Simple exploration of 129799-15-1

129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (2-isopropylphenyl)[2-nitro-4-E-(carboxyethenyl)phenyl]sulfide (prepared according to the procedures of Example 32), the amine from Example 71A (1.0 eq), 2-(1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium tetrafluoroborate (1.0 eq), and diisopropylethylamine (2.0 eq) in DMF was stirred at ambient temperature for 4 hr.ethyl acetate was added, and the mixture was washed sequentially with 1N HCl, aq. NaHCO3, and brine.The resultant yellow solid was treated with 1:1 TFA/dichloromethane at ambient temperature to give the title compound as a yellow solid. 1HNMR (DMSO-d6, 300 MHz) delta 1.15 (d, J=6.6 Hz, 6H); 2.52-3.16 (br m, 4H); 3.25-3.47 (m, 1H); 3.60-3.65 (br d, 3H); 3.60, 3.66 (br s, br s, 3H); 6.61-6.67 (br m, 1H); 7.30-7.62 (m, 6H); 7.88-7.93 (br m, 1H); 8.58-8.65 (br m, 1H). MS (APCI) (M+H)+ at m/z 470.Anal calcd for C24H27N3S1O5: C, 61.39; H, 5.80; N, 8.95. Found: C, 61.51; H, 5.87; N, 8.68., 129799-15-1

129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Abbott Laboratories; US2004/116518; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about 129799-15-1

129799-15-1, As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

1-tert-butyl 2-methyl 4-(6-Bromo-7-chloro-2-methylquinazolin-4-yl)piperazine- 1,2-dicarboxylate To a solution of 6-bromo-4,7-dichloro-2-methylquinazoline (435 mg, 1.49 mmol) and 1-tert-butyl 2-methyl piperazine-1,2-dicarboxylate (437 mg, 1.79 mmol in 1,4-dioxane (30 mL), DIEA (769 mg, 5.96 mmol) was added. The mixture was stirred at 80C for 1.5 h. The mixture was allowed to cool to RT and partitioned between water and ethyl acetate. The organic layer was washed with brine, dried over Na2SO4 and concentrated. The residue was purified by flash column chromatography on silica gel (5-50 % ethyl acetate/petroleum ether) to afford the desired product (224 mg, 30 % yield) as a yellow solid.

129799-15-1, As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference£º
Patent; ARAXES PHARMA LLC; LI, Liansheng; FENG, Jun; WU, Tao; REN, Pingda; LIU, Yi; LIU, Yuan; LONG, Yun, Oliver; WO2015/54572; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of 129799-15-1

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 3.50 g (14.3 mmol) 1-tert-butyl 2-methyl piperazine-l,2-dicarboxylate in 150 mL anhydrous toluene was added 1.62 mL (11.9 mmol) of 3-bromoquinoline. The resulting solution was purged with nitrogen gas for 15 min, and then purged under vacuum for 5 min. Next, 1.59 g (17.6 mmol) of sodium tert-butoxide was added, and the system was again purged for 2 min under vacuum. To this solution were added 444 mg (0.714 mmol) of (+/-)-2,2′-bis(diphenylphosphino)-l,l’- binaphthalene and 342 mg (0.595 mmol) of bis(dibenzylideneacetone)palladium, and the system was purged one last time for 2 min under vacuum. The mixture was then heated under nitrogen to 95 “C for 3.5 h, taken up in anhydrous diethyl ether, and filtered through a plug of Celite. The filtrate was concentrated in vacuo to yield a red solid, which was purified using a Biotage Horizon system (30% ethyl acetate/ hexanes mixture) to give the title compound as a racemic mixture. Chiral HPLC separation (Chiralcel AD, 60% 2-propanol/heptane) afforded the R enantiomer (first eluting) and the S enantiomer (second eluting), each in ^>9% ee. For the S enantiomer, 1H NMR (CDCl3): delta 8.75 (d, J = 2.1 Hz, IH), 7.99 (d, J = 8.2 Hz, 1 H), 7.68 (dd, J= 6.9, 1.1 Hz, 1 H), 7.53 (ddd, J = 8.7, 7.1, 1.6 Hz, 1 H), 7.48 (td, J = 8.2,1.3 Hz5 1 H) 7.36 (d, J = 2.5 Hz, 1 H), 4.96 (s, 0.55 H) 4.78 (s, 0.45 H), 4.11 (d, J = 7.1, 0.55 H), 4.01 (d, J = 13.0 Hz, 0.45 H), 3.80 (d, J = 8.0 Hz, 3 H), 3.57 (m, 1 H), 3.44 (t, J = 9.4 Hz, 0.55 H), 3.32 (t, J = 9.6 Hz, 0.45 H), 3.04 (m, 1 H), 2.89 (q, J = 8.6 Hz, IH) 1.52 (s, 5 H), 1.48 (s, 4 H). LC/MS 372.3 (M+l).

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK & CO., INC.; WO2007/120688; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Simple exploration of 129799-15-1

129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Int. 149 (0.7 g; 1.51 mmol) and DIPEA (0.77 mL; 4.53 mmol) were dissolved in DMF (8 mL) at 0 C under N2-gas atmosphere. Methanesulfonyl chloride (0.234 mL; 3.02 mmol) was added portionwise (3x 0.078 mL) at intervals of 5 min. The reaction mixture was allowed to warm up to room temperature. The mixture was reacted for 1 h, and then 1 ,2-piperazinedicarboxylic acid, l-(l , l-dimethylethyl) ester (0.738 g; 3.02 mmol) was added. The reaction mixture was heated at 80 C overnight. Subsequently, the mixture was concentrated to dryness. The residue was dissolved in DCM/MeOH 10/1 v/v (25 mL) and this solution was washed with 1 M NaC03solution in H20 (15 mL). The organic layers were combined, dried (MgSC^), filtered and concentrated to dryness. The residue was purified by column chromatography over silica gel eluting with a gradient from 100 % DCM to 100 % DCM/MeOH 9/1 v/v. The desired fractions were collected and the solvent was evaporated. Yield: 0.978 g of Int. 151 (94 %). The intermediates in the table below were prepared according to an analogous reaction protocol as used for Int. 151 :, 129799-15-1

129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; JANSSEN PHARMACEUTICA NV; DIELS, Gaston, Stanislas, Marcella; SCHOENTJES, Bruno; VERSELE, Matthias, Luc, Aime; BERTHELOT, Didier, Jean-Claude; WILLEMS, Marc; VIELLEVOYE, Marcel; EMBRECHTS, Werner, Constant, Johan; WROBLOWSKI, Berthold; MEERPOEL, Lieven; WO2015/150555; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Some tips on 129799-15-1

129799-15-1, 129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

4-Chloro-6-(3,4-dichloro-phenyl)-pyrimidine (0.1 lg, 0.4mmol) was added in one portion to a suspension of piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester (0.21g, 0.85mmol) and in fert-butanol (2ml) in a microwave reactor tube. The tube was sealed and heated to 150C in a microwave for 40 minutes at a pressure of 250psi. After this time the reaction mixture was cooled to room temperature and the solvent was removed. The resulting residue was purified by flash column chromatography (elution: 20% EtOAc, 80% Heptane) to give the title compound (0.36g, 75% yield) as a colourless oil. deltaEta (500 MHz, DMSO) 8.59 (s, 1 H) 8.43 (d, J=2.05 Hz, 1 H) 8.17 (dd, J=8.51, 2.05 Hz, 1 H) 7.74 – 7.81 (m, 1 H) 7.42 (d, J=7.88 Hz, 1 H) 4.88 – 5.09 (m, 1 H) 4.60 – 4.76 (m, 1 H) 4.24 – 4.46 (m, 1 H) 3.76 – 3.88 (m, 1 H) 3.56 (d, J=13.08 Hz, 3 H) 3.38 – 3.51 (m, 1 H) 3.10 – 3.28 (m, 2 H) 1.31 -1.47 (m, 9 H). Tr = 3.71 min m/z (ES+) (M+H+) 283, 285.

129799-15-1, 129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; DOMINGUEZ, Celia; TOLEDO-SHERMAN, Leticia, M.; COURTNEY, Stephen, Martin; PRIME, Michael; MITCHELL, William; BROWN, Christopher, John; DE AGUIAR PENA, Paula, C.; JOHNSON, Peter; WO2013/16488; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Analyzing the synthesis route of 129799-15-1

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

155a) 4-(5-Methoxy-2-pyridin-4-yl-pyrido[3,4-d]pyrimidin-4-yl)-piperazine-l,2- dicarboxylic acid 1-tert-butyl ester 2-methyl ester : 5-Methoxy-2-pyridin-4-yl-pyrido[3,4- d]pyrimidin-4-ol (508 mg, 2.00 mmol), Triethylamine (863 uL, 6.19 mmol), 2,4,6- Triisopropylbenzenesulfonyl Chloride (668 mg, 2.20 mmol), and 4- Dimethylaminopyridine (28 mg, 0.23 mmol) in N,N-Dimethylformamide (10 mL) were stirred at room temperature for 2 hours. Gradual dissolution of starting material was observed and a considerable darkening of the solution. Piperazine-l,2-dicarboxylic acid 1- tert-butyl ester 2-methyl ester (536 mg, 2.20 mmol) was added and the reaction was stirred at room temperature for two hours. Water was added, and the resulting solid product was collected by filtration, washed with water, and dried. Obtained 448 mg (47%) tan colored solid product, which was used for subsequent steps without further manipulation).

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CEPHALON, INC.; CANCER RESEARCH TECHNOLOGY LIMITED; BRESLIN, Henry, J.; DORSEY, Bruce, D.; DUGAN, Benjamin, J.; FOWLER, Katherine, M.; HUDKINS, Robert, L.; MESAROS, Eugen, F.; MONCK, Nathaniel, JT; MORRIS, Emma, L.; OLOWOYE, Ikeoluwa; OTT, Gregory, R.; PAVE, Gregoire, A.; ROFFEY, Jonathan, R. A.; SOUDY, Christelle, N.; TAO, Ming; ZIFICSAK, Craig, A.; ZULLI, Allison, L.; WO2014/52699; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Some tips on 129799-15-1

129799-15-1, 129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

Example 54 – Preparation of Intermediate 19 The synthesis of Intermediate 19 followed the procedure of General Procedure 15 following: Intermediate 18 Intermediate 19 To a cooled solution (0C) of 1-tert-butyl 2-methyl piperazine-1,2-dicarboxylate (Intermediate 18, 3.5 g, 14.3 mmol) in dry dichloromethane (70 mL) was added triethylamine (TEA, 5 mL, 35.9 mmol) followed by morpholine-4-carbonyl chloride (3.35 mL, 28.7 mmol). The reaction mixture was stirred at room temperature for 3 hours. To the mixture was added ice-cold water (20 mL), then it was extracted into EtOAc (2 x 50 mL). The combined organic layers were dried over sodium sulfate, filtered and concentrated under reduced pressure. The crude residue was purified by flash chromatography using 30% EtOAc/n-hexane to afford 1-tert-butyl 2-methyl 4- (morpholine-4-carbonyl)piperazine-1,2-dicarboxylate (Intermediate 19, 3.6 g, yield: 72%) as an off white solid; TLC: 50% ethyl acetate in hexane. Rf-0.5.

129799-15-1, 129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; VERSEON CORPORATION; SHORT, Kevin Michael; ESTIARTE-MARTINEZ, Maria de los Angeles; KITA, David Ben; SHIAU, Timothy Philip; (340 pag.)WO2016/138532; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of 129799-15-1

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-Acetyl-piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 10 mmol of Piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester were dissolved in 20 ml methylenchloride. 1.05 eq of DIPEA and acetychloride were added. The reaction mixture was stirred at room temperature for 30 min. The product was extracted from etylacetate/water. The crude material was re-dissolved in methanol and treated with 2N NaOH. The reaction mixture was stirred at room temperature for 2 h. The mixture was neutralized with HCl and the product isolated via extraction from ethylacetate/water. MS(ISO): 271.3 (M-H+)

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Ackermann, Jean; Bleicher, Konrad; Ceccarelli Grenz, Simona M.; Chomienne, Odile; Mattei, Patrizio; Schulz-Gasch, Tanja; US2007/129544; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of 129799-15-1

The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 6-bromo-4,7-dichloro-2-methylquinazoline (435 mg, 1.49 mmol) and 1 -tert-butyl 2-methyl piperazine- 1 ,2-dicarboxylate (437 mg, 1.79 mmol) in 1,4-dioxane (30 mL), DIEA (769 mg, 5.96 mmol) was added. The mixture was stirred at 80C for 1.5 h. The mixture was allowed to cool to RT and partitioned between water and ethyl acetate. The organic layer was washed with brine, dried over Na2SO4 and concentrated. The residue was purified by flash column chromatography on silica gel (5-50 % ethyl acetate/petroleum ether) to afford the desired product (224 mg,30 % yield) as a yellow solid.

The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ARAXES PHARMA LLC; JANES, Matthew, Robert; PATRICELLI, Matthew, Peter; LI, Liansheng; REN, Pingda; LIU, Yi; (397 pag.)WO2016/44772; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Analyzing the synthesis route of 129799-15-1

The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of piperazine-1, 2-dicarboxylic acid 1-teit-butyl ester2-methyl ester (977 mg, 4.0 mmol) in DCM (20 mL) at 0 00 was added4-bromo-benzenesulfonyl chloride (1.02 mg, 4.0 mmol). Then TEA (404 mg, 4.0mmol) was added dropwise and the mixture was stirred at room temperature for 1hr. The mixture was concentrated and purified by silica gel chromatography(petroleum ether/EtOAc = 20/1 to 5/1) to afford 1.66 g (90%) of the titlecompound as a white solid. 1H NMR (400 MHz, ODd3) O [ppm] 7.69 (d, J = 8.8Hz, 2H), 7.61 (d, J= 8.8 Hz, 2H), 4.89-4.60 (m, 1H), 4.27-4.20 (m, 1H), 4.04-3.82(m, 1H), 3.77 (5, 3H), 3.76-3.61 (m, 1H), 3.35-3.11 (m, 1H), 2.51 (dd, J= 11.6, 4.0Hz, 1H), 2.33 (td, J= 11.6, 4.0 Hz, 1H), 1.44 (5, 9H).

The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PFIZER INC.; ITEOS THERAPEUTICS; NINKOVIC, Sacha; CROSIGNANI, Stefano; SCALES, Stephanie Anne; MCALPINE, Indrawan James; COLLINS, Michael Raymond; MADERNA, Andreas; WYTHES, Martin; (295 pag.)WO2016/147144; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics