Tag: M.W:300-400

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.162046-66-4,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

162046-66-4, (3-Pyrrolidin-l-ylphenyl)methylamine (8 g; 0.0408 mol) was dissolved in DCM (50 ml). Et3N (25 ml; 0.178 mol) was added to a stirring solution. l-(l,l-dimethylethyl)-4- (4-carboxyphenyl)-l-piperazinecarboxylic acid ester (10.429 g; 0.034 mol) was added and the mixture was stirred. CH2Cl2 (100 ml) was added and then DECP (11.9 ml; 0.0796 mol) was added. The reaction mixture was stirred for 18 hours. Then the mixture was stirred in a saturated NaHCO3-solution. The organic layer was separated, dried with MgSO4, filtered off, evaporated and co-evaporated with toluene. Yield : 15.815 g of intermediate 51 (99 %).

As the paragraph descriping shows that 162046-66-4 is playing an increasingly important role.

Reference：
Patent; JANSSEN PHARMACEUTICA N.V.; WO2008/148868; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

149057-19-2, 4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of piperazine-1,2,4-tricarboxylic acid 4-benzyl ester 1-tert-butyl ester (0.364 g, 1 mmol) in dichloromethane (3 mL) was added O-Methyl Hydroxylamine HCl (95 mg, 1.13 mmol), EDC HCl (0.3 g, 1.57 mmol) and DIEA (0.28 g, 2.17 mmol). The resulting mixture was stirred at room temperature overnight and partitioned between dichloromethane and water. The combined organic extracts were washed with brine, dried, and evaporated. The residue was purified by flash column chromatography on silica gel, eluting with EtOAc/n-Hexane (30/70) to afford the title product.LC/MS (m/z) [M]+ 394.2 (calculated for C19H27N3O6, 393.19).

149057-19-2, As the paragraph descriping shows that 149057-19-2 is playing an increasingly important role.

Reference：
Patent; BIGNAN, Gilles; Gaul, Micheal; Xu, Guozhang; Zhao, Bao-Ping; US2011/150864; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1228780-72-0, 1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In a 500-mL three necked round bottom flask equipped with magnetic stirrer, thermometer, condenser, charged 4-bromo-2-(1H-pyrrolo[2,3-b]pyridine-5-yloxy)benzoic acid (8.67 g, 26 mmol), (4-(N,N-dimethylamino)phenyl)-di-tert-butyl-phosphine (APhos, 895 mg, 0.78 mmol, 0.13 equiv), tris(dibenzylideneacetone)-dipalladium(0) (1.54 g, 1.69 mmol, 0.065 equiv), THF (87 mL) and 1-[[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl]methyl]piperazine in toluene (31.2 g, 29 mmol, 1. 12 equiv). The reaction mixture was stirred under inert atmosphere, 1.5 M lithium bis(trimethylsilyl)amide in THF (74 mL, 112 mmol, 4.3 equiv) was added, and heated to 55-56C. The reaction mixture was stirred at 55-56C for 30 min then quenched by addition of cold (2-8C) 12% aqueous NaCl (347 mL). After phase separation the organic layer was filtered and concentrated in vacuum to 1/3 volume. The residue was added to a cold (0-5C) suspension of perlite (22 g) in n-heptane (364 mL). The suspension was stirred for 1 hour at 0-5C then filtered. The wet-cake was washed with n-heptane (3 x87 mL), and dried under vacuum at 20-25C for 2 hours. The solid was suspended in THF (87 mL), filtered and the wet cake was washed with THF (4×87 mL). HPLC-analysis of the combined THF solution comprised 8.3 g of VNT-08 content (yield: 56%).

1228780-72-0, 1228780-72-0 1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine 66713599, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ASSIA CHEMICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; POTARINE JUHASZ, Zsuzsa; STRUBA, Szabolcs; NEMETHNE RACZ, Csilla; TOTH, Zoltan Gabor; SZILAGYI, Andrea; KERTI-FERENCZI, Renata; MOLNAR, Sandor Janos; PASZTOR-DEBRECZENI, Nora; HAJKO, Janos; (100 pag.)WO2017/156398; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1228780-72-0, 1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound J, methyl 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)- 4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)benzoate, may be prepared as follows. A mixture of Compound I (1.55 g), Compound F (2.42 g), and HK2PO4 (1.42 g) in dimethylsulfoxide (20 mL) at 135 C. was stirred for 24 hours. The reaction was cooled, diluted with ether (400 mL), and washed with 3×1M NaOH, and brine, and concentrated. The crude product was chromatographed on silica gel with 10-50% ethyl acetate/hexanes to provide the product (Compound J).

1228780-72-0, As the paragraph descriping shows that 1228780-72-0 is playing an increasingly important role.

Reference：
Patent; ACERTA PHARMA B.V.; HAMDY, Ahmed; ROTHBAUM, Wayne; IZUMI, Raquel; LANNUTTI, Brian; COVEY, Todd; ULRICH, Roger; JOHNSON, Dave; BARF, Tjeerd; KAPTEIN, Allard; (732 pag.)WO2016/24230; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a i-dram vial WaS added 4-(4-(lert-butoxvcarbonvi)piperazin-i-vi)henzoic acid (345 mg, 1127 mrnoi), THF (5 rnL), HATU (514mg, 1.352 mmol) and EtsN (0785 mL,5.63 rnrnol). The reaction was stirred at rt for 10 mm and then Intermediate 4 (450 mg,1.127 mmol) was added and the reaction was continued for 4 hr. The reaction was partitioned between EtOAc (20 ml) and water (15 ml). The organic layer was separated, washed with brine (15 ml). dried over MgSO4, filtered and concentrated. The residue was purified using 1SCO system (0-100% EtOAcLElex gradient, then 0-20%MeOH/CH2CI2 gradient) to give tert-but I 4-(4-(2-(3-methoxy-4-(1H-pyrazoi-4- yi)phenyi)- 1 -oxo-2,S-diazaspiro[4. 51 decane-8-carbonyi)phenyi)piperazine-1 -carboxylate (500 mg, 0.8 13 mrnol, 72.2 % yield) as a light beige solid. 1J4 NMR (500MHz, DMSOd6) oe 809 (hr. s.. 1FI). 793 (hr. s., IH),764 – 7.57 (m, 21:1), 7.31 (d. J:::55 Hz, 2H), 7.15 (dd, J=8.4, 2.1 Hz, 1H), 6.98 (d. J=8,8 Hz, 2H), 3.92 – 383 (m. 5H), 352 – 3.42 (m, 4H),3.28 (s, 414), 3.22 – 319 (m, 4H), 2.15 (t, J=6.9 Hz, 2H), 1.78 – 1.67 (in, 2H), 1.57 (d, .J::129 Hz, 2H). 143 (s, 91-1): MS (ESI) in/z: 615.1 (M+H)., 162046-66-4

162046-66-4 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid 2795508, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BRISTOL-MYERS SQUIBB COMPANY; ZHU, Yeheng; DEWNANI, Sunita, V.; EWING, William, R.; (265 pag.)WO2019/89868; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Synthesis of 7-{4-[l~Chlowmethyi-2-(2-methyl-5-niiro mid zol-l-yl)- ethoxycarbonylmeihyl J-piperazin-1 -yl }-6~fl uoro- 1 ~methyl~4~oxo-4H~2~thia-8b~ aza-cyclobuia[a]naphthalene~3-carboxylic acid (1): To a stirred solution of 6- Fluoro- 1 -methy l-4-oxo-7-piperazin- 1 -y l~4H-2-thia~8b-aza~ cyclobuta[a]naphthalene-3-carboxylic acid, (III) (0.07 Ig, 0.2 mmol) in dimethylformamide (10ml) was added potassium carbonate (0.04g, 0.3 mmol) followed by addition of compound (II) (O.lg, 0.3 mmol) and the reaction mixture was stirred at RT for 3h. The reaction mixture was diluted with ethylacetate, washed two times with water and finally dried over sodium sulphate to obtain the crude mass. The crude was purified by flash column chromatography while eluting with 3-5% methanol/dichloromethane mixture to obtain the pure compound (1), i.e., Compound 90 from Table 1, with 30% isolated yield. H-NMR (400 MHz, DMSO) 6ppm: 2.19 (3H, d, J = 6.4 Hz, CH3), 2.57 (3H, s, CH3), 2.7 (4H, m, 2 x CH2), 3.1-3.3 (2H, s, COCH2), 3.32 (4H, m, 2 x CH2), 3.77-3.90(2H, ddd, Jx = 3.6 Hz, J2 = 12.4 Hz, J3 = 35.2 Hz, CH2C1), 4.40- 4.56 (1H, dd, Ji = 9.6 Hz, J2 = 14 Hz CHN), 4.76 (1H, d, J = 14 Hz, CHN), 5.44 (1H, d , J-5.6Hz CHOCO), 6.0-6.1 1 (1H, q, Jx = 6 Hz, J2 = 12.4 Hz, CHSN), , 6.4 (1H, d, Jx = 6.8 Hz Ar-H), 7.8 (1H, d, J = 14 Hz, Ar-H), 8.04 (1H, s, Ar-H). ESI-MS (m/z): 609 (M+H)+.

112984-60-8, As the paragraph descriping shows that 112984-60-8 is playing an increasingly important role.

Reference：
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; CHAWRAI, Suresh Rameshlal; GHOSH, Shamik; GHOSH, Sumana; JAIN, Nilu; SADHASIVAM, Suresh; BUCHTA, Richard; BHATTACHARYYA, Anamika; WO2015/114666; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

112257-12-2, tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Commercially available imidazole (0.33 g, 4.9 mmol) was dissolved in 2 mL of freshly distilled DMF, under N2, and cooled to 0 C. Sodium hydride (0.14 g, 5.9 mmol) was added to the reaction and stirred for 30 min before a dropwise addition of tert-butyl 4-(2-bromoacetyl)piperazine-1-carboxylate (1.50 g, 4.9 mmol) dissolved in 2 mL of DMF. The mixture was slowly warmed to room temperature and stirred overnight. Addition of 10 mL of water caused a white precipitate to form. The solid was filtered and dried under reduced pressure overnight to afford tert-butyl 4-(2-(1H-imidazol-1-yl)acetyl)piperazine-1-carboxylate 8a (0.97 g,3.3 mmol, 67%); mp: 147-149 C. 1H NMR (400 MHz, CDCl3) delta 7.53(s, 1H), 7.11 (s, 1H), 6.96 (s,1H), 4.80 (s, 2H), 3.62 (bs, 2H), 3.48 (bs,6H), 1.47 (s, 9H); 13C NMR (100 MHz, CDCl3) delta 165.0, 154.5, 138.1, 129.7, 120.2, 80.8, 48.2, 45.1, 43.5, 42.2, 28.5; HRMS (ESI TOF): [M+H]+Calc’d for C14H23N4O3 m/z 295.1770. Found, m/z 295.1751.

112257-12-2, As the paragraph descriping shows that 112257-12-2 is playing an increasingly important role.

Reference：
Article; Abuteen, Akram; Zhou, Feifei; Dietz, Christopher; Mohammad, Innus; Smith, Michael B.; Zhu, Quing; Dyes and Pigments; vol. 126; (2016); p. 251 – 260;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1228780-72-0, 1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound J, methyl 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)- 4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)benzoate, may be prepared as follows. A mixture of Compound I (1.55 g), Compound F (2.42 g), and HK2PO4 (1.42 g) in dimethylsulfoxide (20 mL) at 135 C. was stirred for 24 hours. The reaction was cooled, diluted with ether (400 mL), and washed with 3×1M NaOH, and brine, and concentrated. The crude product was chromatographed on silica gel with 10-50% ethyl acetate/hexanes to provide the product (Compound J).

1228780-72-0, As the paragraph descriping shows that 1228780-72-0 is playing an increasingly important role.

Reference：
Patent; ACERTA PHARMA B.V.; HAMDY, Ahmed; ROTHBAUM, Wayne; IZUMI, Raquel; LANNUTTI, Brian; COVEY, Todd; ULRICH, Roger; JOHNSON, Dave; BARF, Tjeerd; KAPTEIN, Allard; (732 pag.)WO2016/24230; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a i-dram vial WaS added 4-(4-(lert-butoxvcarbonvi)piperazin-i-vi)henzoic acid (345 mg, 1127 mrnoi), THF (5 rnL), HATU (514mg, 1.352 mmol) and EtsN (0785 mL,5.63 rnrnol). The reaction was stirred at rt for 10 mm and then Intermediate 4 (450 mg,1.127 mmol) was added and the reaction was continued for 4 hr. The reaction was partitioned between EtOAc (20 ml) and water (15 ml). The organic layer was separated, washed with brine (15 ml). dried over MgSO4, filtered and concentrated. The residue was purified using 1SCO system (0-100% EtOAcLElex gradient, then 0-20%MeOH/CH2CI2 gradient) to give tert-but I 4-(4-(2-(3-methoxy-4-(1H-pyrazoi-4- yi)phenyi)- 1 -oxo-2,S-diazaspiro[4. 51 decane-8-carbonyi)phenyi)piperazine-1 -carboxylate (500 mg, 0.8 13 mrnol, 72.2 % yield) as a light beige solid. 1J4 NMR (500MHz, DMSOd6) oe 809 (hr. s.. 1FI). 793 (hr. s., IH),764 – 7.57 (m, 21:1), 7.31 (d. J:::55 Hz, 2H), 7.15 (dd, J=8.4, 2.1 Hz, 1H), 6.98 (d. J=8,8 Hz, 2H), 3.92 – 383 (m. 5H), 352 – 3.42 (m, 4H),3.28 (s, 414), 3.22 – 319 (m, 4H), 2.15 (t, J=6.9 Hz, 2H), 1.78 – 1.67 (in, 2H), 1.57 (d, .J::129 Hz, 2H). 143 (s, 91-1): MS (ESI) in/z: 615.1 (M+H)., 162046-66-4

162046-66-4 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid 2795508, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BRISTOL-MYERS SQUIBB COMPANY; ZHU, Yeheng; DEWNANI, Sunita, V.; EWING, William, R.; (265 pag.)WO2019/89868; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Synthesis of 7-{4-[l~Chlowmethyi-2-(2-methyl-5-niiro mid zol-l-yl)- ethoxycarbonylmeihyl J-piperazin-1 -yl }-6~fl uoro- 1 ~methyl~4~oxo-4H~2~thia-8b~ aza-cyclobuia[a]naphthalene~3-carboxylic acid (1): To a stirred solution of 6- Fluoro- 1 -methy l-4-oxo-7-piperazin- 1 -y l~4H-2-thia~8b-aza~ cyclobuta[a]naphthalene-3-carboxylic acid, (III) (0.07 Ig, 0.2 mmol) in dimethylformamide (10ml) was added potassium carbonate (0.04g, 0.3 mmol) followed by addition of compound (II) (O.lg, 0.3 mmol) and the reaction mixture was stirred at RT for 3h. The reaction mixture was diluted with ethylacetate, washed two times with water and finally dried over sodium sulphate to obtain the crude mass. The crude was purified by flash column chromatography while eluting with 3-5% methanol/dichloromethane mixture to obtain the pure compound (1), i.e., Compound 90 from Table 1, with 30% isolated yield. H-NMR (400 MHz, DMSO) 6ppm: 2.19 (3H, d, J = 6.4 Hz, CH3), 2.57 (3H, s, CH3), 2.7 (4H, m, 2 x CH2), 3.1-3.3 (2H, s, COCH2), 3.32 (4H, m, 2 x CH2), 3.77-3.90(2H, ddd, Jx = 3.6 Hz, J2 = 12.4 Hz, J3 = 35.2 Hz, CH2C1), 4.40- 4.56 (1H, dd, Ji = 9.6 Hz, J2 = 14 Hz CHN), 4.76 (1H, d, J = 14 Hz, CHN), 5.44 (1H, d , J-5.6Hz CHOCO), 6.0-6.1 1 (1H, q, Jx = 6 Hz, J2 = 12.4 Hz, CHSN), , 6.4 (1H, d, Jx = 6.8 Hz Ar-H), 7.8 (1H, d, J = 14 Hz, Ar-H), 8.04 (1H, s, Ar-H). ESI-MS (m/z): 609 (M+H)+.

112984-60-8, As the paragraph descriping shows that 112984-60-8 is playing an increasingly important role.

Reference：
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; CHAWRAI, Suresh Rameshlal; GHOSH, Shamik; GHOSH, Sumana; JAIN, Nilu; SADHASIVAM, Suresh; BUCHTA, Richard; BHATTACHARYYA, Anamika; WO2015/114666; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics