Category: 252990-05-9

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.252990-05-9,Methyl (R)-1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

(R)-Piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester (120 mg, 0.49 mmol) and 2-Bromo-5-trifluoromethyl-pyridine (133 mg, 0.59 mmol) were dissolved into 2.0 mL of anhydrous toluene (degassed). In a separate, septum-equipped vial were placed tri(dibenzylideneacetone)dipalladium (0) (22 mg, 0.024 mmol), 1,3-bis(2,6-di-i-propylphenyl)imidazolium chloride (42 mg, 0.1 mmol) and sodium t-butoxide (57 mg, 0.59 mmol). This “catalytic” vial was equipped with a magnetic stir bar and flushed with dry nitrogen. The reactant solution was next transferred to the “catalytic” vial and the mixture was stirred at 100 C. for 5 h. After this period the mixture was combined with 20 mL of hexane/EtOAc (2:1) and was passed through a pad of Celite. The resulting filtrate was evaporated in vacuo and purified using flash silica chromatography (0-20% EtOAc/Hexane) to yield 110 mg (58%) of (R)-4-(5-Trifluoromethyl-pyridin-2-yl)-piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester, intermediate IX-B, as a yellow residue. 1H NMR (400 MHz, CDCl3) delta 8.39-8.38 (m, 1H), 7.65 (d, 1H), 6.68 (m, 1H), 4.89-4.68 (m, 2H), 4.29 (dd, 1H), 3.95 (dd, 1H), 3.69 (s, 3H), 3.43-3.26 (m, 2H), 3.12-2.97 (m, 1H), 1.51-1.46 (m, 9H)., 252990-05-9

The synthetic route of 252990-05-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Kalypsys, Inc.; US2005/234046; (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.252990-05-9,Methyl (R)-1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

Step 1 To a stirred solution of 1-(tert-butyl) 2-methyl (R)-piperazine-1,2-dicarboxylate (2.0 g. 8.2 mmol) in CH2Cl2 was added naphthalen-1-ylboronic acid (9.8 mmol, 1.2 equiv) and Cu(OAc)2 (500 mg) and stirring continued for 48 h under a balloon of air. The solution was washed with H2O, dried over Na2SO4 and evaporated. Column chromatography (20% EtOAc-hexanes) gave 1-(tert-butyl) 2-methyl (R)-4-(naphthalen-1-yl)piperazine-1,2-dicarboxylate (402 mg, 13% yield) as an oil., 252990-05-9

252990-05-9 Methyl (R)-1-Boc-piperazine-2-carboxylate 7009916, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Omeros Corporation; Cutshall, Neil S.; Gage, Jennifer Lynn; Gruswitz, Franz A.; Khalaf, Juhienah; Little, Thomas L.; Metz, Markus; Nguyen, Jeremiah H.; Nollert von Specht, Peter Kurt; Tsoung, Jennifer; Cicirelli, Michael; Goldstein, Sara Rebecca; Keshipeddy, Santosh Kumar; Kwon, Do Yeon; Lemus, Robert Huerta; Vaddela, Sudheer Babu; (638 pag.)US2019/367452; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

252990-05-9, Methyl (R)-1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1-tert-butyl 2-methyl (2R) -piperazine-1, 2-dicarboxylate (500 mg)1-Bromo-4-chlorobenzene (383 mg), palladium (II) acetate(15 mg), BINAP (75 mg),And sodium tert-butoxide (442 mg) were added toluene in a nitrogen stream, and the mixture was stirred at 80 C. for 18 hours.The reaction solution was cooled to room temperature, filtered through celite with ethyl acetate,The solvent was evaporated under reduced pressure to obtain a residue,Silica gel column chromatography (hexane-ethyl acetate)Made,1-tert-butyl 2-methyl (2R) -4- (4-chlorophenyl)Piperazine-1, 2-dicarboxylate240 mg (yield 34%) was obtained, 252990-05-9

252990-05-9 Methyl (R)-1-Boc-piperazine-2-carboxylate 7009916, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; NATIONAL CENTER FOR GERIATRICS AND GERONTOLOGY; YANAGISAWA, KATSUHIKO; KAWAI, AKIYOSHI; (139 pag.)JP2017/171619; (2017); A;,
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.252990-05-9,Methyl (R)-1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

(R)-Piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester (120 mg, 0.49 mmol) and 2-Bromo-5-trifluoromethyl-pyridine (133 mg, 0.59 mmol) were dissolved into 2.0 mL of anhydrous toluene (degassed). In a separate, septum-equipped vial were placed tri(dibenzylideneacetone)dipalladium (0) (22 mg, 0.024 mmol), 1,3-bis(2,6-di-i-propylphenyl)imidazolium chloride (42 mg, 0.1 mmol) and sodium t-butoxide (57 mg, 0.59 mmol). This “catalytic” vial was equipped with a magnetic stir bar and flushed with dry nitrogen. The reactant solution was next transferred to the “catalytic” vial and the mixture was stirred at 100 C. for 5 h. After this period the mixture was combined with 20 mL of hexane/EtOAc (2:1) and was passed through a pad of Celite. The resulting filtrate was evaporated in vacuo and purified using flash silica chromatography (0-20% EtOAc/Hexane) to yield 110 mg (58%) of (R)-4-(5-Trifluoromethyl-pyridin-2-yl)-piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester, intermediate IX-B, as a yellow residue. 1H NMR (400 MHz, CDCl3) delta 8.39-8.38 (m, 1H), 7.65 (d, 1H), 6.68 (m, 1H), 4.89-4.68 (m, 2H), 4.29 (dd, 1H), 3.95 (dd, 1H), 3.69 (s, 3H), 3.43-3.26 (m, 2H), 3.12-2.97 (m, 1H), 1.51-1.46 (m, 9H)., 252990-05-9

The synthetic route of 252990-05-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Kalypsys, Inc.; US2005/234046; (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.252990-05-9,Methyl (R)-1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

In a sealed tube, (R)-1-tert-butyl 2-methyl piperazine-1,2-dicarboxylate (1.00 g, 4.09 mmol) was dissolved in NH3 (2 M in MeOH, 10 mL, 20.00 mmol) at RT. The reaction solution was stirred at 60 C for 3 days. After cooling to RT, the resulting mixture was concentrated under reduced pressure to afford (R)-tert-butyl 2-carbamoylpiperazine-1- carboxylate as a solid. LCMS (ESI) calc?d for C10H19N3O3 [M + 1]+: 230, found 230., 252990-05-9

As the paragraph descriping shows that 252990-05-9 is playing an increasingly important role.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DONG, Shuzhi; SCOTT, Jack, D.; TANG, Haiqun; ZHAO, Zhiqiang; YANG, Dexi; GU, Xin; JIANG, Jinlong; XIAO, Li; (209 pag.)WO2019/18186; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

252990-05-9, Methyl (R)-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 Compound 13A (605 mg, 2.46 mmol), l-(/er/-butyl) 2-methyl (f?)-piperazine-l,2-dicarboxylate (500 mg, 2.05 mmol), and K2CO3 (424 mg, 3.07 mmol) in DMF (10 mL) was stirred at 60 C for 4 hours. The reaction mixture was diluted with water (50 mL) and extracted with ethyl acetate (50 mL x 2). The combined organic extracts were washed with brine (50 mL), dried over anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. The residue was purified with flash column chromatography on silica gel (ethyl acetate in petroleum ether, 10% v/v) to yield Compound 13B-1: LC-MS (ESI) m/z: 411 [M+H]+.

252990-05-9, The synthetic route of 252990-05-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIOMARIN PHARMACEUTICAL INC.; WANG, Bing; (270 pag.)WO2019/104011; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

252990-05-9, Methyl (R)-1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Lithium aluminium hydride (1M in THF, 26 ml) was added to a solution of L-TERT- butyl 2-methyl (2R)-piperazine-1, 2-dicarboxylate (2. 55 g) in THF (70 ml) AT-40C, then the reaction was warmed to room temperature. The solution was stirred for 1 hour, then cooled to 0C and quenched by sequential addition of water (1 ml), sodium hydroxide (2N, 1 ml) and then water (2 ml). The resulting slurry was filtered and concentrated in vacuo to give TERT- butyl (2R)-2-(hydroxymethyl) piperazine-1-carboxylate (2.37 g, > 100%); NMR spectrum (DMSO-d6,373K) 1.40 (s, 9H), 2.58 (m, 1H), 2. 82 (M, 3H), 2. 92 (bs, 1H), 2.98 (d, 1H), 3.43 (m, 1H), 3.65 (M, 2H), 3.80 (M, 1H) ; Mass spectrum MH+ 217.

252990-05-9, The synthetic route of 252990-05-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/26152; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics