Month: June 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

4-Cyclopropylmethyl-piperazine-1-carboxylic Acid 4-(5-trifluoromethyl-pyridin-2-yloxy)-phenyl Ester The hydrochloride of the title compound was prepared from 4-(5-trifluoromethyl-pyridin-2-yloxy)-phenyl chloroformate and 1-cyclopropylpiperazine, yield 62%. Recrystallisation from 0.2 M HCl gave white crystals, m.p. 238-239 C.; 1H NMR (DMSO-d6): delta 11.51 (br s, 1H), 8.61-8.55 (m, 1H), 8.30-8.20 (m, dd, 1H), 7.32-7.19 (m, d+s, 5H), 4.44-4.00 (br, 2H), 3.80-3.40 (br m, 4H), 3.29-2.93 (br m, 4H), 1.28-1.05 (br m, 1H), 0.75-0.58 (m, 2H), 0.50-0.35 (m, 2H).IR (KBr): nu 1730, 1713 (C=O) cm-1.

20327-23-5, The synthetic route of 20327-23-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Ebdrup, Soren; de Jong, Johannes Cornelis; Jacobsen, Poul; Hansen, Holger Claus; Vedso, Per; US2003/166644; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4) Preparation of benzyl 3-oxopiperazine-1-carboxylate 1.4; 10 g of piperazin-2-one and 90 g of sodium carbonate were dissolved in 250 ml of water; 500 ml of ethyl acetate were added to this solution, and 20.45 g of benzyl chloroformate were added dropwise with vigorous stirring. After the addition had ended, the mixture was stirred at room temperature overnight. For workup, the organic phase was removed, dried over magnesium sulfate, filtered and concentrated under reduced pressure. This afforded benzyl 3-oxopiperazine-1-carboxylate 1.4. Molecular weight 234.10 (C12H14N2O3); retention time Rt=1.18 min. [B]; MS (ESI): 235.11 (MH+)., 5625-67-2

As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

Reference：
Patent; SANOFI-AVENTIS; US2011/46105; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To mixture of (2S)(‘/WJ-5-(-1-(tert-butoxy)-2-methoxy-2-oxoethyl)-4-(8-fluoro-5-methylchroman- 6-yl)-1 ,6-dimethyl-1 H-pyrrolo[2,3-b]pyridine-2-carboxylic acid (30 mg, 0.060 mmol) and 1- cyclopentylpiperazine (8.67 pL, 0.060 mmol) in ethyl acetate (1 mL) was added DIEA (0.026 mL, 0.150 mmol) followed by addition of 1-propanephosphonic acid cyclic anhydride (T3P) (0.072 mL, 0.120 mmol) as a 50% solution in ethyl acetate and stirred at room temperature for 30 min. Diluted with ethyl acetate, added water and saturated ammonium chloride and extracted with ethyl acetate. Organic phase was washed with brine, dried over IS^SC^, filtered and concentrated to give (2S (7WJ-methyl 2-(tert-butoxy)-2-(2-(4-cyclopentylpiperazine-1-carbonyl)-4- (8-fluoro-5-methylchroman-6-yl)-1 ,6-dimethyl-1 H-pyrrolo[2,3-b]pyridin-5-yl)acetate (37 mg, 97% yield) as a colorless oil. 1H NMR (400 MHz, CHLOROFORM-d) delta = 6.74 (br. s., 1 H), 5.99 (br. s., 1 H), 5.14 (s, 1 H), 4.32 (t, J=5.0 Hz, 2 H), 3.93 (br. s., 3 H), 3.78 – 3.88 (m, 1 H), 3.59 (s, 3 H), 2.78 – 2.86 (m, 3 H), 2.74 (br. s., 2 H), 2.53 (br. s., 2 H), 2.17 (br. s., 2 H), 1.89 (br. s., 2 H), 1.78 (s, 3 H), 1.57 (br. s., 12 H), 1.06 – 1.17 (m, 9 H); LC/MS (m/z) ES+ = 635 (M+1)

21043-40-3, The synthetic route of 21043-40-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; VIIV HEALTHCARE UK LIMITED; DE LA ROSA, Martha Alicia; JOHNS, Brian, Alvin; KAZMIERSKI, Wieslaw, Mieczyslaw; SAMANO, Vicente; SUWANDI, Lita; TEMELKOFF, David; VELTHUISEN, Emile; WEATHERHEAD, Jason, Gordon; WO2014/9794; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

3022-15-9, Piperazine-2-carboxylic acid dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

N: l,4-bis(tert-butoxycarbonyl)piperazine-2-carboxylic acid 25. To an aqueous solution of Na2C03 (40 g, 380 mmol, in 200 mL of water) at room temperature was added piperazine-2- carboxylic acid dihydro chloride (either an enantiomeric mixture or a specific stereoisomer) (24; 10 g, 50 mmol), followed by di-ieri-butyl dicarbonate (41 g, 183 mmol) in tetrahydrofuran (200 mL). The reaction mixture was stirred at room temperature for 20 hours and then the volatiles were removed under reduced pressure. The resulting mixture was then extracted with diethyl ether (100 mL). The aqueous layer was treated with 3.0 M HC1 until it was slightly acidic (pH = 4) and then extracted with ethyl acetate (150 mL). The organic layer was washed with brine, dried over anhy. Na2SC>4, filtered, and concentrated to afford 16 g of the title compound as a white solid., 3022-15-9

3022-15-9 Piperazine-2-carboxylic acid dihydrochloride 2723757, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; AGIOS PHARMACEUTICALS, INC.; CAO, Sheldon; POPOVICI-MULLER, Janeta; SALITURO, Francesco G.; SAUNDERS, Jeffrey; TAN, Xuefei; TRAVINS, Jeremy; YAN, Shunqi; YE, Zhixiong; WO2012/171506; (2012); 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.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.

At room temperature 1-cyclopropane carboxylic acid piperazine (2.37g, 15.37mmol) and p-formyl benzene boronic acid (1.92g, 12.81mmol) Was dissolved in dichloromethane (40ml), stirred for 1 hour at room temperature, again was added sodium cyanoborohydride (1.77g, 28.18mmol), Was stirred at room temperature until the reaction is complete as monitored by TLC, water was added 20ml, extracted with dichloromethane, washed with saturated brine twice, The organic phase was dried over anhydrous magnesium sulfate, and concentrated under reduced pressure, to give: (4-benzyl-acid – piperazin-1-yl) – cyclopropyl – methanone, (1.6 g of, White solid), yield: 43.4%, was used directly in the next reaction., 59878-57-8

The synthetic route of 59878-57-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SHANGHAI CDYMAXPHARMACEUTICALS CO LTD; An, Xiao Xia; Bie, Ping Yan; Liu, Jun; Yang, Wuli; (43 pag.)CN103087077; (2016); B;,
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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Reference Example 10 benzyl 3-methylpiperazine-1-carboxylate A 4 g portion of 2-methylpiperazine was dissolved in 40 ml of dichloromethane, and 1.71 g of benzyl chloroformate was added dropwise thereto at -78 C. After 1 hour of stirring, the mixture was washed by adding water and dried and then the solvent was evaporated to obtain 2.0 g of the title compound.

109-07-9, As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference：
Patent; Yamanouchi Pharmaceutical Co. Ltd.; US6673799; (2004); B1;,
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

2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)benzoic acid (5) was synthesized by the method reported. [Nat Med. 2013, 19(2): 202-8] To a solution of compound 5 (100 mg, 0.175 mmol) in anhydrous dichloromethane, compound 4g (68 mg, 0.175 mmol), EDCI (167 mg, 0.875 mmol) and DMAP (25.6 mg, 0.21 mmol) were added. Afterwards, the mixture solution was stirred for 24 h at room temperature. Completion of the reaction was confirmed by TCL. The reaction mixture was washed with HCl (1 M), NaHCO3 saturated solution and brine, concentrated and purified to afford 6g (160 mg, 85% yield) as a yellow solid. 1H NMR (300 MHz, DMSO-d6) delta 11.70 (s, 1H), 8.64 – 8.49(m, 2H), 8.03 (d, J= 2.4 Hz, 1H), 7.86 – 7.74 (m, 1H), 7.56 – 7.45 (m, 3H), 7.33 (d, J = 8.2 Hz, 2H), 7.03 (d, J = 8.5 Hz, 3H), 6.67 (d, J = 8.0 Hz, 1H), 6.38 (s, 1H), 6.19 (s, 1H), 4.03 (q, J = 7.1 Hz, 2H), 3.09 (s, 4H), 2.79 (s, 2H), 2.23 (m, 8H), 1.94 (s, 2H), 1.67 – 1.48 (m, 4H), 1.42 – 1.23 (m, 10H), 1.15 (t, J = 7.1 Hz, 3H), 0.91 (s, 6H). MS (ESI) m/z: 940.71 [M+H]+, 938.77 [M-H]-., 1235865-77-6

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 66713100, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Zhou, Ruolan; Fang, Shaoyu; Zhang, Minmin; Zhang, Qingsen; Hu, Jian; Wang, Mingping; Wang, Chongqing; Zhu, Ju; Shen, Aijun; Chen, Xin; Zheng, Canhui; Bioorganic and Medicinal Chemistry Letters; vol. 29; 3; (2019); p. 349 – 352;,
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.

General procedure: To a solution of 3 (100 mg, 0.23 mmol) in acetonitrile (CH3CN, 30 mL) was added thecorresponding arylpiperazine (1.2 equiv.) and potassium carbonate (6.0 equiv.). The reaction mixturewas stirred at reflux for 16 h. After cooling to ambient temperature, the reaction mixture was filteredthrough a Buchner funnel. After filtration, the filtrate was concentrated in vacuo and the residue waspuried by silica gel column chromatography using ethyl acetate/petroleum ether (1/4,v/v) as eluentto afford the corresponding products (4-21).

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

Reference：
Article; Chen, Hong; Xu, Bing-Bing; Sun, Tao; Zhou, Zhan; Ya, Hui-Yuan; Yuan, Mu; Molecules; vol. 22; 11; (2017);,
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.216144-45-5,4-(4-Methylpiperazin-1-yl)benzylamine,as a common compound, the synthetic route is as follows.

Stage 3: 3-isobutyl-1-[4-(4-methylpiperazin-1-yl)benzyl]imidazo[2,1-b]quinazoline-2,5(1H,3H)-dione hydrochloride[4-(4-methylpiperazin-1-yl)benzyl]amine (194 mg) is added to methyl 2-(2-chloro-4-oxoquinazolin-3(4H)-yl)-4-methylpentanoate (150 mg) in anhydrous THF (2 mL) placed in a ?Biotage? reaction tube. The tube is sealed with a cap, stirred at ambient temperature for 1 hour then placed in a ?Biotage? micro-wave and heated under magnetic stirring at 150 C. for 1 hour. The mixture is concentrated under reduced pressure at 40 C. Purification by flash chromatography on silica gel (eluent: dichloromethane/methanol 95:5) produces the expected compound in the form of the free base. The corresponding hydrochloride salt is formed by adding a 1N HCl solution in ethyl ether to the solution of the free base in ethyl acetate. The precipitate obtained is filtered and dried in order to produce the expected hydrochloride compound (145 mg, 60% yield from Stage 2).MS/LC: calculated MM=445.6; m/z=446.3 (MH+)NMR (1H, 400 MHz, DMSO-d6): delta0.81 (m, 6H), 1.80 (m, 1H), 2.01 (m, 2H), 2.77 (s, 3H), 3.06 (m, 4H), 3.40 (m, 2H), 3.77 (m, 2H), 4.79 (AB, 1H), 4.81 (AB, 1H), 4.93 (t, 1H), 6.96 (AB, 1H), 7.32 (AB, 1H), 7.42 (t, 1H), 7.57 (AB, 1H), 7.76 (t, 1H), 8.08 (AB, 1H), 10.96 (s, 1H)., 216144-45-5

As the paragraph descriping shows that 216144-45-5 is playing an increasingly important role.

Reference：
Patent; SOCIETE DE CONSEILS DE RECHERCHES ET D’APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.); US2010/144714; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13484-40-7, 1-(2-Methoxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

13484-40-7, [0560] A mixture of N1-{4-[4-amino-1-(4-formylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-2-methoxyphenyl}-2-fluoro-4-(trifluoromethyl)benzamide (Intermediate 2) (0.075 g, 0.14 mmol), 1-(2-methoxyethyl)-piperazine (0.039 g, 0.27 mmol), and sodium triacetoxyborohydride (0.087 g, 0.41 mmol) in dichloroethane (1.4 mL) was shaken at room temperature for 3 days. Additional portions of 1-(2-methoxyethyl)-piperazine (0.10 mL) and sodium triacetoxyborohydride (0.089 g, 0.41 mmol) were added and the reaction mixture was shaken for 16 h. 1N NaOH (1 mL) was added and the resulting solution was extracted with two portions of dichloromethane (2 mL each). The combined organic portions were concentrated to afford a brown solid which was purified by preparative RP-HPLC (Rainin C18, 8 mum, 300 A, 25 cm; 20-80% acetonitrile-0.05 M ammonium acetate over 25 min, 21 mL/min); the fraction eluting from 16.9-20.2 min was collected, concentrated, and lyopholized to afford N1-{4-[4-amino-1-(4-{[4-(2-methoxyethyl)piperazino]methyl}phenyl)-1H-pyrazolo [3,4-d]pyrimidin-3-yl]-2-methoxyphenyl}-2-fluoro-4-(trifluoromethyl)benzamide as a white solid (0.021 g, 0.031 mmol): 1H NMR (d6-DMSO, 400 MHz): deltaH 9.94 (1H, s), 8.34-8.37 (2H, m), 8.14-8.17 (1H, m), 7.98-8.02 (1H, m), 7.89 (1H, d, J=10.4 Hz), 7.74-7.76 (1H, m), 7.34-7.64 (6H, m), 3.96 (3H, s), 3.51 (2H, s), 3.31-3.43 (2H, m), 3.22 (3H, s), and 2.41-2.45 (10H, m); RP-HPLC (Hypersil C18, 5 mum, 100 , 15 cm; 5%-100% acetonitrile-0.1 M ammonium acetate over 15 min, 1 mL/min). Rt 11.24 min. MS: MH+ 678.7.

As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

Reference：
Patent; Hirst, Gavin C.; Rafferty, Paul; Ritter, Kurt; Calderwood, David; Wishart, Neil; Arnold, Lee D.; Friedman, Michael M.; US2004/6083; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics