Heterocyclic Building Blocks-piperazine

1001180-21-7, (R)-tert-Butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 11: Triethylamine (4.33 mL, 31.1 mmol; degassed with nitrogen 30 minutes prior to use) and formic acid (1.36 mL, 36.1 mmol; degassed with nitrogen 30 minutes prior to use) were added to a solution of (R)-tert-butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H- cyclopenta[d]pyrimidin-4-yl)piperazine-l-carboxylate (9.75 g, 29.3 mmol) in DCM (210 mL; degassed with nitrogen 30 minutes prior to use). The mixture was stirred for 5 minutes, and then a Ru catalyst (0.0933 g, 0.147 mmol) was added. The reaction was stirred under positive nitrogen pressure overnight (18 hours). The reaction mixture was concentrated to dryness and dried on high vacuum. The impure material was flashed on Biotage 65M loaded 1:1 DCM:ethyl acetate 500 mL flushed, then 1 :4 DCM:ethyl acetate until product (2nd spot), then gradient to neat ethyl acetate, then 25:1 DCM:MeOH eluted rest of product. The fractions were combined and concentrated on a rotary evaporator. The residue was concentrated again from DCM/hexanes to give a mixture of tert-butyl 4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H- cyclopenta[d]pyrimidin-4-yl)piperazine-l-carboxylate (major) and tert-butyl 4-((5R,7S)-7- hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-l-carboxylate (minor) (9.35 g, 95.3% yield) as a foam. LC/MS (APCI+) m/z 335 [M+H]+. 1H NMR (CDCl3) showed 88% diastereoselectivity by integration of carbinol methine., 1001180-21-7

As the paragraph descriping shows that 1001180-21-7 is playing an increasingly important role.

Reference：
Patent; ARRAY BIOPHARMA INC.; GENENTECH, INC.; WO2009/89453; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

16154-72-6, 3-Chloro-4-(4-methylpiperazin-1-yl)benzenamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of 4-anilino-pyrimidine intermediate 3 (50 mg, 1.0 equiv.), the corresponding aniline B-ring aniline (1.0 equiv.), 2 drops of 4 M HC1, and EtOH (1 mL) was heated in a microwave reactor at 100 C for 1 h. Sodium bicarbonate (ca. 100 mg) was added to the mixture, stirred for 30 min at room temperature, and concentrated under reduced pressure. Unless otherwise mentioned, all products were purified via column chromatography using DCM/MeOH (0-10%).

16154-72-6, The synthetic route of 16154-72-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; H. LEE MOFFITT CANCER CENTER & RESEARCH INSTITUTE, INC.; SCHOeNBRUNN, Ernst; LAWRENCE, Nicholas J.; LAWRENCE, Harshani R.; (293 pag.)WO2017/66428; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 2 1-(2,4-Difluorophenyl)-1,4-dihydro-4-oxo-6-fluoro-7-(3-methyl-4-tert-butyloxycarbonyl-piperazin-1-yl)-3-quinoline carboxylic acid A 50 gallon glass lined reactor was purged with nitrogen and charged with 44.5 kg of dimethylsulfoxide, 2.3 kg of triethylamine, 6 kg of methanol, 5.0 kg of 1-(2,4-difluorophenyl)-6-fluoro-7-chloro-1,4-dihydro-4-oxo-quinoline carboxylic acid (see U.S. Patent No. 4,730,000) and 12 kg of 1-tert-butyloxycarbonyl-2-methylpiperazine. The slurry was stirred and heated to 95 +- 2C. After 2 hours, 3 kg more of 1-tert-butyloxycarbonyl-2-methylpiperazine and 3 liters of methanol were added. After 4 and 27 hours, respectively 5 kg and 3 kg more of 1-tert-butyloxycarbonyl-2-methylpiperazine were added. After 36 hours, the reaction temperature was lowered to 60C. To the stirred mixture was added 41 liters of isopropanol that had been preheated to 55C. The slurry resulting from the above reaction was cooled to room temperature, filtered and washed with isopropanol. The filter cake was added to 25 liters of 100C acetic acid and heated to reflux. The slurry was cooled to 19C, filtered and washed with isopropanol. The solid was dried at 40C overnight, yielding 3.1 kg of the title compound. m.p. 254-256C. 300 MHz 1H NMR 8.60 (s, 1H), 8.10 (d, 1H), 7.50 (m, 1H), 7.28-7.15 (m, 3H), 6.21 (d, 1H), 4.33 (br d, 1H), 3.94 (br d, 1H), 3.41-3.18 (m, 4H), 2.91 (m, 1H), 2.72 (m, 1H), 1.46 (s, 9H), 1.30 (d, 3H)., 120737-78-2

As the paragraph descriping shows that 120737-78-2 is playing an increasingly important role.

Reference：
Patent; ABBOTT LABORATORIES; EP350950; (1990); 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.548762-66-9,(2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of tert-butyl (2S,5R)-2,5-dimethylpiperazine-1-carboxylate (500 mg, 2.33 mmol) in dry acetonitrile (10 mL), methyl 2-bromopropanoate (468 mg, 2.80 mmol) and DIPEA (1.22 mL, 7.00 mmol) were added at room temperature. The reaction mixture was heated to 85 C for 16 h. The reaction mixture was cooled to room temperature and concentrated under reduced pressure to obtain the crude product, which was purified by Combi flash 24 g silica gel chromatography by using 0-30% ethyl acetate in petroleum ether as eluent to obtain tert-butyl (2S,5R)-4-(1-methoxy-1-oxopropan-2- yl)-2,5-dimethylpiperazine-1-carboxylate (620 mg, 88 % yield) as a light yellow liquid. LCMS: m/z, 301.2 (M+H); retention time 2.941 and 3.094 min. Column: Kinetex XB- C18 (3 x 75 mm) 2.6 mm; Mobile phase A: 10 mM ammonium formate: acetonitrile (98:2), Mobile phase B: 10 mM ammonium formate: acetonitrile (2:98), Gradient = 20- 100 % B over 4 minutes, then a 0.6 minute hold at 100 % B; Temperature: 27 C; Flow rate: 1.0 mL/min; Detection: UV at 220 nm, 548762-66-9

As the paragraph descriping shows that 548762-66-9 is playing an increasingly important role.

Reference：
Patent; BRISTOL-MYERS SQUIBB COMPANY; VELAPARTHI, Upender; CHUPAK, Louis S.; DARNE, Chetan Padmakar; DING, Min; GENTLES, Robert G.; HUANG, Yazhong; KAMBLE, Manjunatha Narayana Rao; MARTIN, Scott W.; MANNOORI, Raju; MCDONALD, Ivar M.; OLSON, Richard E.; RAHAMAN, Hasibur; JALAGAM, Prasada Rao; ROY, Saumya; TONUKUNURU, Gopikishan; VELAIAH, Sivasudar; WARRIER, Jayakumar Sankara; ZHENG, Xiaofan; TOKARSKI, John S.; DASGUPTA, Bireshwar; REDDY, Kotha Rathnakar; RAJA, Thiruvenkadam; (0 pag.)WO2020/6018; (2020); A1;,
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Piperazines – an overview | ScienceDirect Topics

1030377-21-9, (S)-1-Boc-2-(Hydroxymethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (S)-tert-butyl 2-(hydroxymethyl)piperazine-l -carboxylate (850.9 mg, 3.93 mmol) and 2-(tert-butoxymethyl)oxirane (850 mg, 6.46 mmol) in ethanol (10 mL) was heated at 120 C for 30 min using microwave. The mixture was concentrated to dryness. The residue was purified with flash column chromatography on silica gel using 1-10% methanol in dichloromethane to afford a oil as the product in quantitative yield. 1H NMR (500 MHz, Chloroform-^ delta 4.09 (s, lH), 3.84 (m, 3H), 3.38 (dt, J= 9.0, 3.7 Hz, l H), 3.28 (m, 3H), 3.04 (dd, J = 24.2, 1 1.7 Hz, 1H), 2.88 – 2.80 (m, 2H), 2.48 – 2.32 (m, 3H), 2.26 – 2.21 (m, 1H), 2.13-2.08 (m, 1H), 1.44 (s, 9H), 1.17 (d, 9H). MS for ^Eta34Nu205: 347.2 (MH+).

1030377-21-9, 1030377-21-9 (S)-1-Boc-2-(Hydroxymethyl)piperazine 22884145, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; NEKTAR THERAPEUTICS (INDIA) PVT. LTD.; NEKTAR THERAPEUTICS; SHARMA, PANKAJ; KHATRI, VIJAY KUMAR; GU, XUYUAN; SONG, YUAN; SHEN, MICHAEL LIXIN; SAUTHIER, JENNIFER RIGGS; ANAND, NEEL K.; KOZLOWSKI, ANTONI; ODINECS, ALEKSANDRS; RILEY, TIMOTHY A.; REN, ZHONGXU; MU. YONGQI; SHEN, XIAOMING; YUAN. XUEJUN; AURRECOECHEA, NATALIA; O’MAHONY, DONOGH JOHN ROGER; WO2015/92819; (2015); A2;,
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.112984-60-8,6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid,as a common compound, the synthetic route is as follows.

6-Fluoro- 1 -methyl-4-oxo-7-(piperazin- 1 -yl)- 1 H,4H- [1,3 ]thiazeto[3 ,2-a] quinoline-3-carboxylic acid (3 g, 8.60 mmol) was suspended in DMF (50m1) under argon atmosphere and heated at 90 C. After obtaining a clear solution,triethylamine (2.4 ml , 17.10 mmol), compound A (2.12 g, 6.50 mmol) and tetrabutylammonium bromide (107 mg, 0.33 mmol) were added. Then the reaction mixture washeated for another 20 h at 90 C. After completion of the reaction, it was allowed to cool to room temperature and ethyl acetate was added into the reaction mixture. The obtained precipitate was filtered and filtrate was evaporated to dryness. The crude mass was re-dissolved in DCM and methanol and excess amount diethyl ether was added into this solution to obtain a brown mass which was purified by flash column chromatography over silica gel and pure compound 2 was elutedwith3% methanol-DCMmixture as a beige solid (250 mg) with 8% isolated yield. 1H NMR (CDC13):3 14.23 (brs, 1H, COOH), 7.92 (s, 1H, ArH), 7.89 (d, 1H, JAB = 12.0 Hz, ArH), 6.38 (d, 1H, JAB = 8Hz, ArH), 6.09 (q, 1H, JAB = 4 Hz,SCHN), 4.5 1-4.41 (m, 2H, NCH2), 3.26-3.20 (m, 4H, CH2N), 2.74(t, 2H, JAB = 4 Hz, NCH2), 2.69-2.67 (m, 4H, CH2N), 2.20 (d, 3H, JAB = 4 Hz, CH3). ESI-MS (mlz):503.20 (M+H)., 112984-60-8

112984-60-8 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid 124225, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; GHOSH, Shamik; GHOSH, Sumana; SINHA, Mau; SADHASIVAM, Suresh; BHATTACHARYYA, Anamika; MAVUDURU, Siva Ganesh; TANDON, Nupur; KUMAR, Deepak; (149 pag.)WO2017/17631; (2017); A2;,
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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

Compound (R) – 3-methyl-piperazine-1-carboxylic acid T-butyl ester (530 mg, 2 . 6mmol), compound quinoline-2-carboxylic acid (450 mg, 2 . 6mmol), 1-ethyl-3 – (3-dimethylamino-propyl) carbodiimide hydrochloride (996 mg, 5 . 2mmol) and N-hydroxy-7-azabenzene and triazazole (530 mg, 3 . 9mmol) dissolved in dichloromethane (10 ml) in, 0 C to this solution under the conditions of adding dropwisely N, N-diisopropyl ethylamine (1.3 ml, 7 . 8mmol), stirring the mixture at room temperature for 10h, and washing with water (10 ml × 3), the organic phase is dried with anhydrous sodium sulfate, removal of solvent, concentrate under column separation (V (petroleum ether)/ V (ethyl acetate) =1/1) get 820 mg white solid, yield: 88%., 163765-44-4

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd.; Yu, Tianzhu; Liu, Bing; Zhang, Yingjun; Zhang, Xiangyu; Zhang, Zhiguo; Zheng, Changchun; Zhang, Jiancun; Lei, Jianhua; (66 pag.)CN105461693; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

630125-91-6, 4-((4-ethylpiperazin-l-yl)methyl)-3-(trifluoromethyl)benzeneamine (30.6 mg) in 1,4-dioxane (1 mNo.), was added 4-nitrophenylchloroformate (21.6 mg) at room temperature. After 60 0C at 1 h, them mixture was cooled to rt and ethyl 6-(3-aminophenyl)-lH-indazole-3-carboxylate (30 mg) was added. The mixture was stirred at 90 0Cf or 12 h. Ethyl acetate and water were added and the aqueous layer was extracted with ethyl acetate three times. The combined organic layer was dried over magnesium sulfate and concentrated under reduced pressure. The residue was triturated in ethyl acetate/hexane to give6-(3-(3-(4-((4-ethylpiperazin-l-yl)methyl)-3-(trifluoromethyl)phenyl)ureido)phenyl)-l H-indazole-3-carboxylate (16.2 mg).[643] [644] 1H NMR (400 MHz, DMSOd6) 613.98 (s, IH), 9.09 (s, IH), 8.93 (s, IH), 8.15 (8.4 Hz, IH), 7.99 (s, IH), 7.93 (s, IH), 7.81 (s, IH), 7.62 (m, 3H), 7.43 (br d, J = 4.4 Hz, 2H), 7.28 (m, IH), 4.41 (q, J = 7.2 Hz, 2H), 3.54 (s, 2H), 2.49 (m, 10H), 1.39 (t, J = 7.2 Hz, 3H).

As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.

Reference£º
Patent; KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY; KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY; KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY; SIM, Tae Bo; SON, Jung Beom; KIM, Hwan; PARK, Dong Sik; CHOI, Hwan Geun; HAM, Young Jin; HAH, Jung Mi; YOO, Kyung Ho; OH, Chang Hyun; LEE, So Ha; HA, Jae Du; CHO, Sung Yun; KWON, Byoung-Mog; HAN, Dong Cho; WO2010/64875; (2010); A2;,
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.50606-32-1,Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,50606-32-1

Example 11: (lalpha,5alpha,6beta)-3-{6-[(S)-l-(4-Butoxycarbonyl-piperazine-l-carbonyl)-2- methyl-propylcarbamoyll^-phenyl-pyrimidin^-ylJ-S-aza-bicyclop.l.Olhexane– carboxylic acid:11.1. 4-((S)-2-tert-Butoxycarbonylamino-3-methyl-butyryl)-piperazine-l-carboxylic acid butyl ester:To a solution of Boc-(L)-Val-OH (400 mg) in DCM (12 mL) were added DIPEA (0.991 mL), DMAP (22 mg), HOBT hydrate (298 mg), EDCI hydrochloride (423 mg) and intermediate 1.4 (343 mg). The mixture was stirred at RT for 6 h. An aq. NaHCO3 solution was added to the mixture and the phases were separated. The org. phase was washed with brine, dried (MgStheta4) and evaporated off to afford 844 mg of the desired compound as beige oil. LC-MS: tR = 1.02 min; [M+H]+: 386.42.

The synthetic route of 50606-32-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ACTELION PHARMACEUTICALS LTD; CAROFF, Eva; HILPERT, Kurt; HUBLER, Francis; MEYER, Emmanuel; RENNEBERG, Dorte; WO2010/116328; (2010); A2;,
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.154590-35-9,tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1: Cool in ice a solution of glycidol (0.63 g, 8.5 mmol) in ether (30 ml). Add DIPEA (1.6 ml, 8.5 mmol) and phosgene (1.85M in toluene, 5.8 ml, 10.8 mmol). Stir 2 h, filter, and concentrate. Dissolve in ether (50 ml) and add the product of Preparation 13, Step 3 (2.50 g, 7.7 mmol) and DIPEA (1.6 ml, 8.5 mmol). Stir 2 h, wash with sat. NaHCO3, dry (MgSO4), and concentrate to obtain the carbamate as a yellow solid

154590-35-9, The synthetic route of 154590-35-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Schering Corporation; US2004/220194; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics