Category: 163765-44-4

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

A mixture of (R) -tert-butyl 3-methylpiperazine-1-carboxylate (250 mg, 1.25 mmol) , cyclopropanecarboxylic acid (130 mg, 1.50 mmol) , EDCI (480 mg, 2.50 mmol) and HOAT (254 mg, 1.87 mmol) in DCM (10 mL) was stirred at 0 , and DIPEA (0.65 mL, 3.74 mmol) was added dropwise. After the addition, the mixture was stirred at rt for 10 h and washed with water (10 mL × 3) . The organic layer was dried over anhydrous Na2SO4 and concentrated. The residue was purified by silica gel chromatography eluted with Petroleum ether/EtOAc (v/v) 2/1 to give (R) -tert-butyl 4- (cyclopropanecarbonyl) -3-methylpiperazine-1-carboxylate as colorless oil (310 mg, 93) .1H NMR (400 MHz, CDCl3) : delta ppm 4.24-4.50 (m, 1H) , 3.78-4.07 (m, 2H) , 2.90-3.41 (m, 3H) , 2.81 (s, 6H) , 1.50 (s, 9H) , 1.12-1.36 (m, 4H) , 0.96-1.05 (m, 2H) , 0.74-0.82 (m, 2H) and MS-ESI: m/z 213.10 [M-55] +.

163765-44-4, The synthetic route of 163765-44-4 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (2016); 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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: The mixture of 13a (151 mg, 0.423 mmol) and 4 N HCl in 1,4-dioxane solution (1.38 ml) was stirred at room temperature overnight. After concentration, the residue was crystalized with etherto afford the white precipitation. The resulting solid was collected by filtration to afford 14a (121 mg, 98.0%) as the white solid. MSESI (m/z) = 257 [M+H]+. To a solution of 4a (116 mg, 0.35 mmol)in DMF (2.3 ml) was added 14a (120 mg, 0.42 mmol), COMU (225 mg, 0.525 mmol) and Et3N (177 mg, 1.75 mmol) at room temperature.The reaction mixture was stirred at same temperature for 1.5 h. The reaction mixture was diluted with sat. NaHCO3 solution to afford the pale yellow precipitation. The resulting solid was collected by filtration to 16a, 163765-44-4

As the paragraph descriping shows that 163765-44-4 is playing an increasingly important role.

Reference：
Article; Tsuno, Naoki; Yukimasa, Akira; Yoshida, Osamu; Suzuki, Shinji; Nakai, Hiromi; Ogawa, Tomoyuki; Fujiu, Motohiro; Takaya, Kenji; Nozu, Azusa; Yamaguchi, Hiroki; Matsuda, Hidetoshi; Funaki, Satoko; Yamanada, Natsue; Tanimura, Miki; Nagamatsu, Daiki; Asaki, Toshiyuki; Horita, Narumi; Yamamoto, Miyuki; Hinata, Mikie; Soga, Masahiko; Imai, Masayuki; Morioka, Yasuhide; Kanemasa, Toshiyuki; Sakaguchi, Gaku; Iso, Yasuyoshi; Bioorganic and Medicinal Chemistry; vol. 25; 7; (2017); p. 2177 – 2190;,
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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

Intermediate 8 tert-Butyl (3R)-4-(chlorocarbonyl)-3 -methylpiperazine- 1 -carboxylateTo a mixture of triphosgene (23 g, 75 mmol) in anhydrous DCM (250 mL) was added pyridine (18 g, 225 mmol) drop-wise followed by addition of tert-butyl (3R)-3- methylpiperazine-1 -carboxylate (15 g, 75 mmol) at 0 C. The mixture was stirred overnight at RT. TLC showed the starting material had been consumed. The mixture was concentrated to afford Intermediate 8 as yellow solid, which was used without further purification., 163765-44-4

As the paragraph descriping shows that 163765-44-4 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; LI, David, Yunzhi; WANG, Jiabing; YANG, Zhenfan; ZENG, Qingbei; ZHANG, Xiaolin; WO2014/135876; (2014); 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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

Intermediate 8 tert-Butyl (3R)-4-(chlorocarbonyl)-3 -methylpiperazine- 1 -carboxylateTo a mixture of triphosgene (23 g, 75 mmol) in anhydrous DCM (250 mL) was added pyridine (18 g, 225 mmol) drop-wise followed by addition of tert-butyl (3R)-3- methylpiperazine-1 -carboxylate (15 g, 75 mmol) at 0 C. The mixture was stirred overnight at RT. TLC showed the starting material had been consumed. The mixture was concentrated to afford Intermediate 8 as yellow solid, which was used without further purification., 163765-44-4

As the paragraph descriping shows that 163765-44-4 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; LI, David, Yunzhi; WANG, Jiabing; YANG, Zhenfan; ZENG, Qingbei; ZHANG, Xiaolin; WO2014/135876; (2014); 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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

Example 14; l-Methyl-2-[(2R)-2-methyl-4-(quinoline-2-carbonyl)-piperazin-l-yl]- 1eta- [4,4′]bipyrimidinyl-6-one; (3R)-3’Methvl-4′(l-methvl’6-oxo-l,6-dihvdro-[4,4′]bipvrimidinvl-2’vl)-piperazine-l’car boxvlic acid tert-butvl ester; A solution of 2-chloro-3-methyl-6-(pyrimidin-4-yl)-3H-pyrimidin-4-one (5.3 g, 24 mmol), fer^butyl (Si^-S-methylpiperazine-l-carboxylate (5.0 g, 25 mmol) and triethylamine (7.6 g, 75 mmol) in N-methyl”2-pyrrolidone (25 ml) was stirred for 6 hours at 90 0C. The solution was partitioned between water and ethyl acetate, and the organic layer was washed with water, brine, dried over sodium sulfate, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (eluent; ethyl acetate) to afford (3R)-3-methyl-4-(l-methyl-6-oxo-l,6- dihydro-[4,4′]bipyrimidinyl-2-yl)-piperazine”l-carboxylic acid tert-butyl ester (6.9 g, 71 %)..1H NMR; 1.28 (3H, d, J= 7.0 Hz), 1.51 (9H, brs), 3.29-3.52 (4H, m), 3.55 (3H, s), 3.71 (IH, dd, J= 3.9, 13.3 Hz), 3.81-4.02 (2H, m), 7.29 (IH, s), 8.16 (IH, dd, J= 1.6, 5.5 Hz), 8.88 (IH, d, J= 4.7 Hz), 9.25 (IH, s) (CDCl3) MS; [M++ 1] = 387 ., 163765-44-4

As the paragraph descriping shows that 163765-44-4 is playing an increasingly important role.

Reference：
Patent; MITSUBISHI PHARMA CORPORATION; SANOFI-AVENTIS; WO2007/119463; (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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

Compound (R) – 3-methyl-piperazine-1-carboxylic acid T-butyl ester (530 mg, 2 . 6mmol), compound quinoline-2-carboxylic acid (450 mg, 2 . 6mmol), 1-ethyl-3 – (3-dimethylamino-propyl) carbodiimide hydrochloride (996 mg, 5 . 2mmol) and N-hydroxy-7-azabenzene and triazazole (530 mg, 3 . 9mmol) dissolved in dichloromethane (10 ml) in, 0 C to this solution under the conditions of adding dropwisely N, N-diisopropyl ethylamine (1.3 ml, 7 . 8mmol), stirring the mixture at room temperature for 10h, and washing with water (10 ml × 3), the organic phase is dried with anhydrous sodium sulfate, removal of solvent, concentrate under column separation (V (petroleum ether)/ V (ethyl acetate) =1/1) get 820 mg white solid, yield: 88%., 163765-44-4

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd.; Yu, Tianzhu; Liu, Bing; Zhang, Yingjun; Zhang, Xiangyu; Zhang, Zhiguo; Zheng, Changchun; Zhang, Jiancun; Lei, Jianhua; (66 pag.)CN105461693; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The compound (R) -4-Boc-2- methylpiperazine (528mg, 2.64mmol), glacial acetic acid (190mg, 3.16mmol), 1-ethyl-3- (3- Dimethylaminopropyl) carbodiimide hydrochloride (758mg, 3.95mmol) and N- hydroxy-7-azabenzotriazole(897mg, 6.59mmol) was dissolved In dichloromethane (20 mL), and under conditions of 0 C tothis solution was added dropwise N, N- diisopropylethylamine (1.8mL, 10.54mmol), stirred at roomtemperature Stirred 12h, was added water (10mL ¡Á 2) washing the organic phase was dried over anhydrous Na 2SO 4, the solvent was removed concentrate was separated by column chromatography (leaching Lotion: DCM /MeOH (v / v) = 40/1), to give 580mg colorless oil: Compound N- acetyl-4-tert-butoxycarbonyl -2- (R) – methylPiperazine, yield: 90%., 163765-44-4

The synthetic route of 163765-44-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 1 ,1-dimethylethyl (3R)-3-methyl-1-piperazinecarboxylate (301 mg, 1.5 mmol) in anhydrous acetonitrile (1OmL) was added PS-DIEA (925mg) and the solution was stirred gently under an argon atmosphere at room temperature for 15mins. 4-chlorobenzenesulfonyl chloride (371 mg, 1.8 mmol) as a solution in acetonitrile (5ml_) was added and the reaction was stirred for 24hrs. After this time, the reaction was filtered and PS-isocyanate (3g) was added to the solution which was stirred at room temperature over a weekend (approx 64hrs). The reaction was again filtered and PS-trisamine (1.2g) was added to the solution mixture which was stirred for 2hrs at room temperature. Finally the reaction was filtered and reduced in- vacuo to yield the title compound (411 mg, 73%).1H-NMR (CDCI3) 51.02 (3H, d, J= 6.8Hz), 1.43 (9H, s), 2.79 (1 H, br m), 2.97 (1 H, br m), 3.11 (1 H, dt J=12.5, 3.29Hz), 3.60 (1 H, m), 3.80 (1 H, br m), 4.1 1 (2H, br m), 7.48 (2H, m), 7.75 (2H, m)

163765-44-4, 163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXO GROUP LIMITED; BESWICK, Paul, John; CAMPBELL, Alister; CRIDLAND, Andrew; GLEAVE, Robert, James; PAGE, Lee, William; WO2010/102663; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The compound (R) -3- methyl-piperazine-1-carboxylate (500mg, 2.5mmol), isobutyric acid (263mg, 3.0mmol),1- ethyl 3- (3-dimethylaminopropyl) carbodiimide hydrochloride (957mg, 5.0mmol) and N- hydroxy-7-azabenzotriazole(507mg, 3.7mmol) It was dissolved in dichloromethane (10 mL), and the conditions under 0 C,to this solution was added dropwise N, N- diisopropylethylamine (1.3mL, 7.49mmol), chamber Temperature for10H, add water (10mL ¡Á 3), dried over anhydrous Na 2 SO 4 organic phase was dried, the solvent was removedconcentrate was separated by column chromatography (developing Degreasing agent: Petroleumether / EtOAc(v / v) = 2/1), to give 670mg white solid: (R) -4- isobutyryl-3- methyl-piperazine-1-carboxylic acid tert Butyl,yield: 99%., 163765-44-4

The synthetic route of 163765-44-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 27(3R)-tert-butyl 3-methyl-4-(7-(methylsulfonyl)-7-azaspiro[3.5]nonane-2-carbonyl)piperazine-1-carboxylate Oxalyl chloride (0.127 mL, 1.46 mmol) was slowly added to a solution of Intermediate 26 (120 mg, 0.49 mmol) in DCM (12 mL) at 0 C. One drop of DMF was added and the reaction mixture was stirred for 4 h. The solvent was concentrated. The residue was quickly recovered in DCM (5 mL) and added to a solution of (R)-tert-butyl 3-methylpiperazine-1-carboxylate (97 mg, 0.49 mmol) and Et3N (0.338 mL, 2.43 mmol) in DCM (12 mL) at 0 C. The reaction mixture was allowed to warm to ambient temperature and stirred for 1 h. The solvent was concentrated and the product was purified on silica gel (24 g) by MPLC using 5% MeOH and 10% acetone in DCM as the eluent to provide title compound (111 mg, 53.3%) as a solid. 1H NMR (400 MHz, CHLOROFORM-d) delta ppm 1.14 (d, J=7.03 Hz, 2H) 1.22 (d, J=6.64 Hz, 2H) 1.47 (s, 9H) 1.63-1.72 (m, 2H) 1.72-1.84 (m, 2H) 1.92-2.30 (m, 4H) 2.76 (s, 3H) 2.78-3.03 (m, 2H) 3.11 (t, J=5.66 Hz, 2H) 3.14-3.29 (m, 4H) 3.30-3.42 (m, 1H) 3.84 (br. s., 1H) 4.30-4.82 (m, 1H); MS m/z 430.3 [M+H]+ (ES+)., 163765-44-4

As the paragraph descriping shows that 163765-44-4 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; US2010/130477; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics