Month: June 2021

4318-42-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

[18041 Step 1: Synthesis of methyl4-(((3R.55?)-4-(3-((4-isopropylpiperazin- 1 -yflmethyflbenzyfl-3.5-dimethylpiperazin- 1- yl?)methyflbenzoate[18051 Methyl 4-(((3R,55)-4-(3-formylbenzyl)-3 ,5-dimethylpiperazin- 1 -yl)methyl)benzoate (formula 5-1, 0.200 g, 0.526 mmol) and 1-isopropylpiperazine (0.113 mL, 0.788 mmol) were dissolved in methylene chloride (4 mL), and the solution was stirred at room temperature for 1 hour. Na(OAc)3BH (0.223 g, 1.051 mmol) was added to the solution, followed by stirring at the same temperature for 17 hours. Then, a saturated aqueous solution of sodium hydrogen carbonate was added to the reaction mixture, followed by extraction with methylene chloride. The extract was filtered through a plastic filter to remove solid residue and an aqueous layer, and then concentrated under reduced pressure. The concentrate was purified by column chromatography (silicon dioxide, 4 g cartridge; methanol/methylene chloride = from 0 percent to 10 percent) and concentrated to afford the desired compound (0.225 g, 86.9 percent) as a pale brown oil.

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference：
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; SONG, Hyeseung; LEE, Changgon; KWAK, Dalyong; LEE, Jaeyoung; BAE, Suyeal; KIM, Yuntae; BAE, Daekwon; HA, Nina; BAE, Miseon; KIM, Jihyun; WO2015/137750; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of carboxylic acid 6 (3.5 mol), EDC*HCl (5.4 mol), HOBt (5.4 mol) in anhydrous DMF (20 mL) was stirred at RT. Substituted piperazine (3.5 mol) was then added and the mixture was further stirred at RT for 10-12 hr40. After completion of the reaction as indicated by TLC, the reaction mixture was quenched in crushed ice. The precipitated solid was washed with NaHCO3 and dil. HCl. The product thus obtained was purified by silica gel column chromatography using hexane: ethyl acetate as eluent., 30459-17-7

The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Raundal, Hemant N.; Jadhav, Rahul P.; Patil, Amar A.; Bobade, Vivek D.; Indian Journal of Chemistry – Section B Organic and Medicinal Chemistry; vol. 54B; 8; (2015); p. 979 – 987;,
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.1152367-80-0,(S)-1,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Part A 2-[(2S)-2,4-Dimethyl-1-piperazinyl]-4-pyrimidinamine A mixture of 2-chloro-4-pyrimidinamine (200 mg, 1.544 mmol), Hunig’s base (1348 mul, 7.72 mmol) and (3S)-1,3-dimethylpiperazine (Ref.: WO2009061879 (A1)) (318 mg, 1.698 mmol) in N,N-dimethylformamide (DMF) (1.7 ml) was heated to 220 C. via a microwave reactor for 15 min. The reaction mixture was purified by RP-HPLC to yield 2-[(2S)-2,4-dimethyl-1-piperazinyl]-4-pyrimidinamine (88 mg, 0.425 mmol, 28% yield). MS (ES+) m/z 208.0 (MH+).

1152367-80-0, 1152367-80-0 (S)-1,3-Dimethylpiperazine 13152036, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; GlaxoSmithKline Intellectual Property (No. 2) Limited; Aubart, Kelly M.; Benowitz, Andrew B.; Fang, Yuhong; Hoffman, James; Karpinski, Joseph M.; Knox, Andrew Nicholson; Liao, Xiangmin; Qin, Donghui; Shi, Dongchuan; Spletstoser, Jared T.; US8901119; (2014); B2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

55112-42-0, 4-Methyl-1-piperazinecarbonyl Chloride Hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,55112-42-0

Other examples are summarized in the following table:

The synthetic route of 55112-42-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2008/2629; (2008); 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.303-26-4,1-((4-Chlorophenyl)(phenyl)methyl)piperazine,as a common compound, the synthetic route is as follows.

A vessel is charged with 250 ml of tetrahydrofurane, 25 ml of methanol and 5.0 ml (60 mmol) concentrated hydrochloric acid (37% by weight). The mixture is cooled to the temperature of 15 0C and under intense stirring, 5.5 g ( 84 mmol) pulverized zinc are added. Subsequently at a temperature between 5 tolO 0C, 12.5 g (25.1 mmol) (R)-(+)-4- (4-chloropheny l)-phenylmethyl-piperazine- 1 -carboxylic acid 2,2,2-trichloroethylester hydrochloride (compound of the Example 6) are added in several portions. The suspension is stirred for one hour at room temperature. At the end of the reaction, the unreacted zinc is filtered off, the filtrate is mixed with 150 ml of water and 150 ml of ethylacetate, the organic layer is separated, washed with aqueous 5 % by weight sodium hydrogen carbonate solution, dried and the solvent is evaporated. The residue is dissolved in 100 ml of ethylacetate and is added dropwise with stirring to 80 ml of 10 g/100 ml hydrochloric acid solution prepared in ethylacetate. The suspension containing the crystalline salt, which starts precipitating almost instantly after the addition, is cooled, the product is filtered off, washed with diethylether and dried.Yield: 7.7 g (85.4 %) white crystals Melting temperature, 198-202 0C.Elemental Analysis {calculated on the basis of the Formula C17H19C1N2.2HC1 (359.7)}:Calculated:C: 56 .76 H: 5 .88 Cl: 29.57 N: 7.79Measured: C: 56. ,45 H: 5 .74 Cl: 29.25 N: 7.61Optical purity (chiral high performance liquid chromatography): 98.7, 303-26-4

As the paragraph descriping shows that 303-26-4 is playing an increasingly important role.

Reference：
Patent; EGIS GYOGYSZERGYAR NYRT.; WO2007/66163; (2007); 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.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

In a sealed tube, 7-fluoro-2-(2-methylimidazo[1,2-b]pyridazin-6-yl)-4H-pyrido[1,2-a]pyrimidin-4-one (Intermediate 1; 50 mg, 0.169 mmol), and (S)-2-methylpiperazine (68 mg, 0.677 mmol, 4.0 eq.) were stirred in DMSO (2 mL) at 110 C. overnight. The solvent was removed under high vacuum. The residue was taken up in CH2Cl2 and washed with an aqueous saturated solution of NaHCO3. The organic layer was separated and dried over Na2SO4 and concentrated in vacuo. The crude was purified by column chromatography (SiO2, CH2Cl2/MeOH=95/5 to 90/10) to afford the title product (40 mg, 63%) as a light yellow solid. MS m/z 376.2 [M+H+]., 74879-18-8

As the paragraph descriping shows that 74879-18-8 is playing an increasingly important role.

Reference：
Patent; Hoffmann-La Roche Inc.; PTC Therapeutics, Inc.; Ratni, Hasane; Green, Luke; Weetall, Maria L.; Naryshkin, Nikolai A.; (33 pag.)US2019/315773; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

118753-66-5, tert-Butyl 4-aminopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[00229] Step-3: Synthesis tert-butyl 4-((6-bromo-7-fluoro-3-nitroquinolin-4- yl)amino) piperazine- 1 -carboxylate, 4: [00230] DIPEA (26.72mL, 0.15712mo1) was added to a stirred solution of 6- Bromo-4-chloro-7-fluoro-3-nitroquinoline, 9 (24g, 0.07856mo1) and tert-butyl 4-aminopiperazine-1-carboxylate (18.97g, 0.09427mo1) in DMF, 200mL at 0 00. The reaction mixture was allowed to room temperature and stirred for 2h. Reaction was monitored by TLC (30%EtOAc in hexane), after completion of reaction, diluted with water (l5OmL), the precipitated yellow solid was filtered-off, washed with water and dried under vacuum. The crude material was purified by column chromatography by using5i02 (15% EtOAc in Hexane) to afford of tert-butyl4-((6-bromo-7-fluoro-3-nitroquinolin-4- yl) amino) piperazine-1-carboxylate, 4 (30g, 81%). 1H NMR (300MHz, CDCI3): O 10.42 (5, 1H), 10.22-10.19 (d, 1H), 9.36 (5, 1H), 7.67-7.64 (d, 1H), 4.35-4.25 (t, 2H), 3.46-3.08 (t, 4H), 2.84-2.65 (t, 2H), 1.50 (5, 9H); LCMS: mlz= 469.9 (M+1) and 471.9 (M+2).

118753-66-5, As the paragraph descriping shows that 118753-66-5 is playing an increasingly important role.

Reference：
Patent; NOVARTIS AG; BOCK, Mark Gary; MOEBITZ, Henrik; PANIGRAHI, Sunil Kumar; PODDUTOORI, Ramulu; SAMAJDAR, Susanta; WO2015/22663; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

196811-66-2, tert-Butyl 4-carbamothioylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2-chloro-l-(4,5-dihydro-5-phenyl-3-isoxazolyl)ethanone (i.e. the product of Example 7, Step C) (0.450 g, 2.018 mmol) and 1,1-dimethylethyl 4-(amino- thioxomethyl)-l-piperazinecarboxylate (i.e. the product of Example 7, Step A) (0.5 g, 2.04 mmol) in ethanol (10 mL) was added triethylamine (0.204 g, 2.013 mmol), and the reaction mixture was stirred at room temperature for 12 h. The reaction mixture was concentrated 01464783 under reduced pressure, and the residue was partitioned between, ethyl acetate (30 mL) and water (30 mL). The organic layer was separated and washed with brine (25 mL), dried (Na2SO4), and. concentrated under reduced pressure. The crude residue was purified by column chromatography using 20 % ethyl acetate in petroleum ether as eluant to give 700 mg of the title compound as a white solid.1H NMR (CDCl3) delta 1.48 (s, 9H), 3.30 (m. IH), 3.54 (m, 8H)5 3.74 (m, IH)5 5.71 (m, IH)3 6.91 (s, IH), 7.40-7.29 (m, 5H).

196811-66-2, As the paragraph descriping shows that 196811-66-2 is playing an increasingly important role.

Reference：
Patent; E. I. DU PONT DE NEMOURS AND COMPANY; WO2008/13622; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

196811-66-2, tert-Butyl 4-carbamothioylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

196811-66-2, l-[5-methyl-4-(trifluoromethyl)-l,3-thiazol-2-yl]piperazine hydrochloride To a mixture of tert-butyl 4-(aminocarbonothioyl)piperazine-l-carboxylate (200 mg, 0.82 mmol) and 3-bromo-l,l,l-trifluorobutan-2-one (204 mg, 0.99 mmol) in xylene (20 mL) was added triethylamine (454 mul, 3.26 mmol). The reaction mixture was refluxed (140 0C) for 16 hours and concentrated in vacuo. Purification by column chromatography eluting with isohexane to 25% ethyl acetate / isohexane gave a cream solid (210 mg). This was stirred in methanol reagent 10 (15 mL) at room temperature for 16 hours. Reaction mixture was concentrated to dryness to give a pale yellow solid (230 mg) which was used crude directly in the next step (230 mg, > 100 % yield) MS (-ve ESI) : 252 (M-H)+

The synthetic route of 196811-66-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2009/1127; (2008); 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.196811-66-2,tert-Butyl 4-carbamothioylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of tert-butyl 4-carbamothioylpiperazine-1-carboxylate (0.5 g, 2.08 mmol) in dioxane (10 mL), triethyl amine (0.22 mL, 2.6 mmol) and 2-bromo-1-phenylethan-1-one (0.52 g, 2.6 mmol) were added at rt. The resulting mixture was stirred at 90 C for 20 h. The completion of the reaction was monitored by TLC. It was diluted with water and extracted with EtOAc. The organic layer was separated, dried over anhydrous Na2SO4, concentrated under vacuum. The resulting crude product was taken as such for the next step. Yield: 86% (0.5 g, colorless liquid)., 196811-66-2

The synthetic route of 196811-66-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASCENEURON SA; QUATTROPANI, Anna; KULKARNI, Santosh S.; GIRI, Awadut Gajendra; (243 pag.)WO2016/30443; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics