Heterocyclic Building Blocks-piperazine

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

To a stirring solution of piperazine-2-carboxylic acid dihydrochloride (SMI) (5 g, 24.6 mmol) in 1,4-dioxane (40 mL) were added 5 N NaOH solution (3.5 g, 88.6 mmol) and Boc-anhydride (12.9 mL, 56.6 mmol) at 0 C and the reaction mixture was stirred at RT for 16 h. After consumption of the starting material (by TLC), volatiles were evaporated under reduced pressure. Obtained crude was dissolved in water (50 mL) and extracted with Et20 (2 x 100 mL). Organic layer was acidified with 1 N HC1 solution and extracted with EtOAc (2 x 100 mL). Combined organic layer was dried over Na2S04 and concentrated under reduced pressure to afford crude compound which was triturated with n-pentane to obtain compound 1 (6 g, 74%) as white solid. 1H-NMR: (400 MHz, DMSO-rfe): delta 12.91 (br s, 1H), 4.42 (d, / = 24.8 Hz, 1H), 4.35-4.27 (dd, / = 20.4, 13.6 Hz, 1H),3.82 (s, 1H), 3.66 (d, / = 13.2 Hz, 1H), 2.99-2.79 (m, 2H), 2.79 (br s, 1H), 1.37 (s, 18H). LCMS (m/z): 329.3 [M+-l]

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; APTINYX INC.; KHAN, M., Amin; (75 pag.)WO2018/26782; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5317-33-9, 3-(4-Methylpiperazin-1-yl)propan-1-ol is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5317-33-9, Step 7. General procedure 1: Di-tert-butyl azodicarboxylate (0.478 g, 2.08 mmol) was added portionwise to a mixture of product step 6 (1.66 mmol), 3-(4-methylpiperazin-1-yl)-propan-1-ol (synthesis described below, 0.276 g, 1.74 mmol), and triphenylphosphine (0.544 g, 2.08 mmol) in dichloromethane (20 mL) at r.t.. If necessary, further alcohol was added. After stirring for 2 h, the solution was concentrated to 10 mL, mounted on silica and chromatographed (gradient, dichloromethane to dichloromethane : methanol = 3:2) to obtain the desired ethers (~73%). Synthesis of 4-chloro-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazoline: The compound was synthesised according to general procedure 1 from 4-chloro-7-hydroxy-6-methoxyquinazoline. LC/ESI-MS: m/z =351 [M+H].

The synthetic route of 5317-33-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; 4SC AG; EP1785420; (2007); 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,5625-67-2

A 2-L Erlenmeyer flask was charged with 2-piperazinone (36.5 g, 364 mmol, Sigma- Aldrich, St. Louis, MO), sodium carbonate (116 g, 1093 mmol), 600 mL of dioxane, and 150 mL of water. To this was slowly added benzyl chloroformate (62.1 g, 364 mmol, Sigma-Aldrich, St. Louis, MO) at room temperature over 20 min. After the addition was complete, the mixture was stirred for 2 h and then diluted with water and extracted with EtOAc (2 L). The combined organic extracts were dried (MgS04), filtered, and concentrated to give a white solid. To this solid was added 500 mL of DCM, triethylamine (128 mL, 911 mmol), DMAP (4.45 g, 36.4 mmol), and di-tert-butyl dicarbonate (119 g, 546 mmol, Sigma-Aldrich, St. Louis, MO). After 1 h at room temperature, the mixture was diluted with water and the organics were separated. The organics were dried (MgS04), filtered, and concentrated to give a brown oil. To this oil was added 100 mL of DCM followed by 1 L of hexane. The resulting white solid was collected by filtration to give 4-benzyl 1-tert-butyl 2-oxo-l,4- piperazinedicarboxylate (101 g).

5625-67-2 Piperazin-2-one 231360, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; AMGEN INC.; ASHTON, Kate; BOURBEAU, Matthew, Paul; HONG, Fang-Tsao; LIU, Longbin; NISHIMURA, Nobuko; NORMAN, Mark, H.; POON, Steve, F.; STEC, Markian, M.; ST. JEAN, David, J., JR; TAMAYO, Nuria, A.; YANG, Kevin, C.; WO2013/123444; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

PREPARATION EXAMPLE 46 2-(4-Benzyl-1-piperazinyl)ethanol STR95 The title compound was synthesised by using 2-(1-piperazinyl)ethanol and benzyl bromide according to the same process as in Preparation Example 4. 1 H NMR(CDCl3) delta 1.81(bs, 1H), 2.50(bs, 8H), 2.54(t, J=5 Hz, 2H), 3.51(s, 2H), 3.60(t, J=5 Hz, 2H), 7.23-7.27(m, 1H), 7.28-7.34(m, 4H)

103-76-4, As the paragraph descriping shows that 103-76-4 is playing an increasingly important role.

Reference：
Patent; Nisshin Flour Milling Co., Ltd.; US5945434; (1999); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,4318-42-7

General procedure: A mixture of the intermediates 3a-3e (5 mmol) and corresponding secondary amine 4a-4g (5.5 mmol) was added in CH3CN (20 ml) at the presence of anhydrous K2CO3 (6 mmol). The mixture was heated at 65 °C for 6-10 h. The solvent was evaporated in vacuo. The residue was dissolved in CH2Cl2 (25 mL), washed with water (20 mL × 3), and the combined organic phases were washed with saturated aqueous NaCl (30 mL), dried over sodium sulfate, and filtered. The solvent was evaporated under reduced pressure. The residue was purified on a silica gel chromatography using mixtures of petroleum/acetone as eluent to get the target products TM-1~TM-28.

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

Reference：
Article; Sang, Zhipei; Wang, Keren; Wang, Huifang; Yu, Lintao; Wang, Huijuan; Ma, Qianwen; Ye, Mengyao; Han, Xue; Liu, Wenmin; Bioorganic and Medicinal Chemistry Letters; vol. 27; 22; (2017); p. 5053 – 5059;,
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.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

To a solution of CBz-piperazine (0.84 ml_, 4.36 mmol) in CH2CI2 (22 ml_) was added EDC (0.918 g, 4.79 mmol), HOBt (0.645 g, 4.77 mmol), Boc-D-Pip- OH (1.03 g, 4.50 mmol), and triethylamine (0.74 mL, 5.31 mmol) and the reaction stirred at room temperature for 5 days. The reaction was diluted with CH2CI2 and washed with sat. NaHCO3, 1 N HCI, sat. NaHCO3, and brine. The organic layer was dried over Na2SO4, filtered, and concentrated to produce 1.87 g (-99percent) of crude title compound: LCMS (m/z): 432.2 (M + H)., 31166-44-6

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

Reference：
Patent; SMITHKLINE BEECHAM CORPORATION; WO2007/70865; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

(i) 3-((4-((4-Aminonaphthalen-1-yl)oxy)pyrimidin-2-yl)amino)-5-methoxy-N-(2-(4-methylpiperazin-1-yl)ethyl)benzamideHATU (200 mg, 0.526 mmol) was added to a solution of 3-((4-((4-((tert- butoxycarbonyl)amino)naphthalen-1-yl)oxy)pyrimidin-2-yl)amino)-5-methoxybenzoic acid (see Fyfe, M. C. T. et al., WO 2014/162126; 200 mg, 0.398 mmol), 2-(4-methylpiperazin-1- yl)ethanamine (100 mg, 0.698 mmol) and Hunig’s Base (200 muIota_, 1.145 mmol) in DMF (2 mL). The reaction mixture was stirred at rt for 72h. The reaction mixture was partitioned between water (10 mL) and DCM (20 mL). The organics were separated, dried (MgSCu), filtered and evaporated to give a brown gum. This material was dissolved in IPA (2 mL) and HCI, 6N in IPA (2 mL, 12.00 mmol) was added. The reaction mixture was stirred overnight. The solvent was evaporated and the residue partitioned between sat. NaHCC>3 (10 mL) and DCM (20 mL). The organics were separated, dried (MgSO4), filtered and evaporated to afford the subtitle compound (200 mg) as a tan glass. LCMS m/z 528 (M+H)+(ES+)

The synthetic route of 934-98-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; RESPIVERT LIMITED; TOPIVERT PHARMA LIMITED; FYFE, Matthew Colin Thor; THOM, Stephen Malcolm; BAKER, Thomas Matthew; HARBOTTLE, Gareth William; HASIMBEGOVIC, Vedran; RIGBY, Aaron; WO2015/92423; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,154590-35-9

Combine the product of Preparation 17, Step 3 (2.2 g, 6.7 mmol) and 2-chloroethyl isocyanate (0.64 ml, 7.4 mmol) in DMF (30 ml). Heat at 60 C. 18 h, allow to cool and partition with CH2Cl2 and water. Dry (MgSO4) and concentrate to obtain the crude urea as a yellow solid.

As the paragraph descriping shows that 154590-35-9 is playing an increasingly important role.

Reference：
Patent; Schering Corporation; US2005/239795; (2005); 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.

To a solution of 1-(2-hydroxyethyl)piperazine (51.7 g, 398 mmol) in DCM (500 mL) was added NEt3 (70.0 mL, 526 mmol) and di-tert-butyl dicarbonate (80.0 g, 367 mmol). The reaction mixture was stirred overnight at room temperature and then washed with 1M aq Na2CO3 solution (2×300 mL), dried (MgSO4) and concentrated in vacuo to give tert-butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate (66.0 g, 72%) as a colourless oil.Analytical LCMS: (System B, RT=1.54 min), ES+: 231.4 [MH]+.

103-76-4, The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Biovitrum AB; US2009/203695; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

38216-72-7, 1-tert-Butylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

INTERMEDIATE 5 [TERT-BUTYL 4-(6-BROMOQUINOLIN-4-YL) PIPERAZINE-1-CARBOXYLATE] [6-BROMO-4-CHLOROQUINOLINE] (5.0 g, 20.6 mmol), [TERT-BUTYL-L-PIPERAZINE] (4.1 g, 22 mmol), triethylamine (3 mL, 22 mmol) and DMSO (20 [ML)] were mixed and heated overnight in an oil bath at [100C.] The reaction was cooled and diluted with diethyl ether and washed with water [(5X),] dried [(MGS04)] and evaporated. The residue was filtered through a short column of silica (2.5-5 %) MeOH in CH2C12 and evaporated. Yield 8.02 g. (97 %). Brown liquid. HPLC 98 %, [RT=3.] 01 (System [AL,] 10-97 % [MECN] over 3 [MIN). 1H] NMR (400 MHz, [CDC13)] 8 ppm 1.52 (s, 9 H) 3.12-3. 17 (m, 4 H) 3.69-3. 75 (m, 4 H) 6.86 (d, [J=5.] 0 Hz, 1 H) 7.72 [(DD,] [J=9.] 0,2. 26 Hz, 1 H) 7.92 [(D,] [J=8.] 8 Hz, 1 H) 8.14 (d, [J=2.] 3 Hz, 1 H) 8.73 (d, J=5.0 Hz, 1 H). MS (ESI+) for [C18H22BRN302] m/z 392.2 (M+H+)

38216-72-7, As the paragraph descriping shows that 38216-72-7 is playing an increasingly important role.

Reference：
Patent; BIOVITRUM AB; WO2004/828; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics