Tag: M.W:200-300

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.

To a solution of 4- (4-methylpiperazin-1-yl) benzylamine (43 mg, 0.21 mmol) in toluene (4 mL) under nitrogen protection was added trimethylaluminum (0.2 mL, 1 M n-hexane solution), The reaction system was stirred at room temperature for 15 minutes, and 4,9-dioxo-4,9-dihydrothiazolo [5,4-g] isoquinoline-2-carboxylic acid ethyl ester (20 mg, 0.07 mmol) was added. The reaction system Stir at 90 C for 5 hours.The reaction solution was concentrated under reduced pressure andpurifiedby prep-HPLC (NH4HCO3system) to obtain compound 8 (2 mg, yield: 7%) as a yellow solid.

216144-45-5, 216144-45-5 4-(4-Methylpiperazin-1-yl)benzylamine 2776493, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Shanghai Dinuo Pharmaceutical Technology Co., Ltd.; Zhao Zhiming; (42 pag.)CN110467629; (2019); 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.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

?To a solution 6-chiora-M-(3-nitrophenyl)pvrimidin-4-amine (1.0 g, 4.00 minol) in2 -hutanol (10 mL) and trifluoroacetic acid (0.3 mL) was added 2-methoxv-4.4-niethylpiperazin-i-yl)anihne (6o6irig, 4.39 inmol). The reaction mixture was stilTed at 120 C for 10 hrs and the solvent concentrated undcr reduced pressure. The reaction mixture was diluted with dichloromethane and washed with saturated aqueous potassium carbonate solution and brine. The organic layer was dried over Mg504, filtered through a pad of celiteand concentrated under reduced pressure. The residue was purified by column chromatography on silica gel (1:99 to 3:97, ammonia solution 7.0 N in methanol/dichloromethane) to afford N4-(2-methoxy-4-(4-methyipiperazin- 1 -yi)phenyl)-N6- (3-nitrophenyflpyrimidine-4,6-dianiine (1.3 g, 75% yield) as an solid. Rt = 2.73 mm; ?H NMR 600 MHz (DMSO-d6) d 9.50 (s, lH), 8.72 Cc, lH), 8.24 (s, 1H), 8.22 (s, IH), 7.91 (dd, J::: 1.2 Fiz,J 8.4 Hz, iLl), 7.27 (d,J 8.4 Hz, HI), 7.50 (j,J::: 8.4 Hz, iLl), 7.21 (d,J 8.4 Hz, 1H), 6.49 (d,J= 2.4 Hz, 1H). 6.51 (dd,J= 2.4 Hz,J= 9.0 Hz, 1H), 5,76 (s, 1H), 3,77 (s, 3W). 3.16 (in, 4ff). 2,46 (rn, 4ff), 2.32 (s, 3H,); MS mAr: 436.45 [M+i].

122833-04-9, As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference：
Patent; DANA-FARBER CANCER INSTITUTE, INC.; GRAY, Nathanael; CHOI, Hwan Geun; TAN, Li; WO2015/6492; (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.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

To a stirred solution of 1-Z-piperazine (8.5 g, 38.5 mmol) in dry THE (100 mL), 1,1- thiocarbonyldimidazole (12.37 g, 69.4 mmol) was added and the mixture was stirred at 60°C for 5 h. It was concentrated under vacuum and NH3 in EtCH (2 N, 300 mL) was added at 0°C. The resulting mixture was stirred at 55°C for 8 h in an autoclave. It was diluted withwater (100 mL) and extracted with DCM (2 x 100 mL). The DCM layer was washed with water (100 mL), dried over in anhydrous Na2SO4 and concentrated. The resulting crude product was purified by flash chromatography to afford the title product. Yield: 87percent (7 g, white solid). 1H NMR (400 MHz, DMSO-d6): 6 7.51 (5, 2H), 7.38-7.31 (m, 5H), 5.1 (5, 2H), 3.78 (m, 4H), 3.43-3.33 (m, 4H). LCMS: (Method A) 280.2 (M+H), Rt. 2.33 mm, 95.4percent (Max).

31166-44-6, As the paragraph descriping shows that 31166-44-6 is playing an increasingly important role.

Reference：
Patent; ASCENEURON S. A.; QUATTROPANI, Anna; KULKARNI, Santosh, S.; GIRI, Awadut, Gajendra; (280 pag.)WO2017/144633; (2017); 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.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

694499-26-8, To a solution of 150 58a (30mg, 0.08mmol) in 77 DMF (5mL) were added 147 4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (27.3mg, 0.10mmol), 79 HATU (45.6mg, 0.12mmol) and DIEPA (20.6mg, 0.16mmol). The resulting mixture was stirred at room temperature for 2h. Then it was diluted with EtOAc (50mL), washed with water (50mL×3) and brine (100mL). The organic layers were dried over anhydrous sodium sulfate and concentrated. The residue was diluted with DCM (1mL) and CF3COOH (0.5mL). The reaction mixture was stirred at room temperature for 4h and then the pH value was adjusted to 12 with saturated sodium bicarbonate. The mixture was extracted by 80 EtOAc (50mL) and washed with water (50mL×2) followed by brine (50mL). The organic layers were dried over sodium sulfate, filtered, concentrated and purified by silica gel column chromatography (eluting with 0-10% MeOH in 81 DCM) to afford 151 38 (23mg, 52%) as a gray solid.

694499-26-8 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 46838908, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Liu, Xuesong; Wang, Beilei; Chen, Cheng; Jiang, Zongru; Hu, Chen; Wu, Hong; Zhang, Yicong; Liu, Xiaochuan; Wang, Wenliang; Wang, Junjie; Hu, Zhenquan; Wang, Aoli; Huang, Tao; Liu, Qingwang; Wang, Wei; Wang, Li; Wang, Wenchao; Ren, Tao; Li, Lili; Xia, Ruixiang; Ge, Jian; Liu, Qingsong; Liu, Jing; European Journal of Medicinal Chemistry; vol. 160; (2018); p. 61 – 81;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

373608-48-1, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,373608-48-1

Step 3: ieri-butyl 4-{3-[(2-oxo-2H-chromen-4-yl)amino]propyl} piperazine-1 -carboxylate (68c). A solution of intermediate 68b (1 .1 g, 4.5 mmoles, 1 .1 eq.), triethylamine (0.674 mL, 4.8 mmoles, 1 .2 eq.) and 2-oxochromen-4-yl trifluoromethanesulfonate 28a (1 .2 g, 4.1 mmoles, 1 eq.) in acetonitrile (20 mL) was heated to 705C for 1 hour. The reaction mixture was concentrated under reduced pressure and the residue was partitioned between dichloromethane and a brine/sodium bicarbonate mixture (1 :1 ). The mixture was filtered through a hydrophobic frit (Phase Separator) washing with dichloromethane. The organic phase was evaporated under reduced pressure and the residue was chromatographed on silica gel (SNAP50) eluting with a gradient of EtOAc in cyclohexane to give ferf-butyl 4-{3-[(2-oxo- 2H-chromen-4-yl)amino]propyl}piperazine-1 -carboxylate 68c (700 mg, Y=44%). LC-MS (M-H+) = 388.3.

373608-48-1 tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate 17750945, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.; OMBRATO, Rosella; GAROFALO, Barbara; MANGANO, Giorgina; CAPEZZONE DE JOANNON, Alessandra; CORSO, Gaia; MAGARO’, Gabriele; FURLOTTI, Guido; IACOANGELI, Tommaso; (108 pag.)WO2016/96631; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129779-30-2, (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(2R,6S) and (2S,6R)-1,2,6-Trimethylpiperazine. To a solution of cis-3,5-dimethylpiperazine-1-carboxylic acid t-butylester (2.0 g, 9.22 mmol) in MeOH (25 mL), paraformaldehyde (0.84 g, 28 mmol) and zinc chloride (3.83 g, 28 mmol) were added. Then sodium cyanoborohydride (1.76 g, 28 mmol) was added in portions. The reaction mixture was stirred at rt. for 4 hr. Then insoluble solid was filtered out and the filtrated was concentrated. The residue was participated between saturated NaHCO3 solution and CH2Cl2 (2×50 mL). The organic layers were combined, dried (MgSO4) and concentrated to give a colorless oil. It was then dissolved in CH2Cl2 (10 mL) and TFA (2.5 mL) was added. The reaction mixture was stirred at rt. for overnight. TFA and solvent were evaporated to give a white solid as final product as TFA salt. (2.6 g, 86% yield); MS m/129(MH+). 1H NMR (500 MHz, CHLOROFORM-D) delta ppm 1.41 (d, J=6.41 Hz, 6H) 2.87 (s, 3H) 3.38-3.56 (m, 4 H) 3.71-3.90 (m, 2H).

129779-30-2, The synthetic route of 129779-30-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Bristol-Myers Squibb Company; US2007/270406; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-08-2, 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

To a solution of 4,4′-(chloromethylene)bis(fluorobenzene) (1.5 g, 6.29 mmol) in acetonitrile (15 mL) was added 1-(tert-butyl) 3-methyl piperazine-1,3-dicarboxylate (1.842 g, 7.54 mmol), followed by DIPEA (3.29 mL, 18.86 mmol). The reaction mixture was stirred at 85 C overnight. The reaction mixture was concentrated under reduced pressure to remove the volatiles and the residue was dissolved in ethyl acetate (150 mL) and washed with water. The aqueous layer was back-extracted with ethyl acetate (100 mL x 2). The combined organic layer was washed with brine, dried over Na2SO4, filtered and the filtrate was concentrated under reduced pressure to give the crude product. The crude residue was purified via silica gel chromatography on ISCO (5-10 % (0493) EtOAc/petroleum ether; 40 g column) to afford the 1-(tert-butyl) 3-methyl 4-(bis(4- fluorophenyl)methyl)piperazine-1,3-dicarboxylate (2.15 g, 4.82 mmol, 77 % yield). (0494) LCMS: m/z = 447.4 (M+H); rt 2.16 min. (LCMS Method: Column: Waters Acquity UPLC BEH C18 (2.1 x 50 mm) 1.7 mm, Mobile phase A: 10 mM ammonium (0495) acetate:acetonitrile (95:5); Mobile phase B: 10 mM ammonium acetate:acetonitrile (5:95), Gradient = 20-90 % B over 1.1 minute, then a 0.6 minute hold at 90 % B; Temperature: 50 C; Flow rate: 0.7 mL/min; Detection: UV at 220 nm)., 129799-08-2

129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various fields.

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;,
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.115619-01-7,4-(4-Ethylpiperazin-1-yl)phenylamine,as a common compound, the synthetic route is as follows.

(5-Chlorofuro[2,3-c]pyridin-2-yl)(2,6-difluoro-3,5-dimethoxyphenyl)methanone (2 g, 5.65 mmol), 4-( 4-ethylpiperazin-1-yl)aniline (1.36 g, 6.78 mmol), cesium carbonate (2.76 g, 5.65 mmol), XantpHOS (1.3 g, 2.26 mmol) and Pd2dba3 (1 g, 1.1 mmol) were added to 30 ml in order. In toluene.Argon was replaced 3-5 times and heated to 110 C (oil bath) for overnight reaction.The reaction was complete by TLC.The mixture was cooled to rt, filtered, and the filter cake was washed with EA, and the filtrate was evaporated to dryness and purified by column (MeOH: DCM = 0-100: 1-70:1) to give solid (2,6-difluoro-3,5-dimethyl Oxyphenyl)(5-((4-(4-ethylpiperazin-1-yl)-2-nitrophenyl)amino)furo[2,3-c]pyridin-2-yl)methanone (2.5g, 79%)., 115619-01-7

As the paragraph descriping shows that 115619-01-7 is playing an increasingly important role.

Reference：
Patent; Shanghai Xin Qibo Biological Technology Co., Ltd.; Wang Zhaoyin; Ma Jianbin; (39 pag.)CN110092798; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6-Fluoro-2-methyl-3-(oxiran-2-yl)benzonitrile (12.0 g, 67.7 mmol) and (5)-4-N-BOC-2-hydroxymethylpiperazine (22.0 g. 102 mmol) were suspended in ethanol (100 mL) then heated in a microwave apparatus for 30 minutes at 150 C. The reaction mixture was cooled and evaporated dryness. The residue was purified by MPLC chromatography through a 330g Redi-sep column eluting with 5%MeOH/95% EtOAc solvent system to yield the title compound. LC-MS : M+l= 394., 314741-40-7

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PIO, Barbara; PASTERNAK, Alexander; SHAHRIPOUR, Aurash; TANG, Haifeng; WALSH, Shawn; WO2013/90271; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

31166-44-6, 1-Cbz-Piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

31166-44-6, Benzyl Piperazine-1-carboxylate (10.50 g)In tetrahydrofuran (225 mL) were added triethylamine (5.51 g), sodium iodide (0.68 g) and 3-bromo-1-propanol (9.77 g). It was then stirred at 50 ° C. overnight. Thereafter, it was cooled to room temperature. The resulting solution was poured into water and extracted with ethyl acetate. The organic layers were combined and washed with saturated brine to give the title compound (11.62 g, yield 92percent).

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

Reference：
Patent; NIPPON SODA COMPANY LIMITED; IHORI, YOICHI; INOUE, SHUJI; SHIBAYAMA, KOTARO; KANG, CHANG-KYUNG; SHIINOKI, YASUYUKI; NISHIMURA, SATOSHI; (65 pag.)JP2016/222654; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics