Category: 129799-08-2

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The compound (S) -5- (1 – ((tert-butoxycarbonyl) amino) ethyl) -2- (3- (cyclopropylmethoxy) -4-(difluoromethoxy) phenyl ) -oxazole-4-carboxylic Acid (0.6g, 1.28mmol), 1-Boc-3- methyl piperazine (376mg,1.54mmol), 1- ethyl-3- (3-dimethylaminopropyl) carbodiimide salts Salt (368mg, 1.92mmol) and N- hydroxy-7-aza-benzotriazole (435mg, 3.20mmol) was dissolved in dichloromethane (20mL) The conditions at 0 C tothis solution was added dropwise N, N- diisopropylethylamine (0.89mL, 5.12mmol), stirred at rt for 6h,Saturated chlorinated Sodium solution (15mL ¡Á 3) washing the organic phase dried over Na 2 SO 4 anhydrous,solvent was removed concentrate was subjected to column chromatography (eluent: Petroleumether / EtOAc (v/ v) = 4/1), to give 714mg white solid, yield: 80%.

129799-08-2, 129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various fields.

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

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The compound (S) -5- (1 – ((tert-butoxycarbonyl) amino) ethyl) -2- (3- (cyclopropylmethoxy) -4-(difluoromethoxy) phenyl ) -oxazole-4-carboxylic Acid (0.25g, 0.53mmol), the compound 1,3-piperazinecarboxylate hydrochloride (150mg, 0.64mmol), 1- ethyl-3- (3-dimethylamine propyl Yl) carbodiimidehydrochloride (153mg, 0.80mmol) and N- hydroxy-7-aza-benzotriazole (181mg, 1.33mmol) was dissolved indichloromethane Dioxane (20 mL), and under conditions of 0 C to this solution was added dropwise N, Ndiisopropylethylamine(0.37mL, 2.13mmol), stirred at room temperature 17H, The solvent was removed, theconcentrate was subjected to column chromatography (eluent: Petroleumether / EtOAc (v / v) = 2/1), to give260mg yellow viscous Material, yield: 74%., 129799-08-2

129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various fields.

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate (500 mg, 2.05 mmol), (4-fluorophenyl)boronic acid (575 mg, 4.11 mmol), copper(II) acetate (372 mg, 2.05 mmol) and pyridine (0.33 ml, 4.09 mmol) were suspended in anhydrous DCM (10 ml) with 4A molecular sieves (500 mg). The mixture was stirred for 16 hours at ambient temperature, then for 5 hours at 35 C. Air was bubbled through the mixture for 10 min, then it was stirred for 18 hours at ambient temperature. Air was bubbled through the mixture for 10 min, then it was stirred at 35 C. for 6 hours and at ambient temperature for 72 hours. Additional (4-fluorophenyl)boronic acid (286 mg, 2.05 mmol) was added and the reaction was stirred for 4 hours at 35 C. The reaction was cooled to ambient temperature and filtered through celite. The filtrate was partitioned with sat. aq. NaHCO3 (20 ml). The organic layer was separated and the aqueous extracted with DCM (2¡Á20 ml). The organics were combined and concentrated in vacuo to give a green oil. The oil was purified via flash column chromatography using a gradient of 0-50% EtOAc in heptane. The product containing fractions were combined and concentrated in vacuo to afford the title compound as a yellow oil (213 mg, 26%). 1H NMR (250 MHz, Chloroform-d) delta 7.01-6.90 (m, 2H), 6.87-6.78 (m, 2H), 4.47 (d, J=13.4 Hz, 1H), 4.32-4.22 (m, 1H), 4.09 (s, 1H), 3.63 (s, 3H), 3.59-3.46 (m, 1H), 3.37 (dd, J=13.3, 4.2 Hz, 1H), 3.28-3.00 (m, 2H), 1.46 (s, 9H). LCMS Method 3-Tr=1.90 min, (ES+) (M+H+) 339.2.

129799-08-2, As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

Reference£º
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (519 pag.)US2018/127370; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 29 Preparation of 6-(2-carbamoyl-4-methylpiperazin-l-yl)-2-(4-(4- (trifluoromethyl) phenoxy)phenyl)pyrimidine-4-carboxamide (Cpd No. 81) Scheme 61 1 -tert-butyl 3-methyl 4-(2-chloro-6-(methoxycarbonyl)pyrimidin-4-yl)piperazine- 1 ,3-dicarboxylate: A mixture of 1-tert-butyl 3-methyl piperazine-l ,3-dicarboxylate (5.133 g, 21.01 mmol), methyl 2,6-dichloropyrimidine-4-carboxylate (4.354 g, 21.03 mmol), and iPr2NEt (4.0 mL, 23.0 mmol) in acetonitrile (50 mL) was heated at 50C for 4 h. After cooling, the reaction mixture was evaporated in vacuo and the residue chromatographed over silica gel with 20-70% EtOAc in hexanes. The product fractions were evaporated in vacuo to give 1-tert-butyl 3-methyl 4-(2-chloro-6- (methoxycarbonyl)pyrimidin-4-yl)piperazine-l,3-dicarboxylate as a very pale yellow powder (6.626 g, 15.97 mmol, 76% yield). LC/MS: m/z= 415.2 [M+H]+., 129799-08-2

The synthetic route of 129799-08-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PURDUE PHARMA L.P.; NI, Chiyou; PARK, Minnie; SHAO, Bin; TAFESSE, Laykea; YAO, Jiangchao; YOUNGMAN, Mark; WO2013/30665; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0256] Alternatively, the title compound can be prepared via the mono-piperidine compound, shown in the above scheme, beginning with Intermediate C, using two stepwise pairs of (a) amino acid coupling from with l-(tert-butyl) 3-methyl piperazine- 1,3- dicarboxylate, and (b) ester hydrolysis. HATU and DIPEA in DMF were employed at room temperature for 12 hours for the coupling reactions. The hydrolyses were accomplished with LiOH at room temperature for one hour. The combination of coupling and hydrolysis occurred in roughly 60% yield when performed on a gram scale. The steps could be accomplished by someone skilled in the art.

129799-08-2, As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

Reference£º
Patent; BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM; LINK, James, T.; LISSANU DERIBE, Yonathan; (91 pag.)WO2019/200217; (2019); 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.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

To a solution of 53 7-bromo-4,6-dichloro-3-nitroquinoline (2.07 g, 6.43 mmol) in 78 THF (50 ml) was added 242 1-(tert-butyl) 3-methyl piperazine-1,3-dicarboxylate (2.356 g, 9.64 mmol) followed by 56 DIPEA (3.36 ml, 19.29 mmol) under nitrogen. The reaction was then heated at reflux overnight, cooled and evaporated, taken up in water and extracted with DCM then dried by passing through a phase separator cartridge. Evaporation afforded an orange gum which was purified by flash silica chromatography, elution gradient 0 to 50% 57 EtOAc in 58 heptane. Pure fractions were evaporated to dryness to afford 243 1-(tert-butyl) 3-methyl-4-(7-bromo-6-chloro-3-nitroquinolin-4-yl)piperazine-1,3-dicarboxylate (1.66 g, 49%) as a yellow foam. 1H NMR (400 MHz, DMSO, 30 C.) 1.45 (9H, s), 3.30 (1H, s), 3.55 (3H, s), 3.59-3.69 (1H, m), 3.72 (1H, d), 3.75 (1H, d), 3.84 (1H, s), 4.11 (1H, s), 4.35 (1H, s), 8.50 (1H, s), 8.54 (1H, s), 9.12 (1H, s). m/z: ES+ [M+H]+ 529., 129799-08-2

129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; Kettle, Jason Grant; Bagal, Sharanjeet; Robb, Graeme Richard; Smith, James Michael; Goldberg, Frederick Woolf; Cassar, Doyle Joseph; Feron, James Lyman; US2019/177338; (2019); 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.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

To a 50 mL of sealing tube were added 1-tert-butyl 3-methyl piperazine-1,3-dicarboxylate (500 mg, 2.05 mmol) , iodomethane (580mg, 4.10 mmol) , potassium carbonate (424 mg, 3.07 mmol) and acetone (10 mL) .The mixture was stirred at 50 for 6 h and concentrated. The residue was diluted withwater (20 mL) . The resulting mixture was extracted with DCM (10 mL ¡Á 3) . The combined organic layers were dried over anhydrous Na2SO4and concentrated to give 1-tert-butyl 3-methyl 4-methylpiperazine-1,3-dicarboxylate as a light yellow solid (290 mg, 54) . 1H NMR (400 MHz, CDCl3): delta ppm 4.65-4.83 (m, 1H) , 4.29-4.33 (m, 1H) , 4.18-4.23 (m, 1H) , 4.05-4.11(m, 1H) , 3.80-3.94 (m, 3H) , 3.88 (s, 3H) , 3.66 (s, 3H) , 1.48 (s, 9H) and MS-ESI: m/z 259.30 [M+H] +.

129799-08-2, As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

Reference£º
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.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

[0256] Alternatively, the title compound can be prepared via the mono-piperidine compound, shown in the above scheme, beginning with Intermediate C, using two stepwise pairs of (a) amino acid coupling from with l-(tert-butyl) 3-methyl piperazine- 1,3- dicarboxylate, and (b) ester hydrolysis. HATU and DIPEA in DMF were employed at room temperature for 12 hours for the coupling reactions. The hydrolyses were accomplished with LiOH at room temperature for one hour. The combination of coupling and hydrolysis occurred in roughly 60% yield when performed on a gram scale. The steps could be accomplished by someone skilled in the art.

129799-08-2, The synthetic route of 129799-08-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM; LINK, James, T.; LISSANU DERIBE, Yonathan; (91 pag.)WO2019/200217; (2019); 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.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

Step 5: The preparation of 4-(3-Methyl-butyl)-piperazine-1,3-dicarboxylic acid 1-tert-butyl ester 3-methyl ester: Piperazine-1,3-dicarboxylic acid 1-tert-butyl ester 3-methyl ester (6.0 g, 24.6 mmol) was treated with EtOH (100 mL), isovaleraldehyde (5.3 mL, 50 mmol), and 20% Pd/C (1.0 g), then shaken under an atmosphere of H2. The reaction was filtered and concentrated. The residue was chromatographed on silica gel eluding with 2:1 hexanes/EtOAC to give 7.0 g (90%) of the desired product as an oil. MS: 316 (M+1 for C16H30N2O4); colorless liquid; TLC: SiO2, Rf0.8 (50% hexanes/EtOAc);, 129799-08-2

As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

Reference£º
Patent; Warner-Lambert; US6251919; (2001); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of l-tert-butyl 3-methyl piperazine- 1, 3 -dicarboxy late (compound I-3a, 1.22 g, 5 mmol) in anhydrous CH2CI2 (15 mL) was added trimethylsilyl isocyanate (634 mg, 5.5 mmol). The resulting mixture was stirred at room temperature for 64 h. The reaction mixture was directly concentrated under reduced pressure to afford crude O l-tert-butyl 03 -methyl 4- carbamoylpiperazine-l,3-dicarboxylate (1.51 g) as a light-yellow foam which was directly used for next step without purification. MS obsd. (ESI+) [(M+H)+]: 288., 129799-08-2

129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; HAN, Xingchun; JIANG, Min; WANG, Yongguang; YANG, Song; (83 pag.)WO2019/129681; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics