Month: June 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: To the chloro compounds (1.00 mmol) in toluene, were added piperazines 8a-j (1.0 mmol) at room temperature. The reaction mixture was heated at 110 oC for overnight. After completion (TLC), the reaction mixture was extracted with ethyl acetate and water. The organic layer was separated and dried over anhydrous Na2SO4, evaporated to dryness. The residue was purified with column chromatography using an eluent of 25% ethyl acetate in hexane to furnish the compounds with moderate to good yields (64-82%).

30459-17-7, As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference：
Article; Banu, Saleha; Bollu, Rajitha; Naseema, Mohammad; Gomedhika, P. Mary; Nagarapu, Lingaiah; Sirisha; Kumar, C. Ganesh; Gundasw, Shravan Kumar; Bioorganic and Medicinal Chemistry Letters; vol. 28; 7; (2018); p. 1166 – 1170;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1235865-77-6, 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (7:3) acetone-methanol (3 mL), 2-((lH-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4- (4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro[l,l’-biphenyl]-2-yl)methyl)piperazin-l- yl)benzoic acid (0.5 g) and dicyclohexylamine (0.19 g) was stirred at 20-30 degree Celsius for 3-4h. The resulting slurry was filtered, washed with (7:3) acetone-methanol (2 mL) and the solid was dried under vacuum at 40-50 degree Celsius for 16 h to furnish 2-(( lH-pyrrolo[2, 3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3, 4,5,6- tetrahydro[l, l’-biphenyl]-2-yl)methyl)piperazin- l-yl)benzoic acid dicyclohexylamine salt. Yield: 60.6 % (0.4 g) HPLC Purity: 97.2 % 1H NMR (DMSO-d6): d 0.93 (s, 6H), 1.08 (m, 6H), 1.15 (m, 4H), 1.39 (t, J=6.0, 6.4 Hz, 2H), 1.50 (d, J=l2.4 Hz, 2H), 1.60 (d, J=l3.2 Hz, 4H), 1.77 (d, J=l0.8 Hz, 4H),2.l6 (m, br, 6H) 2.58 (m, 2H), 2.73 (s, 2H), 3.04 (s, 4H), 6.31 (d, J=2.8 Hz, 2H), 6.64 (d, J=7.6, Hz, 1H), 7.04 (d, J=8.0 Hz, 2H), 7.33 (d, J=8.0 Hz, 3H), 7.41 (s, 1H), 7.60 (d, J=8.8 Hz, 1H), 7.95 (d, J=2.0 Hz, 1H), 11.55 (s, 1H, NH)

1235865-77-6, As the paragraph descriping shows that 1235865-77-6 is playing an increasingly important role.

Reference：
Patent; FRESENIUS KABI ONCOLOGY LTD.; GUPTA, Chandan Kumar; DHIMAN, Navdeep; SANGHANI, Sunil; SINGH, Govind; LAHIRI, Saswata; CABRI, Walter; GUPTA, Nitin; (0 pag.)WO2020/3272; (2020); 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.

To a stirred solution of tert-butyl 4-(2-chloroethyl)piperazine-l -carboxylate (9.7 g, 38.9 mmol) in ethanol (25 ml) was added hydrazine hydrate (19.5 ml, 38.9 mmol) and resulting recation mixturte was heated to 60 C for 3h. The solvent was evaporated under reduced pressure, diluted with water, extracted with diethyl ether (75 ml x 4) and the organic extract was dried over Na2S04 and concentrated under reduced pressure to give 9.6 g of the desired product as colorless oil. lH NMR (400 MHz, DMSO-ifc): delta 1.45 (s, 9H), 2.38-2.45 (m, 4H), 2.52 (t, J = 6.0 Hz, 2H), 2.88 (t, J = 6.0 Hz, 2H), 3.04 (br, s, 3H), 3.39-3.69 (m, 4H).

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：
Patent; GLENMARK PHARMACEUTICALS S.A.; KUMAR, Sukeerthi; CHAUDHARI, Sachin Sundarlal; GHARAT, Laxmikant Atmaram; KHAIRATKAR-JOSHI, Neelima; SHAH, Daisy Manish; MUKHOPADHYAY, Indranil; (327 pag.)WO2018/203298; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5308-25-8

General procedure: A mixture ofdifferent fluoro substituted 2-nitrobenzoate (1.5 mmol) and various amines (7.5 mmol) in DMF (3 mL) was stirred atroom temperature for 2 h. The reaction mixture was diluted with water and extracted with ethyl acetate. The organic phase was washed with water and brine. After dried by sodium sulfate and concentration, the residue was purified by chromatography on silica gel to give as yellowish solid.

The synthetic route of 5308-25-8 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Fan, Jun; Dai, Yang; Shao, Jingwei; Peng, Xia; Wang, Chen; Cao, Sufen; Zhao, Bin; Ai, Jing; Geng, Meiyu; Duan, Wenhu; Bioorganic and Medicinal Chemistry Letters; vol. 26; 11; (2016); p. 2594 – 2599;,
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.479353-63-4,1-Boc-4-(4-Carboxybenzyl)piperazine,as a common compound, the synthetic route is as follows.

A mixture of compound 16 (Het=3-methylisoxazol-5-yl, 150 mg, 0.42 mmol), compound 7a (134 mg, 0.42 mmol) and HATU (159 mg, 0.42 mmol) in DMF (2 mL) was cooled to 0C and DIPEA (217 mg, 1.68 mmol) was added. The reaction mixture was allowed to warm to room temperature and stirred for 15 min. Saturated aqueous sodium bicarbonate was added and the resulting mixture was extracted with ethyl acetate. The combined extracts were dried over anhydrous sodium sulfate and concentrated. The residue was purified by flash column chromatography on silica gel (Petroleum ether/ethyl acetate = 1 : 1 to ethyl acetate) to afford compound Boc-806 (180 mg, 65.2% yield) as a solid. HCl/EtOAc (2N, 1 mL) was added to a solution of Boc-806 (97 mg, 0.147 mmol) in EtOAc (1 mL) at 0C with stirring. The reaction mixture was stirred for 1 h and the resulting precipitate was collected by filtration, washed with DCM and dried to afford compound 806 (HC1 salt, 80 mg, 100% yield) as a yellow solid.

479353-63-4, As the paragraph descriping shows that 479353-63-4 is playing an increasingly important role.

Reference：
Patent; INHIBIKASE THERAPEUTICS, INC.; WERNER, Milton, H.; KELLY, Terence, A.; (74 pag.)WO2016/172528; (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.

Step A: To a solution of pentafluorophenol in 520 mL of anhydrous ether at 0 C. there are added in succession 49 g of 1-ethyl-3-(3′-dimethylaminopropyl)-carbodiimide (286 mmol) in portions and 12 mL of formic acid (312 mmol). The whole is stirred at ambient temperature for 2 hours. There is subsequently added a mixture of 32 g of 1-tert-butyl 3-methyl 1,3-piperazinedicarboxylate (130 mmol) and 18 mL of triethylamine (130 mmol) in solution in 520 mL of CH2Cl2. The whole is stirred overnight at ambient temperature. The reaction mixture is hydrolysed with an 1N aqueous HCl solution and extracted with CH2Cl2. The organic phases are subsequently combined and then washed with a saturated aqueous NaHCO3 solution and then with a saturated aqueous NaCl solution until neutral. After drying over MgSO4, filtration and concentration to dryness, the product is isolated by chromatography over silica gel (petroleum ether/AcOEt gradient: 0-30%). The title product is obtained in the form of an oil. IR: nu: C=O: 1674-1745 cm-1 m/z (C12H20N2O5): 272.1 (M+); 295.121 (M+Na)+; 567.253 (2M+Na)+

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

Reference：
Patent; Le Diguarher, Thierry; Casara, Patrick; Starck, Jerome-Benoit; Henlin, Jean-Michel; Davidson, James Edward Paul; Murray, James Brooke; Graham, Christopher John; Chen, I-Jen; Geneste, Olivier; Hickman, John; Depil, Stephane; Le Tiran, Arnaud; Nyerges, Miklos; De Nanteuil, Guillaume; US2015/51189; (2015); 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.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.,934-98-5

Example 53: -r2-(4-methv.-piDerazin-1 -vn-ethvi1-3-r3-(5-thioDhen-3-vi-Dvrimidin-2-viamino)-Dhenvt1-urea; To a stirring solution of W (100 mg, 0.23 mmol) in CH2CI2 (20 mL) was added J (33 mg, 0.23 mmol) followed by triethylamine (32 muL, 0.23 mmol). The solution was stirred at room temperature for 12 hours where the reaction was diluted with CH2Cl2 (50 mL) and washed with 2N NaOH (2 x 50 mL), water (2 x 50 mL) and brine (2 x 50 mL). The organics were dried over Na2S04 and concentrated in vacuo. The residue was purified using column chromatography (silica gel, 5percent MeOH in CH2CI2). The fractions containing product were evaporated to dryness under vacuum to yield compound 53 in 45percent yield as a white solid. (at)H NMR (300 MHz, CD30D) No. 2.27 (s, 3H), 2.33-2.55 (m, 7.01-7.02 (m, 1H), 7.04-7.05 (m, 2H), 7.43 (d, 1 H), 7.45 (d, 1 H), 7.64 (d, 1 H), 7.86 (d, 1 H), 8.72 (s, 2H). MS m/z 438 [M++1].

As the paragraph descriping shows that 934-98-5 is playing an increasingly important role.

Reference：
Patent; SUGEN, INC.; WO2005/113548; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

475272-54-9, (S)-1-Boc-3-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

N’N- to carbonyl diimidazole (1.10g, 6.57mmol) in anhydrous DMF (2mL) was added dropwise a solution oftriethylamine (1.10mL, 7.88 mmol) and (S) -1-BOC-3- isopropyl-piperazine (1.00g, 4.38mmol) in anhydrousDMF (2mL) solution at room temperature in a sealed tube 50 min, adding anhydrous methanol (12mL), 80 Cthe reaction 48h, the solvent was removed, a saturated sodium chloride solution (10mL × 3), dried B Acetate(15mL × 2) and the combined organic phases, Na 2 SO 4 dried over anhydrous solvent removed concentratewas separated by column chromatography (leaching Lotion: Petroleumether / EtOAc (v / v) = 4/1), to give339mg of colorless liquid: 4-tert-butoxycarbonyl -2- (S) – isopropyl-piperazin-1-A Methyl, yield: 27%.

475272-54-9, 475272-54-9 (S)-1-Boc-3-Isopropylpiperazine 24820348, apiperazines compound, is more and more widely used in various fields.

Reference：
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.115761-79-0,1-(2,4-Difluorophenyl)piperazine,as a common compound, the synthetic route is as follows.

EXAMPLE 2 2-[4-(2,4-Difluorophenyl)piperazin-1-yl]ethanol Formula IX: n=2, STR13 A solution of 72 g of 4-(2,4-difluorophenyl)piperazine and 50 g of 2-bromoethanol in 300 ml of xylene containing 55 ml of triethylamine is heated under reflux for 6 hours. The solution is then cooled and ether is added. The precipitate of triethylamine hydrobromide formed is filtered off and the filtrate is concentrated in vacuo. The residue obtained is then crystallized from an isopropyl ether/pentane mixture. The crystals are filtered off, washed with the same mixture and then dried. 60 g of 2-[4-(2,4-difluorophenyl)piperazin-1-yl]ethanol are thus recovered in the form of crystals melting at 54 C., 115761-79-0

115761-79-0 1-(2,4-Difluorophenyl)piperazine 2734637, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Centre D’Activite Et De Recherches Pharmaceutique Industrielle Biologique Medicale; US4886805; (1989); 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.162046-66-4,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

A mixture of compound 3 (100 mg, 0.33 mmol),compound 6 (131 mg, 1.4 eq.) and EDCI (250 mg, 4.0 eq.) in pyridine (5 ml) were stirred at room temperature overnight. It was concentrated and extracted with EA (2×70 ml), washed by brine (2×60 ml). It was purified by prep-TLC (PE:EA=1:2). Compound 7 (126 mg, Yield: 67%) was obtained as a white solid., 162046-66-4

As the paragraph descriping shows that 162046-66-4 is playing an increasingly important role.

Reference：
Patent; Regenacy Pharmaceuticals, LLC; van Duzer, John H.; Mazitschek, Ralph; (123 pag.)US2018/141923; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics