Little discovery in the laboratory: a new route for 1,1-Dioxo-isothiazolidine

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An elementary termolecular reaction involves the simultaneous collision of three atoms, molecules, or ions.1438-16-0, name is 3-Aminorhodanine. Here is a downstream synthesis route of the compound 1438-16-0. 1438-16-0

A microwave vial was charged with (5-{7-chloro-6-fluoro-5-[(S)-oxan-4- yl(phenyl)methyl]-5H-pyrido[3,2-b]indol-3-yl}-4-(2H3)methyl-l-methyl-lH-l,2,3- triazole (30 mg, 0.061 mmol), isothiazolidine 1,1-dioxide (11.1 mg, 0.091 mmol), tripotassium phosphate (18.1 mg, 0.085 mmol), Pd2(dba)3 (2.8 mg, 3.0 muiotatauiotaomicron), 2-di-tert- butylphosphino-3,4,5,6-tetramethyl-2′,4′,6′-triisopropyl-l, -biphenyl (2.9 mg, 6.1 mumol), and dry tert-butanol (0.5 mL). The reaction was heated at 84C overnight. It was diluted with water and extracted with ethyl acetate. The organic layer was concentrated and purified by preparative HPLC (Column: XBridge CI 8, 19 x 200 mm, 5-muiotatauiota particles; Mobile Phase A: 5:95 acetonitrile: water with 10-mM ammonium acetate; Mobile Phase B: 95:5 acetonitrile: water with 10-mM ammonium acetate; Gradient: 15-55% B over 15 min, then a 5-min hold at 100% B; Flow: 20 mL/min) to give 2.1 mg (6%). NMR (500 MHz, DMSO) delta 8.61 (s, 1H), 8.11 (m, 1H), 7.96 (s, 1H), 7.64 (m, 2H), 7.45 (m, 1H), 7.35 (m, 2H), 7.28 (m, 1H), 5.91 (m, 1H), 3.9 (m, 5H), 3.77 (m, 1H), 3.52 (m, 3H), 3.29 (m, 1H), 2.55 9m, 2H), 1.78 (m, 1H), 1.35 (m, 2H), 1.1 (m, 1H); LCMS (M+H) = 578.35

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Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; HAN, Wen-Ching; DEGNAN, Andrew P.; DESKUS, Jeffrey A.; GAVAI, Ashvinikumar V.; GILL, Patrice; SCHMITZ, William D.; STARRETT, John E., Jr.; (193 pag.)WO2016/183115; (2016); A1;,
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Fun Route: New Discovery of 5908-62-3

A chemical reaction often occurs in steps, although it may not always be obvious to an observer. Thank you very much for taking the time to read this article. If you are also interested in other aspects of 1,1-Dioxo-isothiazolidine, you can also browse my other articles.

171877-39-7, An elementary termolecular reaction involves the simultaneous collision of three atoms, molecules, or ions.171877-39-7, name is (S)-4-Benzylthiazolidine-2-thione. Here is a downstream synthesis route of the compound 171877-39-7

Procedure E; [00215] To a sealed tube containing CuI (8mg, 0.039mmol), K2CO3 (0.2 Ig, 1.54 mmol) and (IS, 25)-cyclohexane-l,2-diamine (9mg, 0.077 mmol) under a N2 atmosphere was added a solution of 5-bromo-2-(naphthalene-2-yl)benzo[d]oxazole (0.25g, 0.77 mmol) in anhydrous toluene (2.5 mL), followed by a solution of isothiazolide-l,2-dioxide (0.12g, 0.96 mmol) in anhydrous toluene (2.5 mL). The resulting reaction mixture was heated to HO0C for 12h, cooled to room temperature, filtered over celite and concentrated under reduced pressure. The residue was purified by column chromatography eluting with petroleum ether/EtOAc (1/0 to 0/1, v/v), followed by a crystallisation from industrial methylated spirits to give 30mg (11%) of 5-(isothiazolidin-dioxide-2-yl)-2-(naphthalene-2-yl)benzo[d]oxazole. LCMS RT = 2.24 min, M+H+ 364.8. 1H NMR (D6-DMSO): 8.84 (IH, br s), 8.26 (IH, dd, J 1.6 &; 8.6), 8.20- 8.13 (2H, m), 8.06-8.03 (IH, m), 7.85 (IH, d, J 8.8), 7.70-7.63 (3H, m), 7.38 (IH, dd, J2.3 &; 8.9), 3.84 (2H, t, J6.5), 3.55 (2H, t, J7.3), 2.45 (2H, m).

A chemical reaction often occurs in steps, although it may not always be obvious to an observer. Thank you very much for taking the time to read this article. If you are also interested in other aspects of 1,1-Dioxo-isothiazolidine, you can also browse my other articles.

Reference£º
Patent; BioMarin IGA, Ltd.; WREN, Stephen, Paul; WYNNE, Graham, Michael; WILSON, Francis, Xavier; POIGNANT, Severine, Danielle; WO2010/112093; (2010); A1;,
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Derivation of elementary reaction about 5908-62-3

This molecular description is the mechanism of the reaction; it describes how individual atoms, ions, or molecules interact to form particular products.If you are interested, you can also browse other articles of 1,1-Dioxo-isothiazolidine, We look forward to the emergence of more reaction modes in the future.

26364-65-8, Rate laws may be derived directly from the chemical equations for elementary reactions. This is not the case, however, for ordinary chemical reactions.26364-65-8, name is 2-Cyanoimino-1,3-thiazolidine, below Introduce a new synthetic route.

1,2-thiazolidine 1,1-dioxide (0.031 g, 0.259 mmol) in dimethylformamide (1 mL) was treated with 60% sodium hydride (0.012g, 0.518 mmol, 0.021 g of a 60%> in oil dispersion). The reaction mixture was stirred for 5 min. To this solution was added Example 41b (0.05 g, 0.086 mmol). The reaction mixture was stirred at room temperature for 2 hours. 2 N NaOH (1 mL) was added and the reaction mixture was heated at 65 C for 2 hours. After cooling to room temperature, the reaction mixture was partitioned between water and ethyl acetate. The aqueous layer was extracted with additional ethyl acetate twice. The combined organic layers were washed with brine, dried over MgSC^, filtered, and concentrated. The residue was purified by preparative HPLC (CI 8, 10-80% acetonitrile in 0.1% TFA water) to afford 0.025 g (64%) of the title compound. 1H NMR (500 MHz, DMSO-d6) delta 2.21-2.25 (m, 2H), 3.15 (t, J=6.97 Hz, 2H), 3.23-3.27 (m, 2H), 3.50 (s, 3H), 4.13 (s, 2H), 6.25-6.26 (m, 1H), 6.88 (d, J=7.63 Hz, 2H), 7.00 (d, J=8.54 Hz, 1H), 7.03-7.05 (m, 1H), 7.25-7.30 (m, 4H), 7.34 (dd, J=8.39, 2.29, 1H), 7.48 (d, J=2.44 Hz, 1H), 12.00 (s, 1 H). MS (ESI+) m/z 450.2 (M+H)+.

This molecular description is the mechanism of the reaction; it describes how individual atoms, ions, or molecules interact to form particular products.If you are interested, you can also browse other articles of 1,1-Dioxo-isothiazolidine, We look forward to the emergence of more reaction modes in the future.

Reference£º
Patent; ABBVIE INC.; ABBOTT LABORATORIES TRADING (SHANGHAI) COMPANY, LTD.; WANG, Le; PRATT, John K.; MCDANIEL, Keith F.; DAI, Yujia; FIDANZE, Steven D.; HASVOLD, Lisa; HOLMS, James H.; KATI, Warren M.; LIU, Dachun; MANTEI, Robert A.; MCCLELLAN, William J; SHEPPARD, George S.; WADA, Carol K.; WO2013/97601; (2013); A1;,
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The effect of the change of 1,1-Dioxo-isothiazolidine synthetic route on the product

Thank you very much for taking the time to read this article. If you are also interested in other aspects of 5908-62-3, you can also browse my other articles.

One of the major reasons is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time, to discover the sequence of events that occur at the molecular level.7025-19-6, name is 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid, introduce a new downstream synthesis route. , 7025-19-6

5908-62-3, A flask was charged under nitrogen with 3-bromo-5-iodo-benzoic acid tert-butyl ester D8b (1 g, 2.6 mmol, 1 equiv), Cs2CO3 (1.26 g, 3.9 mmol, 1.5 equiv), tris (DIBENZYLIDENEACETONE) DIPALLADIUM (0) (12 mg, 0.013 mmol, 0.005 equiv), Xantphos (22 mg, 0.038 mmol, 0.015 equiv) and toluene (20 ML). ISOTHIAZOLIDINE 1,1-dioxide (D22a) (350 mg, 2.9 mmol, 1.1 equiv) was then added and the resulting mixture was stirred at 100C for 16 h then cooled to room temperature and diluted with AcOEt. The organic phase was washed with saturated aqueous NAHC03 solution, dried over MGS04 and concentrated in vacuo. The residue was triturated with Et20 to give 3-BROMO-5-(1, 1-DIOXO-116-ISOTHIAZOLIDIN-2-YL)-BENZOIC acid tert-butyl ester (D17) (350 mg 38%) as a white solid.

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Reference£º
Patent; GLAXO GROUP LIMITED; WO2004/50619; (2004); A1;,
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Little discovery in the laboratory: a new route for 1,1-Dioxo-isothiazolidine

Thank you very much for taking the time to read this article. If you are also interested in other aspects of 1,1-Dioxo-isothiazolidine, you can also browse my other articles.

An elementary termolecular reaction involves the simultaneous collision of three atoms, molecules, or ions.7025-19-6, name is 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid. Here is a downstream synthesis route of the compound 7025-19-6. 7025-19-6

To a mixture of Cs2C03(41 mg, 0.12 mmol), 5-(5-(4-bromophenyl)- l,2,4-oxadiazol-3-yl)-l-(3-(2-methoxyethoxy)benzyl)pyridin-2(lH)-one(synthesized with analogous method to Example 65, using 4-bromobenzoic acid instead of 4-(trifluoromethoxy)benzoic acid; 30 mg, 0.062 mmol), Pd2(dba)3 (0.6 mg, 0.62 muiotaetaomicron), and XPhos (1.1 mg, 2.5 muiotaetaomicron) in toluene (311 muEpsilon) previously degassed with N2, was added isothiazolidine 1,1 -dioxide (6.4 mu, 0.075 mmol). The mixture was heated to 80 C for 12 h, cooled to RT, filtered through a pad Celite and concentrated under reduced pressure. The residue was purified by prep-HPLC (Mobile phase: A = 0.1% TFA/H20, B = 0.1% TFA/ MeCN; Gradient: B = 30% – 70% in 12 min; Column: CI 8) to give the title compound; H NMR (600 MHz, Chloroform-if) delta 8.25 (d, J = 2.4 Hz, IH), 8.13 (d, J = 8.8 Hz, 2H), 8.04 (dd, J = 9.5, 2.4 Hz, IH), 7.35 (d, / = 8.8 Hz, 2H), 7.28 (m, IH), 6.95 (d, / = 8.0 Hz, IH), 6.93 (m, IH), 6.88 (dd, / = 8.1, 2.4 Hz, IH), 6.77 (d, / = 9.5 Hz, IH), 5.22 (s, 2H), 4.14 – 4.04 (m, 2H), 3.87 (t, / = 6.5 Hz, 2H), 3.79 – 3.68 (m, 2H), 3.46 – 3.43 (m, 2H), 3.43 (s, 3H), 2.67 – 2.56 (m, 2H); MS (ES+) C26H26N406S requires: 522, found: 523 [M+H]+

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Reference£º
Patent; JONES, Philip; DIFRANCESCO, Maria, Emilia; PETROCCHI, Alessia; MARSZALEK, Joe; LIU, Gang; KANG, Zhijun; CARROLL, Christopher, L.; MCAFOOS, Timothy; CZAKO, Barbara; WO2014/31928; (2014); A2;,
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The effect of 1,1-Dioxo-isothiazolidine reaction temperature change on equilibrium

This molecular description is the mechanism of the reaction; it describes how individual atoms, ions, or molecules interact to form particular products.If you are interested, you can also browse other articles of 5908-62-3, We look forward to the emergence of more reaction modes in the future.

One of the major reasons is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time, to discover the sequence of events that occur at the molecular level.7025-19-6, name is 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid, introduce a new downstream synthesis route. , 7025-19-6

To a mixture of tert-butyl (6S)-3-iodo-6-methyl-6,7-dihydro-4H-pyrazolo[l,5-a]pyrazine- 5-carboxylate (intermediate 1-1, 100 mg, 0.28 mmol), 1,2-thiazolidine 1,1-dioxide (compound la, 50 mg, 0.41 mmol), trans-N,N’-dimethylcyclohexane-l,2-diamine (8 mg, 0.055 mmol) and Cul (10 mg, 0.055 mmol) in DMSO (5 mL) was added K2C03 (114 mg, 0.83 mmol). The reaction mixture was stirred at 100 C for 12 hours, and then concentrated under reduced pressure. The residue was purified by prep-HPLC to give tert-butyl (6S)-3-(l,l-dioxo-l,2-thiazolidin-2-yl)-6- methyl-6,7-dihydro-4H-pyrazolo[l,5-a]pyrazine-5-carboxylate (compound lb, 72 mg) as a yellow solid. MS obsd. (ESI+) [(M+H)+]: 357., 5908-62-3

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Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; HAN, Xingchun; LIN, Xianfeng; SHEN, Hong; HU, Taishan; ZHANG, Zhisen; (96 pag.)WO2018/11163; (2018); A1;,
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The influence of catalyst in 1,1-Dioxo-isothiazolidine reaction

There are, however, a few established termolecular elementary reactions. The reaction of nitric oxide with oxygen appears to involve termolecular steps. you can also browse my other articles about 5908-62-3

Rate laws may be derived directly from the chemical equations for elementary reactions. This is not the case, however, for ordinary chemical reactions.1438-16-0, name is 3-Aminorhodanine,below Introduce a new synthetic route., 1438-16-0

5908-62-3, To a solution of 6-(6-fluoro-4-iodo-2-pyridyl)-5-methyl-2-pyrimidin-2-yl-7,8-dihydro-5H- pyrido[4,3-d]pyrimidine (the product of step 1 in Example 96, 100 mg, 223 muiotaetaomicron) in dioxane ( 3mL) was added isothiazolidine-1,1-dioxide (54.1 mg, 446 muiotaetaomicron), cesium carbonate (145 mg, 446 muetaiotaomicron), Xantphos (25.8 mg, 44.6 muetaiotaomicron) and Pd(OAc)2(5.01 mg, 22.3 muetaiotaomicron). After being heated at 100 C with stirring for 20 hrs under argon, the resulting reaction mixture was then filtered and the filtrate was concentrated in vacuo. The residue was purified by prep-HPLC to give 2-[2-fluoro-6-(5-methyl-2-pyrimidin-2-yl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl)-4- pyridyl]-1,2-thiazolidine-1,1-dioxide (8 mg) as a light yellow solid. 1H NMR (400MHz, DMSO- d6) delta ppm: 8.99 (d, 2H), 8.95 (s, 1H), 7.64 (t, 1H), 6.32 (s, 1H), 6.15 (s, 1H), 5.69-5.64 (m, 1H), 4.47-4.36 (m, 1H), 3.89 – 3.79 (m, 2H), 3.68-3.59(m, 2H), 3.54 – 3.43 (m, 1H), 3.14 – 2.98 (m, 2H), 2.42-2.37 (m, 2H), 1.52 (d, 3H). MS obsd (ESI) [(M+H)+]: 442.

There are, however, a few established termolecular elementary reactions. The reaction of nitric oxide with oxygen appears to involve termolecular steps. you can also browse my other articles about 5908-62-3

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; CHENG, Zhanling; HAN, Xingchun; JIANG, Min; WANG, Jianhua; WANG, Yongguang; YANG, Song; (211 pag.)WO2018/1952; (2018); A1;,
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Little discovery in the laboratory: a new route for 1,1-Dioxo-isothiazolidine

Thank you very much for taking the time to read this article. If you are also interested in other aspects of 1,1-Dioxo-isothiazolidine, you can also browse my other articles.

An elementary termolecular reaction involves the simultaneous collision of three atoms, molecules, or ions.26364-65-8, name is 2-Cyanoimino-1,3-thiazolidine. Here is a downstream synthesis route of the compound 26364-65-8. 26364-65-8

Into a 4 mL vial was added isothiazolidine 1,1-dioxide (9.04 mg, 0.075 mmol) and (S)-6-chloro-3-(1-(4-chloropyrimidin-2-ylamino)ethyl)quinolin-2(1H)-one IV-1 (25 mg, 0.075 mmol) in DMF (250 muL). To this solution was added Cs2CO3 (48.6 mg, 0.149 mmol) and DIEA (26.1 muL, 0.149 mmol) and the reaction mixture was stirred at 110 C. for 1.5 hours. The mixture was then diluted with EtOAc and washed with brine (*2). The organic extract was dried over Na2SO4, filtered, and concentrated under reduced pressure to provide the crude product. This crude material was purified by column chromatography on a Biotage chromatography system (eluted with 0-100% EtOAc in hexanes) to afford the title compound (5.2 mg, 17% yield). 1H NMR (300 MHz, CDCl3): delta ppm 8.03 (br s, 1H), 7.93 (br s, 1H), 7.61 (br s, 1H), 7.41 (br d, J=8.50 Hz, 2H), 6.70 (br s, 1H), 5.42 (br s, 1H), 4.03 (br s, 1H), 3.83 (br s, 1H), 3.46 (m, 2H), 3.38 (m, 2H), 1.55-1.71 (m, 3H). LCMS (Method 1): Rt 2.02 min, m/z 419.89[M+H]+.

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Reference£º
Patent; Forma Therapeutics, Inc.; Lin, Jian; Ericsson, Anna; Campbell, Ann-Marie; Gustafson, Gary; Wang, Zhongguo; Diebold, R Bruce; Ashwell, Susan; Lancia, JR., David R.; Caravella, Justin Andrew; Lu, Wei; (171 pag.)US2016/83365; (2016); A1;,
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The effect of the change of 5908-62-3 synthetic route on the product

A chemical reaction often occurs in steps, although it may not always be obvious to an observer. Thank you very much for taking the time to read this article. If you are also interested in other aspects of 1,1-Dioxo-isothiazolidine, you can also browse my other articles.

5908-62-3, An elementary termolecular reaction involves the simultaneous collision of three atoms, molecules, or ions.5908-62-3, name is 1,1-Dioxo-isothiazolidine. Here is a downstream synthesis route of the compound 5908-62-3

[0831] Preparation Example 231: Preparation of methyl 2-(1,1-dioxo-1lambda6-isothiazolidin-2-yl)pyrimidine-5-carboxylate[0832][0833] Methyl 2-chloropyrimidine-5-carboxylate (173 mg) and isothiazolidine 1,1-dioxide (145 mg) were dissolved inN,N-dimethylformamide (1 mL), and sodium hydride (48mg, 60% in oil) was added under ice-cooling. After stirring atroom temperature for 6 hr, water was added, and the mixture was extracted with ethyl acetate. The solvent was evaporated,diisopropyl ether and ethyl acetate were added, and the precipitated solid was collected by filtration to give thetitle compound (185 mg).MS(ESI)m/z:258(M+H)+.

A chemical reaction often occurs in steps, although it may not always be obvious to an observer. Thank you very much for taking the time to read this article. If you are also interested in other aspects of 1,1-Dioxo-isothiazolidine, you can also browse my other articles.

Reference£º
Patent; Mitsubishi Tanabe Pharma Corporation; MAEDA, Kazuhiro; ENDOH, Jun-ichi; TARAO, Akiko; TASHIRO, Kaoru; ISHIBUCHI, Seigo; HIKAWA, Hidemasa; EP2565182; (2013); A1;,
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Little discovery in the laboratory: a new route for 1,1-Dioxo-isothiazolidine

Thank you very much for taking the time to read this article. If you are also interested in other aspects of 1,1-Dioxo-isothiazolidine, you can also browse my other articles.

An elementary termolecular reaction involves the simultaneous collision of three atoms, molecules, or ions.7025-19-6, name is 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid. Here is a downstream synthesis route of the compound 7025-19-6. 7025-19-6

5908-62-3, Example 60: 5-{5-[(3-{(1R,5S/1S,5R)-1-[4-(1,1-Dioxido-2-isothiazolidinyl)phenyl]-3- azabicyclo [3. 1.0] hex-3-yl} propyl) thio]-4-methyl-4H-1, 2, 4-triazol-3-yl}-2- methylquinoline hydrochloride; A Schlenk tube was charged with 5-[5-({3-[(1R,5S/1S,5R)-1-(4-bromophenyl)-3- azabicyclo [3.1. 0] hex-3-yl] propyl} thio)-4-methyl-4H-1, 2, 4-triazol-3-yl]-2-methylquinoline (cf. Example 2; 0.15 g), isothiazolidine 1,1-dioxide (46 mg), tris (dibenzylideneacetone)- dipalladium (0) (6 mg), 4,5-bis (diphenylphosphino)-9, 9-dimethylxanthene (10 mg), cesium carbonate (130 mg) and 1,4-dioxane (2 mL). The Schlenk tube was sealed with a teflon screwcap and the reaction mixture was stirred at 100 C for 12 h. The reaction mixture was allowed to cool to room temperature, diluted with dichloromethane (10 mL), filtered and concentrated in vacuo. The crude product was purified by flash chromatography (dichloromethane to 10% MeOH in dichloromethane) to give 50 mg of the free base of the title compound. To a solution of this material in dichloromethane (0.3 mL) was added HCI (0.087 mL, 1 M in Et20), the solvent evaporated in vacuo and the material thus obtained triturated with Et20 to give 52 mg of the title compound as a white solid. NMR (‘H, DMSO): 8 10.57 (bs, 1H), 8.27 (bd, 1H), 8.19 (d, 1H), 7.94 (t, 1H), 7.82 (d, 1H), 7.55 (d, 1H), 7.32 (d, 2H), 7.18 (d, 2H), 4.03 (dd, 1H), 3.72 (m, 3H), 3.60/3. 20 (bm, 8H), 3.45 (s, 3H), 2.75 (s, 3H), 2.41 (m, 2H), 2.25 (m, 2H), 2.14 (m, 1H), 1.66/1. 10 (t/m, 2H). MS (m/z) : 575 [MH] +.

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Patent; GLAXO GROUP LIMITED; WO2005/80382; (2005); A1;,
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