Month: July 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.162046-66-4,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

A stock solution of SOCl2-benzotriazole in dry DCM (1.5 M) was prepared by making up volume of a viscous clear solution of thionyl chloride (leq) and benzotriazole (1 eq) with dry DCM (1.5 M) – cf, Synlett 1999, 1763. 1.25 eq of this stock solution was added to a solution of4-(4-tert- butoxycarbonyl)piperazin-l-yl)benzoic acid (1 eq) (prepared as described in published International patent application WO98/00134) in dry DCM (0.05 M). With the addition, a precipitate formed that was indicative of acyl chloride formation. The reaction was left at RT for 10 min before being filtered through a pad of anhydrous sodium sulfate.

162046-66-4, 162046-66-4 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid 2795508, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Istituto Di Ricerche Di Biologia Molecolare P. Angeletti SpA; WO2006/38039; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The 2L glass reaction flask was 900 ml purged of unitz methanol, 90.0g 1 – acetyl -3 – [methoxy (phenyl) methylene] -2 – oxodihydroindole -6 – methyl formate (compound A) and 80.6g compound N – (4 – aminophenyl) – N, respectively. 4 -Dimethyl -1 18.2g – piperazine acetamide 45 – 50 C (25 – 30 C Compound 3h B), heating and 45 – 50 C temperature-2h raising to 1h 10:1 Drying, yield (3Z) -3 – {[ (4 – {methyl – [(4 – methylpiperaz -1 – yl) acetyl] amino} phenyl} amino} – (phenyl) methylene} -2 – oxo -2, 3 -dihydroindole -6 – methyl formate (compound C) 126.3g, CFC-91.37%,99.89%., 262368-30-9

262368-30-9 N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide 21927707, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Shiyao Group Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd.; Shiyao Group Enbipu Pharmaceutical Co., Ltd.; Wu Lihong; Liang Min; Zhong Wenhui; Zhang Sujuan; Li Dongmei; Wang Yue; Sun Wentao; Chi Xiaolei; (10 pag.)CN109988094; (2019); 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.170911-92-9,tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A mixture of 8-cyclopentyl-2-methanesulfinyl-6-(5-methyl-[1,3,4]oxadiazol-2-ylmethyl)-8H-pyrido[2,3-d]pyrimidin-7-one (185 mg, 0.495 mmol) and 4-(4-amino-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (247 mg, 0.892 mmol, 1.8 eq) were dissolved in DMSO (2.5 mL) and heated at 80 C. for 2 days. Succinic anhydride (70 mg) was added to react with the excess aniline and the mixture was heated at 80 C. for 3 h. The reaction mixture was partitioned between ethyl acetate and H2O. The organic layer was washed with saturated NaHCO3 (2×), H2O and brine, dried over Na2SO4 and concentrated to give an orange foam. Purification by liquid chromatography (2-4% MeOH/CH2Cl2) gave 4-{4-[8-cyclopentyl-6-(5-methyl-[1,3,4]oxadiazol-2-ylmethyl)-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidin-2-ylamino]-phenyl}-piperazine-1-carboxylic acid tert-butyl ester as a yellow foam (202 mg, 0.344 mmol, 70%). The structure was confirmed by NMR and mass spectrometry. MS: APCl: M+1: 587.1 (Exact Mass: 586.30)., 170911-92-9

The synthetic route of 170911-92-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; PFIZER INC; US2006/142312; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

655225-01-7,655225-01-7, tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 2-(5-chloro-2,4-dimethoxyphenyl)-7-(piperazin-1-yl)imidazo[1,2-a]pyridme 12 (200 mg, 0.50 mmol), tert-butyl 4-(2-bromoethyl)piperazine-1-carboxylate (160 mg, 0.53 mmol), and potassium carbonate ( 140 mg, 1.00 mmol) in acetonitriie (4 mL) was heated to reflux for 3 h. The reaction mixture was filtered and the filtrate was distilled under reduced pressure. The residue was purified by combi-flash chromatography (silica gel, 9: 1 DCM/MeOH) to afford tert-butyl 4-(2-(4-(2-(5-chloro-2,4- dimethoxyphenyl)imidazo[1 2-a]-pyridin-7-yl)piperazin-1-yl)ethyl)piperazine-1-carboxylate 13k (130 mg, 42percent) as a pale yellow solid. 1H NMR (400 MHz, CDCl3): delta 8.38 (s, 1H), 7.88 (d, J= 7.6 Hz, 1H), 7.86 (s, 1H). 6.80 (d, J= 7.5 Hz, 1H), 6.57 (s, 1H), 6.55 (dd, J=2.3, 7.6 Hz, 1H), 3.99 (s, 3H), 3.95 (s, 3H), 3.44 (t, J= 5.1 Hz, 4H), 3.24 (t, J= 5.1 Hz, 4H), 2.66 (t, J= 5.0 Hz, 4H), 2.61-2.54 (m, 4H), 2.44 (t, J= 5.0 Hz, 4H), 1.46 (s, 9H); HPLC ( Method 1) 99.0percent (AUC), tR = 9.55 min. ; ESI MS m/z 585 [M + H]+.

As the paragraph descriping shows that 655225-01-7 is playing an increasingly important role.

Reference：
Patent; ONCOTHERAPY SCIENCE, INC.; MATSUO, Yo; HISADA, Shoji; NAKAMURA, Yusuke; CHAKRABARTI, Anjan; RAWAT, Manish; RAI, Sanjay; SATYANARAYANA, Arvapalli, Venkata; DUAN, Zhiyong; TALUKDAR, Arindam; RAVULA, Srinivas; DECORNEZ, Helene; (491 pag.)WO2017/58503; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

170911-92-9, tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

mCPBA (<77% pure) (4.5 mg, assumed 0.020 mmol) in DCM (0.5 ml) was added to a stirred solution of 6- (2 , 6 -dichlorophenyl ) -8-methyl-2- (methylthio)pyrido [4 , 3 -d] pyrimidin-5 (6H) -one (6.1 mg, 0.017 mmol) in toluene (1.0 mL) at RT under nitrogen. After 1.5 h, DIPEA (9.0 mu-,, 0.052 mmol) and tert-butyl 4-(4- aminophenyl) piperazine-l-carboxylate (5.3 mg, 0.019 mmol) [commercially available] in toluene (0.5 ml) were added, successively, and the temperature was increased to 60 C. After 16 h, the reaction mixture was allowed to cool to RT, and was loaded directly onto a column and purified by flash chromatography (0-100%, EtOAc in cyclohexane) to give the title compound (5.4 mg, 54%) as a yellow oil. LCMS (Method A): RT = 1.61 min, m/z = 581, 583 [M+H]+ 170911-92-9, The synthetic route of 170911-92-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ALMAC DISCOVERY LIMITED; O’DOWD, Colin Roderick; ROUNTREE, James Samuel Shane; BURKAMP, Frank; WILKINSON, Andrew John; WO2014/167347; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

197638-83-8, 1-Boc-4-(4-Formylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Reference Example 21 4-[4-(t-Butoxycarbonyl)piperazin-1-yl]benzaldehyde and [3-(ethoxycarbonyl)propyl]triphenylphosphonium bromide were reacted in THF in the presence of potassium t-butoxide to obtain ethyl 5-{4-[4-(t-butoxycarbonyl)piperazin-1-yl]phenyl}-4-pentenoate, which was then subjected to catalytic reduction using palladium/carbon to obtain an objective compound., 197638-83-8

197638-83-8 1-Boc-4-(4-Formylphenyl)piperazine 2795509, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; YAMANOUCHI PHARMACEUTICAL CO. LTD.; EP1396487; (2004); 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.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

75336-86-6, Synthesis of (3R)-3-methyl-1-(phenyl(3-(trifluoromethyl)phenyl)-methyl)piperazine To a solution of (R)-(-)-2-methylpiperazine (2.2 g, 22 mmol) in CH3CN (20 mL) was added 1-(chloro(phenyl)methyl)-3-(trifluoromethyl)benzene (2.0 g, 7.4 mmol) and heated to 100° C. for 12 h and concentrated under vacuum. The residue was dissolved in CH2Cl2 (150 mL) and washed with 1N NaOH (150 mL). The organic layer was dried with K2CO3 or Na2SO4, filtered, and concentrated. The crude product was purified by ISCO using 0-20percent 2N NH3/MeOH solution in CH2Cl2 to give the title compound (2.00 g, 81percent yield) as oil. MS (ESI, pos. ion) m/z: 335.1 (M+1).

As the paragraph descriping shows that 75336-86-6 is playing an increasingly important role.

Reference：
Patent; Hitchcock, Stephen; Amegadzie, Albert; Qian, Wenyuan; Xia, Xiaoyang; Harried, Scott S.; US2008/4289; (2008); 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.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

75336-86-6, (R)-2-methylpiperazine (5.025 g, 50.2 mmol) was dissolved in DCM (100 mL). A solution of boc anhydride (5.47 g, 25.1 mmol) in DCM (50 mL) was added dropwise at 0 C. The reaction mixture was stirred at rt for 1 h. The solution was filtered and concentrated under reduced pressure. Water (100 mL) was added to the residue, which was filtered again. The filtrate was saturated with K2CO3 and extracted with Et2O (3×150 mL). The combined organic layers were dried over anhydrous Na2SO4, filtered and concentrated under reduced pressure to provide 5.04 g title compound (50%) as a solid. 1H NMR (300 MHz, CDCl3) delta ppm 1.03 (d, J=6.3 Hz, 3H) 1.45 (s, 9H) 1.56 (s, 1H) 2.30-2.46 (m, 1H) 2.65-2.72 (m, 1H) 2.74-2.76 (m, 2H) 2.93-2.95 (m, 1H) 3.93 (br s, 2H).

The synthetic route of 75336-86-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; US2010/216812; (2010); 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.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

74879-18-8, (S)-(+)-3-methyl-1-(2-nitrophenyl)-piperazine: To a solution of 2-bromonitrobenzene (0.600 g, 3.00 mmoi) in 1,4-dioxane (15 mL) was added (S)-(+)-2-methylpiperazine (0.500 g, 0.500 mmol) and powdered K2C03 (15.0 mmol, 1.50 g) and the resulting suspension was heated at reflux for 10 h. After the suspension was cooled, it was filtered through a sintered glass funnel and the solvent was removed in vacuo. The resulting residue was purified by column chromatography (1/1 hexane/EtOAc followed by 4/1 EtOAc/MeOH), giving (S)-(+)-3-methyl-1-(2-nitrophenyl)-piperazine as an orange oil (0.53 g, 80%).

As the paragraph descriping shows that 74879-18-8 is playing an increasingly important role.

Reference：
Patent; Borowsky, Beth; Blackburn, Thomas P.; Ogozalek, Kristine; US2003/82623; (2003); 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.181955-79-3,1,4-Di-Boc-piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.,181955-79-3

The resulting 1,4-di-tert-butoxycarbonylpiperazine-2-carboxylic acid (13-2) (500 mg, 1.5 mmol)Was dissolved in dry THF (10 mL)Under nitrogen protection,After borane tetrahydrofuran (4.5 mL, 4.5 mmol) was added dropwise,Heated to 40 for 2 hours,Cold to 0 ,The reaction was quenched by the dropwise addition of methanol and the reaction was concentrated to dryness to give 470 mg of 1,4-di-tert-butoxycarbonyl-2-hydroxymethylene-piperazine (13-3) in a yield of 98%

The synthetic route of 181955-79-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Fujian Jinle Pharmaceutical Technology Co., Ltd.; Zhou Zhongxiang; Xing Yuanyuan; Chen Yingzhong; Deng Chengjun; Deng Honggui; Xue Wanhua; Zhang Shuzu; Chen Weipeng; Li Fang; (27 pag.)CN107174584; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics