Month: July 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

Cbz lnt-1 a A mixture of 5-fjiioro-2-nitrobenzaldehyde (20 g, 118 mmol) in DMF (150 mL), benzyl 1-piperazine carboxylate (31.2 g, 142 mmol), and triethylamine (14.3 g,142 mmol) was heated to 80 °C for 15 hours. After cooling to room temperature, the reaction mixture was diluted with EtOAc (300 mL), washed with brine (3 x 150 mL), dried over Na2S04, filtered, and concentrated. The resulting thick oil was purified by a flash column, eiuting with 20percent EtOAc/hexanes to yield 36.2 g (86percent) of Int-la as a yellow solid., 31166-44-6

The synthetic route of 31166-44-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SCHERING CORPORATION; XIAO, Dong; PALANI, Anandan; ASLANIAN, Robert, G.; DEGRADO, Sylvia; HUANG, Xianhai; ZHOU, Wei; SOFOLARIDES, Michael; CHEN, Xiao; WO2011/75375; (2011); 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.208167-83-3,tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

General procedure: A mixture of compound 9 (200mg, 0.8mmol), sodium iodine (289mg, 1.93mmol) and substituted amines (1.61mmol) in methanol (30mL) was stirred at 40C for 5h. After the reaction was completed (monitored by TLC), the solution was concentrated under vacuum. Then the crude residue was purified by column chromatography (dichloromethane/methanol), affording pure product 10., 208167-83-3

208167-83-3 tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate 22106269, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Liang, Yu-Kun; Yue, Zhi-Zhou; Li, Jia-Xin; Tan, Cun; Miao, Ze-Hong; Tan, Wen-Fu; Yang, Chun-Hao; European Journal of Medicinal Chemistry; vol. 84; (2014); p. 505 – 515;,
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.142-64-3,Piperazine Dihydrochloride,as a common compound, the synthetic route is as follows.

A solution of 1-5 – [(3,4-dihydro-4-oxo-l-phthalazinyl) methyl] -2- fluorobenzoic acid (60.0 g, 0.20 mol)Suspended in 600 mL of acetonitrile,Anhydrous piperazine (43.0 g, 0.50 mol)Piperazine dihydrochloride (79.0 g, 0.50 mol)Concentrated sulfuric acid (2.78 ml, 0.04 mol)Heated to 78-80 C under reflux for 7 to 8 hours,Drop to room temperature,Concentrated under reduced pressure acetonitrile, water was added 1000ml, stirred for 30min; concentrated ammonia was added dropwise to a PH value of 7-8, stirred 2h, suction filtration,44.1 g of 1- [5 – [(3,4-dihydro-4-oxo-1-phthalazinyl) methyl] -2-fluorobenzoyl] piperazine was obtained in a yield of 60.1%.1- [5 – [(3,4-dihydro-4-oxo-1-phthalazin-yl) methyl] -2-fluorobenzoyl] piperazine 1H NMR, (400 MHz) see Figure 1., 142-64-3

142-64-3 Piperazine Dihydrochloride 8893, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Shanghai Pharmaceutical Group Co., Ltd.; Deng Yu; (7 pag.)CN106554316; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

694499-26-8, Pyridine (163 ul, 2.01 mmol) and 4-nitrophenyl chloroformate (Combi-Blocks, CatNo. OT-0341, CAS [7693-46-1]) (369 mg, 1.83 mmol) were added to the mixed solution comprising 4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (AK Scientific Co., CatNo. AK-83227, CAS [694499-26-8]) (500 mg, 1.83 mmol) and CH2Cl2 (10 ml), followed by stirring at room temperature for 3 hours. The reaction mixture was concentrated. The obtained residue was treated with diethyl ether. As a result, a target compound was obtained as a brown solid (611 mg, 76% yield). MS m/z: 439[M+H]

As the paragraph descriping shows that 694499-26-8 is playing an increasingly important role.

Reference：
Patent; DAEGU-GYEONGBUK MEDICAL INNOVATION FOUNDATION; Choi, Hwan Geun; Son, Jung Beom; Kim, Shinae; Lee, Seungyeon; Ko, Eunhwa; Cho, Joongheui; Kang, Seock Yong; Kim, So Young; Park, Jin-Hee; Ko, Yi Kyung; Ryu, Hee Yoon; Kim, Nam Doo; Kim, Hyunkyoung; Lee, Younho; Lee, Sun-Hwa; Kim, Dayea; Lee, Sun Joo; Hong, Seongho; Min, Sang Hyun; Lee, Sungwoo; Choi, Dong Kyu; Bae, Jae Hyun; Hong, Eunmi; Jang, Tae-ho; Song, Jaeyoung; Kim, Sangbum; Yoon, Suk Kyoon; (108 pag.)US2019/315738; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Descriptions 150 (S)-tert-butyl 4-(5-chloro-2-methyl-3-nitrobenzyl)-2-methylpiperazine-1-carboxylate (DiSO)To a solution of 5-chloro-2-methyl-3-nitrobenzaldehyde (D143, 20 g) in DCM (260 mL), (S)-tertbutyl 2-methylpiperazine- 1 -carboxylate (24.08 g) was added. The mixture was stirred for 10 mm atroom temperture, sodium triacetoxyhydroborate (25.4 g) was added portionwise. The reaction mixtiure was stirred overnight at 20 C. The mixture was washed with brine, dried with anhydrous Na2SO4. Filtered, the filtrate was concentrated to give crude product, which was purified by column chromatography (silica gel, petroleum ether/EtOAc = 20:1) to afford the title compound (37 g) as white solid. MS (ESI): C18H26C1N3O4 requires 383; found 384 [M+Hf., 169447-70-5

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXOSMITHKLINE (CHINA) R&D COMPANY LIMITED; DENG, Jing; LEI, Hui; MA, Xin; LIN, Xichen; WO2015/180612; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109384-27-2, 1-Methylpiperazin-2-one hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A solution of tert-butyl 3-oxa-7,9-diazabicyclo [3.3.1 jnonane-9-carboxylate(1 g, 4.38 mmol) 2-fluoro-5-iodopyridine (1.12 g, 5.04 mmol), and sodium carbonate (0.84 g,7.88 mmol) in 1-Methyl-2-pyrrolidinone (4 ml) was heated at 85 C overnight. The mixture wascooled to room temperature, diluted with water and extracted into DCM. The organic extract was dried over Na2SO4 filtered and concentrated under reduced pressure. The residue waspurified by silica chromatography to yield Sia (1.57 g, 62.3%). MS (ESI) mlz 431.9 [M+Hj . 1HNMR (400 MHz, Chloroform-d) oe 8.30 (dd, J = 2.4, 0.7 Hz, 1H), 7.66 (dd, J = 9.0, 2.3 Hz, 1H), 6.44 (d, J = 9.0 Hz, 1H), 4.25 (d, J = 12.7 Hz, 1H), 4.21 – 4.00 (m, 3H), 3.97 – 3.86 (m,2H), 3.80 (t, J= 11.9 Hz, 2H), 3.26 (t, J= 15.1 Hz, 2H), 1.48 (s, 9H)., 109384-27-2

109384-27-2 1-Methylpiperazin-2-one hydrochloride 17060766, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; GILEAD SCIENCES, INC.; BACON, Elizabeth M.; CHIN, Elbert; COTTELL, Jeromy J.; KATANA, Ashley Anne; KATO, Darryl; LINK, John O.; SHAPIRO, Nathan; TREJO MARTIN, Teresa Alejandra; YANG, Zheng-Yu; (395 pag.)WO2018/145021; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: A mixture of 2-chloro-N-(5-methyl/ethyl-1,3,4-thiadiazol-2-yl)acetamide (1a or 1b) (2.6 mmol), appropriate piperazine derivatives (2.6 mmol) and potassium carbonate (2.6 mmol, 0.363 g) as acatalytic agent were stirred in acetone (100 mL) for 5 h at 25 °C. The mixture was filtered to remove potassium carbonate and acetone was evaporated. The residue was recrystallized from EtOH.

4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Can, Nafiz nc; Can, zg r Devrim; Osmaniye, Derya; Zkay, mide Demir; Molecules; vol. 23; 4; (2018);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,694499-26-8

General procedure: To amixture of substituted benzoic acid obtained in the last step (0.12 mmol) in 5mL DMF, 2-(7-aza-1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluroniumhexafluorophosphate (HATU, 0.18 mmol), ethyldiisopropylamine (DIPEA, 0.24 mmol)and 4-((4-methylpiperazin-1-yl)methyl)-3- (trifluoromethyl)aniline (0.1 mmol)was added. The resulting mixture was stirred at room temperature overnight. Thenthe reaction was extracted with ethyl acetate, washed with brine, dried overanhydrous Na2SO4, filtered and concentrated to give thecrude product, which was further purified by column chromatography to affordthe final compounds.

694499-26-8 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 46838908, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Han, Mei; Li, Shan; Ai, Jing; Sheng, Rong; Hu, Yongzhou; Hu, Youhong; Geng, Meiyu; Bioorganic and Medicinal Chemistry Letters; vol. 26; 23; (2016); p. 5679 – 5684;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6-Chloropyridine-2-carbonitrile (250 mg, 1.8 mmol) and tert-butyl (2S)-2- methylpiperazine-1-carboxylate (433 mg, 2.17 mmol) were added to a reaction tube with DIPEA (377 pi, 2.17 mmol) in DMF (2.5 ml). The tube was then sealed and the reaction stirred at 80 C for 20 hours. The reaction mixture was concentrated in vacuo and the residue was partitioned between EtOAc (25 ml) and sat aq NaHCO3 (25 ml). The organics were separated and the aqueous phase extracted with EtOAc (2 x 20 ml). The combined organics were washed with water (20 ml), brine (20 ml), dried over MgSO4 and filtered. The filtrate was concentrated in vacuo and the residue was purified via flash column chromatography (gradient of 0 – 100% EtOAc in heptane followed by 0-100% MeOH in EtOAc). The product-containing fractions were combined and concentrated in vacuo to give the title compound as a yellow oil (321 mg, 51 %).1HNMR(500 MHz, Chloroform-d) 7.51 (dd, J = 8.8, 7.2 Hz, 1H), 6.96 (d, J = 7.1 Hz, 1H), 6.76 (d, J = 8.8 Hz, 1H), 4.32 (s, 1H), 4.11 (s, 1H), 4.03 -3.88 (m, 2H), 3.36-3.19 (m, 2H), 3.11 – 2.98 (m, 1H), 1.48 (s,9H), 1.17 (d, J = 6.7 Hz, 3H).LCMS Method 2 – Tr = 1.23 mm (ES+) (M+H)+ 288.0, 169447-70-5

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NAVITOR PHARMACEUTICALS, INC.; O’NEILL, David John; SAIAH, Eddine; KANG, Seong Woo Anthony; BREARLEY, Andrew; BENTLEY, Jonathan; (565 pag.)WO2018/89433; (2018); 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.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

103-76-4, Benzylchloroformate (4.72g, 27.69mmol) in acetonitrile (30mL) was added dropwise over 30min to a solution of 1-(2-hydroxyethyl)piperazine (3g, 23.08mmol) in water (30mL) via an isobar cylindrical funnel. The pH was maintained around 8-9 by addition of 4N NaOH. The reaction was stirred overnight at room temperature. The mixture was first extracted with dichloromethane (100mL) in order to remove the fully protected compound and then acidified with 4N HCl. The acidic aqueous phase was extracted twice with dichloromethane (2×100mL). The organic phase was washed with brine and dried over anhydrous Na2SO4. The solvent was removed in vacuum and the crude was purified by flash chromatography (0-8% of methanol in dichloromethane) to afford 22 (5.41g, 88.8%) as a colorless oil. 1H NMR (400MHz, DMSO-d6): delta 7.37-7.29 (m, 5H, CHarom.), 5.05 (s, 2H, CH2Phi), 4.41 (s, 1H, OH), 3.47 (m, 2H, HOCH2), 3.35 (m, 4H, (CH2)2NCO), 2.38-2.35 (m, 6H, CH2N, CH2NCH2). 13C NMR (100.6MHz, DMSO-d6): delta 155.04, 137.59, 129.09 (2C), 128.49, 128.22 (2C), 66.81, 60.82, 59.14, 53.51 (2C), 44.16 (3C). MS (ESI) m/z 265.02 (M+H)+.

103-76-4 N-(2-Hydroxyethyl)piperazine 7677, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Denoyelle, Severine; Chen, Ting; Yang, Hongwei; Chen, Limo; Zhang, Yingzhen; Halperin, Jose A.; Aktas, Bertal H.; Chorev, Michael; European Journal of Medicinal Chemistry; vol. 69; (2013); p. 537 – 553;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics