Heterocyclic Building Block-benzofuran

37418-88-5, 4-Hydroxyisobenzofuran-1,3-dione is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 4-hydroxyisobenzofuran-1,3-dione (1.2 g, 7.3 mmol) in pyridine (25 mL) was added 3-aminopiperidine-2,6-dione-TFA salt (1.8 g, 7.3 mmol) at room temperature. The resulting reaction mixture was then warmed to 110 C. and stirred for 16 h. The reaction mixture was then evaporated under reduced pressure. The crude product was purified using silica gel column chromatography (4% MeOH-DCM) to give 2-(2,6-dioxopiperidin-3-yl)-4-hydroxyisoindoline-1,3-dione as yellow solid (1 g, 50%). LC-MS (ESI) m/z 273.2 (M-H)+., 37418-88-5

37418-88-5 4-Hydroxyisobenzofuran-1,3-dione 96580, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; Kymera Therapeutics, Inc.; Mainolfi, Nello; Ji, Nan; Kluge, Arthur F.; Weiss, Matthew M.; Zhang, Yi; (1443 pag.)US2019/192668; (2019); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.496-16-2,2,3-Dihydrobenzo[b]furan,as a common compound, the synthetic route is as follows.

EXAMPLE 4 Preparation of 2,3-dihydrobenzofuran-5-sulfonyl chloride Sulfur trioxide-N,N-dimethylformamide complex (9.2 g, 60 mmoles) and N,N-dimethylformamide (20 ml) were added to a 250 ml, 3-necked flask under nitrogen purge. The solution was stirred at room temperature and 2,3-dihydrobenzofuran (6.0 g, 50 mmoles) was added dropwise. The solution was slowly heated to 85¡ã-90¡ã C. over the course of one hour. The light brown solution was allowed to come to room temperature and thionyl chloride (7.2 g, 60 mmoles) was added dropwise. The mixture was allowed to stir one hour at room temperature. The solution was slowly heated to 85¡ã C. and was maintained at that temperature for 1 hour. The solution was allowed to cool to 40¡ã C. Toluene (25 ml) was added to the solution, which was then poured into a mixture of ice and water (50 ml). Another 25 ml aliquot of toluene was added. The mixture was stirred for 10 minutes to dissolve any solids and the layers were separated. The aqueous layer was extracted with toluene (3*25 ml). The combined toluene layers were washed with water and dried over magnesium sulfate. The magnesium sulfate was removed and washed with toluene. The toluene was removed under vacuum, leaving 10.0 g of the title product (91.7percent yield). Nuclear magnetic resonance assays confirmed the identity of the title compound. FDMS (MeOH) m/e 218 (M+). Analysis for C8 H7 ClO3 S: Theory: C, 43.94; H, 3.23. Found: C, 44.14; H, 3.24., 496-16-2

The synthetic route of 496-16-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Eli Lilly and Company; US5387681; (1995); A;,
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87-41-2, Isobenzofuran-1(3H)-one is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Isobenzofuran-1(3H)-one (0.4 mmol), KOH (0.4 mmol), PhSiH3 (1.2 mmol), dried THF (2 mL) were charged in a Schlenk tube(15 mL) under N2 atmosphere. The mixture was refluxed for 4 h. After cooling to rt, the reaction was quenched with EtOH(0.5-1 mL). Solvent was removed under reduced pressure and the crude residue was purified by column chromatography on silica gel with petroleum ether-ethyl acetate as the eluent to afford the desired product., 87-41-2

As the paragraph descriping shows that 87-41-2 is playing an increasingly important role.

Reference£º
Article; Liu, Bin; Zhou, Xigeng; Chinese Chemical Letters; vol. 30; 3; (2019); p. 725 – 728;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.28281-76-7,5-Methoxyisobenzofuran-1,3-dione,as a common compound, the synthetic route is as follows.

28281-76-7, EXAMPLE 158 N-[2-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-4-methoxyphthalimide A stirred mixture of 2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethylamine (2.63 g, 0.01 mole) and 4-methoxyphthalic anhydride (1.78 g, 0.01 mole) in dichloromethane (100 ml) is stirred at room temperature for 3 hours. The solvent is then removed under reduced pressure and the residual material is purified by flash chromatography. The product is purified further by recrystallization to give N-[2-[4-(6-fluoro-1,2-benzisoxazol-3yl)-1-piperidinyl]ethyl]-4-methoxyphthalimide.

The synthetic route of 28281-76-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Hoechst-Roussel Pharmaceuticals, Inc.; US5364866; (1994); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.58546-89-7,Benzofuran-5-amine,as a common compound, the synthetic route is as follows.

58546-89-7, To a solution of benzofuran-5-amine (CAS No. 58546-89-7, 200 mg, 1.5 mmol) in acetic acid (8 mL) was added ammonium thiocyanate (456 mg, 6.0 mmol) at RT under nitrogen atmosphere. After stirring for 10 min, bromine (480 mg, 3.0 mmol) was added dropwise at about 10 C. The resulting mixture was slowly warmed to RT and stirred for 12 h. The precipitate was collected by filtration to afford the title compound as pale brown solid (200 mg, 70%). LC/MS (ES+) calcd for C9H6N2OS: 190.0; found: 193.0 [M+3]. 1H NMR (400 MHz, DMSO-d6): delta 8.01 (d, J=2.0 Hz, 1H), 7.46 (d, J=8.4 Hz, 1H), 7.36 (s, 2H), 7.32 (d, J=8.4 Hz, 1H), 6.99 (d, J=2.0 Hz, 1H).

As the paragraph descriping shows that 58546-89-7 is playing an increasingly important role.

Reference£º
Patent; Kineta Immuno-Oncology LLC; Goldberg, Daniel R.; Probst, Peter; Bedard, Kristin M.; (72 pag.)US2020/55871; (2020); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.496-16-2,2,3-Dihydrobenzo[b]furan,as a common compound, the synthetic route is as follows.

2,3-dihydrobenzofuran (6.0 g, 49.94 mmol) is added over 20 minutes to chlorosulfonic acid (29.09 g, 249.69 mmol) at -20¡ã C. The reaction mixture is quenched by addition of ice followed by water (20 mL). The mixture is then extracted with ethyl acetate. The combined organic estracts are washed with brine, dried (Na2 SO4), and the solvent is evaporated. The crude product is purified by silica gel chromatography (30percent ethyl acetate/hexane) to give 2,3-dihydrobenzofuran-5-sulfonyl chloride (3.3 g).

496-16-2, As the paragraph descriping shows that 496-16-2 is playing an increasingly important role.

Reference£º
Patent; Ciba-Geigy Corporation; US5455258; (1995); A;; ; Patent; Ciba-Geigy Corporation; US5552419; (1996); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.496-16-2,2,3-Dihydrobenzo[b]furan,as a common compound, the synthetic route is as follows.

Bromination using NBS has been found to be applicable for use with a wide range of aromatic starting materials or substrates, as is EPO summarized in Table 1 . For example, anisole can be brominated by use of 1 equivalent of NBS in the presence of 5 mol % of ZrCI4 at -78 0C to afford p- bromoanisole in 98% yield as sole product (Table 1 , Entry 1 ). However, in the absence of ZrCI4 the halogenation does not proceed, even at room temperature (Table 1 , Entry 1 ).[00111] All of the substrates shown in Table 1 were brominated to give the corresponding monobromo products in excellent yield and regioselectivity. In most cases, the reaction can proceed at very low temperature and no further purification is necessary. In addition. Table 1 reveals that the halogenation of the present invention is compatible with a variety of substituents.Table 1 ZrCI4 Catalyzed Bromination of Aromatic Compounds EPO (5 mol %), CH2CI2 (4d See spectroscopic data for characterization.

496-16-2, 496-16-2 2,3-Dihydrobenzo[b]furan 10329, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; UNIVERSITY OF CHICAGO; JAPAN SCIENCE AND TECHNOLOGY AGENCY; WO2007/27917; (2007); A2;,
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10242-08-7, 5-Methoxybenzofuran-2-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Under ice-cooling,2-hydroxy-5-methoxybenzaldehyde (3.0g, 20mmol) and anhydrous K2CO3 (3.3g,23.4mmol) (50ml) was dissolved in DMF, was slowly added dropwise ethylbromoacetate (3.3g, 20mmol). After dropping Bi, 0 C was stirred for 30min,then at 60 C in an oil bath, the reaction 12h. The reaction solution waspoured into ice water, over Filtered, the solid was dissolved in chloroform,dried over anhydrous Na2SO4, filtered, and spin dry the solvent, by silica gelcolumn chromatography, To give 3.24 g of a yellow solid (75% yield), which was dissolved indioxane (30ml) was added 1N hydrogen Sodium hydroxide solution (15ml), stirredat room temperature 2h, the dioxane was evaporated to dryness, the residualliquid was poured into ice water, washed with diethyl Washed with methylenechloride, adjusting the PH value to 2, the solid was collected by filtration 2.68g (92% yield), whichwas dissolved in methylene Dioxane (50ml), was added DIC (1.51g, 11.98mmol),after stirring at room temperature 1h, was added DMAP (0.24g, 1.96 mmol) anddimethyl hydroxyethyl phosphonate (1.84g, 10.95mmol), heated to reflux after6h, water and saturated brine The reaction solution was washed with water,dried over anhydrous magnesium sulfate, filtered and evaporated to dryness,ethyl acetate – petroleum ether system recrystallized To (dimethoxyphosphoryl)ethyl 5-methoxybenzofuran-2-carboxylate 3.67g (77% yield), which was Was dissolved indichloromethane (50ml), was added trimethylsilyl bromide (9.85g, 64.8mmol) atroom temperature was stirred for 3h, with Quench with methanol, evaporated todryness to give the product 5-methoxy-benzofuran-2-carboxylic acid ethyl esterphosphono 2.38 g (yield, 74%)., 10242-08-7

As the paragraph descriping shows that 10242-08-7 is playing an increasingly important role.

Reference£º
Patent; Institute of Medicinal Biotechnology Chinese Academy of MedicalSciences; Li, Zhuorong; Liu, Zongying; Xue, Situ; He, Xiaobo; Jin, Jie; Si, Shuyi; Ye, Weidong; (43 pag.)CN103130705; (2016); B;,
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166599-84-4, Benzofuran-4-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a mixture of benzofuran-4-carboxylic acid (Eissenstat M. A. et al, J. Med. Chem. 1995, 38, 16, 3094-3105 (61 mg), PyBOP (196 mg), DIEA (0.15 mL) in dry DMF (0.5 mL), was added a solution of (2RS)-(2-aminomethyl-azetidin-1-yl)-biphenyl-2-yl-methanone (100 mg) in dry DMF (0.5 mL). The resulting reaction mixture was stirred at RT for 20 h. The reaction mixture was diluted with EA, washed with water. The aqueous phase was extracted once again with EA, the combined organic extracts were dried (MgSO4), filtered and concentrated to yield the crude product as light brown oil.FC (EA) gave 140 mg (71%) of the title compound as a light yellow oilLC-MS: rt=0.99 min, 411 [M+H]+., 166599-84-4

As the paragraph descriping shows that 166599-84-4 is playing an increasingly important role.

Reference£º
Patent; Actelion Pharmaceuticals Ltd.; US2010/222600; (2010); A1;,
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64169-34-2, 5-Bromoisobenzofuran-1(3H)-one is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Add phenol (20.4g, 0.22mol) and DMF 50mL to the reaction flask and start stirring.5-Bromoisobenzofuran-1(3H)-one (34.0 g, 0.16 mmol), acetylacetone (3.2 g, 0.03 mol), cuprous bromide (3.6 g, 0.03 mol), potassium carbonate (at room temperature) 30.8g, 0.22mol), three times of nitrogen replacement, heating to 90 C, stirring reaction overnight, adding 1000 mL of purified water to the reaction solution, suction filtration, the filter cake was dissolved in 800 mL of dichloromethane, and the organic phase was washed with 800 mL of 1N hydrochloric acid solution, with purified water. 1000 mL washing, drying the organic phase, and concentrating to dryness under reduced pressure to give a yellow solid.The title compound 2b (22.5 g, 63%) was obtained.

64169-34-2, 64169-34-2 5-Bromoisobenzofuran-1(3H)-one 603144, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; Sichuan Kelun Botai Bio-pharmaceutical Co., Ltd.; Cai Jiaqiang; Xie Yinong; You Zejin; Song Changwei; Zhang Jichao; Li Lu; Zhang Qiaoling; Wang Yongqiang; Chen Xing; Jiao Shihu; Li Youqiang; Wang Tao; Zeng Hong; Song Hongmei; Ye Qijun; Su Donghai; Zhou Xin; Zhang Shaohua; Wang Lichun; Wang Jingyi; (122 pag.)CN108341777; (2018); A;,
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