBBARD, Robert Dale; MCDANIEL, Keith F.; PARK, Chang Hoon; PRATT, John K.; SOLTWEDEL, Todd; SUN, Chaohong; WANG, Le; WENDT, Michael D; WO2013/185284; (2013); A1;,
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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, -CH-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

54699-92-2 4-Methyl-1-piperazineacetic acid 2762732, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Applera Corporation.; US2005/148773; (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.115761-79-0,1-(2,4-Difluorophenyl)piperazine,as a common compound, the synthetic route is as follows.

1.0 g of 1-(2,4-fluorophenyl)-piperazine (Compound A-1c), 15 mL of acetic acid was added to the sealed reactor, followed by the addition of 3 mL of hydrated formaldehyde, 1.0 g of sodium acetate;The reaction mixture was warmed to 60 C and stirred for 18 hours;The residue obtained was purified to give 1-(2,4-fluorophenyl)-4-methylpiperazine (A-c) (0.92 g, yield 86%)., 115761-79-0

As the paragraph descriping shows that 115761-79-0 is playing an increasingly important role.

Reference£º
Patent; Chengdu Ruizhi Chemical Co., Ltd.; Zhou Zhen; Zhu Mingkui; Li Kun; (9 pag.)CN109897014; (2019); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.208167-83-3,tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

General procedure: A mixture of compound 9 (200mg, 0.8mmol), sodium iodine (289mg, 1.93mmol) and substituted amines (1.61mmol) in methanol (30mL) was stirred at 40C for 5h. After the reaction was completed (monitored by TLC), the solution was concentrated under vacuum. Then the crude residue was purified by column chromatography (dichloromethane/methanol), affording pure product 10.

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

Reference£º
Article; Liang, Yu-Kun; Yue, Zhi-Zhou; Li, Jia-Xin; Tan, Cun; Miao, Ze-Hong; Tan, Wen-Fu; Yang, Chun-Hao; European Journal of Medicinal Chemistry; vol. 84; (2014); p. 505 – 515;,
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169447-86-3, (S)-tert-Butyl 2-benzylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 5 – Hybrid Analogs of Ureas and Carbamates; The synthesis of compounds of this embodiment is shown in FIGs. 14A through 14D. In this embodiment, the isoquinolinyl areas and carbamates were synthesized stepwise with a trichloroacetyl chloride., 169447-86-3

The synthetic route of 169447-86-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; UNIVERSITY OF SOUTH FLORIDA; YALE UNIVERSITY; WO2008/79945; (2008); A2;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

To n-butanol (2 mL) was added compound 4A-3 (30 mg, 0.135 mmol) and compound 5A-2 (47 mg, 0.135 mmol), and then p-toluenesulfonic acid (23.3 mg, 0.135mmol) was added under stirring. The mixture was heated to 100C and stirred for 5 hours. After TLC indicated the reaction was completed, the reaction mixture was concentrated under reduced pressure to give a crude product, which was further purified and isolated by column chromatography to obtain an off-white solid proudct, compound I-5 (59 mg, yield 81.8%). 1H NMR (400 MHz, cd3od) delta 9.09 (d, J=8.2 Hz, 1H), 8.33 (dd, J=4.3, 1.2 Hz, 1H), 8.09 (s, 1H), 7.54 (d, J=8.7 Hz, 1H), 7.48 (dd, J=8.7, 4.3 Hz, 1H), 6.67 (d, J=2.2 Hz, 1H), 6.54 (dd, J=8.7, 2.4 Hz, 1H), 3.89-3.73 (m, 4H), 3.27 (dd, J=9.3, 4.9 Hz, 4H), 2.89-2.73 (m, 4H), 2.49 (s, 3H), 1.30 (d, J=6.9 Hz, 6H). LCMS: t=0.662 min, 532.3 (M), 534.3 (M+1)., 122833-04-9

As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference£º
Patent; Humanwell Healthcare (Group) Co., Ltd.; WANG, Xuehai; XU, Yong; SHENG, Xijun; ZHANG, Xiaolin; XIA, Hangui; YANG, Zhongwen; YUE, Yang; HUANG, Lu; XIAO, Qiang; (80 pag.)EP3372594; (2018); A1;,
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438049-35-5,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.438049-35-5,N-Boc-3-Ethylpiperazine,as a common compound, the synthetic route is as follows.

Anhydrous DMF solution N’N- carbonyl diimidazole (468mg, 2.80mmol) of (2mL) was added dropwisetriethylamine (0.59mL, 4.20 mmol) and N- tert-butoxycarbonyl-3-ethylpiperazine (500mg, 2.33mmol) inanhydrous DMF (2mL) solution at room temperature in a sealed tube 30min, adding anhydrous methanol(12mL), 60 C the reaction 24h, the solvent was removed, a saturated sodium chloride solution (30 mL), ethyl acetate (15mL ¡Á 2) and the combined organic phases, Na 2 SO 4 dried over anhydrous solvent removedconcentrate was subjected to column chromatography (eluent: Petroleum ether / EtOAc (v / v) = 5/1), to give260mg of colorless liquid: 4-tert-butoxycarbonyl-2-ethyl-piperazine-1-carboxylate, yield: 40%.

As the paragraph descriping shows that 438049-35-5 is playing an increasingly important role.

Reference£º
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); 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

(S)-l-Allyl 4-tert-butyl 2- (hydroxymethyl) piperazine-1 , 4- dicarboxylate (22) was prepared from amino alcoholhydrochloride 21’HCl, applying allyl chloroformate in CH2CI2 in the presence of aqueous NaHCO3 solution; as leading references cf. T. W. Greene, P. G. M. Wuts, Protective Groups in Organic Synthesis, 3rd edition, John Wiley & Sons, 1999;P.J. Kocienski, Protecting Groups, 3rd edition, Georg Thieme Verlag, 2005.Data of 22: Ci4H24N2O5 (300.4): LC-MS (method 9a): Rt = 1.70, 201 ([M+H]+). 1H-NMR (DMSO-d6): 5.90 (m, 1 H), 5.29 (qd, J = 1.7,17.3, 1 H), 5.18 (qd, J = 1.5, 10.5, 1 H), 4.81 (t, J = 4.9, 1 H), 4.53 (d-like m, J ca . 5.1, 2 H), 4.04-3.75 (br. m, 4 H), 3.39 (m, 2 H), 2.95-2.70 (br. m, 3 H), 1.40 (s, 9 H).

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

Reference£º
Patent; POLYPHOR AG; OBRECHT, Daniel; ERMERT, Philipp; OUMOUCH, Said; LACH, Franck; LUTHER, Anatol; MARX, Karsten; MOeHLE, Kerstin; WO2011/15241; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics