Heterocyclic Building Blocks-piperazine

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

Step B. 4-[4-(2-Ethyl-butyrylamino)-2-fluoro-phenvH-piperazine-1-carboxylic acid tert-butyl ester. 4-(4-Amino-2-fluoro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester(4.54 g, 15.4 mmol) and DIPEA (2.95 ml_, 16.9 mmol) were dissolved in DCM (90.0 ml.) and cooled to 00C. 2-Ethyl-butyryl chloride (2.28 ml_, 16.2 mmol) was added slowly. The resulting mixture was then stirred at 00C for 1 h and at room temperature for 4 h. The resulting mixture was then washed with water, 1 N NaOH solution and water. The organic phase was dried (Na2SO4), filtered and concentrated to yield a residue. Chromatography of the residue (SiO2, 0-8 % acetone/DCM) yielded the title compound.MS (ESI) mass calculated for C21H32FN3O3, 393.50, m/z measured, 394.6 [M+H]+ 1H NMR (CDCI3): 7.50 (dd, J = 13.9, 2.4, 1 H), 7.22 (s, 1 H), 7.15-7.07 (m,1 H), 6.88 (t, J = 9.0, 1 H), 3.63-3.52 (m, 4H), 3.00-2.92 (m, 4H), 2.06-1.93 (m, 1 H), 1.75-1.65 (m, 2H), 1.59-1.52 (m, 2H), 1.48 (s, 9H), 1.00-0.88 (m, 6H)., 154590-35-9

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

Reference：
Patent; JANSSEN PHARMACEUTICA N.V.; WO2009/79597; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

848482-93-9,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.848482-93-9,(S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

(S)-4-Boc-2-piperazinecarboxylic acid (530 mg, 2.17 mmol) was dissolved in MeOH (25 mL) and formaldehyde (1.76 mL, 37 wt % in water, 21.7 mmol) was added. The reaction mixture was stirred for 30 min, NaBH(OAc)3 (0.92 g, 4.34 mmol) was added and the reaction mixture was stirred for 2 h. The solvents were removed in vacuo and the residue was purified by reverse phase column chromatography. The residue and benzyl homopiperazine (0.41 g, 2.17 mmol) were dissolved in DMF (20 mL) and cooled to 0 C. DIPEA (0.59 g, 4.56 mmol) and HBTU (0.82 g, 2.17 mmol) were added and the reaction mixture was stirred for 3 h. The solvents were removed in vacuo and the residue was partitioned between DCM (100 mL) and water (50 mL). The organic fraction was washed with 1M aq Na2CO3 (25 mL), brine (25 mL), dried (MgSO4) and concentrated in vacuo. The residue was purified by reverse phase column chromatography to give the title compound (0.64 g, 71%) as a light yellow gum. LCMS (ES+): 417.4 [MH]+.

The synthetic route of 848482-93-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Proximagen Limited; Savory, Edward Daniel; Stewart, Allson; Cartey, Allison; Brown, Giles; Simpson, Iain; Oliver, Kathryn; Patient, Lee; Higginbottom, Michael; Cole, Andrew Graham; US2013/289020; (2013); A1;,
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

60% Sodium hydride (60 mg, 1.49 mmol) was added to a suspension of te/t-butyl (S)-3- (hydroxymethyl)piperazine-l-carboxylate (161 mg, 0.75 mmol) and 7-bromo-6-chloro-5-fluoro-2- morpholinoquinazolin-4(3/-/)-one (208 mg, 0.57 mmol) in THF (10 ml) at 0C under nitrogen and stirred for 5 minutes. The reaction mixture was allowed to warm to room temperature then stirred at 65C for 1 hour, allowed to cool, then quenched at 0C with acetic acid (0.1 ml). The reaction mixture was diluted with ethyl acetate (50 ml), washed with aqueous 2M potassium carbonate solution (10 ml) then dried (MgS04) and the solvent evaporated. The residue was purified by flash silica chromatography, elution gradient 0 to 10% 2N methanolic ammonia in DCM. Pure fractions were evaporated to dryness to afford te/t-butyl (S)-3-(((7-bromo-6-chloro-2-morpholino-4-oxo-3,4-dihydroquinazolin-5- yl)oxy)methyl)piperazine-l-carboxylate (215 mg, 67%) as a white foam, m/z: ES+ [M+H]+ 558 / 560., 314741-40-7

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

Reference：
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; BOYD, Scott; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; RAUBO, Piotr, Antoni; (144 pag.)WO2018/206539; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of [2-(4-methyl-naphthalen-1-yl)-3H-imidazol-4-yl]-methanol (50 mg, 0.21 mmol) in 1 ,2-dichloroethane (5 ml) at 0C is added thionylchloride (5 eq.). The resulting mixture is stirred at 50C for 1 hr. Solvent and remaining thionylchloride are evaporated, and the residue is dissolved in acetonitrile (3 ml), followed by the addition of substituted 4-cyclopentylpiperazine (1.0 eq.) and potassium carbonate (2.0 eq.). The resulting mixture is stirred at rt overnight. The reaction is diluted with EtOAc (10 ml), washed with brine, dried, and solvent is removed. The crude product is purified through PTLC to give l-cyclopentyl-4-[2-(4-methyl-naphthalen-1-yl)-3H-imidazol-4- ylmethyl]-piperazine. LCMS 375 (M+ +1).

21043-40-3, As the paragraph descriping shows that 21043-40-3 is playing an increasingly important role.

Reference：
Patent; NEUROGEN CORPORATION; WO2006/89076; (2006); 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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

Piperazine-2-one (1 g, 10 mmol) is added to ethyl acetate (40 mL),In the solution of 20 ml ,K2CO3 is added at the room temperature followed by Benzyloxycarbonyl chloride (2.1 mL, 15 mmol) is added dropwise to the reaction flask,and reaction is stirred at room temperature . The reaction stopped next day, and the organic layer is washed with 20 mL of X saturated NaCl solution, dried over anhydrous magnesium sulfate,Column chromatography (D: Mu = 75: 1) to obtain a white solid 1.48, 59.8%.yield.

5625-67-2, As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

Reference：
Patent; Chinese Academy Of Medical Sciences Pharmaceutical Institute; Xu Boling; Chen Xiaoguang; Zhou Jie; Ji Ming; Yao Haiping; Zhou Qin; (57 pag.)CN107098886; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8,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.

In 5 mL of acetonitrile was dissolved 500 mg (1.693 mmol) of 11-piperazin-l- yldibenzo[b,f][l,4]thiazepine. In 5 mL of acetonitrile was dissolved 197 mg fumaric acid (1.693 mmol) with heating. The solutions were combined resulting in precipitation. The solid redissolved upon heating and then crystallized more slowly upon cooling, generating a free- flowing solid. The mixture did not change overnight. The solids were collected, washed with acetonitrile (5 mL), and dried under vacuum at 400C resulting in 574 mg (82.3%) of crystalline solid, mp 159-163 0C (dec). 1H NMR (DMSOd6) was consistent with the title salt.Polarized light microscopy revealed the rod-shaped crystalline particles. DSC revealed one endotherm at 153.3 0C which appeared to be a melt event preceding eventual decomposition at higher temperatures (Figure 3). TGA revealed 1.4% weight loss in the water/solvent temperature region (Figure 3). DVS indicated that the salt was hygroscopic with isotherms characteristic of hydrate formation (Figure 4). The sorption isotherms of each cycle were different, indicating possible form change. The plateau of the first cycle (diamond) between 50 and 80% RH was about equal to 1 mole equivalent of water. The plateau in the same region of the second cycle (triangle) was equal to about 2.5 mole equivalents gained from the starting point of the second cycle at 0% RH. The observation that the second cycle started at a lower mass than the first cycle was probably due to incomplete drying of the sample prior to the cycling.

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

Reference：
Patent; ASTRAZENECA AB; WO2007/62336; (2007); A2;,
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

2,6-Difluoro-3-(oxiran-2-yl)benzonitrile (1.50 g, 8.28 mmol) and (5)-4-N-BOC-2-hydroxymethylpiperazine (2.40 g, 11.1 mmol) were suspended in ethanol (15 mL) then heated in a microwave apparatus for 30 min at 150 C. The reaction mixture was cooled and evaporated dryness. The residue was purified by chromatography through a 120g Redi-sep column eluting with 5%>MeOH/95%> EtOAc to yield the title compound LC-MS: M+l= 398., 314741-40-7

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

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

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.

General procedure: To a stirred solution of compound 5a-b (2 mmol) in dry DCM (10 mL) was added K2CO3 (1.1 equiv, 2.2 mmol, 304 mg). The mixture was cooled with a bath of ice/water, and then the appropriate N-substituted piperazine (2 equiv, 4 mmol), dissolved in DCM (2 mL), was added slowly over 30 min. The mixture was then stirred at room temperature for two hours, diluted with DCM (10 mL), washed with water (10 mL) and then with brine (10 mL). The organic layer was dried (Na2SO4), filtered and concentrated in vacuo to give a brown residue that was purified by column chromatography to furnish the derivatives 6a-aq.

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

Reference：
Article; Romagnoli, Romeo; Baraldi, Pier Giovanni; Carrion, Maria Dora; Cara, Carlota Lopez; Cruz-Lopez, Olga; Salvador, Maria Kimatrai; Preti, Delia; Tabrizi, Mojgan Aghazadeh; Shryock, John C.; Moorman, Allan R.; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Bioorganic and Medicinal Chemistry; vol. 20; 2; (2012); p. 996 – 1007;,
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.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

13484-40-7, A mixture of 1.0 g (6.9 mmol) of the compound from Example 7A and 1.1 g (7.6 mmol) 1-(2-methoxyethyl)piperazine in 10 ml water is stirred at 100 C. for 2 h. A further 0.9 g (6.2 mmol) 1-(2-methoxyethyl)piperazine is added and the reaction mixture is stirred further at 100 C. for 16 h. After concentration in vacuo, the residue is stirred in acetonitrile. The solid which has precipitated out is filtered off, washed first with ethanol and then with diethyl ether and dried in vacuo.Yield: 0.8 g (42% of th.)LC-MS (Method 8): Rt=0.22 min; MS (ESIpos): m/z=253 [M+H]+;1H-NMR (400 MHz, DMSO-d6): delta=7.93 (s, 1H), 7.64 (s, 1H), 5.91 (s, 1H), 4.14 (s, 2H), 3.50-3.40 (m, 6H), 3.24 (s, 3H), 2.47-2.39 (m, 4H).

13484-40-7 1-(2-Methoxyethyl)piperazine 2734638, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BAYER SCHERING PHARMA AKTIENGESELLSCHAFT; US2010/305085; (2010); A1;,
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

57260-71-6, (q) tert-butyl4-(2-bromoacetyl)piperazine-1-carboxylate (6q) Under inert atmosphere and at -78C, bromoacetylbromide (53.7 mmol, 1 eq.) was slowly added to a solution of Boc-piperazine(53.7 mmol, 1 eq.) and TEA (59.1 mmol, 1.1 eq.) in DCM (150 ml). The reactionmixture was stirred at -78C for 3h, diluted with DCM (75 ml) and washed withwater. The recovered organic layer was dried over magnesium sulfate and thesolvent was evaporated under vacuum. The obtained crude product was furthertriturated with diethyl ether, filtered and dried under vacuum to conduct tothe desired acetylated compound. CnHi 9BrN 20 3; yield 78%; white solid; m.p.243-244 C; M = 307.18 g/mol; IR (KBr): v = 2965 (m), 1689 (s), 1632 (s), 1417(s), 1246 (s), 1167 (s), 1023 (m); cm – ; NMR (250 MHz, CDCI 3) delta 3.87 (s, 2H), 3.61-3.57 (m, 2H), 3.55-3.47 (m,4H), 3.46- 3.41 (m, 2H), 1.46 (s, 9H); C NMR (63 MHz, CDCI 3) delta 165.5 (C q), 154.5 (C q), 80.5 (C q), 46.6 (2CH2), 40.9 (2CH 2), 28.4 (3CH 3), 25.7 (CH 2);

As the paragraph descriping shows that 57260-71-6 is playing an increasingly important role.

Reference：
Patent; ASTON UNIVERSITY; GRIFFIN, Martin; RATHBONE, Daniel; BADARAU, Leonas Eduard; WO2014/57266; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics