Heterocyclic Building Blocks-piperazine

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.

Example 28 2-(Phenoxy)ethyl 3-(3-methyl-1-piperazinyl)-2-pyrazinyl Ether The title compound was prepared according to the procedure described in Example 4, Step 2, starting from 2-chloro-3-(2-phenoxyethoxy)pyrazine (150 mg, 0.54 mmol; from Example 1, Step 1) and 2-methylpiperazine (250 mg, 2.5 mmol) with the exception that a final extraction step between EtOAc and 5% aqueous NaOH was carried out. This gave 138 mg (73%) of the title product. Anal. (C17H22N4O2) C, H, N. *Prepared according to the procedure described in Example 4, Step 1., 109-07-9

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

Reference：
Patent; Biovitrum AB; US6465467; (2002); B1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-31-7,1-Ethylpiperazine-2,3-dione,as a common compound, the synthetic route is as follows.,59702-31-7

(2)–To a suspension of 0.71 g of the abovementioned 1-ethyl-2,3-dioxo-piperazine in 15 ml of anhydrous dioxane were added with stirring 0.70 g of trimethylsilyl chloride and 0.83 ml of triethylamine. The resulting mixture was stirred at room temperature for 20 hours to deposit triethylamine hydrochloride. This hydrochloride was separated by filtration, and the filtrate was dropped at 5 to 10 C. into a solution of 0.70 g of phosgene in 10 ml of anhydrous tetrahydrofuran. Subsequently, the resulting mixture was reacted at 5 to 10 C. for 30 minutes and at room temperature for 2 hours, and then the solvent was removed by distillation under reduced pressure to obtain 1.0 g of pale yellow crystals of 4-ethyl-2,3-dioxo-1-piperazinocarbonyl chloride. IR (KBr) cm-1: — nuC=O 1780, 1660

59702-31-7 1-Ethylpiperazine-2,3-dione 108812, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Toyama Chemical Co., Ltd.; US4112090; (1978); A;,
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934-98-5, 2-(4-Methylpiperazin-1-yl)ethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

934-98-5, General procedure: A mixture of celastrol (45mg, 0.1mmol), BOP (53mg, 0.12mmol), DIEA (53muL, 0.3mmol) and 2-dimethylaminoethylamine (28muL, 0.3mmol) in DCM (5.0mL) was stirred at room temperature overnight. Then the mixture was concentrated and purified by normal phase column chromatography (DCM/MeOH=30:1) to afford the target compound as a red solid (35mg, 75.6percent).

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

Reference：
Article; Jiang, Fen; Wang, Hui-Jie; Bao, Qi-Chao; Wang, Lei; Jin, Yu-Hui; Zhang, Qiong; Jiang, Di; You, Qi-Dong; Xu, Xiao-Li; Bioorganic and Medicinal Chemistry; vol. 24; 21; (2016); p. 5431 – 5439;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

To a stirring solution of piperazin-2-one 16 (500 mg, 5.00 mmol) in CH2C12 (5 mL) under argon atmosphere were added triethylamine (1.5 mL, 10.00 mmol) and Boc- anhydride (1.3 mL, 6.00 mmol) at 0 C; warmed to RT and stirred for 18 h. The reaction was monitored by TLC; after completion of the reaction, the volatiles were removed in vacuo. The crude was purified through silica gel flash column chromatography using 2% MeOH/ CH2C12 to afford compound 17 (450 mg, 45%) as pale yellow solid. TLC: 10% MeOH/ CH2C12 (R/. 0.6); 1H-NMR (DMSO-i/tf, 400 MHz): delta 8.02 (br s, IH), 3.81 (s, 2H), 3.48-3.45 (m, 2H), 3.19-3.14 (m, 2H), 1.41 (s, 9H)., 5625-67-2

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

Reference：
Patent; INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION; ARNOLD, Lee Daniel; MAAG, Hans; TURNER, JR., William W.; (274 pag.)WO2016/168619; (2016); A1;,
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20327-23-5, 1-Cyclopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of N-(l-(lH-indol-3-yl)hexan-2-yl)-2-bromothiazole-5- carboxamide (0.20 g, 0.49 mmol) and 1-cyclopropylpiperazine (0.07 g, 0.54 mmol) in CH3CN (4.5 mL) was added K2CO3 (0.20 g, 1.47 mmol) and the reaction mixture was heated at 80 C for 16 h. The reaction mixture was concentrated in vacuo. The residue was diluted with H20 (10 mL) and extracted with 10% MeOH in DCM (10 mL). The organic layer was separated, dried over anhydrous Na2S04 and concentrated in vacuo. The crude obtained was purified by column chromatography (silica 230-400 mesh, 0 to 10% MeOH in DCM) and then triturating with petroleum ether (6 mL), pentane (10 mL) and DCM (2 mL) to afford N-(l-(lH-indol-3- yl)hexan-2-yl)-2-(4-cyclopropylpiperazin-l-yl)thiazole-5-carboxamide (0.14 g, 63%) as an off- white solid. HPLC Purity: 99.0%. LC/MS (ESI) m/e [M+H]+/RT (min)/%: (0271) 452.00/2.91/98.8%. 1H NMR (400 MHz, DMSO- 6) delta 0.35-0.44 (m, 4H), 0.82 (t, = 6.9 Hz, 3H), 1.16-1.37 (m, 4H), 1.40-1.60 (m, 2H), 1.62-1.68 (m, 1H), 2.60-2.68 (m, 4H), 2.73-2.98 (m, 2H), 3.40-3.48 (m, 4H), 4.04-4.18 (m, 1H), 6.92-6.99 (m, 1H), 7.04 (t, = 7.6 Hz, 1H), 7.09 (s, 1H), 7.31 (d, = 8.3 Hz, 1H), 7.57 (d, = 7.8 Hz, 1H), 7.80 (s, 1H), 7.94 (d, = 8.8 Hz, 1H), 10.75 (brs, 1H).

20327-23-5, 20327-23-5 1-Cyclopropylpiperazine 4742004, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; NEUROPORE THERAPIES, INC.; WRASIDLO, Wolfgang; STOCKING, Emily, M.; HALL, Adrian; MACCOSS, Malcolm; (139 pag.)WO2017/20010; (2017); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.262368-30-9,N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide,as a common compound, the synthetic route is as follows.

130 g of compound C and 89.9 g of material D were added to the reaction flaskCounted as the molar ratio to match the delivery ratio,Compound C was purified) and 1.8 L of methanol,Under the protection of nitrogen, the temperature was stirred to reflux, 1.5-2h after the reaction solution was dissolved, stirring 9-10h, the sample solution for TLC, no compound C was observed, slightly cool to the reaction system by adding 22g25% aqueous ammonia (mass percentage), continue to warm up to reflux for 2h, there is a clear yellow particles solid precipitation, every 2h sampling for HPLC, detected to the compound E residue of less than 0.1%; the end of the reaction slow mixing speed to room temperature (15-20 ), Filtered, 1.2L of water to wash the filter cake, fully dried to dry the dark yellow powder solid, 60 C blast dry to give compound F 170.5g dark brown powder. The molar yield of the Nidanibu free base (Compound F) was 89%, the purity was 99.8%, and the maximum single impurity was less than 0.1%.

262368-30-9, As the paragraph descriping shows that 262368-30-9 is playing an increasingly important role.

Reference：
Patent; Changzhou Jiade Pharmaceutical Technology Co., Ltd.; Wang Zifu; (7 pag.)CN107011241; (2017); A;,
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848482-93-9, (S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

848482-93-9, To a stirred solution of (S)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (CAS Number 848482-93-9; 0.540 g, 2.35 mmol) in MeOH (15 ml) was added 37% aqueous formaldehyde solution (0.2 ml) and a catalytic amount of acetic acid, followed by 10% dry Pd/C (0.100 g) under nitrogen atmosphere at rt. The reaction mixture was purged with H2 gas at rt for 2 h. The resulting reaction mixture was carefully filtered through celite hyflow and the filtrate was concentrated under reduced pressure. The residue was triturated with n-pentane (5 ml) to obtain a solid material, which was dried under high vacuum to yield (S)-4-(tert-butoxycarbonyl)-1 – methylpiperazine-2-carboxylic acid (0.300 g, 1 .23 mmol). This material was used directly for the next step without further purification. LCMS: Method C, 1 .560 min, MS: ES+ 245.33.

848482-93-9 (S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid 1501850, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; MISSION THERAPEUTICS LIMITED; STOCKLEY, Martin Lee; KEMP, Mark Ian; MADIN, Andrew; (167 pag.)WO2018/65768; (2018); A1;,
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Piperazines – an overview | ScienceDirect Topics

314741-39-4, (S)-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

(S)-Methyl piperazine-2-carboxylate hydrochloride A mixture of (S)-tert-butyl methyl piperazine-1,3-dicarboxylate (366 mg, 1.5 mmol) and HCl in MeOH (20 mL, 2.9 M) was stirred at RT for 1 h. The mixture was concentrated in vacuo to yield the crude product (270 mg) as a yellow solid which was used directly in next step without further purification

314741-39-4, As the paragraph descriping shows that 314741-39-4 is playing an increasingly important role.

Reference：
Patent; ARAXES PHARMA LLC; LI, Liansheng; FENG, Jun; WU, Tao; REN, Pingda; LIU, Yi; LIU, Yuan; LONG, Yun, Oliver; WO2015/54572; (2015); A1;,
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120737-59-9, tert-Butyl 3-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 139; N-1,2-Benzisoxazol-3-yl-3-methyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide; [Show Image] (1) tert-Butyl 3-methyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxylate; To a solution of 1-tert-butoxycarbonyl-3-methylpiperazine (5.00 g, 24.0 mmol) and 4-tert-butoxycarbonylaminopiperidine (5.20 g, 26.4 mmol) in dimethylformamide (100 ml) was added triethylamine (3.35 ml, 24.0 mmol) at room temperature and the mixture was stirred at room temperature for 3 hours and at 70°C for 1 hour. The reaction mixture was poured into water and the mixture was extracted with ethyl acetate. The extract was washed with water and dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure. The residue was recrystallized from a mixed solvent of ethyl acetate and hexane to obtain the desired product (6.75 g, 78.0percent) as a solid. 1H-NMR (CDCl3) delta; 1.31 (3H, d, J = 6.6 Hz), 1.50 (9H, s), 3.04 (1H, br s), 3.21 (1H, br s), 3.43 – 3.52 (1H, m), 3.74 – 3.79 (1H, m), 3.98 – 4.35 (3H, m), 7.40 – 7.44 (3H, m), 8.17 – 8.20 (2H, m)., 120737-59-9

As the paragraph descriping shows that 120737-59-9 is playing an increasingly important role.

Reference：
Patent; Takeda Pharmaceutical Company Limited; EP1813606; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8,5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 3; Preparation of the dihydrochloride salt of ll-piperazinyldibenzo[b,f][l,4]thiazepme; [0038] The dewatered MTBE solution of 11 -rhoirhoerazinyldibenzo[b,f] [1 ,4]- thiazepine recovered in accordance with Example 2 is cooled to ambient temperature. 1200 ml of isopropanol are added, followed by 72 ml of concentrated hydrochloric acid. The mixture is stirred at ambient temperature for about 4 hours during which time the dihydrochloride salt of 1 l-piperazinyldibenzo[b,f][l,4]thiazepine begins to crystallize. The mixture is cooled to a temperature below 15 0C {e.g., to 10 0C), and filtered. The solids can be washed with cold isopropyl alcohol. Solvent-free solids can be recovered by vacuuming drying at 60-70 0C.

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CAMBREX CHARLES CITY, INC.; WO2006/135544; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics