Tag: M.W:100-200

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.

Reference Example 46] 1-Methylpiperazin-2-one [Show Image] An aqueous 1 N sodium hydroxide solution was added to a suspension of 1-methylpiperazin-2-one hydrochloride (19.6 g) of Reference Example 21-(3) in dichloromethane, and the resultant mixture was partitioned. Further, sodium chloride was added to the aqueous layer to saturate the layer, and then the aqueous layer was extracted with dichloromethane. The organic layers were combined and dried over anhydrous sodium sulfate. After separation by filtration, the solvent was evaporated under reduced pressure, and the title compound (5.90 g) was obtained as an oily product. ESI-MSm/z: 115(M+H)+., 109384-27-2

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

Reference：
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1785418; (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.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

tert-Butyl 4-(4-formylphenyl)piperazinecarboxylate (Compound 28) 1-(t-Butoxycarbonyl)piperazine (1.86 g, 10 mmol), p-fluorobenzaldehyde 27 (1.24 g, 10 mmol), and K2CO3 (1.74 g, 11 mmol) in dry pyridine (10 mL) are stirred at reflux under a nitrogen atmosphere for 24 h. Most of the solvent is removed under vacuum and the residue is partitioned between EtOAc (150 mL) and water (100 mL). The aqueous layer is washed with EtOAc (2*50 mL) and the combined organic layers are sequentially washed with 3% aq. citric acid (2*100 mL), water (100 mL), brine (100 mL), and dried (MgSO4). The solvent is removed under vacuum and the residue washed with hexanes and dried under vacuum. The product can be used as such, or further purified by silica gel column chromatography (dichloromethane-MeOH gradient)., 57260-71-6

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Gordeev, Mikhail F.; Patel, Dinesh V.; Barbachyn, Michael R.; Gage, James R.; US2003/13737; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5625-67-2, General procedure: To a solution of 3-aminopyrrolidine-1-carboxylate (744 mg, 4 mmol) in DCM (10 mL) , DIEA(1.04 mL, 6 mmol) and benzyl chloroformate (0.72 mL, 5 mmol) were added at 0. The reactionmixture was stirred at room temperature until TLC monitoring showed that the reaction wascomplete. The mixture was diluted with DCM and washed with water and brine. The organic layerwas dried over anhydrous MgSO4andevaporated, and column chromatography (petroleum ether /ethyl acetate =8:1 to 5:1) to give the corresponding product I-4 as light yellow oil (1.05 g, 82%).

5625-67-2 Piperazin-2-one 231360, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Zhou, Jie; Ji, Ming; Zhu, Zhixiang; Cao, Ran; Chen, Xiaoguang; Xu, Bailing; European Journal of Medicinal Chemistry; vol. 132; (2017); p. 26 – 41;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 28: Piperazine-1-carboxylic acid amide hydrochloride; [] 4-Piperazine-1-carboxylic acid tert-butyl ester (1.0g, 5.4mmol), acetic acid (3ml) and water (5ml) were mixed together. Potassium cyanate (2.25g, 27.7mmol) was added portionwise as a solution in water (5ml) and stirred for 4 hours, during which time a solid precipitated. The solid was filtered, re-dissolved in DCM (20ml), dried over MgSO4, filtered, the filter cake washed with DCM (5vol) and concentrated in vacuo to give a white solid (0.38g). The white solid (0.38g) was dissolved in methanol (3.8ml) and 1,4-dioxane (0.7ml), 4M HCl in 1,4-dioxane (2.5ml, 10mmol) was added to the reaction and stirred overnight. The reaction was concentrated in vacuo to give the title compound (0.28g, 31% over 2 steps) as a white solid.1H NMR (400MHz, DMSO-d6) delta9.18 (br s, 2H), 3.91 (br s, 2H), 3.45 (br s, 4H), 2.93 (br s, 4H)., 57260-71-6

The synthetic route of 57260-71-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Warner-Lambert Company LLC; EP1593679; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 2 [3-(1-Benzyl-piperidin-2-yl)-1H-indol-6-yl]-(4-isopropyl-piperazin-1-yl)-methanone A mixture of 1.25 g (4 mmol) 3-(1-benzyl-piperidin-2-yl)-1H-indole-6-carboxylic acid methyl ester and 0.2 g (4.8 mmol) LiOH.H2O in 40 mL water and 40 mL methanol was heated to reflux for 20 h. After 4 h additional 0.56 g LiOH.H2O and 30 mL water was added. After evaporation of the methanol the mixture was adjusted to pH=2 and evaporated to dryness. 25 mL DMF was added and together with 1.4 g (4 mmol) TBTU, 2.8 g (22 mmol) DIPEA and 0.55 g (4 mmol) 1-(2-propyl)-piperazine stirred at room temperature for 3 h. Isolute was added and after evaporation purified by column chromatography on silica eluding with a gradient formed from DCM/methanol/NH3 aq. The product fractions were evaporated to yield 1.14 g (71percent) of the title compound as light brown solid. MS (m/e): 445.3 (MH+)., 4318-42-7

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Nettekoven, Matthias; Roche, Olivier; US2008/32976; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5308-25-8, To a solution of 1-ethylpiperazine (1 g, 8.771 mmol, 1.0 eq) in DMF were added K2CO3 (3 g, 21.927 mmol, 2.5 eq.) and ethyl 2-bromoacetate (2.19 g, 13.156 mmol, 1.5 eq.). The mixture was stirred at RT for 16 h. The mixture was quenched and extracted as in Intermediate Example 5(a). The solvent was distilled off to afford the product in 76.4% yield (1.3 g).

The synthetic route of 5308-25-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Linnanen, Tero; Wohlfahrt, Gerd; Nanduri, Srinivas; Ujjinamatada, Ravi; Rajagopalan, Srinivasan; Mukherjee, Subhendu; US2015/11548; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

68104-63-2, 4-(Piperazin-1-yl)benzonitrile is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

68104-63-2, To a solution of 6.1 mmol 2-iodo-5-methanesulfonyl-benzoic acid in 20 ml dimethyl formamide were added successively 6.75 mmol TBTU, 43 mmol N-ethyldiisopropylamine and 6.75 mmol 4-piperazin-1-yl-benzonitrile (commercially available, e.g. from Fluka). The reaction mixture was stirred at 20 C. for 1.5 h and then concentrated in vacuo. Addition of 200 ml water followed by filtration yielded the crude product which was recrystallized from methanol to afford the title compound as a white solid (yield 87%). MS (m/e): 495.9 (M+H+, 100%).

The synthetic route of 68104-63-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Jolidon, Synese; Narquizian, Robert; Norcross, Roger David; Pinard, Emmanuel; US2006/149062; (2006); 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.5317-33-9,3-(4-Methylpiperazin-1-yl)propan-1-ol,as a common compound, the synthetic route is as follows.

5317-33-9, Di- tert-butyl azodicarboxylate (0.478 g, 2.08 mmol) was added portionwise to a mixture of 4-chloro-7-hydroxy-6-methoxyquinazoline (0.350 g, 1.66 mmol), 3-(4-methyl-piperazin-1-yl)-propan-1-ol (Intermediate 7, 0.276 g, 1.74mmol), and triphenylphosphine (0.544 g, 2.08 mmol) in dichloromethane (20 mL) at r.t.. If necessary, further alcoholwas added. After stirring for 2 h, the solution was concentrated to 10 mL, mounted on silica and chromatographed(gradient, dichloromethane to dichloromethane : methanol = 3:2 within 1 h) to obtain 4-chloro-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazoline (brownish solid, 0.431 g, 1.23 mmol, 74 %). LC/ESI-MS: m/ z = 351 [M(35Cl) +H]+;Rt = 1.88 min. Cf. also WO 04/043472, page 32.

5317-33-9 3-(4-Methylpiperazin-1-yl)propan-1-ol 79208, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; 4SC AG; EP1674467; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

52385-79-2, 2-(3-Chlorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

52385-79-2, 218A (65 mg, 0.075 mmol), 2-(3-chlorophenyl)piperazine (29 mg, 0.15 mmol), BINAP (9 mg, 0.02 mmol), NaOtBu (36 mg, 0.37 mmol) andtris(dibenzylideneacetone)dipalladium(0) (6.9 mg, 7.5 imol) were charged to a vial, which was then evacuated and back-filled with argon (3x). Degassed toluene (0.25 mL) was added. The reaction mixture was stirred at 100 C overnight, then filtered through CELITE, and the solids rinsed with EtOAc. The filtrate was evaporated, and productpurified by flash chromatography to provide a mixture of 218B (22 mg, 30%), MS(ESI) m/z 984.2 (M+H). 7-(( 1 -(3 -(3 -Phenylpiperazin- 1 -yl)benzyl)- 1H-pyrazol-4-yl)methyl)- ditrityl-3H- [1 ,2,3jtriazolo [4,5 -bj pyridin-5 -amine was also obtained.

52385-79-2 2-(3-Chlorophenyl)piperazine 5225638, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BRISTOL-MYERS SQUIBB COMPANY; SMALLHEER, Joanne, M.; SHAW, Scott, A.; HALPERN, Oz, Scott; HU, Carol, Hui; KICK, Ellen, K.; (311 pag.)WO2017/40449; (2017); 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.55112-42-0,4-Methyl-1-piperazinecarbonyl Chloride Hydrochloride,as a common compound, the synthetic route is as follows.,55112-42-0

Other examples are summarized in the following table:

As the paragraph descriping shows that 55112-42-0 is playing an increasingly important role.

Reference：
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2008/2629; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics