Category: 1228780-72-0

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

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1228780-72-0,1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine,as a common compound, the synthetic route is as follows.

round bottom flask equipped with mechanical stirrer and thermometer, to dimethylsulfoxide (250 ml), pyrrolopyridine ester (IV X = F & R = CH3) (50 g) and piperazine dihydrochloride (III) (89 g) were added. To this reaction mixture, 1,8- diazabicyclo[5.4.0]undec-7-ene (DBU) (157 ml) was added and the reaction mixture washeated to 75-85 C and maintained for 48 hrs. The reaction mixture was then cooled to room temperature and ice cooled water (1000 ml) was added. Solid separated was filtered, washed with water and then dissolved in ethyl acetate (500 ml). To the ethyl acetate layer was added water (500 ml) and ethyl acetate (500 ml), organic layer was extracted, washed with water, dried and concentrated to obtain gummy mass. To thisgummy mass was added isopropyl alcohol (200 ml), stirred and filtered to obtain the crude title compound which was recrystallized from isopropyl alcohol to give the pure title compound (47 g)

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; LUPIN LIMITED; RAJPUT, Lalitkumar, Dilipsing; VYAVHARE, Vasant, Chhabu; SHIVDAVKAR, Radhakrishna, Bhikaji; SUDRIK, Yuvraj, Dadasaheb; MITRA, Rangan; GOKHALE, Sangram; GOHEL, Sunilkumar, Vinubhai; SIYAN, Rajinder, Singh; BHISE, Nandu, Baban; SINGH, Girij, Pal; (54 pag.)WO2018/225043; (2018); 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.1228780-72-0,1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine,as a common compound, the synthetic route is as follows.

A mixture of EXAMPLE 1H (1.55 g), EXAMPLE IE (2.42 g), and HK2P04 (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 three times with 1M aqueous NaOH, and brine, and concentrated. The residue was purified by flash chromatography, eluting with 10-50% ethyl acetate in hexanes to provide the title compound., 1228780-72-0

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

Reference：
Patent; ABBOTT LABORATORIES; TAO, Zhi-Fu; WANG, Xilu; SOUERS, Andrew J.; CATRON, Nathaniel D.; SULLIVAN, Gerard; WO2011/150016; (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

1228780-72-0, Example 30H ethyl 2-(1H-indol-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)benzoate EXAMPLE 30A (330 mg), EXAMPLE 30G (335 mg), and HK2PO4 (191 mg) were stirred in dimethylsulfoxide (5 mL) at 140 C. for 24 hours. The reaction was diluted with ethyl acetate, washed three times with water, washed with brine, dried over Na2SO4, filtered, and concentrated. The crude product was chromatographed on silica gel with 30% ethyl acetate/hexanes.

The synthetic route of 1228780-72-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ABBOTT LABORATORIES; US2010/184750; (2010); 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

A mixture of methyl 2-((lH-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-fluorobenzoate (500.0 g), l-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[l,l’-biphenyl]-2-yl)- methyljpiperazine (1114.0 g) and N,N-diisopropylethylamine (225.8 g) in dimethylsulphoxide (1500 mL) was heated to 90 to 105 degree Celsius for 26h. The reaction mixture was diluted with ethyl acetate (2500 ml) and washed with water (2500 mL). The organic layer was concentrated under vacuum. The residue was taken up in methanol (2500 mL) at 60 to 65 degree Celsius and cooled to 20 to 30 degree Celsius and stirred for 4h, followed by 0 to 5 degree Celsius for 3h. The resulting slurry was filtered and washed with cold methanol (500 mL). The filtered solid was treated with concentrated hydrochloric acid (218.3 g) in methanol (3200 mL) followed by addition of water (1600 mL). The resulting slurry was cooled to 0 to 5 degree Celsius, filtered and washed with a 2:1 mixture of methanol-water and the solid dried under vacuum at 50 to 60 degree Celsius for 16 h to provide methyl 2-((lH-pyrrolo[2,3-b]pyridin-5- yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro[l,l’-biphenyl]-2- l)methyl)piperazin- 1 -yl)-benzoate. HC1. Yield: 74.14% (805g) HPLC Purity: -99.3% 1H NMR data-(DMS 0-d6) : d 0.942 (s, 6H), 1.444 (t, J=6.4 Hz, 2H), 2.014 (s, 2H), 2.366 (t, br, 2H), 2.723 (d, 2H), 3.281 (m, 4H), 3.702 (m, 2H), (m, d, J=12.8 Hz, 8H), 3.542 (s, 2H), 3.659 (s, 3H), 6.385 (dd, J= 1.6, 2.0, 3.2, 3.6Hz, 1H), 6.414-6.420 (d, =2.4Hz, 1H), 6.776 (dd, J=2.4, 9.2Hz, 1H), 7.105 (d, J=8.4Hz, 2H), 7.395( d, J=8.4Hz, 2H), 7.438 (d, J=2.0, 1H), 7.483 (t, J=2.8Hz, 1H), 7.781 (d, J=9.2Hz, 1H), 7.999 (d, J=2.8Hz, 1H), 10.752 (s, br, 1H), 11.666 (s,lH)., 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; FRESENIUS KABI ONCOLOGY LTD.; GUPTA, Chandan Kumar; DHIMAN, Navdeep; SANGHANI, Sunil; SINGH, Govind; LAHIRI, Saswata; CABRI, Walter; GUPTA, Nitin; (0 pag.)WO2020/3272; (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.1228780-72-0,1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine,as a common compound, the synthetic route is as follows.

Example 33G ethyl 2-(1H-indol-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)benzoate EXAMPLE 33A (225 mg), EXAMPLE 33F (240 mg), and HK2PO4 (131 mg) were stirred in dimethylsulfoxide (4 mL) at 135 C. for 24 hours. The reaction was diluted with ethyl acetate, washed three times with water, washed with brine, dried, and concentrated. The crude product was chromatographed on silica gel with 30% ethyl acetate/hexanes., 1228780-72-0

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

Reference：
Patent; ABBOTT LABORATORIES; US2010/184766; (2010); 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

EXAMPLE 2OD ethyl 2-(lH-indazol-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-l- enyl)methyl)piperazin- 1 -yl)benzoate; EXAMPLE 2OA (330 mg), EXAMPLE 2OC (335 mg), and HK2PO4 (191 mg) were stirred in dimethylsulfoxide (5 mL) at 14O0C for 24 hours. The reaction was diluted with ethyl acetate, washed three times with water, washed with brine, dried, and concentrated. The crude product was chromatographed on silica gel with 30% ethyl acetate/hexanes., 1228780-72-0

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

Reference：
Patent; ABBOTT LABORATORIES; BRUNCKO, Milan; DING, Hong; DOHERTY, George, A.; ELMORE, Steven, W.; HASVOLD, Lisa; HEXAMER, Laura; KUNZER, Aaron, R.; MANTEI, Robert, A.; MCCLELLAN, William, J.; PARK, Chang, H.; PARK, Cheol-min; PETROS, Andrew, M.; SONG, Xiaohong; SOUERS, Andrew, J.; SULLIVAN, Gerard, M.; TAO, Zhi-fu; WANG, Gary, T.; WANG, Le; WANG, Xilu; WENDT, Michael, D.; WO2010/65865; (2010); A2;,
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

EXAMPLE 2OD ethyl 2-(lH-indazol-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-l- enyl)methyl)piperazin- 1 -yl)benzoate; EXAMPLE 2OA (330 mg), EXAMPLE 2OC (335 mg), and HK2PO4 (191 mg) were stirred in dimethylsulfoxide (5 mL) at 14O0C for 24 hours. The reaction was diluted with ethyl acetate, washed three times with water, washed with brine, dried, and concentrated. The crude product was chromatographed on silica gel with 30% ethyl acetate/hexanes., 1228780-72-0

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

Reference：
Patent; ABBOTT LABORATORIES; BRUNCKO, Milan; DING, Hong; DOHERTY, George, A.; ELMORE, Steven, W.; HASVOLD, Lisa; HEXAMER, Laura; KUNZER, Aaron, R.; MANTEI, Robert, A.; MCCLELLAN, William, J.; PARK, Chang, H.; PARK, Cheol-min; PETROS, Andrew, M.; SONG, Xiaohong; SOUERS, Andrew, J.; SULLIVAN, Gerard, M.; TAO, Zhi-fu; WANG, Gary, T.; WANG, Le; WANG, Xilu; WENDT, Michael, D.; WO2010/65865; (2010); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics