Simple exploration of 152265-57-1

152265-57-1 7-Bromophthalazin-1(2H)-one 22265317, aphthalazine compound, is more and more widely used in various.

152265-57-1, 7-Bromophthalazin-1(2H)-one is a phthalazine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 7-bromo-l,2-dihydrophthalazin-l-one (4.1 g, 18.22 mmol) and bis(pinacolato)diboron (12.95 g, 51.01 mmol) was dissolved in 1,4-dioxane (150 mL) under nitrogen. Potassium acetate (5.36 g, 54.66 mmol) was added, and the reaction mixture was degassed with N2 for 5 minutes. Pd(dppf)Cl2 (0.74 g, 0.91 mmol) was added and the mixture was heated at 110C for 1.5 h, then cooled and diluted with DCM. The solids were removed by filtration through celite. The residue was washed with DCM and the combined organic phases were concentrated in vacuo. The resulting solid was triturated in heptane (30 mL) and diethyl ether (15 mL). The solid was further triturated with heptane (30 mL) and diethyl ether (15 mL), then the precipitate was collected by filtration, to give the title compound (5.1 g, 81%). deltaEta (250 MHz, DMSO-d6) 12.68 (s, 1H), 8.50 (s, 1H), 8.37 (s, 1H), 8.10 (dd, J7.8, 1.1 Hz, 1H), 7.88 (d, J7.8 Hz, 1H), 1.30 (s, 12H). Method B: HPLC-MS MH+ mlz 273, RT 1.78 minutes (97%)

152265-57-1 7-Bromophthalazin-1(2H)-one 22265317, aphthalazine compound, is more and more widely used in various.

Reference£º
Patent; UCB BIOPHARMA SPRL; BRACE, Gareth Neil; CHOVATIA, Prafulkumar Tulshibhai; FOULKES, Gregory; JOHNSON, James Andrew; JONES, Severine Danielle; KROEPLIEN, Boris; LECOMTE, Fabien Claude; LOKE, Pui Leng; LOWE, Martin Alexander; MANDAL, Ajay; NORMAN, Timothy John; PALMER, Christopher Francis; PEREZ-FUERTES, Yolanda; PORTER, John Robert; SMYTH, Donald; TRANI, Giancarlo; UDDIN, Muhammed; ZHU, Zhaoning; (207 pag.)WO2016/198400; (2016); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

Some tips on 152265-57-1

152265-57-1 7-Bromophthalazin-1(2H)-one 22265317, aphthalazine compound, is more and more widely used in various.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.152265-57-1,7-Bromophthalazin-1(2H)-one,as a common compound, the synthetic route is as follows.

A mixture of compound 50-d (600mg, 2.67mmol) and POCl3 (8mL) was heated to reflux for 1.5h, cooled toroom temperature and concentrated under reduced pressure. The residue was dissolved in DCM (40mL), washed inturn with saturated sodium bicarbonate (40mL) and saturated brine (10mL), dried over anhydrous sodium sulfate, filteredand concentrated under reduced pressure. The residue was purified by silica column chromatography (PE:EA = 3:1) togive compound 50-c (500mg, yield 75%). LC-MS (ESI): m/z = 243 [M+H]+.

152265-57-1 7-Bromophthalazin-1(2H)-one 22265317, aphthalazine compound, is more and more widely used in various.

Reference£º
Patent; Shanghai Yingli Pharmaceutical Co. Ltd.; XU, Zusheng; ZHANG, Nong; SUN, Qingrui; WU, Tianzhi; (104 pag.)EP3275867; (2018); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

Analyzing the synthesis route of 152265-57-1

The synthetic route of 152265-57-1 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.152265-57-1,7-Bromophthalazin-1(2H)-one,as a common compound, the synthetic route is as follows.

Bis(pinacolato)diboron (1.1 equiv), potassium acetate (3.5 equiv) and 1,1′- bis(diphenylphosphino)ferrocene (0.05 equiv) were dissolved in dioxane. The mixture was degassed with nitrogen for 20 minutes before the addition of PdCl2(dppf) (0.05 equiv). The mixture was degassed for a further 5 minutes. The mixture was heated to reflux for 16 hours and then allowed to cool to room temperature. Water was added to the mixture before it was extracted with EtOAc (2 X 2 reaction volumes). The combined organic fractions were dried (MgSO4), filtered aned concentrated in vacuo before being purified by flash chromatography (SiO2) neat hexanes going to 1 : 1 – Hexanes:EtOAc then neat EtOAc to give the desire product as a white crystalline solid.7-(4,4,5,5-Tetramethyl-[l,3,2]dioxaborolan-2-yl)-2H-phthalazin-l-one: (86 % yield, 92 % purity) m/z (LC-MS5ESP): 191.3 [M+H]+, R/T = 2.29 min)

The synthetic route of 152265-57-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; KUDOS PHARMACEUTICALS LIMITED; WO2008/23161; (2008); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

Downstream synthetic route of 152265-57-1

As the paragraph descriping shows that 152265-57-1 is playing an increasingly important role.

152265-57-1, 7-Bromophthalazin-1(2H)-one is a phthalazine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 7-bromophthalazin-l(2H)-one (1,00 g, 4.44 mmol, 1,0 eq) in DMF (10 ml) was added 2-(chloromethyl)- oxirane (1.24 g, 13 3 mmol, 3.0 eq) and CS2CO3 (4.35 g, 13.3 mmol, 3.0 eq), and the resultant mixture was heated to 90 C for 0.5 hour. The reaction mixture was diluted with cold water, and was extracted with EA. Organic phase was washed with water twice followed by brine, dried over MgS04, and was concentrated to dryness. The obtained residue was used directly in next step without further purification.

As the paragraph descriping shows that 152265-57-1 is playing an increasingly important role.

Reference£º
Patent; PHARMABLOCK SCIENCES (NANJING), INC.; LIU, Liu; LI, Jin; YANG, Minmin; (126 pag.)WO2019/173804; (2019); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem